Enhanced Propertied Pharmaceuticals This invention relates to compounds which are useful as enhanced propertied pharmaceutical compounds for both human and veterinary application. The pharmaceutical compounds which are suitable for use in this invention are those compounds which can be substituted with a moiety, said moiety comprising a substituent which enhances or changes the properties of the pharmaceutical compound. The chemical modification of drugs into labile derivatives with enhanced physicochemical properties that enable better transport through biological barriers is a useful approach for improving-drug delivery. This modification can be conveniently practiced on ionizable molecules containing moieties such as a carboxy group, an amino group, a hydroxy group, a mercapto group or a group containing an appropriately substituted phosphorous atom that can be utilized for derivatization in order to modify their ionization at physiological pH and to render desirable partition and solubility properties. A necessary requirement of this approach is that the enhanced propertied drug is non-toxic and, when administered to a warm-blooded animal including a human being, is enzymatically and/or chemically cleaved in such a manner as to release the drug at its target or site of activity, quantitatively and at a desirable rate, while the remaining cleaved moiety remains non-toxic and is metabolized in such a manner that non-toxic metabolic products are produced. It is naturally also desirable that the enhanced propertied drug can be provided without excessive costs in connection with its production, in particular without an appreciable loss of the unmodified drug itself during its production and recovery, since the unmodified drug is usually the more expensive part of the enhanced propertied drug.

Furthermore, the new substituent on the original pharmaceutical compound may itself optionally comprise a pharmaceutical compound which may be the same as or different from the original pharmaceutical compound. This allows a combination of pharmaceutical compounds to be applied simultaneously as a single compound to the host. The application of such a compound provides many advantages such as a greater spectrum of activity against the disease being treated and an attenuation of the build up of disease resistance since the disease is being controlled with two different modes of action. This type of enhanced propertied

pharmaceutical compound will naturally comprise two different pharmaceutical moieties which are compatible with one another and which can be used without an antagonistic interactive effect upon the host. Such combinations should be apparent to one of ordinary skill in the art.

U. S. 4, 760, 057, U. S. 4, 916, 230, U. S. 5, 401, 868, U. S. 5, 459, 155, U. S. 5, 583, 148, U. S. 5, 684, 018, WO 98/16537, WO 98/43970 and WO 99/61017 describe certain pharmaceutical compounds which are substituted with moieties to alter the properties of pharmaceutical compounds ; however, the moieties employed in the compounds of the present invention are neither disclosed nor suggested.

U. S. 5, 284, 863, U. S. 4, 912, 090, U. S. 5, 385, 880, U. S. 5, 391, 537, JP 1275565 A2, WO 96/36613, WO 99/35141, WO 00/29378, WO 00/40582, DE 4343831 Al, JP 53-43571 B and JP 54-1771 B disclose certain pesticidal compounds which are substituted with moieties to alter the properties of pesticidal compounds ; however, the moieties employed in the compounds of the present invention are neither disclosed nor suggested.

The pharmaceutical compounds which may be advantageously employed to produce the enhanced propertied human health pharmaceutical compounds of this invention include, but are not limited to, 1-cyclopropyl-6-fluoro-1, 4-dihydro-4-oxo-7- (1-piperezinyl)-3-quinolinecarboxylic acid, 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7- (1- piperazinyl)-1, 8-naphthyridine-3-carboxylic acid, accolate, acebutolol, acetaminophen, acetazolamide, acrivistine, acyclovir, adamantamine, adapalene, adenosine phosphate, adrenelone, albendazole, albuterol, albutoin, alendronate sodium, aletamine, aliconazole, alinidine, alisobumal, alizapride, allopurinol, alprazolam, alprenolol, amethopterine, amidephrine, aminorex, amiodarone, amitriptyline, amlodipine, amoxapine, amoxicillin, amphetamine, amrinone, apraclonidine, aprinocid, arthrocine, arthrotec, aspartame, astemizole, atenolol, atorvastatin, atropine, azatadine, azathioprine, azithromycin, aztreonam, baclofen, bamethan, becliconazole, beclomet, benazepril, benzatropine, benzonatate, benzphetamine, benztropine, beperiden, betahistine, bicalutamide, bisacodyl, botalol hydrochloride, brimonidine tartrate, brolaconazole, bromocriptine, bromopheniramine, bucindolol, budesonide, bufenox, bunolol, bupivacaine,

buprenorphine, bupropion, buspirone, butaconazole, butopamine, butorphanol, butoxamine, caffeine, cafiminol, cambendazole, captopril, carbamazepam, carbinoxamine, carbuterol, carisoprodal, cartelolol, carvedilol, cefachlor, cefadroxil, cefamandole, cefazolin, cefixime, cefmetazole, cefonicid, cefoperazone, cefotaxime, cefotetan, cefpodoxime, cefprozil, ceftriaxone, celecoxib, centerdrine, cephapirin, cetirizine, chlorambucil, chloramiphene, chlorazepate, chlordiazepoxide, chloroprocaine, chloroquine, chloroxazone, chlorpheniramine, chlorpromazine, chlortermine, chlorthiazide, cimetidine, cinnarizine, ciprofloxacin, cisapride, cisconazole, citalopram, cladribine, clarithromycin, clemastine, clindamycin, clobesol, clofazimine, clomiphene, clonazepam, clonidine, clopidrogrel, clorprenaline, clotrimazole, cloxacillin, clozapine, cocaine, codeine, colchicine, colterol, combivir, cortisine, croconazole, cromolyn sodium, cyclobendazole, cyclobenzaprine, cyclopentolate, cyclophosphamide, cyclopsporin, cyproheptadine, dacarbazine, dactinomycin, dantrolene, deacetylketoconazole, demeclocycline, demethylamitriptyline, demethylimipramine, democonazole, deprenil, desipramine, deterenol, dexpropranolol, diacetolol, diazepam, diazoxide, dibucaine, diclofenac sodium, dicodid, dicyclomine, didanosine, diethylproprion, diflunisal, dihydroergotamine, dilantin, diltiazem, dimenhydrinate, dimethoxyphenethylmine, diphenhydramine, diphenidol, diphenoxylate hydrochloride, dipyridamole, disopyramide, dobutamine, doconazole, donezapil hydrochloride, dopamine, dotycin, doxapram, doxazosin, doxepin, doxylamine, dypyridamole, eberconazole, econazole, EDTA, efavirenz, enalapril, enoxacin, enviroxime, epinephrine, ergotamine, erythromycin, estazolam, ethionamide, etintidine, etodolac, etryptamine, exaprolol, exprenolol, famciclovir, famotidine, felodipine, fenbendazole, fenfluramine, fenmetazole, fenoterol, fentanyl, fenticonazole, fenyripol, fexofenadine, finasteride, flavoxate, fluazepam, flubendazole, fluconazole, fludarabine, fludorex, flufenazin, fluoxetine hydrochloride, fluphenazine, flurazepam, flurbiprofen, fluticasone propionate, fluvastatin, fluvoxamine maleate, folic acid, fosphenytoin, furazolidone, furosemide, gabapentin, ganciclovir, gemfibrozil, genaconazole, gentian violet, glimepiride, glipizide, glyburide, granisetron, guaifenesin, guanethidine, guanfacine hydrochloride, halazepam, haloperidol, homatropine, hydrochlorothiazide, hydrocodone, hydromorphone, hydroxychloroquine, hydroxyitraconazole, hydroxyzine, hyoscyamine, ibuprofen, imipramine hydrochloride, indapamide,

indinivar sulfate, indomethacin, iodoquinol, ipratropium bromide, irbesartan, isoconazole, isoniazid, isosornide monnitrate, isotretinoin, itraconazole, ketoconazole, ketoprofen, ketorolac, ketorolac, labetalol, labotolol, lamivudine, lamotrigin, lamotrigine, lansoprazole, levobunolol, levocabastine, levofloxacin, levomethadyl, levorphanol, lidocaine, lincomycin, lisinopril, lomefloxacin, loperidine hydrochloride, loratadine, lorazepam, losartan, lotrisone, lovastatin, loxapine, L-thyroxine, mazindol, mebendazole, mechlorethamine, meclizine hydrochloride, medroxyprogesteron, megestrol, melphalan, meperidine, mepivacaine, mercaptopurine, mesalamine, mesoridazine, metaproterenol, metazoline, methadone, methdilazine, methenamine, methimazol, methocarbamol, methochlopramide, methotrexate, methotrimeprazine, methyl dopa, methylphenidate, methysergide, metoclopramide, metolol, metolprolol tartrate, metoprolol, metoprolol succinate, metronidazole, miconazole, midazolam, miloride, minocycline, minoxidil, mitazapine, molindone, mometasone furoate, monopril, monozid, montelukast, morphine, mycophenolate mofetil hydrochloride, N- [3 (R)- [2- (piperidin-4-yl) ethyl]-2-piperidon-1- yl] acetyl-3 (R)-methyl-beta-alanine, nadolol, nafazodone, naftifine, nalbuphine, nalidixic acid, nalmefene, naloxone, naphazoline, naproxen, natrexone, nedocromil, nefazodone, nelfinavir mesylate, neticonazole, niacin, nicardipine, nicotine, nifedinpine, nifurantin, nimodipine, nitrofurantoin, nitrofurazone, nizatidine, nocodazole, norepinephrine, norfloxacin, odensetron, ofloxacin, olanzapine, olopatadine hydrochloride, omeprazole, omoconazole, ondansetron, orconazole, orphenadrine, oxaprozin, oxazepam, oxfendazole, obendazole, oxibendazole, oxiconazole, oxmetidine, oxybutynin, oxycodone, oxymetazoline, oxymorphone, oxytetracycline, pamatolol, papaverine, parbendazole, parconazole, paroxetine, pemoline, penbutalol, penicillin VK, pentazocine, pentostatin, pentoxifylline, perphenazine, phenazopyridine, phenobarbitol, phenoxybenzamine, phentermine, phentolamine, phenytoin, physostigmine, pilocarpine, pimozide, pindolol, pipemidic acid, pirbuterol, piroxicam, polymixin, posaconazole, practolol, pramoxine, pravastatin, prazosin, prednisolone, prenalterol, primaquine, primidolol, prizidilol, procainamide, procaine, procaterol, prochlorperazine, promazine, promethazine, propanolol, proparacaine, proparacaine, propoxyphene, propranolol, pyrazinamide, pyrimethamine, pyroxidine, quazepam, quetiapine fumarate, quinapril, quinidine, quinine, quinterenol, raloxifen hydrochloride, ramipril, ranitidine, ranitidine

hydrochloride, ravuconazole, retinoic acid, ribavarin, riboflavin, rifabutin, rifampin, rimiterol, risperidone, ritodrine, rocuronium, rosiglitazone, salmeterol, saperconazole, scopolamine, sertaconazole, sertraline, sibutramine, simvastatin, soterenol, sotolol, stavudine, sufentanil, sulconazole, sulfadiazine, sulfamethizole, sulfamethoxazole, sulfasalazine, sulfasoxazole, sulfinolol, sulfonterol, suloctidil, sumatriptan succinate, tacrine, tamoxifen, tamulosin hydrochloride, tazolol, temazepam, tenormin, tentrahydrozoline, terazosin, terbinafine, terbutaline, terconazole, terfenadine, tetracaine, tetracycline, tetrahydrazoline, tetrahydrolipstatin, theophylline, thiabendazole, thiamine, thiethylperazine, thioguanine, thioridazine, thiothixene, tiarnenidine, ticlopidine, timolol, tinazoline, tioconazole, tiotidine, tiprenolol, tipropidil, tocainide, tolamolol, tolazamide, tolazoline, tolmetin, tolteridine, toprimate, tramadol, tramazoline, trazodone, triamcinolone acetonide, triamterene, triazolam, trifluoroperazine, triflupromazine, trihexyphenidyl, trimeprazine, trimethoprin, trimetrexate, trimipramine, triplenamine, troglitazone, troleandomycin, tropicamide, tubocurarine, uracil mustard, valacyclovir hydrochloride, valconazole, valproic acid, valsartan, vecuronium, venlafaxine, verapamil, vidarabine, vinblastine, vincristine, vinorelbine, voriconazole, warfarin, xylometazoline, zinoconazole, zoficonazole and zolmitriptan.

The preferred pharmaceutical compounds which may be advantageously employed to produce the enhanced propertied human health pharmaceutical compounds of this invention include, but are not limited to, acrivistine, adapalene, aletamine, aliconazole, amiodarone, amitriptyline, amoxapine, amoxicillin, amphetamine, amrinone,, arthrocine, astemizole, atorvastatin, atropine, becliconazole, benazepril, benzatropine, benzphetamine, beperiden, betahistine, bicalutamide, bisacodyl, brolaconazole, bromopheniramine, bupivacaine, buprenorphine, bupropion, caffeine, cafiminol, carbamazepam, cefachlor, cefadroxil, centerdrine, chlordiazepoxide, chloroprocaine, chloroquine, ciprofloxacin, citalopram, clemastine, clobesol, clomiphene, clonazepam, clonidine, clotrimazole, cloxacillin, clozapine, colchicine, croconazole, cyclobenzaprine, cyclopentolate, cyproheptadine, demethylimipramine, democonazole, deprenil, desipramine, dicodid, dicyclomine, diethylproprion, diltiazem, diphenidol, diphenoxylate hydrochloride, diphenhydramine doconazole, donezapil hydrochloride, doxapram, doxazosin, doxepin, eberconazole, econazole, enalapril, enoxacin, etintidine, famciclovir,

fentanyl, fenfluramine, fenticonazole, flavoxate, fluazepam, fluconazole, fludorex, fluoxetine hydrochloride, flurbiprofen, fluticasone propionate, gabapentin, gemfibrozil, genaconazole, halazepam, haloperidol, hydroxyitraconazole, hydroxyzine, ibuprofen, indomethacin, iodoquinol, isoconazole, ketoprofen, ketorolac, lansoprazole, levomethadyl, lomefloxacin, loperidine hydrochloride, loratadine, lorazepam, lovastatin, mazindol, mechlorethamine, meperidine, mepivacaine, methadone, methimazole, methylphenidate, metronidazole, miconazole, minoxidil, molindone, monopril, monozid, naftifine, naphazoline, naproxen, nefazodone, neticonazole, nifedinpine, nifurantin, norfloxacin, olanzapine, omeprazole, omoconazole, orconazole, orphenadrine, oxaprozin, oxiconazole, oxmetidine, oxybutynin, oxycodone, oxymetazoline, papaverine, parconazole, paroxetine, pentazocine, perphenazine, phenoxybenzamine, phentermine, pilocarpine, pimozide, piroxicam, posaconazole, pramoxine, prazosin, procaine, proparacaine, propoxyphene, pyrazinamide, pyroxidine, quinapril, quinidine, ravuconazole, retinoic acid, risperidone, scopolamine, sertaconazole, sertraline, sibutramine, simvastatin, sufentanil, sulconazole, sulfamethizole, tacrine, tamoxifen, temazepam, terazosin, terbinafine, tetrahydrazoline, thiabendazole, ticlopidine, timolol, tioconazole, tocainide, tolazoline, tolteridine, tramadol, triamterene, trihexyphenidyl, troglitazone, troleandomycin, tropicamide, valconazole, valproic acid, verapamil, voriconazole, warfarin, xylometazoline and zinoconazole.

The pharmaceutical compounds which may be advantageously employed to produce the enhanced propertied veterinary pharmaceutical compounds of this invention include, but are not limited to, acepromazine, acetaminophen, acetazolamide, acetohydroxamic acid, acetylcysteine, acetylcysteine, acyclovir, aggrastat, albendazole, albuterol, allopurinol, altrenogest, aminocaproic acid, aminopentamide, aminophylline, aminopropazine, amiodarone, amitraz, amitriptyline, amlodipine, amoxicillin, ampicillin, amprolium, amrinone, apomorphine, apramycin, ascorbic acid, aspirin, atenolol, atipamezole, atropine, aurothioglucose, azaperone, azathioprine, benazepril, betamethasone, boldenone, bromocriptine, buprenorphine, buspirone, butorphanol, captopril, carbenicillin, carnitine, carprofen, cefadroxil, cefazolin, cefoperazone, cefotaxime, cefoxitin, ceftiofur, ceftriaxone, cephalexin, cephalothin, cephapirin, chloramphenicol,

chlorothiazide, chlorpheniramine, chlorpromazine, chlorpropamide, cilastatin, cimetidine, ciprofloxacin, cisapride, clavuianate, clemastine, clenbuterol, clioquinol, clomipramine, clonazepam, cloprostenol, clorazepate, clorsulon, cloxacillin, codeine, colchicine, cyclophosphamide, cyproheptadine, cytarabine, cythioate, danazol, decoquinate, desoxycorticosterone Piv, detomidine, dexamethasone, dexpanthenol, diazoxide, dichlorphenamide, dicloxacillin, diethylcarbamazine, difloxacin, digitoxin, dioxin, dihydrotachysterol, diltiazem, dimenhydrinate, dimercaprol, dinoprost, diphenhydramine, diphenoxylate, disopyramide, dobutamine, dopamine, doramectin, doxapram, doxepin, doxorubicin, doxylamine, droperidol, edetate calcium, enalapril, enrofloxacin, ephedrine, epinephrine, esmolol, estradiol, ethacrynic acid, ethylisobutrazine, etidronate, etodolac, famotidine, febantel, fenbendazole, fenprostalene, fentanyl, fipronil, florfenicol, fluconazole, flucytosine, fludrocortisone, flumazenil, flumethasone, flunixin, fluprostenol, fomepizole-4-MP, furosemide, glipizide, glycopyrrolate, guaifenesin, hetacillin, hydralazine, hydrochlorothiazide, hydrocodone, hydrocortisone, hydroxyurea, hydroxyzine, imidacloprid, imidocarb, imipenem, imipramine, isopropamide, isoproterenol, isotretinoin, isoxsuprine, itraconazole, ketamine, ketoconazole, ketoprofen, levamisole, levothyroxine, lidocaine, lincomycin, liothyronine, lomustine, lufenuron, mechlorethamine, meclizine, meclofenamic acid, medetomidine, medroxyprogesterone, megestrol, melphalan, meperidine, mephenytoin, mercaptopurine, methenamine, methimazole, methionine, methocarbamol, methotrexate, methylprednisolone, metoclopramide, metoprolol, metronidazole, mexiletine, mibolerone, midazolam, misoprostol, morantel, morphine, naloxone, naltrexone, nandrolone, naproxen, nitrofurantoin, omeprazole, orbifloxacin, ormetoprim, oxacillin, oxazepam, oxfendazole, oxibendazole, oxybutynin, oxymorphone, penicillamine, penicillin G, penicillin V, pentazocine, pentoxifylline, phenoxybenzamine, phenylephrine, phenylpropanolamine, phenytoin, phytonadione, piperazine, pirlimycin, piroxicam, pralidoxime, prazosin, prednisolone, prednisone, primidone, procainamide, promazine, propofol, propranolol, prostaglandin E1, pyrantel, pyrilamine, pyrimethamine, quinacrine, quinidine, ranitidine, selegiline, stanozolol, sulfachlorpyridazine, sulfadiazine, sulfadimethoxine, sulfamethoxazole, sulfasalazine, terbutaline, testosterone, theophylline, thiabendazole, thiamine, thiotepa, tiamulin, ticarcillin, tiletamine, tiopronin, tocainide, tolazoline,

triamcinolone, trimeprazine, trimethoprim, tripelennamine, ursodiol, valproic acid, verapamil, vinblastine, vincristine, warfarin, xylazine and yohimbine.

The preferred pharmaceutical compounds which may be advantageously employed to produce the enhanced propertied veterinary pharmaceutical compounds of this invention include, but are not limited to, acepromazine, albendazole, aminocaproic acid, aminophylline, aminopropazine, amiodarone, amitriptyline, amprolium, atipamezole, atropine, azaperone, benazepril, buspirone, captopril, cephapirin, chlorpheniramine, cisapride, clemastine, clioquinol, clomipramine, cyproheptadine, detomidine, diethylcarbamazine, diltiazem, diphenhydramine, diphenoxylate, disopyramide, doxapram, doxepin, doxylamine, droperidol, enalapril, febantel, fenbendazole, fentanyl, fluconazole, guaifenesin, hetacillin, hydrocodone, hydroxyzine, imidacloprid, itraconazole, ketamine, ketoprofen, levamisole, lidocaine, lincomycin, lomustine, mechlorethamine, meclizine, meclofenamic acid, meperidine, mercaptopurine, methenamine, methotrexate, mexiletine, mibolerone, morantel, naltrexone, omeprazole, ormetoprim, oxazepam, oxybutynin, pentazocine, piroxicam, primidone, procainamide, promazine, prostaglandin E1, pyrantel, quinacrine, quinidine, selegiline, sulfachlorpyridazine, sulfadiazine, sulfamethoxazole, theophylline, thiabendazole, tiamulin, tiletamine, tocainide, valproic acid, verapamil, vincristine, warfarin and xylazine.

A first embodiment of this invention relates to a pharmaceutical moiety represented by Zl (Xl) m wherein X'is an oxygen atom, a sulfur atom, a phosphorous atom or a nitrogen atom attached to Zl, Z'represents the remainder of said pharmaceutical moiety, m is 1, and Zl (Xl) =-H represents the complete pharmaceutical compound, said pharmaceutical moiety ZI (Xl) m being substituted with a second moiety on XI, said second moiety comprising a substituent which enhances or changes the properties of said pharmaceutical compound, said substituent having the formula

wherein Gl°, G"and G20 are each independently an oxygen atom or a sulfur atom, G21 is an oxygen atom, a sulfur atom or NR3, q is 0, t is 0 or 1, represents the connection point of said substituent to said pharmaceutical moiety ZI (XI) m, Z2 (X2) q is a hydrogen atom, alkyl, alkylcarbonyloxyalkyl, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl, hydroxyalkyl, alkylsulfonylalkyl, alkylcarbonylaminoalkyl, arylcarbonylaminoalkyl, heteroarylcarbonylaminoalkyl, haloalkyl, alkenyl, acetylaminoalkenyl, alkylcarbonylaminoalkenyl, arylcarbonylaminoalkenyl, heteroarylcarbonylaminoalkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, cycloalkenyl, carboxycycloalkyl, carboxycycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, carboxycycloalkylalkyl, carboxycycloalkylalkenyl, carboxycycloalkenylalkyl, carboxycycloalkenylalkenyl, carboxycycloalkylalkynyl, carboxycycloalkenylalkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, alkoxyalkyl, alkoxyalkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, haloalkoxyalkyl, haloalkoxyalkenyl, haloalkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, haloalkylthioalkyl, haloalkylthioalkenyl, haloalkylthioalkynyl, NR3R4, SO2NR3R4, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, dialkoxyphosphorylalkyl, aryl, aryl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, alkyl, alkylsulfonylalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, C (=O) OR2, C (=O) SR2, C (=S) OR2, C (=S) SR2, C (=O) NR3R4, C (=S) NR3R4, C (=O) R2, C (=S) R2, C (=N-R3) R2, C (=N-OR3) R2, C (=N-NR3R4) R2, OP (=O) (OR2) 2, SO2NR3R4, NR3R4 and alkylNR3R4, aralkyl, aralkenyl, aralkynyl, arcycloalkyl,

aroxyalkyl, or aralkyl, aralkenyl, aralkynyl, arcycloalkyl, aroxyalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, or heteroaralkyl, heteroaralkenyl, heteroaralkynyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, alkylcarbonylalkyl, alkenylcarbonylalkyl, alkynylcarbonylalkyl, heterocyclylcarbonyl, heterocyclylcarbonylalkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonylalkyl, arylcarbonyl, arylcarbonylalkyl, aralkylcarbonyl, aralkylcarbonylalkyl, aroxycarbonyl, aroxycarbonylalkyl, aralkoxycarbonyl, aralkoxycarbonylalkyl, heteroarylcarbonyl, heteroarylcarbonylalkyl, heteroaroxycarbonyl, heteroaroxycarbonylalkyl, or heterocyclylcarbonyl, heterocyclylcarbonylalkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonylalkyl, arylcarbonyl, arylcarbonylalkyl, aralkylcarbonyl, aralkylcarbonylalkyl, aroxycarbonyl, aroxycarbonylalkyl, aralkoxycarbonyl, aralkoxycarbonylalkyl, heteroarylcarbonyl, heteroarylcarbonylalkyl, heteroaroxycarbonyl, heteroaroxycarbonylalkyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, and C (=N-G22) R2 when q is 0 and t is 1, G22 is OR3, OCOR3, S (O) jR3, OS (O) jR3, NR3R4, OSO2NR3R4, OP (=O) OR3NR3R4, OP (=O) (OR3) 2 or N=CR3R4, j is 0, 1 or 2, Z2 (X2) q is halo, NR3R4, {(NR3R4R5) + M}, OR3, S (O) jR3 or S02NR3R4 when both q and t are 0 wherein M-is halo, hydroxy, alkoxy or the anion of a carboxylic acid and j is 0, 1 or 2, R1 is

wherein G30 is an oxygen atom or a sulfur atom, z, G31 is an oxygen atom, a sulfur atom or NR3, d is 0, t'is 0 or 1, Z3 (X3) d, when d is 0 and t'is 1, is a hydrogen atom, alkyl, alkylcarbonyloxyalkyl, alkylcarbonyl, alkylcarbonylalkyl, alkenylcarbonyl, alkenylcarbonylalkyl, alkynylcarbonyl, alkynylcarbonylalkyl, hydroxyalkyl, alkylsulfonylalkyl, alkylcarbonylaminoalkyl, arylcarbonylaminoalkyl, heteroarylcarbonylalkylamino, acetylaminoalkyl, haloalkyl, alkenyl, acetylaminoalkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, cycloalkenyl, carboxycycloalkyl, carboxycycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, carboxycycloalkylalkyl, carboxycycloalkylalkenyl, carboxycycloalkenylalkyl, carboxycycloalkenylalkenyl, carboxycycloalkylalkynyl, carboxycycloalkenylalkynyl, alkoxyalkyl, alkoxyalkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, haloalkoxyalkyl, haloalkoxyalkenyl, haloalkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, haloalkylthioalkyl, haloalkylthioalkenyl, haloalkylthioalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, NR3R4, OR3, S (O) jR3, aryl, arylcarbonyloxyalkyl, arylcarbonylalkyl, aroxycarbonylalkyl, or aryl, arylcarbonyloxyalkyl, arylcarbonylalkyl, aroxycarbonylalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, alkyl, alkylsulfonylalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, aralkyl, aralkylcarbonyloxyalkyl, aralkylcarbonylalkyl, aralkoxycarbonylalkyl, aralkenyl, aralkynyl, arcycloalkyl, aroxyalkyl, or aralkyl, aralkylcarbonyloxyalkyl, aralkylcarbonylalkyl, aralkoxycarbonylalkyl, aralkenyl, aralkynyl, arcycloalkyl, aroxyalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, S02NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyloxyalkyl, heteroarylcarbonylalkyl., heteroaroxycarbonylalkyl, or heteroaryl, heteroarylcarbonyloxyalkyl, heteroarylarylcarbonylalkyl, heteroaroxycarbonylalkyl

substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, or heteroaralkyl, heteroaralkenyl, heteroaralkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclylcarbonyloxyalkyl, heterocyclylcarbonylalkyl, heterocyclyloxycarbonylalkyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, or heterocyclyl, heterocyclylcarbonyloxyalkyl, heterocyclylcarbonylalkyl, heterocyclyloxycarbonylalkyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, S02NR3R4 and NR3R4 wherein j is 0, 1 or 2, Z3 (X3) d is halo, NR3R4, OR3, N (R3)-N=CR3R4, S (O) jR3 or SO2NR3R4 when both d and t'are 0 and j is 0, 1 or 2, R2 is a hydrogen atom, alkyl, alkenyl, alkynyl, alkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, carboxy, a carboxylate salt, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, cycloalkylalkenyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, or alkyl, alkenyl, alkynyl, alkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, cycloalkylalkenyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, S02NR3R4 and NR3R4, aryl or aryl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl,

haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, carboxy, alkoxycarbonyl, SO2NR3R4 and NR3R4, aralkyl, aralkenyl, aralkynyl or aralkyl, aralkenyl, aralkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, arylcarbonyl, aralkylcarbonyl, aralkenylcarbonyl, aralkynylcarbonyl, aroxycarbonylalkyl, or arylcarbonyl, aralkylcarbonyl, aralkenylcarbonyl, aralkynylcarbonyl, aroxycarbonylalkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, S02NR3R4 and NR3R4, heteroaryl or heteroaryl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaralkyl, heteroaralkenyl, heteroaralkynyl or heteroaralkyl, heteroaralkenyl, heteroaralkynyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroarylcarbonyl, heteroaralkylcarbonyl, heteroaralkenylcarbonyl, heteroaralkynylcarbonyl, heteroaroxycarbonylalkyl, heterocyclylcarbonyl, heterocyclyloxycarbonylalkyl, or heteroarylcarbonyl, heteroaralkylcarbonyl, heteroaralkenylcarbonyl, heteroaralkynylcarbonyl, heteroaroxycarbonylalkyl, heterocyclylcarbonyl, heterocyclyloxycarbonylalkyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, R3, R4 and R5 are each independently a hydrogen atom, alkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkenylalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxyalkyl, alkenyl, alkynyl, or alkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkenylalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxyalkyl, alkenyl or alkynyl substituted with one or more halo, aryl, aralkyl, aralkenyl, aralkynyl, or aryl, aralkyl, aralkenyl, aralkynyl substituted with one or more substituents independently selected from halo, alkyl, alkenyl,

alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy and haloalkoxy, heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, or heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl substituted with one or more substituents independently selected from halo, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy and haloalkoxy, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, or heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl substituted with one or more substituents independently selected from halo, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy and haloalkoxy, or R3 and R4 taken together with the nitrogen atom to which they are attached form a 5-or 6-membered saturated or unsaturated heterocyclic ring, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof A second embodiment of this invention relates to a pharmaceutical moiety represented by ZI (Xl) m wherein XI is an oxygen atom, a sulfur atom, a phosphorous atom or a nitrogen atom attached to Z', Z'represents the remainder of said pharmaceutical moiety, m is 1, and ZI (Xl) m-H represents the complete pharmaceutical compound, said pharmaceutical moiety ZI (Xl) m being substituted with a second moiety on XI, said second moiety comprising a substituent which enhances or changes the properties of said pharmaceutical compound, said substituent having the formula wherein G10, G and G20 are-each independently an oxygen atom or a sulfur atom, G21 is an oxygen atom, a sulfur atom or NR3, q is 0 or 1,

represents the connection point of said substituent to said pharmaceutical moiety Zl (XI) m, X2 is an oxygen atom, a sulfur atom, a phosphorous atom, a nitrogen atom or a carbon atom attached to Z2, t is 0 or 1, Z2 (X2) q (C (=G20) G21) t is a second pharmaceutical moiety when q is 1 wherein Z2 (X2) q (C (=G20) G21) t or Z2 (X2) q (C (=G20) G21) t-H represents the second pharmaceutical, Z2 represents the remainder of said second pharmaceutical moiety, R'is wherein G30 is an oxygen atom or a sulfur atom, G31 is an oxygen atom, a sulfur atom or NR3, t'and d are each independently 0 or 1, X3 is an oxygen atom, a sulfur atom, a nitrogen atom, a phosphorous atom or a carbon atom attached to Z3 when t'is 0, a nitrogen atom attached to Z3 when t'is 1 and G31 is NR3, or a carbon atom attached to Z3 when t'is 1 and G31 is an oxygen atom or a sulfur atom, Z3 (X3) d (G31) t is a second alternative pharmaceutical moiety when d is 1 wherein Z3 (X3) d (G3') t'-H represents the second alternative pharmaceutical, Z3 represents the remainder of said second alternative pharmaceutical moiety, Z3 (X3) d, when d is 0 and t'is 1, is a hydrogen atom, alkyl, alkylcarbonyloxyalkyl, alkylcarbonyl, alkylcarbonylalkyl, alkenylcarbonyl, alkenylcarbonylalkyl, alkynylcarbonyl, alkynylcarbonylalkyl, hydroxyalkyl, alkylsulfonylalkyl, alkylcarbonylaminoalkyl, arylcarbonylaminoalkyl, heteroarylcarbonylalkylamino, acetylaminoalkyl, haloalkyl, alkenyl, acetylaminoalkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, cycloalkenyl, carboxycycloalkyl, carboxycycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, carboxycycloalkylalkyl, carboxycycloalkylalkenyl, carboxycycloalkenylalkyl, carboxycycloalkenylalkenyl, carboxycycloalkylalkynyl, carboxycycloalkenylalkynyl,

alkoxyalkyl, alkoxyalkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, haloalkoxyalkyl, haloalkoxyalkenyl, haloalkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, haloalkylthioalkyl, haloalkylthioalkenyl, haloalkylthioalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, NR3R4, OR3, S (O) jR3, aryl, arylcarbonyloxyalkyl, arylcarbonylalkyl, aroxycarbonylalkyl, or aryl, arylcarbonyloxyalkyl, arylcarbonylalkyl, aroxycarbonylalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, alkyl, alkylsulfonylalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, aralkyl, aralkylcarbonyloxyalkyl, aralkylcarbonylalkyl, aralkoxycarbonylalkyl, aralkenyl, aralkynyl, arcycloalkyl, aroxyalkyl, or aralkyl, aralkylcarbonyloxyalkyl, aralkylcarbonylalkyl, aralkoxycarbonylalkyl, aralkenyl, aralkynyl, arcycloalkyl, aroxyalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, S02NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyloxyalkyl, heteroarylcarbonylalkyl, heteroaroxycarbonylalkyl, or heteroaryl, heteroarylcarbonyloxyalkyl, heteroarylarylcarbonylalkyl, heteroaroxycarbonylalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, or heteroaralkyl, heteroaralkenyl, heteroaralkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclylcarbonyloxyalkyl, heterocyclylcarbonylalkyl, heterocyclyloxycarbonylalkyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, or heterocyclyl, heterocyclylcarbonyloxyalkyl, heterocyclylcarbonylalkyl, heterocyclyloxycarbonylalkyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4 wherein j is 0, 1 or 2,

Z3 (X3) d is halo, NR3R4, OR3, N (R3)-N=CR3R4, S (O) jR3 or SO2NR3R4 when both d and t'are 0 and j is 0, 1 or 2, R2 is a hydrogen atom, alkyl, alkenyl, alkynyl, alkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, carboxy, a carboxylate salt, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, cycloalkylalkenyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, or alkyl, alkenyl, alkynyl, alkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, cycloalkylalkenyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, S02NR3R4 and NR3R4, aryl or aryl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, carboxy, alkoxycarbonyl, SO2NR3R4 and NR3R4, aralkyl, aralkenyl, aralkynyl or aralkyl, aralkenyl, aralkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, arylcarbonyl, aralkylcarbonyl, aralkenylcarbonyl, aralkynylcarbonyl, aroxycarbonylalkyl, or arylcarbonyl, aralkylcarbonyl, aralkenylcarbonyl, aralkynylcarbonyl, aroxycarbonylalkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaryl or heteroaryl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, S02NR3R4 and NR3R4, heteroaralkyl, heteroaralkenyl, heteroaralkynyl or heteroaralkyl, heteroaralkenyl, heteroaralkynyl substituted with one or more

substituents independently selected from halo, cyano, hydroxy, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloall : ynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroarylcarbonyl, heteroaralkylcarbonyl, heteroaralkenylcarbonyl, heteroaralkynylcarbonyl, heteroaroxycarbonylalkyl, heterocyclylcarbonyl, heterocyclyloxycarbonylalkyl, or heteroarylcarbonyl, heteroaralkylcarbonyl, heteroaralkenylcarbonyl, heteroaralkynylcarbonyl, heteroaroxycarbonylalkyl, heterocyclylcarbonyl, heterocyclyloxycarbonylalkyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, R3, R4 and R5 are each independently a hydrogen atom, alkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkenylalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxyalkyl, alkenyl, alkynyl, or alkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkenylalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxyalkyl, alkenyl or alkynyl substituted with one or more halo, aryl, aralkyl, aralkenyl, aralkynyl, or aryl, aralkyl, aralkenyl, aralkynyl substituted with one or more substituents independently selected from halo, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy and haloalkoxy, heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, or heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl substituted with one or more substituents independently selected from halo, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy and haloalkoxy, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, or heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl substituted with one or more substituents independently selected from halo, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy and haloalkoxy, or R3 and R4 taken together with the nitrogen atom to which they are attached form a 5-or 6-membered saturated or unsaturated heterocyclic ring, (q + d) is 1, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof

A third embodiment of this invention relates to a pharmaceutical compound of formula (I) wherein A is Gi°, G"and G20 are each independently an oxygen atom or a sulfur atom, G21 is an oxygen atom, a sulfur atom or NR3, X'is an oxygen atom, a sulfur atom, a phosphorous atom or a nitrogen atom attached to Z', X2 is an oxygen atom, a sulfur atom, a phosphorous atom, a nitrogen atom or a carbon atom attached to Z2, m, q and t are each independently 0 or 1, n is 1 or 2, ZI (X') m is a pharmaceutical moiety when m is 1 wherein Zl (X') m-H represents the pharmaceutical, Z2 (X2) q (C (=G20) G21) t is a pharmaceutical moiety when q is 1 wherein Z2 (X2) q (C (=G20) G2') t-H or Z2 (X2) q (C (=G20) G2l) t represents the pharmaceutical, Zl (XI) m, when m is 0, is a hydrogen atom, halo, alkyl, alkylcarbonyloxyalkyl, alkylcarbonyl, hydroxyalkyl, alkylsulfonylalkyl, acetylaminoalkyl, alkylcarbonylaminoalkyl, arylcarbonylaminoalkyl, heteroarylcarbonylaminoalkyl, haloalkyl, alkenyl, acetylaminoalkenyl, alkylcarbonylaminoalkenyl, arylcarbonylaminoalkenyl, heteroarylcarbonylaminoalkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, cycloalkenyl, carboxycycloalkyl, carboxycycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, carboxycycloalkylalkyl, carboxycycloalkylalkenyl, carboxycycloalkenylalkyl, carboxycycloalkenylalkenyl,

carboxycycloalkylalkynyl, carboxycycloalkenylalkynyl, alkoxyalkyl, alkoxyalkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, haloalkoxyalkyi, haloalkoxyalkenyl, haloalkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, haloalkylthioalkyl, haloalkylthioalkenyl, haloalkylthioalkynyl, NR3R4, SO2NR3R4, OR3, S (O) jR3, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, aryl, arylcarbonyl, arylcarbonylalkyl, aroxycarbonyl, aroxycarbonylalkyl, or aryl, arylcarbonyl, arylcarbonylalkyl, aroxycarbonyl, aroxycarbonylalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, alkyl, alkylsulfonylalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, aralkyl, aralkenyl, aralkynyl, arcycloalkyl, aroxyalkyl, aralkylcarbonyl, aralkenylcarbonyl, aralkylcarbonylalkyl, aralkenylcarbonylalkyl, or aralkyl, aralkenyl, aralkynyl, arcycloalkyl, aroxyalkyl, aralkylcarbonyl, aralkenylcarbonyl, aralkylcarbonylalkyl, aralkenylcarbonylalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyl, heteroarylcarbonylalkyl, heteroaroxycarbonyl, heteroaroxycarbonylalkyl, or heteroaryl, heteroarylcarbonyl, heteroarylcarbonylalkyl, heteroaroxycarbonyl, heteroaroxycarbonylalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, heteroaralkylcarbonyl, heteroaralkylcarbonylalkyl, heteroaralkenylcarbonyl, heteroaralkenylcarbonylalkyl, or heteroaralkyl, heteroaralkenyl, heteroaralkynyl, heteroaralkylcarbonyl, heteroaralkylcarbonylalkyl, heteroaralkenylcarbonyl, heteroaralkenylcarbonylalkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, heterocyclylcarbonyl, heterocyclylcarbonylalkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonylalkyl, or heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, heterocyclylcarbonyl, heterocyclylcarbonylalkyl,

heterocyclyloxycarbonyl, heterocyclyloxycarbonylalkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, S02NR3R4 and NR3R4 wherein j is 0, 1 or 2, Z2 (X2) q is a hydrogen atom, alkyl, alkylcarbonyloxyalkyl, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl, hydroxyalkyl, alkylsulfonylalkyl, alkylcarbonylaminoalkyl, arylcarbonylaminoalkyl, heteroarylcarbonylaminoalkyl, haloalkyl, alkenyl, acetylaminoalkenyl, alkylcarbonylaminoalkenyl, arylcarbonylaminoalkenyl, heteroarylcarbonylaminoalkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, cycloalkenyl, carboxycycloalkyl, carboxycycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, carboxycycloalkylalkyl, carboxycycloalkylalkenyl, carboxycycloalkenylalkyl, carboxycycloalkenylalkenyl, carboxycycloalkylalkynyl, carboxycycloalkenylalkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, alkoxyalkyl, alkoxyalkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, haloalkoxyalkyl, haloalkoxyalkenyl, haloalkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, haloalkylthioalkyl, haloalkylthioalkenyl, haloalkylthioalkynyl, NR3R4, SO2NR3R4, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, dialkoxyphosphorylalkyl, aryl, aryl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, alkyl, alkylsulfonylalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, C (=O) OR2, C (=O) SR2, C (=S) OR2, C (=S) SR2, C (=O) NR3R4, C (=S) NR3R4, C (=O) R2, C (=S) R2, C (=N-R3) R2, C (=N-OR3) R, C (=N-NR3R4) R2, OP (=O) (OR2) 2, SO2NR3R4, NR3R4 and alkylNR3R4, aralkyl, aralkenyl, aralkynyl, arcycloalkyl, aroxyalkyl, or aralkyl, aralkenyl, aralkynyl, arcycloalkyl, aroxyalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, or heteroaralkyl,

heteroaralkenyl, heteroaralkynyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, alkylcarbonylalkyl, alkenylcarbonylalkyl, alkynylcarbonylalkyl, heterocyclylcarbonyl, heterocyclylcarbonylalkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonylalkyl, arylcarbonyl, arylcarbonylalkyl, aralkylcarbonyl, aralkylcarbonylalkyl, aroxycarbonyl, aroxycarbonylalkyl, aralkoxycarbonyl, aralkoxycarbonylalkyl, heteroarylcarbonyl, heteroarylcarbonylalkyl, heteroaroxycarbonyl, heteroaroxycarbonylalkyl, or heterocyclylcarbonyl, heterocyclylcarbonylalkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonylalkyl, arylcarbonyl, arylcarbonylalkyl, aralkylcarbonyl, aralkylcarbonylalkyl, aroxycarbonyl, aroxycarbonylalkyl, aralkoxycarbonyl, aralkoxycarbonylalkyl, heteroarylcarbonyl, heteroarylcarbonylalkyl, heteroaroxycarbonyl, heteroaroxycarbonylalkyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, and C (=N-G22) R2 when q is 0 and t is 1, G22 is OR3, OCOR3, S (O) jR3, OS (O) jR3, NR3R4, OSOzNR3R4, OP (=O) OR3NR3R4, OP (=O) (OR3) 2 or N=CR3R4, j is 0, 1 or 2, Z2 (X2) q is halo, NR3R4, {(NR3R4R5) + M}, OR3, S (O) jR3 or S02NR3R4 when both q and t are 0 wherein M-is halo, hydroxy, alkoxy or the anion of a carboxylic acid and j is 0, 1 or 2, RI is wherein G30 is an oxygen atom or a sulfur atom, G31 is an oxygen atom, a sulfur atom or NR3, t'and d are each independently 0 or 1, X3 is an oxygen atom, a sulfur atom, a nitrogen atom, a phosphorous atom or a carbon atom attached to Z3 when t'is 0, a nitrogen atom attached to Z3 when t'is 1 and G31 is NR3, or a carbon atom attached to Z3 when t'is 1 and G31 is an oxygen atom or a sulfur atom,

Z3 (X3) d (G31) t' is a pharmaceutical moiety when d is 1 wherein3 (X3) d (G3l) t-H represents the pharmaceutical, Z3 (X3) d, when d is 0 and t'is 1, is a hydrogen atom, alkyl, alkylcarbonyloxyalkyl, alkylcarbonyl, alkylcarbonylalkyl, alkenylcarbonyl, alkenylcarbonylalkyl, alkynylcarbonyl, alkynylcarbonylalkyl, hydroxyalkyl, alkylsulfonylalkyl, alkylcarbonylaminoalkyl, arylcarbonylaminoalkyl, heteroarylcarbonylalkylamino, acetylaminoalkyl, haloalkyl, alkenyl, acetylaminoalkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, cycloalkenyl, carboxycycloalkyl, carboxycycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, carboxycycloalkylalkyl, carboxycycloalkylalkenyl, carboxycycloalkenylalkyl, carboxycycloalkenylalkenyl, carboxycycloalkylalkynyl, carboxycycloalkenylalkynyl, alkoxyalkyl, alkoxyalkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, haloalkoxyalkyl, haloalkoxyalkenyl, haloalkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, haloalkylthioalkyl, haloalkylthioalkenyl, haloalkylthioalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, NR3R4, OR3, S (O) jR3, aryl, arylcarbonyloxyalkyl, arylcarbonylalkyl, aroxycarbonylalkyl, or aryl, arylcarbonyloxyalkyl, arylcarbonylalkyl, aroxycarbonylalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, alkyl, alkylsulfonylalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, S02NR3R4 and NR3R4, aralkyl, aralkylcarbonyloxyalkyl, aralkylcarbonylalkyl, aralkoxycarbonylalkyl, aralkenyl, aralkynyl, arcycloalkyl, aroxyalkyl, or aralkyl, aralkylcarbonyloxyalkyl, aralkylcarbonylalkyl, aralkoxycarbonylalkyl, aralkenyl, aralkynyl, arcycloalkyl, aroxyalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, S02NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyloxyalkyl, heteroarylcarbonylalkyl, heteroaroxycarbonylalkyl, or heteroaryl, <BR> <BR> <BR> <BR> heteroarylcarbonyloxyalkyl, heteroarylarylcarbonylalkyl, heteroaroxycarbonylalkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaralkyl, heteroaralkenyl, heteroaralkynyl,

or heteroaralkyl, heteroaralkenyl, heteroaralkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclylcarbonyloxyalkyl, heterocyclylcarbonylalkyl, heterocyclyloxycarbonylalkyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, or heterocyclyl, heterocyclylcarbonyloxyalkyl, heterocyclylcarbonylalkyl, heterocyclyloxycarbonylalkyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4 wherein j is 0, 1 or 2, Z3 (X3) d is halo, NR3R4, OR3, N (R3)-N=CR3R4, S (O) jR3 or S02NR3R4 when both d and t'are 0 and j is 0, 1 or 2, each R2 is independently a hydrogen atom, alkyl, alkenyl, alkynyl, alkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, carboxy, a carboxylate salt, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, cycloalkylalkenyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, or alkyl, alkenyl, alkynyl, alkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkylthioalkyl, alkylthioalkenyl, alkylthioalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, alkoxycarbonylalkynyl, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, cycloalkylalkenyl, cycloalkenylalkenyl, cycloalkylalkynyl, cycloalkenylalkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, SO2NR3R4 and NR3R4, aryl or aryl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, carboxy, alkoxycarbonyl, S02NR3R4 and NR3R4, aralkyl, aralkenyl, aralkynyl or aralkyl, aralkenyl, aralkynyl substituted with one or more substituents

independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, S02NR3R4 and NR3R4, arylcarbonyl, aralkylcarbonyl, aralkenylcarbonyl, aralkynylcarbonyl, aroxycarbonylalkyl, or arylcarbonyl, aralkylcarbonyl, aralkenylcarbonyl, aralkynylcarbonyl, aroxycarbonylalkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, S02NR3R4 and NR3R4, heteroaryl or heteroaryl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroaralkyl, heteroaralkenyl, heteroaralkynyl or heteroaralkyl, heteroaralkenyl, heteroaralkynyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, heteroarylcarbonyl, heteroaralkylcarbonyl, heteroaralkenylcarbonyl, heteroaralkynylcarbonyl, heteroaroxycarbonylalkyl, heterocyclylcarbonyl, heterocyclyloxycarbonylalkyl, or heteroarylcarbonyl, heteroaralkylcarbonyl, heteroaralkenylcarbonyl, heteroaralkynylcarbonyl, heteroaroxycarbonylalkyl, heterocyclylcarbonyl, heterocyclyloxycarbonylalkyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, haloalkoxy, SO2NR3R4 and NR3R4, R3, R4 and R5 are each independently a hydrogen atom, alkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkenylalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxyalkyl, alkenyl, alkynyl, or alkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, cycloalkenylalkyl, cycloalkenylalkenyl, cycloalkenylalkynyl, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, alkoxyalkyl, alkenyl or alkynyl substituted with one or more halo, aryl, aralkyl, aralkenyl, aralkynyl, or aryl, aralkyl, aralkenyl, aralkynyl substituted with one or more substituents independently selected from halo, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy and haloalkoxy, heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, or heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl substituted with one or more substituents

independently selected from halo, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy and haloalkoxy, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, or heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl substituted with one or more substituents independently selected from halo, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy and haloalkoxy, or R3 and R4 taken together with the nitrogen atom to which they are attached form a 5-or 6-membered saturated or unsaturated heterocyclic ring, or A is

wherein each R2, G20, G2l, G30 and G31 are as previously defined, provided that when both m and q are 0, A is

within the definition of RI d is 1, G30, G31, Z3, X3 and t'are as previously defined and Z3 (X3) d (G31) t' is a pharmaceutical moiety wherein Z3 (X3) d (G31) t'-H represents the pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof In a preferred third embodiment of this invention, the pharmaceutical compound is represented by the compound of formula (I) wherein t is 1, m is 1, q is 0, (X') m is a nitrogen atom and ZI (XI) m-H is a pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof.

In another preferred third embodiment of this invention, the pharmaceutical compound is represented by the compound of formula (I) wherein t is 1, m is 1, q is 0, (X1) m is a phosphorous, oxygen or sulfur atom and ZXm-H is a pharmaceutical, or t is 1, m is 0, q is 1, (X2) q is a phosphorous, oxygen or sulfur atom and Z2 (X2) q-[(C=G20)-G2l] t-H is a pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof In another preferred third embodiment of this invention, the pharmaceutical compound is represented by the compound of formula (I) wherein t is 1, m is 0, q is 1, (X2) q is a carbon atom and Z2 (X2) q-[(C=G20)-G2l] t-H is a pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof In another preferred third embodiment of this invention, the pharmaceutical compound is represented by the compound of formula (I) wherein t is 0, m is 1, q is 0, (X) m is a nitrogen, phosphorous, oxygen or sulfur atom and Zl (XI) m-H is a pharmaceutical, or t is 0, m is 0, q is 1, (X2) q is a nitrogen, phosphorous, oxygen, sulfur or carbon atom and Z2 (X2) q-[(C=G20)-G2l] t-H is a pharmaceutical or Z2 (X2) q- [ (C=G)-G'] t is a pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof.

In another preferred third embodiment of this invention, the pharmaceutical compound is represented by the compound of formula (I) wherein t is 0 or 1, m is 1, q is 1, (X1) m is a nitrogen, phosphorous, oxygen or sulfur atom, (X2) q is a nitrogen, phosphorous, oxygen, sulfur or carbon atom, Z' (X') m-H is a pharmaceutical and Z2(X2)q-(C=G20 - G21)t-H or Z2 (X2) q-(C=G20 ^ G2l) t is a pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof In another preferred third embodiment of this invention, the pharmaceutical compound is represented by the compound of formula (I) wherein A is

m and q are 0, ZI (X1)m and Z2(X2) q are non-pharmaceutical moieties, Ru ils wherein G30 is an oxygen atom or a sulfur atom, G31 is an oxygen atom, a sulfur atom or NR3, d is 1, t' is 0 or 1, X3 is an oxygen atom, a sulfur atom, a nitrogen atom, a phosphorous atom or a carbon atom attached to Z3 when t'is 0, a nitrogen atom attached to Z3 when t'is 1 and G31 is NR3, or a carbon atom attached to Z3 when t'is 1 and G31 is an oxygen atom or a sulfur atom, Z3 (X3) d (G31) t' is a pharmaceutical moiety wherein Z3 (X3) d (G31) t-H represents the pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof.

In another preferred third embodiment of this invention, a pharmaceutical compound is represented by formula (I) wherein A is

RI is (d+m+q) is lor2, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof.

In another preferred third embodiment of this invention, a pharmaceutical compound is represented by formula (I) wherein A is RI is both q and t are 1, X2 is a carbon atom, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof In another preferred third embodiment of this invention, a pharmaceutical compound is represented by formula (I) wherein A is

Gl°, G11 and G20 are each independently an oxygen atom or a sulfur atom, G21 is an oxygen atom, a sulfur atom or NR3, XI is an oxygen atom, a sulfur atom, a phosphorous atom or a nitrogen atom attached to Z1, X2 is an oxygen atom, a sulfur atom, a phosphorous atom, a nitrogen atom or a carbon atom attached to Z2, m, q and t are each independently 0 or 1, n is 1 or 2, Zl (X1)m is a pharmaceutical moiety when m is 1 wherein Zl (Xl) m-H represents the pharmaceutical, Z2 (X2) q (C (=G20) G21) t is a pharmaceutical moiety when q is 1 wherein Z2 (X2) q (C (=G20) G21) t or Z2 (X2) q (C (=G20) G2') t-H represents the pharmaceutical, Zl (X1) m, when m is 0, is a hydrogen atom, halo, (C1-C20) alkyl, (C1- (C10) alkylcarbonyloxy (Ci-Cio) alkyl, (C1-C20) alkylcarbonyl, hydroxy (Ci-C2o) alkyl, (C1- Cio) alkylsulfonyl (Ci-Cio) alkyl, (Ci-Cio) alkylcarbonylamino (Ci-Cio) alkyl, arylcarbonylamino (Ci-Cio) alkyl, heteroarylcarbonylamino (Ci-Cio) alkyl, halo (C1- C2o) alkyl, (C2-C2o) alkenyl, halo (C2-C2o) alkenyl, (C1-C10) alkylcarbonylamino (C2- Clo) alkenyl, arylcarbonylamino (C2-Cio) alkenyl, heteroarylcarbonylamino (C2- Cio) alkenyl, (C2-C2o) alkynyl, halo (C2-C2o) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3- C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1- Clo) alkyl, cyclo (C3-Cs) alkyl (C2-Cio) alkenyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3- C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2- Cio) alkynyl, carboxycyclo (C3-C8) alkyl (Ci-Cio) alkyl, carboxy (C3-C8) cycloalkyl (C2- Cio) alkenyl, carboxycyclo (C3-C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2- Cio) alkenyl, carboxycyclo (C3-C8) alkyl (C2-Cio) alkynyl, carboxycyclo (C3-C8) alkenyl (C2- Cio) alkynyl, (Ci-Cio) alkoxy (Ci-Cio) alkyl, (C1-C5) alkoxy (Ci-C5) alkoxy (Ci-Cio) alkyl, (C1- Clo) alkoxy (C2-C10) alkenyl, (Ci-Cio) alkoxy (C2-C10) alkynyl, (C1-C10) alkoxycarbonyl, (Ci- Cio) alkoxycarbonyl (Ci-Cio) alkyl, (Ci-Cio) alkoxycarbonyl (C2-C10) alkenyl, (Ci- Cio) alkoxycarbonyl (C2-C10) alkynyl, halo (Ci-Cio) alkoxy (Ci-Cio) alkyl, halo (Ci-

Cio) alkoxy (C2-Cio) alkenyl, halo (C1-C10) alkoxy (C2-Cio) alkynyl, (Ci-Cio) alkylthio (Ci- Cio) alkyl, (C1-C10) alkylthio (C2-Cio) alkenyl, (C1-C10) alkylthio (C2-Cio) alkynyl, halo (Cl- Cio) alkylthio (C1-C10) alkyl, halo (Ci-Cio) alkylthio (C2-C10) alkenyl, halo (Ci- Cio) alkylthio (C2-Cio) alkynyl, SO2NR3R4, NR3R4, OR3, S (O) jR3, carboxy (C1-C20) alkyl, carboxy (C2-C2o) alkenyl, carboxy (C2-C2o) alkynyl, aryl, arylcarbonyl, arylcarbonyl (C1- Cio) alkyl, aroxycarbonyl, aroxycarbonyl (Ci-Cio) alkyl, or aryl, arylcarbonyl, arylcarbonyl (C1-C10) alkyl, aroxycarbonyl, aroxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, (Ci-Cio) alkyl, (Ci-Cio) alkylsulfonyl (C1-C10) alkyl, (C1-C10) alkylsulfonyl, thiocyanato, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Clo) alkoxy, S02NR3R4, and NR3R4, ar (Ci- Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, ar (Ci-Cio) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (C2- Clo) alkenylcarbonyl, ar (C2-C10) alkenylcarbonyl (Ci-Cio) alkyl, or ar (Ci-Cio) alkyl, ar (C2- Cio) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, ar (Ci- Cio) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (C2-C10) alkenylcarbonyl, ar (C2-C10) alkenylcarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, cyclo (C3- C8) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, S02NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Clo) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, or heteroaryl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (C1- Clo) alkyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci- Clo) alkyl, halo (C2-C10) alkenyl, halo (C2-Clo) alkynyl, (Ci-Co) alkoxy, halo (C1-C10) alkoxy and NR3R4, heteroar (Ci-Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-Cio) alkynyl, heteroar (C1-C10) alkylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, heteroar (C2-C10) alkenylcarbonyl, heteroar (C2-Clo) alkenylcarbonyl (C1-C10) alkyl, or heteroar (Ci-Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl, heteroar (Ci- Clo) alkylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, heteroar (C2- Clo) alkenylcarbonyl, heteroar (C2-C10) alkenylcarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro,

(C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-Clo) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4, heterocyclyl, heterocyclyl (C1-C10) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2- Cio) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl, or heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-C10) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (Cl-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4 wherein j is 0, 1 or 2, Z2 is a hydrogen atom, (C1-C20) alkyl, (Ci-Cio) alkylcarbonyloxy (C1- Cio) alkyl, (C1-C20) alkylcarbonyl, (C1-C20) alkenylcarbonyl, (C1-C20) alkynylcarbonyl, hydroxy (C1-C20) alkyl, (C1-C10) alkylsulfonyl (Ci-Cio) alkyl, (Ci- C10) alkylcarbonylamino (Cl-Cio) alkyl, arylcarbonylamino (Ci-Clo) alkyl, heteroarylcarbonylamino (Ci-Clo) alkyl, halo (C1-C20) alkyl, (C2-C2o) alkenyl, halo (C2- C2o) alkenyl, (Ci-Cio) alkylcarbonylamino (C2-Cio) alkenyl, arylcarbonylamino (C2- Cio) alkenyl, heteroarylcarbonylamino (C2-Cio) alkenyl, (C2-C2o) alkynyl, halo (C2- C2o) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Cio) alkenyl, cyclo (C3-C8) alkenyl (Ci-Clo) alkyl, cyclo (C3-C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxycyclo (C3- Cs) alkyl (C1-C10) alkyl, carboxy (C3-C8) cycloalkyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkyl (C2-C10) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkynyl, (C1-C10) alkoxy (C1- Clo) alkyl, (Ci-C5) alkoxy (Ci-C5) alkoxy (C1-C10) alkyl, (C1-C10) alkoxy (C2-C10) alkenyl, (C1- Clo) alkoxy (C2-Cio) alkynyl, (C1-C10) alkoxycarbonyl, (Ci-Cio) alkoxycarbonyl (C1- Clo) alkyl, (Ci-Cio) alkoxycarbonyl (C2-C10) alkenyl, (Ci-Cio) alkoxycarbonyl (C2- Clo) alkynyl, halo (Ci-Cio) alkoxy (Ci-Cio) alkyl, halo (Ci-Cio) alkoxy (C2-C10) alkenyl, halo (Ci-Cio) alkoxy (C2-C10) alkynyl, (C1-C10) alkylthio (C1-C10) alkyl, (C1-C10) alkylthio (C2- Cio) alkenyl, (Cl-Clo) alkylthio (C2-C10) alkynyl, halo (Ci-Cio) alkylthio (Ci-Cio) alkyl, halo (Ci-Cio) alkylthio (C2-C10) alkenyl, halo (Ci-Cio) alkylthio (C2-C10) alkynyl, SO2NR3R4,

NR3R4, carboxy (C1-C20) alkyl, carboxy (C2-C2o) alkenyl, carboxy (C2-C2o) alkynyl, di (C1- Cio) alkoxyphosphoryl (Ci-Cio) alkyl, aryl, aryl substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, (Ci-Cio) alkyl, (Ci-Cio) alkylsulfonyl (C1-C10) alkyl, (Ci-Cio) alkylsulfonyl, thiocyanato, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Clo) alkenyl, halo (C2-C10) alkynyl, (Ci- Clo) alkoxy, halo (C1-C10) alkoxy, C (=O) OR2, C (=O) SR2, C (=S) OR2, C (=S) SR2, C (=O) NR3R4, C (=S) NR3R4, C (=O) R2, C (=S) R2, C (=N-R3) R2, C (=N-OR3) R2, C (=N- NR3R4) R2, OP (=O) (OR2) 2, SO2NR3R4, NR3R4 and (C1-C10) alkylNR3R4, ar (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-Clo) alkynyl, arcyclo (C3-C8) alkyl, aroxy (C1-C10) alkyl, or ar (C1- Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (C1- Clo) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (Ci- Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy and NR3R4, heteroar (C1- Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-Cio) alkynyl, or heteroar (Cl-Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, (C1- Cio) alkylcarbonyl (Ci-Cio) alkyl, (C2-Cio) alkenylcarbonyl (Ci-Clo) alkyl, (C2- Cio) alkynylcarbonyl (Ci-Cio) alkyl, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-C10) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl, arylcarbonyl, arylcarbonyl (Ci-Cio) alkyl, ar (C1- Cio) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl, aroxycarbonyl (Ci-Cio) alkyl, ar (Ci-Cio) alkoxycarbonyl, ar (Ci-Cio) alkoxycarbonyl (Ci- Clo) alkyl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, or heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Clo) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (C1-C10) alkyl, heterocyclyloxycarbonyl,

heterocyclyloxycarbonyl (Ci-Clo) alkyl, arylcarbonyl, arylcarbonyl (C1-C10) alkyl, ar (C1- Clo) alkylcarbonyl, ar (C1-C10) alkylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl, aroxycarbonyl (Ci-Cio) alkyl, ar (Ci-Cio) alkoxycarbonyl, ar (Ci-Cio) alkoxycarbonyl (Cl- Cio) alkyl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (Cl-Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, and C (=N- G22) R2 when q is 0 and t is 1, G22 is OR3, OCOR3, S (O) jR3, OS (O) jR3, NR3R4, OSO2NR3R4, OP (=O) OR3NR3R4, OP (=O) (OR3) 2 or N=CR3R4, j is 0, 1 or 2, Z2 (X2) q is halo, NR3R4, {(NR3R4R5) + M-}, OR3, S (O) jR3 or SO2NR3R4 when both q and t are 0 wherein M-is halo, hydroxy, (Ci-Cs) alkoxy or the anion of a carboxylic acid and j is 0, 1 or 2, Rl is wherein G30 is an oxygen atom or a sulfur atom, G3'is an oxygen atom, a sulfur atom or NR3, t'and d are each independently 0 or 1, X3 is an oxygen atom, a sulfur atom, a nitrogen atom, a phosphorous atom or a carbon atom attached to Z3 when t'is 0, a nitrogen atom attached to Z3 when t'is 1 and G31 is NR3, or a carbon atom attached to Z3 when t'is 1 and G31 is an oxygen atom or a sulfur atom, Z3 (X3) d (G31) t' is a pharmaceutical moiety when d is 1 wherein Z3 (X3) d (G3l) t'-H represents the pharmaceutical, Z3 (X3) d, when d is 0 and t'is 1, is a hydrogen atom, (C1-C20) alkyl, (Cl- Cio) alkylcarbonyloxy (Ci-Cio) alkyl, (C1-C20) alkylcarbonyl, (Ci-Cio) alkylcarbonyl (C1- Cio) alkyl, hydroxy (Ci-C2o) alkyl, (Ci-Cio) alkylsulfonyl (Ci-Cio) alkyl, (C1- Clo) alkylcarbonylamino (Cl-Clo) alkyl, arylcarbonylamino (Ci-Clo) alkyl, heteroarylcarbonylamino (Ci-Cio) alkyl, acetylamino (C1-C10) alkyl, halo (C1-C20) alkyl,

(C2-C10) alkenyl, (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl, acetylamino (C2-C10) alkenyl, halo (C2-Cio) alkenyl, (C2-Cio) alkynyl, (C2-C10) alkynylcarbonyl(C1-C10) alkyl, halo (C2- Cio) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Clo) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, carboxycyclo (C3- C8) alkyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkyl (C2-C10) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-C10) alkynyl, (Ci-Cio) alkoxy (C1- Cio) alkyl, (Ci-Cio) alkoxy (C1-C10) alkoxy (Ci-Clo) alkyl, (C1-C10) alkoxy (C2-C10) alkenyl, (C1-C10) alkoxy (C2-Cio) alkynyl, (C1-C10) alkoxycarbonyl (C1-C10) alkyl, (C1- Clo) alkoxycarbonyl (C2-C10) alkenyl, (Ci-Cio) alkoxycarbonyl (C2-C10) alkynyl, halo (Ci- Cio) alkoxy (C1-C10) alkyl, halo (C1-C10) alkoxy (C2-C10) alkenyl, halo (C1-C10) alkoxy (C2- Cio) alkynyl, (C1-C10) alkylthio (C1-C10) alkyl, (Ci-Cio) alkylthio (C2-C10) alkenyl, (C1- Cio) alkylthio (C2-C10) alkynyl, halo (Ci-Cio) alkylthio (C1-C10) alkyl, halo (Ci- Cio) alkylthio (C2-Cio) alkenyl, halo (C1-C10) alkylthio (C2-C10) alkynyl, carboxy (Ci- C2o) alkyl, carboxy (c2-clo) alkenyl, carboxy (C2-Cio) alkynyl, NR3R4, OR3, S (O) jR3, aryl, arylcarbonyloxy (Ci-Clo) alkyl, arylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl (C1-C10) alkyl, or aryl, arylcarbonyloxy (Ci-Cio) alkyl, arylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl (Ci- Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, (Ci-Cio) alkyl, (Ci-Cio) alkylsulfonyl (C1- Clo) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Cl-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, ar (Ci- Clo) alkyl, ar (Ci-Cio) alkylcarbonyloxy (Ci-Cio) alkyl, ar (Ci-Cio) alkylcarbonyl (C1- Cio) alkyl, ar (Ci-Cio) alkoxycarbonyl (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, or ar (Ci-Cio) alkyl, ar (C1- Cio) alkylcarbonyloxy (Ci-Cio) alkyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (Ci- Cio) alkoxycarbonyl (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3- C8) alkyl, aroxy (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, (C2- Clo) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyloxy (C1-C10) alkyl, heteroarylcarbonyl (Ci-Cio) alkyl,

heteroaroxycarbonyl (Cl-Cio) alkyl, or heteroaryl, heteroarylcarbonyloxy (C1-C10) alkyl, heteroarylcarbonyl (Cl-Clo) alkyl, heteroaroxycarbonyl (Cl-Clo) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4, heteroar (C1-C10) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl, or heteroar (Ci-Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2- Clo) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclylcarbonyloxy (Ci-Cio) alkyl, hetercyclylcarbonyl (C1- Clo) alkyl, heterocyclyloxycarbonyl (C1-C10) alkyl, or heterocyclyl, heterocyclylcarbonyloxy (C1-C10) alkyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, (C2- Clo) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-Cio) alkenyl, halo (C2- C10)alkynyl, (C1-C10)alkoxy, halo(C1-C10)alkoxy, SO2NR3R4 and NR3R4, wherein j is 0, 1 or 2, Z3 (X3) d is halo, NR3R4, OR3, N (R3)-N=CR3R4, S (O) jR3 or SO2NR3R4 when both d and t'are 0 and j is 0, 1 or 2, each R2 is independently a hydrogen atom, (C1-C20) alkyl, (C2-C10) alkenyl, (C2- Clo) alkynyl, (Ci-Cio) alkoxy (C1-C10) alkyl, (Cl-Clo) alkoxy (C2-C10) alkenyl, (C1- Cio) alkoxy (C2-C10) alkynyl, (Ci-Cio) alkylthio (Ci-Cio) alkyl, (Ci-Cio) alkylthio (C2- Clo) alkenyl, (C1-C10) alkylthio (C2-C10) alkynyl, carboxy, a carboxylate salt, carboxy (C1- C20) alkyl, carboxy (C2-C2o) alkenyl, carboxy (C2-C2o) alkynyl, (C1-C20) alkoxycarbonyl, (Cl- Clo) alkoxycarbonyl (Ci-Cio) alkyl, (C1-C10) alkoxycarbonyl (C2-C10) alkenyl, (C1- Clo) alkoxycarbonyl (C2-Cio) alkynyl, (Ci-C2o) alkylcarbonyl, (C2-C2o) alkenylcarbonyl, (C2-C2o) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci- Cio) alkyl, cyclo (C3-C8) alkenyl (C1-C10)alkyl, cyclo(C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3- C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2- Cio) alkynyl, heterocyclyl, heterocyclyl (C1-C10) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-Cio) alkynyl, or (C1-C20) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, (C1- Cio) alkoxy (C1-C10) alkyl, (C1-C10) alkoxy (C2-Cio) alkenyl, (C1-C10) alkoxy (C2-C10) alkynyl,

(Ci-Cio) alkylthio (Cl-Clo) alkyl, (C1-C10) alkylthio (C2-C10) alkenyl, (C1-C10) alkylthio (C2- Clo) alkynyl, carboxy (C1-C20) alkyl, carboxy (C2-Cio) alkenyl, carboxy (C2-Cio) alkynyl, (C1- C2o) alkoxycarbonyl, (C1-C10) alkoxycarbonyl (Cl-Cio) alkyl, (C1-C10) alkoxycarbonyl (C2- Clo) alkenyl, (Ci-Co) alkoxycarbonyl (C2-Cio) alkynyl, (C1-C20) alkylcarbonyl, (C2- Cio) alkenylcarbonyl, (C2-Cio) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Cio) alkenyl, cyclo (C3-C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, heterocyclyl, heterocyclyl (Ci-Clo) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, SO2NR3R4 and NR3R4, aryl or aryl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2- Clo) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Cl-Cio) alkoxy, carboxy, (Cl- C4) alkoxycarbonyl, S02NR3R4 and NR3R4, ar (C1-C10) alkyl, ar (C2-C10) alkenyl, ar (C2- Clo) alkynyl, or ar (C1-C10) alkyl, ar (C2-Cio) alkenyl, ar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Clo) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, arylcarbonyl, ar (C1-C10) alkylcarbonyl, ar (C2-C10) alkenylcarbonyl, ar (C2-Cio) alkynylcarbonyl, aroxycarbonyl (Ci-Clo) alkyl, or arylcarbonyl, ar (Ci-Cio) alkylcarbonyl, ar (C2- Cio) alkenylcarbonyl, ar (C2-Cio) alkynylcarbonyl, aroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (C1- Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2- Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (Ci- Cio) alkoxy, halo (Ci-Cio) alkoxy and NR3R4, heteroar (Ci-Cio) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-C10) alkynyl or heteroar (Ci-Cio) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci- Clo) alkoxy, SO2NR3R4 and NR3R4, heteroarylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl,

heteroar (C2-Cio) alkenylcarbonyl, heteroar (C2-C10) alkynylcarbonyl, heteroaroxycarbonyl (C1-C10) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (C1- Cio) alkyl, or heteroarylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl, heteroar (C2- Cio) alkenylcarbonyl, heteroar (C2-C10) alkynylcarbonyl, heteroaroxycarbonyl (Ci- Cio) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4, or RI and R2 taken together with the carbon atom to which they are attached form a 5-7 membered saturated or unsaturated ring, R3, R4 and R5 are each independently a hydrogen atom, (C1-C20) alkyl, cyclo (C3- C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1-C10) alkyl, cyclo (C3-C8) alkyl (C2- Cio) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxy (Ci- C2o) alkyl, carboxy (C2-C10) alkenyl, carboxy (C2-Cio) alkynyl, (C1-C10) alkoxy (Cl-Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, or (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, cyclo (C3- C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2-C10) alkenyl, cyclo (C3- C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, carboxy (C1-C20) alkyl, carboxy (C2- Clo) alkenyl, carboxy (C2-Cio) alkynyl, (C1-C10) alkoxy (Ci-Cio) alkyl, (C2-Cio) alkenyl or (C2-Cio) alkynyl substituted with one or more halo, aryl, ar (Ci-Cio) alkyl, ar (C2- Cio) alkenyl, ar (C2-C10) alkynyl or aryl, ar (C1-C10) alkyl, ar (C2-C10) alkenyl, ar (C2- Cio) alkynyl substituted with one or more substituents independently selected from halo, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Cl-Cio) alkyl, halo (C2- Clo) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy and halo (Ci-Cio) alkoxy, heteroaryl, heteroar (Ci-Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl or heteroaryl, heteroar (Ci-Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, (Ci-Cio) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy and halo (C1-C10) alkoxy, heterocyclyl, heterocyclyl (C1- Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-C10) alkynyl, or heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-C10) alkynyl substituted with one or more substituents independently selected from halo,

hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Cl- Clo) alkyl, halo (C2-Clo) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Ciu) alkoxy, SO2NR3R4 and NR3R4, or R3 and R4 taken together with the nitrogen atom to which they are attached form a 5-or 6-membered saturated or unsaturated heterocyclic ring, or A is wherein each R2, G20, G2', G30 and G31 are as previously defined, provided that when both m and q are 0, A is. within the definition of R d is 1, G30, G31, Z3, X3 and t'are as previously defined and Z3 (X3) d (G31) t' is a pharmaceutical moiety wherein Z3 (X3) d (G31) t'-H represents the pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof In a fourth embodiment of this invention, a human health pharmaceutical compound is represented by formula (I) wherein A is

Gl°, G"and G20 are each independently an oxygen atom or a sulfur atom, G21 is an oxygen atom, a sulfur atom or NR3, XI is an oxygen atom, a sulfur atom, a phosphorous atom or a nitrogen atom attached to Zl, X2 is an oxygen atom, a sulfur atom, a phosphorous atom, a nitrogen atom or a carbon atom attached to Z2, m is 1, q and t are each independently 0 or 1, n is 1 or 2, Zl (Xl) m is a pharmaceutical moiety when m is 1 wherein ZI (Xl) m-H represents the pharmaceutical selected from the group consisting of aletamine, amoxapine, amoxicillin, amphetamine, atorvastatin, benazepril, betahistine, bupropion, carbamazepam, cefachlor, cefadroxil, centerdrine, chlordiazepoxide, chloroquine, ciprofloxacin, clonazepam, clonidine, clozapine, demethylimipramine, deprenil, desipramine, enoxacin, etintidine, fenfluramine, fludorex, fluoxetine hydrochloride, gabapentin, lansoprazole, mepivacaine, methylphenidate, molindone, naphazoline, norfloxacin, olanzapine, omeprazole, oxmetidine, paroxetine, phentermine, pimozide, piroxicam, posaconazole, prazosin, procaine, propanolol, proparacaine, quinapril, sertraline, sulfamethizole, tacrine, temazepam, terazosin, tetrahydrazoline, thiabendazole, timolol, tocainide, tolazoline, tramadol, triamterene, troglitazone and xylometazoline when X'is a nitrogen atom, or the pharmaceutical selected from the group consisting of atorvastatin, atropine, bicalutamide, buprenorphine, cafiminol, clobesol, deprenil, doxazosin, enalapril, famciclovir, fluconazole, fluticasone propionate, genaconazole, haloperidol, hydroxyitraconazole, hydroxyzine, iodoquinol, loperidine hydrochloride, lorazepam, lovastatin, mazindol, metronidazole, oxycodone, quinidine, scopolamine, simvastatin, tramadol and voriconazole when Xl is an oxygen atom, or the pharmaceutical methimazole when XI is a sulfur atom,

Z2 (X2)q(C(=G20)G21)t is a pharmaceutical moiety when q is 1 wherein Z2 (X2) q (C (=G20) G21) t or Z2 (X2) q (C (=G20) G21)t-H represents the pharmaceutical, Z2 (X2) q is a hydrogen atom, (C1-C20) alkyl, (C1-C10) alkylcarbonyloxy (C1- Cio) alkyl, (C1-C20) alkylcarbonyl, (C1-C20) alkenylcarbonyl, (Ci-C2o) alkynylcarbonyl, hydroxy (Ci-C2o) alkyl, (Cl-Clo) alkylsulfonyl (Ci-Cio) alkyl, (C1- Cio) alkylcarbonylamino (Ci-Clo) alkyl, arylcarbonylamino (Ci-Clo) alkyl, heteroarylcarbonylamino (C1-C10) alkyl, halo (Ci-C2o) alkyl, (C2-C2o) alkenyl, halo (C2- C2o) alkenyl, (Ci-Cio) alkylcarbonylamino (C2-Cio) alkenyl, arylcarbonylamino (C2- Clo) alkenyl, heteroarylcarbonylamino (C2-Cio) alkenyl, (C2-C2o) alkynyl, halo (C2- C2o) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Cio) alkenyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxycyclo (C3- C8) alkyl (C1-C10) alkyl, carboxy (C3-C8) cycloalkyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkenyl (C1-C10) alkyl, carboxycyclo (C3-C8) alkenyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkyl (C2-C10) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-Clo) alkynyl, (C1-C10) alkoxy (C1- Cio) alkyl, (C1-C5) alkoxy (Ci-C5) alkoxy (Ci-Cio) alkyl, (C1-C10) alkoxy (C2-C10) alkenyl, (C1- Cio) alkoxy (C2-C10) alkynyl, (C1-C10) alkoxycarbonyl, (C1-C10) alkoxycarbonyl (Ci- Clo) alkyl, (Ci-Cio) alkoxycarbonyl (C2-Cio) alkenyl, (Ci-Cio) alkoxycarbonyl (C2- Clo) alkynyl, halo (C-Clo) alkoxy (Ci-Cio) alkyl, halo (Ci-Cio) alkoxy (C2-C10) alkenyl, halo (Ci-Cio) alkoxy (C2-C10) alkynyl, (Ci-Cio) alkylthio (Ci-Cio) alkyl, (Ci-Cio) alkylthio (C2- Cio) alkenyl, (C1-C10) alkylthio (C2-C10) alkynyl, halo (Ci-Cio) alkylthio (Cl-Cio) alkyl, halo (Ci-Cio) alkylthio (C2-C10) alkenyl, halo (Ci-Cio) alkylthio (C2-C10) alkynyl, S02NR3R4, NR3R4, carboxy (C1-C20) alkyl, carboxy (C2-C20) alkenyl, carboxy (C2-C20) alkynyl, di (Ci- Cio) alkoxyphosphoryl (Ci-Cio) alkyl, aryl, aryl substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, (Ci-Cio) alkyl, (C1-C10) alkylsulfonyl (C1-C10) alkyl, (C1-C10) alkylsulfonyl, thiocyanato, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1- Cio) alkoxy, halo (Ci-Cio) alkoxy, C (=O) OR2, C (=O) SR2, C (=S) OR2, C (=S) SR2, C (=O) NR3R4, C (=S) NR3R4, C (=O) R2, C (=S) R2, C (=N-R3) R2, C (=N-OR3) R2, C (=N- NR3R4) R2, OP (=O) (OR2) 2, SO2NR3R4, NR3R4 and (Ci-Cio) alkylNR3R4, ar (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, or ar (Ci- Clo) alkyl, ar (C2-C10) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl

substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, cyclo (C3-Cs) alkyl, (C2-Cio) alkenyl, (C2-C10)alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci- Cio) alkoxy, S02NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (Cl- Cio) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (Ci-Clo) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Cl-Cio) alkoxy and NR3R4, heteroar (Ci- Cio) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl, or heteroar (Ci-Cio) alkyl, heteroar (C2-Clo) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Clo) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-Cio) alkenyl, halo (C2- Cio) alkynyl, (Cl-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, (Cl- Clo) alkylcarbonyl (C1-C10) alkyl, (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl, (C2- C10)alkynylcarbonyl(C1-C10)alkyl, heterocyclyl, heterocyclyl (Ci-Clo) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Cio) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (C1-C10) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl, arylcarbonyl, arylcarbonyl (Cl-Clo) alkyl, ar (Ci- Clo) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl, aroxycarbonyl (C1-C10) alkyl, ar (C1-C10) alkoxycarbonyl, ar (Cl-Cio) alkoxycarbonyl (C1- Cio) alkyl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (C1-C10) alkyl, or heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Clo) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (Ci-Clo) alkyl, arylcarbonyl, arylcarbonyl (Ci-Clo) alkyl, ar (C1- C io) alkylcarbonyl, ar (Ci-Clo) alkylcarbonyl (C1-C10)alkyl, aroxycarbonyl, aroxycarbonyl (Ci-Cio) alkyl, ar (C1-C10) alkoxycarbonyl, ar (Ci-Cio) alkoxycarbonyl (Ci- Cio) alkyl, heteroarylcarbonyl, heteroarylcarbonyl (C1-C10) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2- Clo) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, and C (=N- G22) R2 when q is 0 and t is 1,

G22 is OR3, OCOR3, S (O) jR3, OS (O) jR3, NR3R4, OSO2NR3R4, OP (=O) OR3NR3R4, OP (=O) (OR3) 2 or N=CR3R4, j is 0, 1 or 2, Z2 (X2) q is halo, NR3R4, {(NR3R4R5)+ M-}, OR3, S (O) jR3 or SO2NR3R4 when both q and t are 0 wherein M-is halo, hydroxy, (C1-C8) alkoxy or the anion of a carboxylic acid and j is 0, 1 or 2, RI is wherein G30 is an oxygen atom or a sulfur atom, G31 is an oxygen atom, a sulfur atom or NR3, t'and d are each independently 0 or 1, X3 is an oxygen atom, a sulfur atom, a nitrogen atom, a phosphorous atom or a carbon atom attached to Z3 when t'is 0, a nitrogen atom attached to Z3 when t'is 1 and G3'is NR3, or a carbon atom attached to Z3 when t'is 1 and G31 is an oxygen atom or a sulfur atom, Z3 (X3) d (G31) t is a pharmaceutical moiety when d is 1 wherein Z3 (X3) d (G3') t-H represents the pharmaceutical, Z3 (X3) d, when d is 0 and t'is 1, is a hydrogen atom, (C1-C20) alkyl, (C1- Cio) alkylcarbonyloxy (Ci-Cio) alkyl, (C1-C20) alkylcarbonyl, (Ci-Cio) alkylcarbonyl (C1- Clo) alkyl, hydroxy (Ci-C2o) alkyl, (Ci-Cio) alkylsulfonyl (Ci-Cio) alkyl, (C1- Cio) alkylcarbonylamino (C1-C10) alkyl, arylcarbonylamino (C1-C10) alkyl, heteroarylcarbonylamino (Ci-Cio) alkyl, acetylamino (Ci-Cio) alkyl, halo (C1-C20) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl, acetylamino (C2-Cio) alkenyl, halo (C2-C10) alkenyl, (C2-Cio) alkynyl, (C2-Cio) alkynylcarbonyl (Ci-Cio) alkyl, halo (C2- Clo) alkynyl, cyclo (C3-C8) alkyl, cyclo (Cs-C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1-C10) alkyl, cyclo (C3-C8) alkyl (C2- Cio) alkenyl, cyclo (C3-C8) alkenyl (Cl-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-Clo) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxycyclo (C3- C8) alkyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkyl (C2-C10) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkynyl, (C1-C10) alkoxy (C1-

Cio) alkyl, (C1-C10) alkoxy (C1-C10)alkoxy(C1-C10) alkyl, (C1-C10)alkoxy(C2-C10) alkenyl, (C-Clo) alkoxy (C2-C10) alkynyl, (Ci-C : o) alkoxycarbonyl (Ci-Clo) alkyl, (C1- Cio) alkoxycarbonyl (C2-Cio) alkenyl, (C1-C10) alkoxycarbonyl (C2-C10) alkynyl, halo (Ci- Cio) alkoxy (Ci-Cio) alkyl, halo (Ci-Cio) alkoxy (C2-Cio) alkenyl, halo (Ci-Cio) alkoxy (C2- Cio) alkynyl, (C1-C10) alkylthio (C1-C10) alkyl, (C1-C10) alkylthio (C2-C10) alkenyl, (C1- Clo) alkylthio (C2-Cio) alkynyl, halo (Ci-Cio) alkylthio (Ci-Cio) alkyl, halo (C1- Clo) alkylthio (C2-Cio) alkenyl, halo (C1-C10) alkylthio (C2-C10) alkynyl, carboxy (C1- C2o) alkyl, carboxy (C2-C10) alkenyl, carboxy (C2-C10) alkynyl, NR3R4, OR3, S (O) jR3, aryl, arylcarbonyloxy (Ci-Cio) alkyl, arylcarbonyl (C1-C10) alkyl, aroxycarbonyl (C1-C10) alkyl, or aryl, arylcarbonyloxy (C1-C10) alkyl, arylcarbonyl (Cl-Cio) alkyl, aroxycarbonyl (C1- Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, (C1-C10) alkyl, (Ci-Cio) alkylsulfonyl (Ci- Clo) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, ar (C1- Clo) alkyl, ar (C1-C10) alkylcarbonyloxy (Ci-Cio) alkyl, ar (C1-C10) alkylcarbonyl (Cl- Clo) alkyl, ar (Ci-Cio) alkoxycarbonyl (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (C1-C10) alkyl, or ar (Ci-Clo) alkyl, ar (C1- Cio) alkylcarbonyloxy (Ci-Clo) alkyl, ar (C1-C10)alkylcarbonyl(C1-C10) alkyl, ar (C1- Clo) alkoxycarbonyl (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3- Cs) alkyl, aroxy (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, (C2 Clo) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2- Clo) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyloxy (C1-C10) alkyl, heteroarylcarbonyl (C1-C10) alkyl, heteroaroxycarbonyl (Ci-Cio) alkyl, or heteroaryl, heteroarylcarbonyloxy (Cl-Cio) alkyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heteroar (C1-C10) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl, or heteroar (C1-C10) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-

Cio) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclylcarbonyloxy (C1-C10) alkyl, hetercyclylcarbonyl (C1- Clo) alkyl, heterocyclyloxycarbonyl (C1-C10) alkyl, or heterocyclyl, heterocyclylcarbonyloxy (Ci-Cio) alkyl, heterocyclylcarbonyl (C1-C10) alkyl, heterocyclyloxycarbonyl (Cl-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Clo) alkoxy, S02NR3R4 and NR3R4, wherein j is 0, 1 or 2, Z3 (X3) d is halo, NR3R4, OR3, N (R3)-N=CR3R4, S (O) jR3 or SO2NR3R4 when both d and t'are 0 and j is 0, 1 or 2, each R2 is independently a hydrogen atom, (C1-C20) alkyl, (C2-C10) alkenyl, (C2- Cio) alkynyl, (C1-C10) alkoxy (Ci-Cio) alkyl, (C1-C10) alkoxy (C2-Cio) alkenyl, (Ci- Clo) alkoxy (C2-C10) alkynyl, (C1-C10) alkylthio (Ci-Cio) alkyl, (C1-C10) alkylthio (C2- Clo) alkenyl, (C1-C10) alkylthio (C2-Cio) alkynyl, carboxy, a carboxylate salt, carboxy (C1- C2o) alkyl, carboxy (C2-C2o) alkenyl, carboxy (C2-C2o) alkynyl, (C1-C20) alkoxycarbonyl, (C1- Cio) alkoxycarbonyl (Ci-Cio) alkyl, (C1-C10) alkoxycarbonyl (C2-C10) alkenyl, (C1- Clo) alkoxycarbonyl (C2-C10) alkynyl, (C1-C20) alkylcarbonyl, (C2-C2o) alkenylcarbonyl, (C2-C2o) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci- Cio) alkyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3- C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2- Clo) alkynyl, heterocyclyl, heterocyclyl (C1-C10) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-Cio) alkynyl, or (C1-C20) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, (C1- Cio) alkoxy (Ci-Cio) alkyl, (C1-C10) alkoxy (C2-Cio) alkenyl, (Ci-Cio) alkoxy (C2-Cio) alkynyl, (Ci-Cio) alkylthio (Ci-Cio) alkyl, (C1-C10) alkylthio (C2-Cio) alkenyl, (C1-C10) alkylthio (C2- Clo) alkynyl, carboxy (Ci-C2o) alkyl, carboxy (C2-C10) alkenyl, carboxy (C2-C10) alkynyl, (Ci- C2o) alkoxycarbonyl, (C1-C10) alkoxycarbonyl (Ci-Cio) alkyl, (C1-C10)alkoxycarbonyl(C2- Cio) alkenyl, (Ci-Cio) alkoxycarbonyl (C2-C10) alkynyl, (C1-C20) alkylcarbonyl, (C2- Clo) alkenylcarbonyl, (C2-C10) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1-C10) alkyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3-C8) alkyl (C2- Cio) alkenyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-Clo) alkynyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-C10) alkynyl substituted with one or more

substituents independently selected from halo, cyano, hydroxy, nitro, SO2NR3R4 and NR3R4, aryl or aryl substituted with one or more substituents independently selected from halo, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2- Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, carboxy, (Ci- C4) alkoxycarbonyl, SO2NR3R4 and NR3R4, ar (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2- Cio) alkynyl, or ar (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, arylcarbonyl, ar (Ci-Cio) alkylcarbonyl, ar (C2-Cio) alkenylcarbonyl, ar (C2-C10) alkynylcarbonyl, aroxycarbonyl (C1-C10) alkyl, or arylcarbonyl, ar (Ci-Clo) alkylcarbonyl, ar (C2- Cio) alkenylcarbonyl, ar (C2-C10) alkynylcarbonyl, aroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (C1- Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2- Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1- Cio) alkoxy, halo (Ci-Clo) alkoxy and NR3R4, heteroar (C1-C10) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-Cio) alkynyl or heteroar (Ci-Cio) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (C1- Cio) alkoxy, SO2NR3R4 and NR3R4, heteroarylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl, heteroar (C2-C10) alkenylcarbonyl, heteroar (C2-C10) alkynylcarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (Ci- Clo) alkyl,'or heteroarylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl, heteroar (C2- Cio) alkenylcarbonyl, heteroar (C2-C10) alkynylcarbonyl, heteroaroxycarbonyl (Ci- Cio) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (C2-C10) alkoxy, SO2NR3R4 and NR3R4, or RI

and R2 taken together with the carbon atom to which they are attached form a 5-7 membered saturated or unsaturated ring, R3, R4 and R5 are each independently a hydrogen atom, (C1-C20) alkyl, cyclo (C3- C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxy (C1- C2o) alkyl, carboxy (C2-Cio) alkenyl, carboxy (C2-Cio) alkynyl, (C1-C10) alkoxy (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, or (Ci-Clo) alkyl, cyclo (C3-C8) alkyl, cyclo (C3- C8) alkenyl, cyclo C3-C8) alkyl (C1-C10) alkyl, cyclo (C3-C8) alkyl (C2-C10) alkenyl, cyclo (C3- C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2- Cio) alkenyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxy (C1-C20) alkyl, carboxy (C2- Clo) alkenyl, carboxy (C2-C10) alkynyl, (C1-C10) alkoxy (C1-C10) alkyl, (C2-Cio) alkenyl or (C2-Cio) alkynyl substituted with one or more halo, aryl, ar (Ci-Cio) alkyl, ar (C2- Cio) alkenyl, ar (C2-Cio) alkynyl or aryl, ar (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2- Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2- Clo) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy and halo (Ci-Cio) alkoxy, heteroaryl, heteroar (C1-C10) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl or heteroaryl, heteroar (Ci-Cio) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy and halo (Ci-Cio) alkoxy, heterocyclyl, heterocyclyl (Ci- Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-C10) alkynyl, or heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1- Clo) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Cl-Cio) alkoxy, S02NR3R4 and NR3R4, or R3 and R4 taken together with the nitrogen atom to which they are attached form a 5-or 6-membered saturated or unsaturated heterocyclic ring, or A is wherein each R2, G20, G2', G30 and G31 arE as previously defined, provided that when both m and q are 0, A is

within the definition of RI d is 1, G30, G31, Z3, X3 and t'are as previously defined and Z3 (X3) d (G31) t' is a pharmaceutical moiety wherein Z3 (X3) d (G3l) t-H represents the pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof In a fifth embodiment of this invention, a human health pharmaceutical compound is represented by formula (I) wherein A is

G10, G"and G20 are each independently an oxygen atom or a sulfur atom, G21 is an oxygen atom, a sulfur atom or NR3, XI is an oxygen atom, a sulfur atom, a phosphorous atom or a nitrogen atom attached to Zl,

is is an oxygen atom, a sulfur atom, a phosphorous atom, a nitrogen atom or a carbon atom attached to Z2, m and t are each independently 0 or 1, qis 1, n is 1 or 2, Zl (Xl) m is a pharmaceutical moiety when m is 1 wherein ZI (Xl) m-H represents the pharmaceutical, Z2 (X2) q (C (=G20) Gel) t is a pharmaceutical moiety when q is 1 wherein Z2 (X2) q (C (=G20) G21) t or Z2 (X2) q (C (=G20) G2l) t-H represents the pharmaceutical selected from the group consisting of acrivistine, aliconazole, amiodarone, amitriptyline, amoxapine, amrinone,, astemizole, atropine, becliconazole, benzatropine, benzphetamine, beperiden, bisacodyl, brolaconazole, bromopheniramine, bupivacaine, caffeine, chloroprocaine, citalopram, clemastine, clomiphene, clotrimazole, colchicine, croconazole, cyclobenzaprine, cyclopentolate, cyproheptadine, democonazole, dicodid, dicyclomine, diethylproprion, diphenhydramine, diphenidol, diltiazem, diphenoxylate hydrochloride, doconazole, donezapil hydrochloride, doxapram, doxepin, eberconazole, econazole, fentanyl, fenticonazole, flavoxate, fluazepam, fluconazole, halazepam, hydroxyitraconazole, isoconazole, lansoprazole, levomethadyl, loratadine, mechlorethamine, meperidine, mepivacaine, methadone, methimazole, miconazole, minoxidil, naftifine, nefazodone, neticonazole, nifurantin, omoconazole, orconazole, orphenadrine, oxiconazole, oxybutynin, oxymetazoline, papaverine, parconazole, phenoxybenzamine, pilocarpine, pramoxine, propoxyphene, pyrazinamide, pyroxidine, ravuconazole, retinoic acid, risperidone, sertaconazole, sibutramine sufentanil, sulconazole, tamoxifen, terbinafine, ticlopidine, tioconazole, tolteridine, trihexyphenidyl, troleandomycin, tropicamide, valconazole, verapamil and zinoconazole when X2 is a nitrogen atom, or the pharmaceutical selected from the group consisting of fluconazole, genaconazole, hydroxyitraconazole, iodoquinol, lovastatin, mazindol, metronidazole, posaconazole, voriconazole and warfarin when x2 is an oxygen atom, or the pharmaceutical selected from the group consisting of adapalene, arthrocine, cloxacillin, flurbiprofen, gemfibrozil, hydroxyitraconazole, ibuprofen, indomethacin, ketoprofen, ketorolac, loratadine, monopril, oxaprozin, valproic acid and verapamil when X2 is an carbon atom,

Z' (X1)m, when m is 0, is a hydrogen atom, halo, (C1-C20) alkyl, (Ci- Cto) alkylcarbonyloxy (Ci-Cio) alkyl, (C1-C20) alkylcarbonyl, hydroxy (C1-C20) alkyl, (Cl- Cio) alkylsulfonyl (Ci-Cio) alkyl, (C1-C10) alkylcarbonylamino (Ci-Cio) alkyl, arylcarbonylamino (Cl-Cio) alkyl, heteroarylcarbonylamino (Cl-Cio) alkyl, halo (C1- C2o) alkyl, (C2-C2o) alkenyl, halo (C2-C2o) alkenyl, (Ci-Cio) alkylcarbonylamino (C2- Cio) alkenyl, arylcarbonylamino (C2-Cio) alkenyl, heteroarylcarbonylamino (C2- Cio) alkenyl, (C2-C2o) alkynyl, halo (C2-C2o) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3- Cs) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci- Clo) alkyl, cyclo (C3-C8) alkyl (C2-C10) alkenyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3- C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2- Cio) alkynyl, carboxycyclo (C3-C8) alkyl (C1-C10) alkyl, carboxy (C3-C8) cycloalkyl (C2- Clo) alkenyl, carboxycyclo (C3-C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2- Cio) alkenyl, carboxycyclo (C3-C8) alkyl (C2-Cio) alkynyl, carboxycyclo (C3-C8) alkenyl (C2- Clo) alkynyl, (C1-C10) alkoxy (Ci-Cio) alkyl, (Ci-C5) alkoxy (C1-C5) alkoxy (Ci-Cio) alkyl, (C1- Cio) alkoxy (C2-Cio) alkenyl, (C1-C10) alkoxy (C2-C10) alkynyl, (C1-C10) alkoxycarbonyl, (Ci- Clo) alkoxycarbonyl (C1-C10) alkyl, (C1-C10) alkoxycarbonyl (C2-Cio) alkenyl, (Cl- Cio) alkoxycarbonyl (C2-C10) alkynyl, halo (C1-C10) alkoxy (C1-C10) alkyl, halo (C1- Cio) alkoxy (C2-Cio) alkenyl, halo (Ci-Cio) alkoxy (C2-C10) alkynyl, (Ci-Clo) alkylthio (Cs- Clo) alkyl, (Ci-Cio) alkylthio (C2-C10) alkenyl, (Ci-Cio) alkylthio (C2-C10) alkynyl, halo (Ci- C10) alkylthio (Ci-Cio) alkyl, halo (Ci-Cio) alkylthio (C2-Cio) alkenyl, halo (Ci- Cio) alkylthio (C2-C10) alkynyl, S02NR3R4, NR3R4, OR3, S (O) jR3, carboxy (C1-C20) alkyl, carboxy (C2-C20) alkenyl, carboxy (C2-C20) alkynyl, aryl, arylcarbonyl, arylcarbonyl (C1- Cio) alkyl, aroxycarbonyl, aroxycarbonyl (C1-C10) alkyl, or aryl, arylcarbonyl, arylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl, aroxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, (Cl-Cio) alkyl, (C1-C10) alkylsulfonyl (Cl-Cio) alkyl, (Ci-Cio) alkylsulfonyl, thiocyanato, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2- Clo) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4, and NR3R4, ar (Ci- Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (C1-C10) alkyl, ar (C1-C10) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (C2- Cio) alkenylcarbonyl, ar (C2-C10) alkenylcarbonyl (Ci-Cio) alkyl, or ar (C1-C10) alkyl, ar (C2- Clo) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, ar (C1- Cio) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (C2-Cio) alkenylcarbonyl,

ar (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, cyclo (Cs- Cs) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyl, heteroarylcarbonyl (Cl-Clo) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, or heteroaryl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (Ci- Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (C1- Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy and NR3R4, heteroar (C1-C10) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-C10) alkynyl, heteroar (Ci-Cio) alkylcarbonyl, heteroar (C1-C10) alkylcarbonyl (Ci-Cio) alkyl, heteroar (C2-C10) alkenylcarbonyl, heteroar (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl, or heteroar (Ci-Cio) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl, heteroar (Ci- Cio) alkylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl (C1-C10)alkyl, heteroar (C2- Cio) alkenylcarbonyl, heteroar (C2-Cio) alkenylcarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Cl-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclyl (C1-C10) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2- Clo) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl, or heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-C10) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4 wherein j is 0, 1 or 2, Ru ils

wherein G30 is an oxygen atom or a sulfur atom, G31 is an oxygen atom, a sulfur atom or NR3, t'and d are each independently 0 or 1, X3 is an oxygen atom, a sulfur atom, a nitrogen atom, a phosphorous atom or a carbon atom attached to Z3 when t'is 0, a nitrogen atom attached to Z3 when t'is 1 and G31 is NR3, or a carbon atom attached to Z3 when t'is 1 and G31 is an oxygen atom or a sulfur atom, Z3 (X3) d (G31) t' is a pharmaceutical moiety when d is 1 wherein Z3 (X3) d (G31) t'-H represents the pharmaceutical, Z3 (X3) d, when d is 0 and t'is 1, is a hydrogen atom, (C1-C20) alkyl, (Cl- Clo) alkylcarbonyloxy (Cl-Cio) alkyl, (C1-C20) alkylcarbonyl, (C1-C10) alkylcarbonyl (C1 Clo) alkyl, hydroxy (C1-C20) alkyl, (C1-C10) alkylsulfonyl (Ci-Cio) alkyl, (C1- Cio) alkylcarbonylamino (Ci-Cio) alkyl, arylcarbonylamino (C1-C10) alkyl, heteroarylcarbonylamino (Ci-Cio) alkyl, acetylamino (C1-C10) alkyl, halo (C1-C20) alkyl, (C2-Cio) alkenyl, (C2-C10) alkenylcarbonyl (Ci-Cio) alkyl, acetylamino (C2-Cio) alkenyl, halo (C2-Cio) alkenyl, (C2-C10) alkynyl, (C2-Cio) alkynylcarbonyl (Ci-Cio) alkyl, halo (C2- Clo) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (Ci-Clo) alkyl, cyclo (C3-C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxycyclo (C3- C8) alkyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2-Clo) alkenyl, carboxycyclo (C3- C8) alkyl (C2-Cio) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-C10) alkynyl, (Ci-Cio) alkoxy (Ci- Cio) alkyl, (Ci-Cio) alkoxy (Ci-Cio) alkoxy (Ci-Cio) alkyl, (C1-C10) alkoxy (C2-C10) alkenyl, (C1-C10) alkoxy (C2-C10) alkynyl, (C1-C10) alkoxycarbonyl (C1-C10) alkyl, (C1- Cio) alkoxycarbonyl (C2-C10) alkenyl, (C1-C10) alkoxycarbonyl (C2-C10) alkynyl, halo (C1- Clo) alkoxy (Ci-Cio) alkyl, halo (Ci-Cio) alkoxy (C2-C10) alkenyl, halo (C1-C10) alkoxy (C2- Cio) alkynyl, (C1-C10) alkylthio (Ci-Cio) alkyl, (Ci-Cio) alkylthio (C2-C10) alkenyl, (C1- Clo) alkylthio (C2-Cio) alkynyl, halo (Ci-Cio) alkylthio (Ci-Cio) alkyl, halo (Ci- Clo) alkylthio (C2-C10) alkenyl, halo (C1-C10) alkylthio (C2-C10) alkynyl, carboxy (C1- C2o) alkyl, carboxy (c2-clo) alkenyl, carboxy (C2-Cio) alkynyl, NR3R4, OR3, S (O) jR3, aryl, arylcarbonyloxy (Ci-Cio) alkyl, arylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl (Ci-Cio) alkyl,

or aryl, arylcarbonyloxy (C1-C10) alkyl, arylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl (C1- C10) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, (Ci-Cio) alkyl, (C1-C10) alkylsulfonyl (C1- Cio) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, ar (C1- C10)alkyl, ar (C1-C10) alkylcarbonyloxy (C1-C10)alkyl, ar (C1-C10)alkylcarbonyl(C1- Cio) alkyl, ar (Ci-Cio) alkoxycarbonyl (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, or ar (Ci-Cio) alkyl, ar (Ci- Clo) alkylcarbonyloxy (Ci-Cio) alkyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (Ci- Ciao) alkoxycarbonyl (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3- C8) alkyl, aroxy (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, S02NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyloxy (Ci-Cio) alkyl, heteroarylcarbonyl (Ci-Clo) alkyl, heteroaroxycarbonyl (Ci-Cio) alkyl, or heteroaryl, heteroarylcarbonyloxy (Ci-Cio) alkyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, heteroar (Ci-Clo) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl, or heteroar (C1-C10) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2- Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci-Clo) alkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclylcarbonyloxy (Ci-Cio) alkyl, hetercyclylcarbonyl (Ci- Cio) alkyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl, or heterocyclyl, heterocyclylcarbonyloxy (Ci-Cio) alkyl, heterocyclylcarbonyl (C1-C10) alkyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2- Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, wherein j is 0, 1 or 2,

Z3 (X3) d is halo, NR3R4, OR3, N (R3)-N=CR3R4, S (O) jR3 or SO2NR3R5 when both d and t' are 0 and j is 0, 1 or 2, each R2 is independently a hydrogen atom, (C1-C20) alkyl, (C2-Cio) alkenyl, (C2- Cio) alkynyl, (Ci-Cio) alkoxy (Ci-Cio) alkyl, (C1-C10) alkoxy (C2-Cio) alkenyl, (Ci- Clo) alkoxy (C2-C10) alkynyl, (C1-C10) alkylthio (C1-C10) alkyl, (Ci-Cio) alkylthio (C2- Cio) alkenyl, (C1-C10) alkylthio (C2-Cio) alkynyl, carboxy, a carboxylate salt, carboxy (C1- C2o) alkyl, carboxy (C2-C2o) alkenyl, carboxy (C2-C2o) alkynyl, (C1-C20) alkoxycarbonyl, (C1- Clo) alkoxycarbonyl (Ci-Cio) alkyl, (Ci-Cio) alkoxycarbonyl (C2-C10) alkenyl, (C1- Clo) alkoxycarbonyl (C2-Cio) alkynyl, (C1-C20) alkylcarbonyl, (C2-C2o) alkenylcarbonyl, (C2-C2o) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-Cs) alkenyl, cyclo (C3-C8) alkyl (C1- Cio) alkyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2-C10) alkenyl, cyclo (C3- C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2- Clo) alkynyl, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-Cio) alkynyl, or (C1-C20) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, (C1- Cio) alkoxy (Ci-Cio) alkyl, (C1-C10) alkoxy (C2-Cio) alkenyl, (Ci-Cio) alkoxy (C2-C10) alkynyl, (C1-C10) alkylthio (Ci-Cio) alkyl, (C1-C10) alkylthio (C2-Cio) alkenyl, (C1-C10) alkylthio (C2- Cio) alkynyl, carboxy (C1-C20) alkyl, carboxy (C2-C10) alkenyl, carboxy (C2-C10) alkynyl, (Cl- C2o) alkoxycarbonyl, (Ci-Cio) alkoxycarbonyl (Ci-Clo) alkyl, (C1-C10)alkoxycarbonyl(C2- Cio) alkenyl, (C1-C10) alkoxycarbonyl (C2-Cio) alkynyl, (Ci-C2o) alkylcarbonyl, (C2- Cio) alkenylcarbonyl, (C2-C10) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (Ci-Clo) alkyl, cyclo (C3-C8) alkyl (C2- Cio) alkenyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, SO2NR3R4 and NR3R4, aryl or aryl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2- Clo) alkenyl, halo (C2-Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Clo) alkoxy, carboxy, (C1- C4) alkoxycarbonyl, SO2NR3R4 and NR3R4, ar (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2- Clo) alkynyl, or ar (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, arylcarbonyl,

ar (Ci-Cio) alkylcarbonyl, ar (C2-C10) alkenylcarbonyl, ar (C2-C10)alkynylcarbonyl, aroxycarbonyl (Ci-Cio) alkyl, or arylcarbonyl, ar (Ci-Cio) alkylcarbonyl, ar (C2- Clo) alkenylcarbonyl, ar (C2-Cio) alkynylcarbonyl, aroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (Ci- Clo) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2- Clo) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (Cl- Cio) alkoxy, halo (Ci-Cio) alkoxy and NR3R4, heteroar (Ci-Cio) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-Cio) alkynyl or heteroar (Ci-Cio) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci- Cio) alkoxy, SO2NR3R4 and NR3R4, heteroarylcarbonyl, heteroar (Ci-Clo) alkylcarbonyl, heteroar (C2-Cio) alkenylcarbonyl, heteroar (C2-Cio) alkynylcarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (C1- Cio) alkyl, or heteroarylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl, heteroar (C2- Cio) alkenylcarbonyl, heteroar (C2-Cio) alkynylcarbonyl, heteroaroxycarbonyl (Ci- Cio) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, or RI and R2 taken together with the carbon atom to which they are attached form a 5-7 membered saturated or unsaturated ring, R3, R4 and R5 are each independently a hydrogen atom, (C1-C20) alkyl, cyclo (C3- Cs) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1-C10) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxy (Ci- C2o) alkyl, carboxy (C2-Cio) alkenyl, carboxy (C2-Cio) alkynyl, (Ci-Cio) alkoxy (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, or (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, cyclo (C3- C8) alkenyl, cyclo (C3-C8) alkyl (C1-C10) alkyl, cyclo (C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3- C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-

Cio) alkenyl, cyclo (C3-Cs) alkenyl (C2-C10) alkynyl, carboxy (Ci-C2o) alkyl, carboxy (C2- Clo) alkenyl, carboxy (C2-C10)alkynyl, (C1-C10)alkoxy(C1-C10) alkyl, (C2-Clo) alkenyl or (C2-C10) alkynyl substituted with one or more halo, aryl, ar (C1-C10) alkyl, ar (C2- Cio) alkenyl, ar (C2-C10) alkynyl or aryl, ar (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2- Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2- Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy and halo (Ci-Cio) alkoxy, heteroaryl, heteroar (C1-C10) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-Cio) alkynyl or heteroaryl, heteroar (Ci-Clo) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy and halo (C1-C10) alkoxy, heterocyclyl, heterocyclyl (C1- Clo) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Cio) alkynyl, or heterocyclyl, heterocyclyl (C1-C10) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (C1- Clo) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R', or R3 and R4 taken together with the nitrogen atom to which they are attached form a 5-or 6-membered saturated or unsaturated heterocyclic ring, or A is wherein each R2, G20, G2l, G30 and G3'are as previously defined, provided that when both m and q are 0, A is within the definition of RI d is 1,

G30, G31, Z3, X3 and t'are as previously defined and Z3 (X3) d (G3l) t is a pharmaceutical moiety wherein Z3 (X3) d (G31) t'-H represents the pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof In a sixth embodiment of this invention, a veterinary pharmaceutical compound is represented by formula (I) wherein A is

GIO, G"and G20 are each independently an oxygen atom or a sulfur atom, G2'is an oxygen atom, a sulfur atom or NR3, XI is an oxygen atom, a sulfur atom, a phosphorous atom or a nitrogen atom attached to Zl, X2 is an oxygen atom, a sulfur atom, a phosphorous atom, a nitrogen atom or a carbon atom attached to Z2, m is 1, q and t are each independently 0 or 1, n is 1 or 2, ZI (Xl) m is a pharmaceutical moiety when m is 1 wherein ZXm-H represents the pharmaceutical selected from the group consisting of albendazole, aminocaproic acid, aminophylline, amprolium, atipamezole, benazepril, cisapride, detomidine, disopyramide, enalapril, febantel, fluconazole, imidacloprid, ketamine, lidocaine, lincomycin, lomustine, mechlorethamine, meclofenamic acid, mercaptopurine, methotrexate, mexiletine, ormetoprim, piroxicam, primidone, procainamide, prostaglandin E1, quinacrine, quinidine, sulfachlorpyridazine, sulfadiazine,

sulfamethoxazole, theophylline, thiabendazole, tiletamine, tocainide, vincristine and xylazine when XI is a nitrogen atom, or the pharmaceutical selected from the group consisting of clioquinol, enalapril, guaifenesin, mibolerone, oxazepam, prostaglandin E1 and warfarin when XI is an oxygen atom, Z2 (X2) q (C (=G20) G21) t is a pharmaceutical moiety when q is 1 wherein Z2 (X2) q (C (=G20) Gel) t or Z2 (X2) q (C (=G20) G2') t-H represents the pharmaceutical, Z2 (X2) q is a hydrogen atom, (C1-C20) alkyl, (Ci-Cio) alkylcarbonyloxy (C1- Clo) alkyl, (C1-C20) alkylcarbonyl, (C1-C20) alkenylcarbonyl, (C1-C20) alkynylcarbonyl, hydroxy (Ci-C2o) alkyl, (Cl-Clo) alkylsulfonyl (Ci-Clo) alkyl, (Cl- Clo) alkylcarbonylamino (Ci-Cio) alkyl, arylcarbonylamino (C1-C10) alkyl, heteroarylcarbonylamino (Ci-Cio) alkyl, halo (C1-C20) alkyl, (C2-C2o) alkenyl, halo (C2- C2o) alkenyl, (C1-C10) alkylcarbonylamino (C2-Cio) alkenyl, arylcarbonylamino (C2- Clo) alkenyl, heteroarylcarbonylamino (C2-Cio) alkenyl, (C2-C2o) alkynyl, halo (C2- C2o) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1-C10) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxycyclo (C3- C8) alkyl (Ci-Cio) alkyl, carboxy (C3-C8) cycloalkyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkenyl, carboxycyclo (C3- C8) alkyl (C2-Cio) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkynyl, (C1-C10) alkoxy (C1- Clo) alkyl, (C1-C5) alkoxy (Ci-C5) alkoxy (C1-C10) alkyl, (C1-C10) alkoxy (C2-C10) alkenyl, (C1- Cio) alkoxy (C2-Cio) alkynyl, (C1-C10) alkoxycarbonyl, (Ci-Cio) alkoxycarbonyl (Ci- Cio) alkyl, (Ci-Cio) alkoxycarbonyl (C2-Cio) alkenyl, (Ci-Cio) alkoxycarbonyl (C2- Clo) alkynyl, halo (C1-C10) alkoxy (Ci-Cio) alkyl, halo (Ci-Cio) alkoxy (C2-C10) alkenyl, halo (Ci-Cio) alkoxy (C2-Cio) alkynyl, (C1-C10) alkylthio (Ci-Cio) alkyl, (C1-C10) alkylthio (C2- Clo) alkenyl, (Ci-Cio) alkylthio (C2-Cio) alkynyl, halo (C1-C10) alkylthio (Ci-Cio) alkyl, halo (Ci-Clo) alkylthio (C2-C10) alkenyl, halo (Ci-Cio) alkylthio (C2-C10) alkynyl, SO2NR3R4, NR3R4, carboxy (Ci-C2o) alkyl, carboxy (C2-C20) alkenyl, carboxy (C2-C20) alkynyl, di (C1- Cio) alkoxyphosphoryl (C1-C10) alkyl, aryl, aryl substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, (C1-C10) alkyl, (C1-C10) alkylsulfonyl (C1-C10) alkyl, (C1-C10) alkylsulfonyl, thiocyanato, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (Cl-

Clo) alkoxy, halo (Ci-Cio) alkoxy, C (=O) OR2, C (=O) SR2, C (=S) OR2, C (=S) SR2, C (=O) NR3R4, C (=S) NR3R4, C (=O) R2, C (=S) R2, C (=N-R3) R2, C (=N-OR3) R2, C (=N- NR3R4) R2, OP (=O) (OR2) 2, SO2NR3R4, NR3R4 and (C1-C10) alkylNR3R4, ar (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, or ar (C1- Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci- Cio) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (Ci- Clo) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy and NR3R4, heteroar (C1- Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl, or heteroar (Ci-Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, (Cl- Cio) alkylcarbonyl (Ci-Cio) alkyl, (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl, (C2- Cio) alkynylcarbonyl (Ci-Cio) alkyl, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-C10) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (C1-C10) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl, arylcarbonyl, arylcarbonyl (Ci-Cio) alkyl, ar (C1- Clo) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl, aroxycarbonyl (Ci-Cio) alkyl, ar (Ci-Cio) alkoxycarbonyl, ar (C1-C10) alkoxycarbonyl (C1- Cio) alkyl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, or heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-C10) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl, arylcarbonyl, arylcarbonyl (Ci-Cio) alkyl, ar (C1- Cio) alkylcarbonyl, ar (C1-C10)alkylcarbonyl(C1-C10) alkyl, aroxycarbonyl, aroxycarbonyl (Ci-Cio) alkyl, ar (Ci-Clo) alkoxycarbonyl, ar (Ci-Co) alkoxycarbonyl (Ci- Cio) alkyl, heteroarylcarbonyl, heteroarylcarbonyl (Cl-Clo) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (C1-C10) alkyl substituted with one or more substituents

independently selected from halo, hydroxy, nitro, cyano, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (Ct-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, and C (=N- G22) R2 when q is 0 and t is 1, G22 is OR3, OCOR3, S (O) jR3, OS (O) jR3, NR3R4, OS02NR3R4, OP (=O) OR3NR3R4, OP (=O) (OR3) 2 or N=CR3R4, j is 0, 1 or 2, Z2 (X2) q is halo, NR3R4, {(NR3R4R5)+ M-}, OR3, S (O) jR3 or SO2NR3R4 when both q and t are 0 wherein M-is halo, hydroxy, (Ci-Cs) alkoxy or the anion of a carboxylic acid and j is 0, 1 or 2, RI is wherein G30 is an oxygen atom or a sulfur atom, G31 is an oxygen atom, a sulfur atom or NR3, t'and d are each independently 0 or 1, X3 is an oxygen atom, a sulfur atom, a nitrogen atom, a phosphorous atom or a carbon atom attached to Z3 when t'is 0, a nitrogen atom attached to Z3 when t'is 1 and G31 is NR3, or a carbon atom attached to Z3 when t'is 1 and G31 is an oxygen atom or a sulfur atom, Z3 (X3) d (G3l) t is a pharmaceutical moiety when d is 1 wherein Z3 (X3) d (G3l) t-H represents the pharmaceutical, Z3 (X3) d, when d is 0 and t'is 1, is a hydrogen atom, (C1-C20) alkyl, (Ci- Clo) alkylcarbonyloxy (C1-C10) alkyl, (C1-C20) alkylcarbonyl, (C1-C10) alkylcarbonyl (Ci- Cio) alkyl, hydroxy (C1-C20) alkyl, (C1-C10) alkylsulfonyl (Ci-Cio) alkyl, (C1- C10) alkylcarbonylamino (C1-C10)alkyl, arylcarbonylamino (C1-C10)alkyl, heteroarylcarbonylamino (Ci-Cio) alkyl, acetylamino (Cl-Cio) alkyl, halo (C1-C20) alkyl, (C2-Cio) alkenyl, (C2-C10) alkenylcarbonyl (Ci-Cio) alkyl, acetylamino (C2-Cio) alkenyl, halo (C2-Cio) alkenyl, (C2-Cio) alkynyl, (C2-Cio) alkynylcarbonyl (Ci-Cio) alkyl, halo (C2- Cio) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1-C10) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-Cio) alkenyl,

cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxycyclo (C3- C8) alkyl (C1-C10) alkyl, carboxycyclo(C3-C8) alkyl (C2-Cio) alkenyl, carboxycyclo (Cs- C8) alkenyl (C1-C10) alkyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkenyl, carboxycyclo (C3- C8) alkyl (C2-Cio) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkynyl, (C1-C10) alkoxy (Ci- Clo) alkyl, (C1-C10) alkoxy (C1-C10) alkoxy (Ci-Clo) alkyl, (Ci-Cio) alkoxy (C2-C10) alkenyl, (Ci-Cio) alkoxy (C2-C10) alkynyl, (Ci-Cio) alkoxycarbonyl (Ci-Cio) alkyl, (Ci- Clo) alkoxycarbonyl (C2-C10) alkenyl, (C1-C10) alkoxycarbonyl (C2-Cio) alkynyl, halo (Ci- Clo) alkoxy (Ci-Cio) alkyl, halo (Ci-Cio) alkoxy (C2-Cio) alkenyl, halo (Ci-Cio) alkoxy (C2- Cio) alkynyl, (C1-C10) alkylthio (C1-C10) alkyl, (C1-C10) alkylthio (C2-C10) alkenyl, (Ci- Clo) alkylthio (C2-Cio) alkynyl, halo (Ci-Cio) alkylthio (Ci-Cio) alkyl, halo (Ci- Cio) alkylthio (C2-C10) alkenyl, halo (Ci-Cio) alkylthio (C2-Cio) alkynyl, carboxy (Ci- C2o) alkyl, carboxy (c2-clo) alkenyl, carboxy (C2-Cio) alkynyl, NR3R4, OR3, S (O) jR3, aryl, arylcarbonyloxy (Ci-Cio) alkyl, arylcarbonyl (C1-C10) alkyl, aroxycarbonyl (Ci-Cio) alkyl, or aryl, arylcarbonyloxy (Ci-Cio) alkyl, arylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl (C1- Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, (C1-C10) alkyl, (C1-C10) alkylsulfonyl (C1- Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, ar (Ci- Cio) alkyl, ar (Ci-Cio) alkylcarbonyloxy (Ci-Cio) alkyl, ar (Ci-Cio) alkylcarbonyl (Ci- Ciao) alkyl, ar (Ci-Cio) alkoxycarbonyl (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (C1-C10) alkyl, or ar (Ci-Cio) alkyl, ar (C1- Clo) alkylcarbonyloxy (Ci-Cio) alkyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (Ci- Cio) alkoxycarbonyl (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3- C8) alkyl, aroxy (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, (C2- Clo) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2- Ciao) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyloxy (Ci-Cio) alkyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl (Ci-Cio) alkyl, or heteroaryl, heteroarylcarbonyloxy (Ci-Cio) alkyl, heteroarylcarbonyl (C1-C10) alkyl, heteroaroxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4,

heteroar (Ci-Cio) alkyl, heteroar (C2-C10)alkenyl, heteroar (C2-Cio) alkynyl, or heteroar (Ci-Clo) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Clo) alkyl, halo (C2- Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclylcarbonyloxy (Ci-Clo) alkyl, hetercyclylcarbonyl (C1- Cio) alkyl, heterocyclyloxycarbonyl (C1-C10) alkyl, or heterocyclyl, heterocyclylcarbonyloxy (Ci-Clo) alkyl, heterocyclylcarbonyl (Ci-Clo) alkyl, heterocyclyloxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, wherein j is 0, 1 or 2, Z3 (X3) d is halo, NR3R4, OR3, N (R3)-N=CR3R4, S (O) jR3 or S02NR3R4 when both d and t'are 0 and j is 0, 1 or 2, each R2 is independently a hydrogen atom, (C1-C20) alkyl, (C2-C10) alkenyl, (C2- Cio) alkynyl, (Ci-Cio) alkoxy (Ci-Cio) alkyl, (Ci-Cio) alkoxy (C2-C10) alkenyl, (Ci- Clo) alkoxy (C2-Cio) alkynyl, (C1-C10) alkylthio (Ci-Cio) alkyl, (C1-C10) alkylthio (C2- Cio) alkenyl, (C1-C10) alkylthio (C2-Cio) alkynyl, carboxy, a carboxylate salt, carboxy (Ci- C2o) alkyl, carboxy (C2-C2o) alkenyl, carboxy (C2-C2o) alkynyl, (C1-C20) alkoxycarbonyl, (Ci- Clo) alkoxycarbonyl (Ci-Cio) alkyl, (Ci-Cio) alkoxycarbonyl (C2-Cio) alkenyl, (Ci- C10)alkoxycarbonyl(C2-C10) alkynyl, (C1-C20) alkylcarbonyl, (C2-C20) alkenylcarbonyl, (C2-C2o) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1- Clo) alkyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3- C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2- Cio) alkynyl, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-Cio) alkynyl, or (C1-C20) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, (Ci- Clo) alkoxy (C1-C10) alkyl, (C1-C10)alkoxy(C2-C10) alkenyl, (C1-C10) alkoxy (C2-C10) alkynyl,.

(Ci-Cio) alkylthio (Ci-Cio) alkyl, (C1-C10)alkylthio(C2-C10) alkenyl, (C1-C10) alkylthio (C2- Cio) alkynyl, carboxy (Ci-C2o) alkyl, carboxy (C2-Cio) alkenyl, carboxy (C2-C10) alkynyl, (Ci- C2o) alkoxycarbonyl, (C1-C10) alkoxycarbonyl (C1-C10) alkyl, (C1-C10) alkoxycarbonyl (C2- Cio) alkenyl, (C1-C10) alkoxycarbonyl (C2-Clo) alkynyl, (C1-C20) alkylcarbonyl, (C2- Clo) alkenylcarbonyl, (C2-Cio) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl,

cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Cio) alkenyl, cyclo (C3-C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, heterocyclyl, heterocyclyl (C1-C10) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, SO2NR3R4 and NR3R4, aryl or aryl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2- Clo) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, carboxy, (Ci- C4) alkoxycarbonyl, S02NR3R4 and NR3R4, ar (C1-C10) alkyl, ar (C2-C10) alkenyl, ar (C2- Clo) alkynyl, or ar (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, arylcarbonyl, ar (Ci-Cio) alkylcarbonyl, ar (C2-C10) alkenylcarbonyl, ar (C2-Cio) alkynylcarbonyl, aroxycarbonyl (Ci-Clo) alkyl, or arylcarbonyl, ar (Ci-Cio) alkylcarbonyl, ar (C2- Clo) alkenylcarbonyl, ar (C2-Clo) alkynylcarbonyl, aroxycarbonyl (CI-Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (C1- Clo) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-C10) alkenyl, (C2- Clo) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (Ci- Cio) alkoxy, halo (Ci-Cio) alkoxy and NR3R4, heteroar (C1-C10) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-C10) alkynyl or heteroar (C1-C10) alkyl, heteroar (C2- Clo) alkenyl, heteroar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-C10) alkenyl, (Ca-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci- Cio) alkoxy, SO2NR3R4 and NR3R4, heteroarylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl, heteroar (C2-C10) alkenylcarbonyl, heteroar (C2-C10) alkynylcarbonyl, heteroaroxycarbonyl (C1-C10) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (C1- Clo) alkyl, or heteroarylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl, heteroar (C2- Clo) alkenylcarbonyl, heteroar (C2-C10) alkynylcarbonyl, heteroaroxycarbonyl (Ci- Clo) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl substituted with

one or more substituents independently selected from halo, cyano, hydroxy ; nitro, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SOzNR3R4 and NR3R4, or Ri and R2 taken together with the carbon atom to which they are attached form a 5-7 membered saturated or unsaturated ring, R3, R4 and R5 are each independently a hydrogen atom, (C1-C20) alkyl, cyclo (C3- C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3-C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, carboxy (Ci- C2o) alkyl, carboxy (C2-Cio) alkenyl, carboxy (C2-C10) alkynyl, (Ci-Cio) alkoxy (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, or (Ci-Clo) alkyl, cyclo (C3-C8) alkyl, cyclo (C3- C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3- C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3-C8) alkenyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxy (C1-C20) alkyl, carboxy (C2- Clo) alkenyl, carboxy (C2-C10) alkynyl, (C1-C10) alkoxy (Ci-Cio) alkyl, (C2-C10) alkenyl or (C2-C10) alkynyl substituted with one or more halo, aryl, ar (C1-C10) alkyl, ar (C2- Cio) alkenyl, ar (C2-Cio) alkynyl or aryl, ar (C1-C10) alkyl, ar (C2-Cio) alkenyl, ar (C2- Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Clo) alkyl, halo (C2- Clo) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy and halo (Ci-Cio) alkoxy, heteroaryl, heteroar (C1-C10) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl or heteroaryl, heteroar (C1-C10) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2- Cio) alkynyl, (Ci-Cio) alkoxy and halo (Ci-Cio) alkoxy, heterocyclyl, heterocyclyl (Ci- C10) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Cio) alkynyl, or heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-Clo) alkynyl, halo (C1- Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, or R3 and R4 taken together with the nitrogen atom to which they are attached form a 5-or 6-membered saturated or unsaturated heterocyclic ring, or A is wherein each R2, G20, G2', G30 and G31 are as previously defined, provided that when both m and q are 0, A is

within the definition of RI d is 1, G30, G31, Z3, X3 and t'are as previously defined and Z3 (X3) d (G31) t is a pharmaceutical moiety wherein Z3 (X3) d (G31) t'-H represents the pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof In a seventh embodiment of this invention, a veterinary pharmaceutical compound is represented by formula (I) wherein A is Gl°, G"and G20 are each independently an oxygen atom or a sulfur atom, G21 is an oxygen atom, a sulfur atom or NR3, XI is an oxygen atom, a sulfur atom, a phosphorous atom or a nitrogen atom attached to Zl,

X2 is an oxygen atom, a sulfur atom, a phosphorous atom, a nitrogen atom or a carbon atom attached to Z2, m and t are each independently 0 or 1, q is 1, n is 1 or 2, ZI (Xl) m is a pharmaceutical moiety when m is 1 wherein ZXm-H represents the pharmaceutical, Z2(X2)q(C(=G20)G21)t is a pharmaceutical moiety when q is 1 wherein Z2 (X2) q (C (=G20) G21) t or Z2 (X2) q (C (=G20) G2l) t-H represents the pharmaceutical selected from the group consisting of acepromazine, albendazole, aminopropazine, amiodarone, amitriptyline, atropine, azaperone, buspirone, captopril, cephapirin, chlorpheniramine, clemastine, clomipramine, cyproheptadine, diethylcarbamazine, diltiazem, diphenhydramine, diphenoxylate, doxapram, doxepin, doxylamine, droperidol, febantel, fenbendazole, fentanyl, hetacillin, hydrocodone, hydroxyzine, itraconazole, levamisole, meclizine, meperidine, methenamine, morantel, naltrexone, omeprazole, oxybutynin, pentazocine, piroxicam, primidone, procainamide, promazine, pyrantel, selegiline, thiabendazole, tiamulin and verapamil when X2 is a nitrogen atom, or the pharmaceutical selected from the group consisting of clioquinol, guaifenesin, mibolerone, oxazepam and warfarin when X2 is an oxygen atom, or the pharmaceutical selected from the group consisting of ketoprofen and valproic acid when x2 is a carbon atom, Z' (Xl) m, when m is 0, is a hydrogen atom, halo, (C1-C20) alkyl, (Ci- Cio) alkylcarbonyloxy (Ci-Cio) alkyl, (Ci-C2o) alkylcarbonyl, hydroxy (Ci-C2o) alkyl, (C1- Cio) alkylsulfonyl (Ci-Cio) alkyl, (C1-C10) alkylcarbonylamino (Ci-Cio) alkyl, arylcarbonylamino (Ci-Cio) alkyl, heteroarylcarbonylamino (Cl-Clo) alkyl, halo (C1- C2o) alkyl, (C2-C20) alkenyl, halo (C2-C2o) alkenyl, (Cl-Clo) alkylcarbonylamino (C2- Clo) alkenyl, arylcarbonylamino (C2-Cio) alkenyl, heteroarylcarbonylamino (C2- Cio) alkenyl, (C2-C2o) alkynyl, halo (C2-C2o) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3- C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci- Clo) alkyl, cyclo (C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3- C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-Clo) alkynyl, cyclo (C3-C8) alkenyl (C2- Cio) alkynyl, carboxycyclo (C3-C8) alkyl (Cl-Clo) alkyl, carboxy (C3-C8) cycloalkyl (C2-

Cio) alkenyl, carboxycyclo (C3-C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2- Cio) alkenyl, carboxycyclo (C3-C8) alkyl (C2-Cio) alkynyl, carboxycyclo (C3-Cs) alkenyl (C2- Clo) alkynyl, (Ci-Cio) alkoxy (Ci-Cio) alkyl, (Ci-C5) alkoxy (C1-C5) alkoxy (Ci-Cio) alkyl, (Ci- Cio) alkoxy (C2-Cio) alkenyl, (C1-C10) alkoxy (C2-Cio) alkynyl, (Ci-Cio) alkoxycarbonyl, (C1- Cio) alkoxycarbonyl (Ci-Clo) alkyl, (C1-C10) alkoxycarbonyl (C2-C10) alkenyl, (Cl- Cio) alkoxycarbonyl (C2-C10) alkynyl, halo (Ci-Cio) alkoxy (C1-C10) alkyl, halo (Cs- Clo) alkoxy (C2-Cio) alkenyl, halo (Ci-Cio) alkoxy (C2-Cio) alkynyl, (Ci-Cio) alkylthio (Ci- Cio) alkyl, (Ci-Cio) alkylthio (C2-Cio) alkenyl, (C1-C10) alkylthio (C2-C10) alkynyl, halo (Ci- Clo) alkylthio (Ci-Cio) alkyl, halo (Ci-Cio) alkylthio (C2-Cio) alkenyl, halo (Ci- Cio) alkylthio (C2-C10) alkynyl, SO2NR3R4, NR3R4, OR3, S (O) jR3, carboxy (Ci-C2o) alkyl, carboxy (C2-C2o) alkenyl, carboxy (C2-C2o) alkynyl, aryl, arylcarbonyl, arylcarbonyl (C1- Cio) alkyl, aroxycarbonyl, aroxycarbonyl (Ci-Cio) alkyl, or aryl, arylcarbonyl, arylcarbonyl (C1-C10) alkyl, aroxycarbonyl, aroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, (C1-C10) alkyl, (C1-C10) alkylsulfonyl (C1-C10) alkyl, (C1-C10) alkylsulfonyl, thiocyanato, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4, and NR3R4, ar (Ci- Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (C1-C10) alkyl, ar (Ci-Cio) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (C2- Cio) alkenylcarbonyl, ar (C2-C10) alkenylcarbonyl (Ci-Cio) alkyl, or ar (Ci-Cio) alkyl, ar (C2- Clo) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, ar (C1- Cio) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (C2-Cio) alkenylcarbonyl, ar (C2-C10) alkenylcarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, cyclo (C3- Cs) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, S02NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyl, heteroarylcarbonyl (C1-C10) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, or heteroaryl, heteroarylcarbonyl, heteroarylcarbonyl (C1-C10) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (C1- Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (C1- Clo) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy and NR3R4, heteroar (C1-C10) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl,

heteroar (Ci-Cio) alkylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, heteroar (C2-C10) alkenylcarbonyl, heteroar (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl, or heteroar (Ci-Cio) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl, hetercar (Cs- C10) alkylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, heteroar (C2- Cio) alkenylcarbonyl, heteroar (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Cl-Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Clo) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Clo) alkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclyl (C1-C10) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2- Cio) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (C1-C10) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl, or heterocyclyl, heterocyclyl (C1-C10) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Cio) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4 wherein j is 0, 1 or 2, Rl is wherein G30 is an oxygen atom or a sulfur atom, G31 is an oxygen atom, a sulfur atom or NR3, t'and d are each independently 0 or 1, X3 is an oxygen atom, a sulfur atom, a nitrogen atom, a phosphorous atom or a carbon atom attached to Z3 when t'is 0, a nitrogen atom attached to Z3 when t'is 1 and G31 is NR3, or a carbon atom attached to Z3 when t'is 1 and G3'is an oxygen atom or a sulfur atom, Z3 (X3) d (G31) t is a pharmaceutical moiety when d is 1 wherein Z3(X3) d (G31) t'-H represents the pharmaceutical, Z3 (X3) d, when d is 0 and t'is 1, is a hydrogen atom, (C1-C20) alkyl, (Ci- Cio) alkylcarbonyloxy (C1-C10)alkyl, (C1-C20) alkylcarbonyl, (C1-C10) alkylcarbonyl (C1-

Cio) alkyl, hydroxy (Cl-C20) alkyl, (Ci-Cio) alkylsulfonyl (Ci-Cio) alkyl, (Cl- Cio) alkylcarbonylamino (Ci-Cio) alkyl, arylcarbonylamino (Ci-Cio) alkyl, heteroarylcarbonylamino (C1-C10) alkyl, acetylamino (C1-C10) alkyl, halo (Cl-C20) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl, acetylamino (C2-Cio) alkenyl, halo (C2-C10) alkenyl, (C2-Cio) alkynyl, (C2-Cio) alkynylcarbonyl (Ci-Cio) alkyl, halo (C2- Cio) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3-Cs) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Cl-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, carboxycyclo (C3- C8) alkyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkyl (C2-Cio) alkenyl, carboxycyclo (C3- C8) alkenyl (C1-C10) alkyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkenyl, carboxycyclo (C3- C8) alkyl (C2-Cio) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-C10) alkynyl, (Ci-Cio) alkoxy (Ci- Clo) alkyl, (C1-C10) alkoxy (Ci-Cio) alkoxy (Ci-Cio) alkyl, (Ci-Cio) alkoxy (C2-Cio) alkenyl, (C1-C10) alkoxy (C2-C10) alkynyl, (C1-C10) alkoxycarbonyl (C1-C10) alkyl, (Ci- Clo) alkoxycarbonyl (C2-C10) alkenyl, (C1-C10) alkoxycarbonyl (C2-C10) alkynyl, halo (Ci- C10) alkoxy (Ci-Cio) alkyl, halo (Ci-Cio) alkoxy (C2-Cio) alkenyl, halo (Ci-Cio) alkoxy (C2- Clo) alkynyl, (Ci-Cio) alkylthio (Ci-Cio) alkyl, (C1-C10) alkylthio (C2-C10) alkenyl, (Ci- Cio) alkylthio (C2-Cio) alkynyl, halo (C1-C10) alkylthio (Ci-Cio) alkyl, halo (Ci- Cio) alkylthio (C2-C10) alkenyl, halo (C1-C10) alkylthio (C2-C10) alkynyl, carboxy (Ci- C2o) alkyl, carboxy (C2-C10) alkenyl, carboxy (C2-C10) alkynyl, NR3R4, OR3, S (O) jR3, aryl, arylcarbonyloxy (C1-C10) alkyl, arylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl (C1-C10) alkyl, or aryl, arylcarbonyloxy (C1-C10) alkyl, arylcarbonyl (Ci-Clo) alkyl, aroxycarbonyl (C1- Clo) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, (C1-C10) alkyl, (C1-C10) alkylsulfonyl (Ci- Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, ar (Ci- Cio) alkyl, ar (C1-C10) alkylcarbonyloxy (Cl-Cio) alkyl, ar (C1-C10) alkylcarbonyl (Ci- Cio) alkyl, ar (C1-C10) alkoxycarbonyl (C1-C10) alkyl, ar (C2-C10) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, or ar (Ci-Cio) alkyl, ar (Ci- Ciao) alkylcarbonyloxy (Ci-Clo) alkyl, ar (C1-C10) alkylcarbonyl (Ci-Clo) alkyl, ar (Ci- Cio) alkoxycarbonyl (C1-C10) alkyl, ar (C2-C10) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3- C8) alkyl, aroxy (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, cyclo (C3-C8) alkyl, (C2-

Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cic) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyloxy (Ci-Cio) alkyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl (Cl-Cio) alkyl, or heteroaryl, heteroarylcarbonyloxy (Ci-Clo) alkyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, heteroar (Cl-Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-Cio) alkynyl, or heteroar (Ci-Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Cl-Cio) alkyl, halo (C2- Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclylcarbonyloxy (Cl-Cio) alkyl, hetercyclylcarbonyl (C1- Cio) alkyl, heterocyclyloxycarbonyl (Ci-Clo) alkyl, or heterocyclyl, heterocyclylcarbonyloxy (Ci-Cio) alkyl, heterocyclylcarbonyl (C1-C10)alkyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (Cl-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, wherein j is 0, 1 or 2, Z3 (X3) d is halo, NR3R4, OR3, N (R3)-N=CR3R4, S (O) jR3 or SO2NR3R4 when both d and t'are 0 and j is 0, 1 or 2, each R2 is independently a hydrogen atom, (C1-C20) alkyl, (C2-Cio) alkenyl, (C2- Cio) alkynyl, (Ci-Cio) alkoxy (C1-C10) alkyl, (Ci-Cio) alkoxy (C2-C10) alkenyl, (C1- Cio) alkoxy (C2-C10) alkynyl, (Ci-Cio) alkylthio (Ci-Cio) alkyl, (Ci-Cio) alkylthio (C2- Cio) alkenyl, (C1-C10) alkylthio (C2-C10) alkynyl, carboxy, a carboxylate salt, carboxy (C1- C2o) alkyl, carboxy (C2-C2o) alkenyl, carboxy (C2-C20) alkynyl, (C1-C20) alkoxycarbonyl, (Ci- Clo) alkoxycarbonyl (Ci-Cio) alkyl, (Ci-Cio) alkoxycarbonyl (C2-C10) alkenyl, (Ci- Cio) alkoxycarbonyl (C2-C10) alkynyl, (C1-C20) alkylcarbonyl, (C2-C2o) alkenylcarbonyl, (C2-C2o) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1- Clo) alkyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3- C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-

Cio) alkynyl, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Cio) alkynyl, or (CK1-C20) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, (Ci- C10) alkoxy (Cl-Cio) alkyl, (Ci-Cio) alkoxy (C2-Cio) alkenyl, (C1-C10) alkoxy (C2-Clo) alkynyl, (Ci-Cio) alkylthio (Ci-Cio) alkyl, (C1-C10) alkylthio (C2-C10) alkenyl, (C1-C10) alkylthio (C2- Clo) alkynyl, carboxy (CI-C2o) alkyl, carboxy (C2-Cio) alkenyl, carboxy (C2-C10) alkynyl, (C1- C2o) alkoxycarbonyl, (Ci-Cio) alkoxycarbonyl (Ci-Cio) alkyl, (Ci-Cio) alkoxycarbonyl (C2- Clo) alkenyl, (C1-C10) alkoxycarbonyl (C2-Cio) alkynyl, (C1-C20) alkylcarbonyl, (C2- Clo) alkenylcarbonyl, (C2-Cio) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, heterocyclyl, heterocyclyl (Ci-Clo) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, SO2NR3R4 and NR3R4, aryl or aryl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2- Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, carboxy, (Ci- C4) alkoxycarbonyl, SO2NR3R4 and NR3R4, ar (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2- Cio) alkynyl, or ar (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2- Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4, arylcarbonyl, ar (Ci-Cio) alkylcarbonyl, ar (C2-Cio) alkenylcarbonyl, ar (C2-C10)alkynylcarbonyl, aroxycarbonyl (Cl-Cio) alkyl, or arylcarbonyl, ar (C1-C10) alkylcarbonyl, ar (C2- Clo) alkenylcarbonyl, ar (C2-Clo) alkynylcarbonyl, aroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-C10) alkenyl ; (C2-Cio) alkynyl, halo (Ci- Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2- Cio) alkynyl, halo (Ci-Clo) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1- Clo) alkoxy, halo (C1-C10) alkoxy and NR3R4, heteroar (Ci-Cio) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-C10) alkynyl or heteroar (Ci-Cio) alkyl, heteroar (C2- Clo) alkenyl, heteroar (C2-C10) alkynyl substituted with one or more substituents

independently selected from halo, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (C1- Cio) alkoxy, SO2NR3R4 and NR3R4, heteroarylcarbonyl, heteroar (Ci-Clo) alkylcarbonyl, heteroar (C2-C10) alkenylcarbonyl, heteroar (C2-Cio) alkynylcarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (C1- Clo) alkyl, or heteroarylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl, heteroar (C2- Cio) alkenylcarbonyl, heteroar (C2-Cio) alkynylcarbonyl, heteroaroxycarbonyl (Ci- Clo) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, or RI and R2 taken together with the carbon atom to which they are attached form a 5-7 membered saturated or unsaturated ring, R3, R4 and R5 are each independently a hydrogen atom, (C1-C20) alkyl, cyclo (C3- C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Cio) alkenyl, cyclo (C3-C8) alkyl (C2-Clo) alkynyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxy (C1- C2o) alkyl, carboxy (C2-Cio) alkenyl, carboxy (C2-Cio) alkynyl, (Cl-Clo) alkoxy (Cl-Cio) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, or (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, cyclo (C3- C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3- C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (Ci-Clo) alkyl, cyclo (C3-C8) alkenyl (C2- Cio) alkenyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxy (C1-C20) alkyl, carboxy (C2- Clo) alkenyl, carboxy (C2-C10) alkynyl, (C1-C10) alkoxy (Ci-Cio) alkyl, (C2-C10) alkenyl or (C2-C10) alkynyl substituted with one or more halo, aryl, ar (Ci-Cio) alkyl, ar (C2- Cio) alkenyl, ar (C2-C10) alkynyl or aryl, ar (Cl-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2- Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2- Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy and halo (Ci-Cio) alkoxy, heteroaryl, heteroar (C1-C10) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl. or heteroaryl, heteroar (C1-C10) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (Ci-Cio) alkoxy and halo (Ci-Cio) alkoxy, heterocyclyl, heterocyclyl (Ci-

Cio) alkyl, heterocyclyl (Cz-Cio) alkenyl, heterocyclyl (C2-Clo) alkynyl, or heterocyclyl, heterocyclyl (Ci-Clo) alkyl, heterocyclyl (C2-Clo) alkenyl, heterocyclyl (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-CIo) alkynyl, halo (C1- Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (Ci-Clo) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, or R3 and R4 taken together with the nitrogen atom to which they are attached form a 5-or 6-membered saturated or unsaturated heterocyclic ring, or A is wherein each R2, G20, G21, G30 and G31 are as previously defined, provided that when both m and q are 0, A is within the definition of RI d is 1, G30, G31, Z3, X3 and t'are as previously defined and Z3 (X3) d (G31) t' is a pharmaceutical moiety wherein Z3 (X3) d (G3l) t'-H represents the pharmaceutical, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof In an eighth embodiment of this invention, the pharmaceutical compound is represented by formula (I) wherein A is

Gl°, Grand G20 are each independently an oxygen atom or a sulfur atom, G21 is an oxygen atom, a sulfur atom or NR3, Xl is a nitrogen atom attached to Zl, X2 is an oxygen atom, a sulfur atom, a phosphorous atom, a nitrogen atom or a carbon atom attached to Z2, m is 1, q and t are each independently 0 or 1, Zl (X') m is a pharmaceutical moiety selected from

wherein Zl (Xl) m-H represents the respective pharmaceutical selected from

~ represents the connection point between said pharmaceutical moiety and the moiety represented by

Z2 (X2) q (C (=G20) Gel) t is a pharmaceutical moiety when q is 1 wherein Z2 (X2)q(C(=G20)G21) t or Z2 (X2) q (C (=G20) G21) t-H represents the pharmaceutical, ZI (XI) m, when m is 0, is a hydrogen atom, halo, (C1-C20) alkyl, (Ci- Clo) alkylcarbonyloxy (Ci-Cio) alkyl, (Ci-C2o) alkylcarbonyl, hydroxy (C1-C20) alkyl, (C1- Cio) alkylsulfonyl (Ci-Cio) alkyl, (C1-C10) alkylcarbonylamino (Ci-Cio) alkyl, arylcarbonylamino (C1-C10) alkyl, heteroarylcarbonylamino (Ci-Cio) alkyl, halo (Ci- C2o) alkyl, (C2-C2o) alkenyl, halo (C2-C2o) alkenyl, (C1-C10) alkylcarbonylamino (C2- Cio) alkenyl, arylcarbonylamino (C2-Cio) alkenyl, heteroarylcarbonylamino (C2- Cio) alkenyl, (C2-C2o) alkynyl, halo (C2-C2o) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3- C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci- Clo) alkyl, cyclo (C3-C8) alkyl (C2-C10) alkenyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3- C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2- Clo) alkynyl, carboxycyclo (C3-C8) alkyl (Ci-Clo) alkyl, carboxy (C3-C8) cycloalkyl (C2- Clo) alkenyl, carboxycyclo (C3-C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2- Cio) alkenyl, carboxycyclo (C3-C8) alkyl (C2-C10) alkynyl, carboxycyclo (C3-C8) alkenyl (C2- Clo) alkynyl, (Ci-Cio) alkoxy (Ci-Cio) alkyl, (C1-C5) alkoxy (C1-C5) alkoxy (Ci-Cio) alkyl, (Ci- Cio) alkoxy (C2-Cio) alkenyl, (C1-C10) alkoxy (C2-C10) alkynyl, (Ci-Cio) alkoxycarbonyl, (Cl- Clo) alkoxycarbonyl (Ci-Cio) alkyl, (Ci-Cio) alkoxycarbonyl (C2-C10) alkenyl, (C1- Clo) alkoxycarbonyl (C2-Cio) alkynyl, halo (Ci-Cio) alkoxy (Cl-Cio) alkyl, halo (C1- Clo) alkoxy (C2-C10) alkenyl, halo (C1-C10) alkoxy (C2-Cio) alkynyl, (C1-C10) alkylthio (C1- Cio) alkyl, (C1-C10) alkylthio (C2-C10) alkenyl, (Ci-Co) alkylthio (C2-C10) alkynyl, halo (Ci- Cio) alkylthio (Ci-Cio) alkyl, halo (Ci-Cio) alkylthio (C2-Cio) alkenyl, halo (Ci- Cio) alkylthio (C2-C10) alkynyl, SO2NR3R4, NR3R4, OR3, S (O) jR3, carboxy (Ci-C2o) alkyl, carboxy (C2-C20) alkenyl, carboxy (C2-C20) alkynyl, aryl, arylcarbonyl, arylcarbonyl (C1- Cio) alkyl, aroxycarbonyl, aroxycarbonyl (C1-C10) alkyl, or aryl, arylcarbonyl, arylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl, aroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, (Ci-Cio) alkyl, (C1-C10) alkylsulfonyl (Ci-Cio) alkyl, (Ci-Cio) alkylsulfonyl, thiocyanato, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4, and NR3R4, ar (Ci- Clo) alkyl, ar (C2-C10) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (C1-C10) alkyl, ar (C1-C10) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (C1-C10) alkyl, ar (C2- Cio) alkenylcarbonyl, ar (C2-C10) alkenylcarbonyl (C1-C10) alkyl, or ar (C1-C10) alkyl, ar (C2-

Cio) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, ar (C1- Cio) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (C2-Clo) alkenylcarbonyl, ar (C2-Cio) alkenylcarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, cyclo (C3- C8) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Cl-Cio) alkoxy, SOR2NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyl, heteroarylcarbonyl (C1-C10) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (C1-C10) alkyl, or heteroaryl, heteroarylcarbonyl, heteroarylcarbonyl (C1-C10) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (C1- Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (C1- Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Cl-Cio) alkoxy and NR3R4, heteroar (C1-C10) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-C10) alkynyl, heteroar (Ci-Cio) alkylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, heteroar (C2-Cio) alkenylcarbonyl, heteroar (C2-Cio) alkenylcarbonyl (C1-C10) alkyl, or heteroar (Ci-Cio) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-C10) alkynyl, heteroar (Ci- Cio) alkylcarbonyl, heteroar (Cl-Cio) alkylcarbonyl (Cl-Cio) alkyl, heteroar (C2- Clo) alkenylcarbonyl, heteroar (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2- Cio) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl, or heterocyclyl, heterocyclyl (Cl-Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-C10) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Cl-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2- C10) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C1-C10) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4 wherein j is 0, 1 or 2, Z2 (X2) q is a hydrogen atom, (C1-C20) alkyl, (C1-C10) alkylcarbonyloxy (C1- Clo) alkyl, (C1-C20) alkylcarbonyl, (C1-C20) alkenylcarbonyl, (C1-C20) alkynylcarbonyl,

hydroxy (Ci-C2o) alkyl, (Ci-Cio) alkylsulfonyl (Ci-Cio) alkyl, (C1- Cio) alkylcarbonylamino (Ci-Cio) alkyl, arylcarbonylamino (Ct-Cio) alkyl, heteroarylcarbonylamino (Ci-Cio) alkyl, halo (Ci-C2o) alkyl, (C2-C2o) alkenyl, halo (C2- C2o) alkenyl, (C1-C10) alkylcarbonylamino (C2-C10) alkenyl, arylcarbonylamino (C2- Cio) alkenyl, heteroarylcarbonylamino (C2-Cio) alkenyl, (C2-C2o) alkynyl, halo (C2- C2o) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, carboxycyclo(C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1-C10) alkyl, cyclo (C3-C8) alkyl (C2- Cio) alkenyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, carboxycyclo (C3- C8) alkyl (C1-C10) alkyl, carboxy (C3-C8) cycloalkyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkenyl, carboxycyclo (C3- C8) alkyl (C2-Cio) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-C10) alkynyl, (Ci-Cio) alkoxy (C1- Cio) alkyl, (C1-C5) alkoxy (Ci-C5) alkoxy (Ci-Clo) alkyl, (Ci-Cio) alkoxy (C2-C10) alkenyl, (Ci- Cio) alkoxy (C2-Cio) alkynyl, (Ci-Cio) alkoxycarbonyl, (Ci-Cio) alkoxycarbonyl (Ci- Cio) alkyl, (C1-C10) alkoxycarbonyl (C2-C10) alkenyl, (C1-C10) alkoxycarbonyl (C2- Cio) alkynyl, halo (Ci-Cio) alkoxy (Ci-Cio) alkyl, halo (Ci-Cio) alkoxy (C2-C10) alkenyl, halo (Ci-Cio) alkoxy (C2-C10) alkynyl, (C1-C10) alkylthio (Ci-Clo) alkyl, (Ci-Cio) alkylthio (C2- Cio) alkenyl, (Ci-Cio) alkylthio (C2-C10) alkynyl, halo (Ci-Cio) alkylthio (Cl-Cio) alkyl, halo (Cl-Cio) alkylthio (C2-C10) alkenyl, halo (Ci-Cio) alkylthio (C2-Cio) alkynyl, SOR2NR3R4, NR3R4, carboxy (Cl-C20) alkyl, carboxy (C2-C20) alkenyl, carboxy (C2-C20) alkynyl, di (Ci- Clo) alkoxyphosphoryl (Ci-Cio) alkyl, aryl, aryl substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, (C1-C10) alkyl, (Ci-Cio) alkylsulfonyl (Ci-Cio) alkyl, (Ci-Cio) alkylsulfonyl, thiocyanato, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (Ci- Clo) alkoxy, halo (C1-C10) alkoxy, C (=O) OR2, C (=O) SR2, C (=S) OR2, C (=S) SR2, C (=O) NR3R4, C (=S) NR3R4, C (=O) R2, C (=S) R2, C (=N-R3) R2, C (=N-OR3) R2, C (=N- NR3R4)R2, OP (=O) (OR2) 2, SO2NR3R4, NR3R4 and (Ci-Cio) alkylNR3R4, ar (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, or ar (C1- Clo) alkyl, ar (C2-C10) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, cyclo (C3-C8) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci- Clo) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or

more substituents independently selected from halo, hydroxy, nitro, cyano, (C1- Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy and NR3R4, heteroar (Ci- Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl, or heteroar (Ci-Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Cio) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, (Ci- Cio) alkylcarbonyl (Ci-Clo) alkyl, (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl, (C2- C10)alkylnylcarbonyl(C1-C10)alkyl, heterocyclyl, heterocyclyl(C1-C10)alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Clo) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl, arylcarbonyl, arylcarbonyl (Ci-Cio) alkyl, ar (C1- Clo) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl, aroxycarbonyl (C1-C10)alkyl, ar (Ci-Cio) alkoxycarbonyl, ar (C1-C10)alkoxycarbonyl(C1- Cio) alkyl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, or heterocyclyl, heterocyclyl (C1-C10) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Clo) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (C1-C10) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl, arylcarbonyl, arylcarbonyl (C1-C10) alkyl, ar (C1- Cio) alkylcarbonyl, ar (Ci-C 10) alkylcarbonyl (Ci-Clo) alkyl, aroxycarbonyl, aroxycarbonyl (Ci-Cio) alkyl, ar (Ci-Cio) alkoxycarbonyl, ar (Ci-Cio) alkoxycarbonyl (Ci- Ciao) alkyl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Clo) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (Ci-Cio) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, and C (=N- G22) R2 when q is 0 and t is 1, G22 is OR3, OCOR3, S (O) jR3, OS (O) jR3, NR3R4, OSO2NR3R4, OP (=O) OR3NR3R4, OP (=O) (OR3) 2 or N=CR3R4, j is 0, 1 or 2,

Z2 (X2) q is halo, NR3R4, {(NR3R4R5)+ M-}, OR3, S (O) jR3 or SO2NR3R4 when both q and t are 0 wherein M-is halo, hydroxy, (Ci-Cs) alkoxy or the anion of a carboxylic acid and j is 0, 1 or 2, R'is G30 is an oxygen atom or a sulfur atom, G31 is an oxygen atom, a sulfur atom or NR3, t'and d are each independently 0 or 1, X3 is an oxygen atom, a sulfur atom, a nitrogen atom, a phosphorous atom or a carbon atom attached to Z3 when t'is 0, a nitrogen atom attached to Z3 when t'is 1 and G31 is NR3, or a carbon atom attached to Z3 when t'is 1 and G3l is an oxygen atom or a sulfur atom, Z3 (X3) d (G3l) t' is a pharmaceutical moiety when d is 1 wherein Z3 (X3) d (G31) t'-H represents the pharmaceutical, Z3 (X3) d, when d is 0 and t'is 1, is a hydrogen atom, (C1-C20) alkyl, (Cl- Clo) alkylcarbonyloxy (Ci-Cio) alkyl, (C1-C20) alkylcarbonyl, (C1-C10) alkylcarbonyl (C1- Cio) alkyl, hydroxy (C1-C20) alkyl, (C1-C10) alkylsulfonyl (Ci-Cio) alkyl, (Ci- Cio) alkylcarbonylamino (Ci-Cio) alkyl, arylcarbonylamino (Ci-Cio) alkyl, heteroarylcarbonylamino (Ci-Cio) alkyl, acetylamino (Ci-Cio) alkyl, halo (Ci-C2o) alkyl, (C2-C10) alkenyl, (C2-Cio) alkenylcarbonyl (Ci-Clo) alkyl, acetylamino (C2-Cio) alkenyl, halo (C2-Cio) alkenyl, (C2-Cio) alkynyl, (C2-Cio) alkynylcarbonyl (Ci-Cio) alkyl, halo (C2- Clo) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxycyclo (C3- C8) alkyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkyl (C2-Cio) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkynyl, (C1-C10) alkoxy (C1- Cio) alkyl, (C1-C10) alkoxy (Ci-Cio) alkoxy (Ci-Cio) alkyl, (C1-C10) alkoxy (C2-Cio) alkenyl, (C1-C10) alkoxy (C2-C10) alkynyl, (C1-C10) alkoxycarbonyl (C1-C10) alkyl, (C1- Clo) alkoxycarbonyl (C2-C10) alkenyl, (C1-C10) alkoxycarbonyl (C2-C10) alkynyl, halo (C1-

Cio) alkoxy (C1-C10) alkyl, halo (Ci-Cio) alkoxy (C2-Cio) alkenyl, halo (Ci-Cio) alkoxy (C2- Cio) alkynyl, (Ci-Cio) alkylthio (C1-C10) alkyl, (C1-C10) alkylthio (C2-C10) alkenyl, (Ci- Cio) alkylthio (C2-Cio) alkynyl, halo (Ci-Cio) alkylthio (Ci-Cio) alkyl, halo (Ci- Clo) alkylthio (C2-Cio) alkenyl, halo (Ci-Cio) alkylthio (C2-Cio) alkynyl, carboxy (C1- C2o) alkyl, carboxy (C2-C10) alkenyl, carboxy (C2-C10) alkynyl, NR3R4, OR3, S (O) jR3, aryl, arylcarbonyloxy (C1-C10)alkyl, arylcarbonyl(C1-C10) alkyl, aroxycarbonyl (C1-C10) alkyl, or aryl, arylcarbonyloxy (Ci-Cio) alkyl, arylcarbonyl (Cl-Cio) alkyl, aroxycarbonyl (C1- Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, (C1-C10) alkyl, (C1-C10) alkylsulfonyl (C1- Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Clo) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (Cl-Cio) alkoxy, SO2NR3R4 and NR3R4, ar (C1- Clo) alkyl, ar (C1-C10) alkylcarbonyloxy (Ci-Cio) alkyl, ar (Ci-Cio) alkylcarbonyl (C1- Clo) alkyl, ar (Ci-Cio) alkoxycarbonyl (C1-C10) alkyl, ar (C2-Cio) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (C1-C10) alkyl, or ar (C1-C10) alkyl, ar (C1- Clo) alkylcarbonyloxy (Ci-Cio) alkyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (C1- Clo) alkoxycarbonyl (Ci-Clo) alkyl, ar (C2-Cio) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3- C8) alkyl, aroxy (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, cyclo (C3-C8) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyloxy (Ci-Cio) alkyl, heteroarylcarbonyl (C1-C10) alkyl, heteroaroxycarbonyl (C1-C10) alkyl, or heteroaryl, heteroarylcarbonyloxy (Ci-Cio) alkyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, heteroar (Ci-Clo) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-C10) alkynyl, or heteroar (Ci-Clo) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-Clo) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Clo) alkyl, halo (C2- Clo) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4, heterocyclyl, heterocyclylcarbonyloxy (C1-C10) alkyl, hetercyclylcarbonyl (Ci- Cio) alkyl, heterocyclyloxycarbonyl (C1-C10) alkyl, or heterocyclyl,

heterocyclylcarbonyloxy (Ci-Cio) alkyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, wherein j is 0, 1 or 2, Z3 (X3) d is halo, NR3R4, OR3, N (R3)-N=CR3R4, S (O) jR3 or SO2NR3R4 when both d and t'are 0 and j is 0, 1 or 2, (d + q) is 0 or 1, R2 is a hydrogen atom, (C1-C20) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, (Ci- Clo) alkoxy (C1-C10) alkyl, (C1-C10) alkoxy (C2-C10) alkenyl, (C1-C10) alkoxy (C2-C10) alkynyl, (Ci-Cio) alkylthio (C1-C10) alkyl, (C1-C10) alkylthio (C2-C10) alkenyl, (Ci-Cio) alkylthio (C2- Cio) alkynyl, carboxy, a carboxylate salt, carboxy (Ci-C2o) alkyl, carboxy (C2-C20) alkenyl, carboxy (C2-C2o) alkynyl, (C1-C20)alkoxycarbonyl, (C1-C10)alkoxycarbonyl(C1-C10)alkyl, (C1-C10) alkoxycarbonyl (C2-C10) alkenyl, (C1-C10) alkoxycarbonyl (C2-C10) alkynyl, (Ci- C2o) alkylcarbonyl, (C2-C2o) alkenylcarbonyl, (C2-C2o) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3- C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, heterocyclyl, heterocyclyl (Cl-Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-C10) alkynyl, or (Ci-C2o) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, (Ci-Cio) alkoxy (Ci-Cio) alkyl, (Ci- Cio) alkoxy (C2-Cio) alkenyl, (C1-C10) alkoxy (C2-C10) alkynyl, (C1-C10) alkylthio (C1- Cio) alkyl, (Ci-Clo) alkylthio (C2-C10) alkenyl, (Ci-Cio) alkylthio (C2-C10) alkynyl, carboxy (Ci-C2o) alkyl, carboxy (C2-C10) alkenyl, carboxy (C2-Cio) alkynyl, (Ci- C2o) alkoxycarbonyl, (Ci-Cio) alkoxycarbonyl (C1-C10) alkyl, (C1-C10) alkoxycarbonyl (C2- Cio) alkenyl, (Ci-Cio) alkoxycarbonyl (C2-C10) alkynyl, (C1-C20) alkylcarbonyl, (C2- Cio) alkenylcarbonyl, (C2-C10)alkynylcarbonyl, cyclo(C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1-C10) alkyl, cyclo (C3-C8) alkenyl (Ci-Clo) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, heterocyclyl, heterocyclyl (Ci-Clo) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, SO2NR3R4 and NR3R4, aryl or aryl substituted with one or more substituents independently selected

from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2- Cio) alkenyl, halo (C2-C10) alkynyl ; (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, carboxy, (C1- C4) alkoxycarbonyl, S02NR3R4 and NR3R4, ar (C1-C10) alkyl, ar (C2-Cio) alkenyl, ar (C2- Clo) alkynyl, or ar (C1-C10) alkyl, ar (C2-Cio) alkenyl, ar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, arylcarbonyl, ar (Cl-Cio) alkylcarbonyl, ar (C2-C10) alkenylcarbonyl, ar (C2-Cio) alkynylcarbonyl, aroxycarbonyl (C1-C10) alkyl, or arylcarbonyl, ar (C1-C10) alkylcarbonyl, ar (C2- Clo) alkenylcarbonyl, ar (C2-C10) alkynylcarbonyl, aroxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (Ci- Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2- Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (C1- Clo) alkoxy, halo (Ci-Clo) alkoxy and NR3R4, heteroar (Cl-Cio) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-Cio) alkynyl or heteroar (Cl-Cio) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2-Cto) alkynyl, (C1-C10) alkoxy, halo (Ci- Cio) alkoxy, SO2NR3R4 and NR3R4, heteroarylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl, heteroar (C2-C10) alkenylcarbonyl, heteroar (C2-C10) alkynylcarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (Ci- Clo) alkyl, or heteroarylcarbonyl, heteroar (C1-C10) alkylcarbonyl, heteroar (C2- Cio) alkenylcarbonyl, heteroar (C2-C10) alkynylcarbonyl, heteroaroxycarbonyl (C1- Cio) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, or Ri and R2 taken together with the carbon atom to which they are attached form a 5-7 membered saturated or unsaturated ring,

R3, R4 and R5 are each independently a hydrogen atom, (C1-C20) alkyl, cyclo (C3- C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Ciao) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3-C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkenyl (C2-Clo) alkynyl, carboxy (C1- C2o) alkyl, carboxy (C2-Cio) alkenyl, carboxy (C2-Cio) alkynyl, (Ci-Cio) alkoxy (Ct-Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, or (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, cyclo (C3- C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3- C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2- Cio) alkenyl, cyclo (C3-Cs) alkenyl (C2-Cio) alkynyl, carboxy (Ci-C2o) alkyl, carboxy (C2- Clo) alkenyl, carboxy (C2-Cio) alkynyl, (Ci-Cio) alkoxy (Ci-Cio) alkyl, (C2-Cio) alkenyl or (C2-Cio) alkynyl substituted with one or more halo, aryl, ar (Ci-Cio) alkyl, ar (C2- Cio) alkenyl, ar (C2-Cio) alkynyl or aryl, ar (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2- Clo) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2- Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy and halo (Ci-Cio) alkoxy, heteroaryl, heteroar (C1-C10) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl or heteroaryl, heteroar (C1-C10) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, (Ci-Cio) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy and halo (C1-C10) alkoxy, heterocyclyl, heterocyclyl (C1- Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-C10) alkynyl, or heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci- Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SORNR3R4 and NR3R4, or R3 and R4 taken together with the nitrogen atom to which they are attached form a 5-or 6-membered saturated or unsaturated heterocyclic ring, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof.

In a ninth embodiment of this invention, the pharmaceutical compound is represented by formula (I)

wherein A is Giro, G"and G20 are each independently an oxygen atom or a sulfur atom, G21 is an oxygen atom, a sulfur atom or NR3, X'is an oxygen atom attached to Zl, X2 is an oxygen atom, a sulfur atom, a phosphorous atom, a nitrogen atom or a carbon atom attached to Z2, m is 1, q and t are each independently 0 or 1, Zl (X1) m is a pharmaceutical moiety selected from wherein ZI (X1)m-H represents the respective pharmaceutical selected from # represents the connection point between said pharmaceutical moiety and the moiety represented by Z2 (X2) q (C (-G20)G21)t is a pharmaceutical moiety when q is 1 wherein Z2 (X2) q (C (=G") G21) t or Z2(X2) q (C (=G20) G2') t-H represents the pharmaceutical,

Z' (XI) m, when m is 0, is a hydrogen atom, halo, (C1-C20) alkyl, (Cl- Cio) alkylcarbonyloxy (Ci-Cio) alkyl, (Ci-C2o) alkylcarbonyl, hydroxy (C1-C20) alkyl, (Ci- Clo) alkylsulfonyl (Ci-Cio) alkyl, (Ci-Cio) alkylcarbonylamino (C1-C10) alkyl, arylcarbonylamino (Cl-Cio) alkyl, heteroarylcarbonylamino (Ci-Cio) alkyl, halo (C1- C20) alkyl, (C2-C2o) alkenyl, halo (C2-C2o) alkenyl, (C1-C10) alkylcarbonylamino (C2- Clo) alkenyl, arylcarbonylamino (C2-C10) alkenyl, heteroarylcarbonylamino (C2- Cio) alkenyl, (C2-C2o) alkynyl, halo (C2-C2o) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3- C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci- Clo) alkyl, cyclo (C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3- C8) alkenyl (C2-Cio) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2- Clo) alkynyl, carboxycyclo (C3-C8) alkyl (Ci-Cio) alkyl, carboxy (C3-C8) cycloalkyl (C2- Clo) alkenyl, carboxycyclo (C3-C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2- Clo) alkenyl, carboxycyclo (C3-C8) alkyl (C1-C10) alkynyl, carboxycyclo (C3-C8) alkenyl (C2- Cio) alkynyl, (C1-C10) alkoxy (C1-C10) alkyl, (C1-C5) alkoxy (Ci-C5) alkoxy (Ci-Cio) alkyl, (Cl- Cio) alkoxy (C2-C10) alkenyl, (Ci-Cio) alkoxy (C2-C10) alkynyl, (C1-C10) alkoxycarbonyl, (Ci- C10)alkoxycarbonyl(C1-C10)alkyl, (C1-C10)alkoxycarbonyl(C2-C10) alkenyl, (C1- Cio) alkoxycarbonyl (C2-C10) alkynyl, halo (Ci-Cio) alkoxy (C1-C10) alkyl, halo (C1- Cio) alkoxy (C2-C10) alkenyl, halo (Ci-Cio) alkoxy (C2-Cio) alkynyl, (Ci-Clo) alkylthio (Ci- Clo) alkyl, (Ci-Cio) alkylthio (C2-C10) alkenyl, (Ci-Cio) alkylthio (C2-C10) alkynyl, halo (C1- Clo) alkylthio (C1-C10) alkyl, halo (Ci-Clo) alkylthio (C2-Cio) alkenyl, halo (Ci- Cio) alkylthio (C2-C10) alkynyl, SO2NR3R4, NR3R4, OR3, S (O) jR3, carboxy (C1-C20) alkyl, carboxy (C2-C20) alkenyl, carboxy (C2-C20) alkynyl, aryl, arylcarbonyl, arylcarbonyl (Ci- Clo) alkyl, aroxycarbonyl, aroxycarbonyl (Cl-Cio) alkyl, or aryl, arylcarbonyl, arylcarbonyl (C1-C10) alkyl, aroxycarbonyl, aroxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, (Ci-Cio) alkyl, (C1-C10) alkylsulfonyl (C1-C10) alkyl, (C1-C10) alkylsulfonyl, thiocyanato, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Cl-Clo) alkyl, halo (C2-C10) alkenyl, halo (C2- Cio) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, S02NR3R4, and NR3R4, ar (Ci- Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, ar (Ci-Cio) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (C2- Cio) alkenylcarbonyl, ar (C2-C10 alkenylcarbonyl (Ci-Clo) alkyl, or ar (C1-C10) alkyl, ar (C2- Cio) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, ar (Ci- Cio) alkylcarbonyl, ar (C1-C10) alkylcarbonyl (C1-C10) alkyl, ar (C2-C10) alkenylcarbonyl,

ar (C2-Cio) alkenylcarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, cyclo (C3- C8) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, or heteroaryl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (C1- Clo) alkyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci- Clo) alkyl, halo (C2-Clo) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (C1-C10) alkoxy and NR3R4, heteroar (Ci-Cio) alkyl, heteroar (C2-Clo) alkenyl, heteroar (C2-Cio) alkynyl, heteroar (C1-C1) alkylcarbonyl, heteroar (C1-C10) alkylcarbonyl (Ci-Cio) alkyl, heteroar (C2-C10) alkenylcarbonyl, heteroar (C2-C10) alkenylcarbonyl (Ci-Cio) alkyl, or heteroar (C1-C10 alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl, heteroar (Ci- Clo) alkylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl (C1-C10) alkyl, heteroar (C2- Clo) alkenylcarbonyl, heteroar (C2-Cio) alkenylcarbonyl (Ci-Clo) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Cl-Cio) alkyl, halo (C2-Clo) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2- Clo) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Cl-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl, or heterocyclyl, heterocyclyl (C1-C10) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-C10) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cjo) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (C1-C10) alkyl, (C2- Clo) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2- Clo) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4 wherein j is 0, 1 or 2, Z2 (X2) q is a hydrogen atom, (Ci-C2o) alkyl, (C1-C10) alkylcarbonyloxy (C1- Cio) alkyl, (C1-C20) alkylcarbonyl, (Ci-C2o) alkenylcarbonyl, (C1-C20) alkynylcarbonyl, hydroxy (Ci-C2o) alkyl, (C1-C10) alkylsulfonyl (Ci-Cio) alkyl, (C1- C to) alkylcarbonylamino (Ci-Cio) alkyl, arylcarbonylamino (Ci-Clo) alkyl,

heteroarylcarbonylamino (Ci-Cio) alkyl, halo (C1-C20) alkyl, (C2-C2o) alkenyl, halo (C2- C2o) alkenyl, (C1-C10) alkylcarbonylamino (C2-C10) alkenyl, arylcarbonylamino (C2- Clo) alkenyl, heteroarylcarbonylamino (C2-Cio) alkenyl, (C2-C2o) alkynyl, halo (C2- C2o) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxycyclo (C3- C8) alkyl (Ci-Cio) alkyl, carboxy (C3-C8) cycloalkyl (C2-Cio) alkenyl, carboxycyclo (C3- (C8) alkenyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkenyl, carboxycyclo (C3- C8) alkyl (C2-Cio) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkynyl, (C1-C10) alkoxy (C1- Clo) alkyl, (C1-C5) alkoxy (Cl-Cs) alkoxy (C1-C10) alkyl, (C1-C10) alkoxy (C2-Cio) alkenyl, (C1- Clo) alkoxy (C2-Cio) alkynyl, (Ci-Cio) alkoxycarbonyl, (Ci-Cio) alkoxycarbonyl (C1- Clo) alkyl, (Cl-Clo) alkoxycarbonyl (C2-Cio) alkenyl, (C1-C10) alkoxycarbonyl (C2- Clo) alkynyl, halo (Ci-Cio) alkoxy (Ci-Cio) alkyl, halo (Ci-Cio) alkoxy (C2-Cio) alkenyl, halo (Ci-Cio) alkoxy (C2-Cio) alkynyl, (C1-C10) alkylthio (Ci-Cio) alkyl, (C1-C10) alkylthio (C2- Clo) alkenyl, (C1-C10) alkylthio (C2-C10) alkynyl, halo (Ci-Cio) alkylthio (Ci-Cio) alkyl, halo (C1-C10) alkylthio (C2-C10) alkenyl, halo (Ci-Cio) alkylthio (C2-C10) alkynyl, SO2NR3R4, NR3R4, carboxy(C1-C20)alkyl, carboxy(C2-C20)alkenyl, carboxy(C2-C20)alkynyl, di (Ci- Clo) alkoxyphosphoryl (C1-C10) alkyl, aryl, aryl substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, (Cl-Cio) alkyl, (C1-C10) alkylsulfonyl (C1-C10) alkyl, (C1-C10) alkylsulfonyl, thiocyanato, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1- Cio) alkoxy, halo (Ci-Cio) alkoxy, C (=O) OR2, C (=O) SR2, C (=S) OR2, C (=S) SR2, C (=O) NR3R4, C (=S) NR3R4, C (=O) R2, C (=S) R2, C (=N-R3) R2, C (=N-OR3) R2, C (=N- NR3R4) R2, OP (=O) (OR2) 2, SO2NR3R4, NR3R4 and (Ci-Cio) alkylNR3R4, ar (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3-C8) alkyl, aroxy (C1-C10) alkyl, or ar (Ci- Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci- Clo) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (Ci- Cio) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl,

halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy and NR3R4, heteroar (Ci- Cio) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl, or heteroar (Ci-Cio) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Clo) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Clo) alkenyl, halo (C2- Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, (C1- Cio) alkylcarbonyl (Ci-Cio) alkyl, (C2-C10) alkenylcarbonyl (Ci-Cio) alkyl, (C2- Clo) alkynylcarbonyl (Ci-Cio) alkyl, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Clo) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (C1-C10) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl, arylcarbonyl, arylcarbonyl (C1-C10) alkyl, ar (C1- Cio) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl, aroxycarbonyl (C1-C10) alkyl, ar (Cz-Clo) alkoxycarbonyl, ar (Ci-Cio) alkoxycarbonyl (Ci- Clo) alkyl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (Ci-Cio) alkyl, or heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Clo) alkynyl, heterocyclylcarbonyl, heterocyclylcarbonyl (Ci-Cio) alkyl, heterocyclyloxycarbonyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl, arylcarbonyl, arylcarbonyl (C1-C10) alkyl, ar (C1- Clo) alkylcarbonyl, ar (Ci-Cio) alkylcarbonyl (C1-C10) alkyl, aroxycarbonyl, aroxycarbonyl (Ci-Cio) alkyl, ar (Ci-Cio) alkoxycarbonyl, ar (Ci-Cio) alkoxycarbonyl (C1- Cio) alkyl, heteroarylcarbonyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl, heteroaroxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, hydroxy, nitro, cyano, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4, and C (=N- G22) R2 when q is 0 and t is 1, G22 is OR3, OCOR3, S (O) jR3, OS (O) jR3, NR3R4, OSO2NR3R4, OP (=O) OR3NR3R4, OP (=O) (OR3) 2 or N=CR3R4, j is 0, 1 or 2, Z2 (X2) q is halo, NR3R4, {(NR3R4R5)+M-}, OR3, S (O) jR3 or S02NR3R4 when both q and t are 0 wherein M-is halo, hydroxy, (Ci-C8) alkoxy or the anion of a carboxylic acid and j is 0, 1 or 2,

R1 is wherein G30 is an oxygen atom or a sulfur atom, G31 is an oxygen atom, a sulfur atom or NR3, t'and d are each independently 0 or 1, X3 is an oxygen atom, a sulfur atom, a nitrogen atom, a phosphorous atom or a carbon atom attached to Z3 when t'is 0, a nitrogen atom attached to Z3 when t'is 1 and G31 is NR3, or a carbon atom attached to Z3 when t'is 1 and G3l is an oxygen atom or a sulfur atom, Z3 (X3) d (G31) t is a pharmaceutical moiety when d is 1 wherein Z3 (X3) d (G31) t'-H represents the pharmaceutical, Z3 (X3) d, when d is 0 and t'is 1, is a hydrogen atom, (C1-C20) alkyl, (Ci- C10) alkylcarbonyloxy (C1-C10)alkyl, (C1-C20) alkylcarbonyl, (C1-C10) alkylcarbonyl (C1- Clo) alkyl, hydroxy (C1-C20) alkyl, (C1-C10) alkylsulfonyl (Ci-Cio) alkyl, (Ci- Cio) alkylcarbonylamino (Ci-Cio) alkyl, arylcarbonylamino (Ci-Cio) alkyl, heteroarylcarbonylamino (Ci-Cio) alkyl, acetylamino (Ci-Cio) alkyl, halo (C1-C20) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkenylcarbonyl (C1-C10) alkyl, acetylamino (C2-Cio) alkenyl, halo (C2-Cio) alkenyl, (C2-Cio) alkynyl, (C2-Cio) alkynylcarbonyl (Ci-Cio) alkyl, halo (C2- Cio) alkynyl, cyclo (C3-C8) alkyl, cyclo (C3-Cs) alkenyl, carboxycyclo (C3-C8) alkyl, carboxycyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Clo) alkyl, cyclo (C3-C8) alkyl (C2- C10) alkenyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2-Cio) alkynyl, carboxycyclo (C3- C8) alkyl (Ci-Cio) alkyl, carboxycyclo (C3-C8) alkyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkenyl (C1-C10) alkyl, carboxycyclo (C3-C8) alkenyl (C2-C10) alkenyl, carboxycyclo (C3- C8) alkyl (C2-Cio) alkynyl, carboxycyclo (C3-C8) alkenyl (C2-Cio) alkynyl, (C1-C10) alkoxy (C1- Cio) alkyl, (C1-C10) alkoxy (C1-C10) alkoxy (Ci-Cio) alkyl, (Ci-Cio) alkoxy (C2-Cio) alkenyl, (C1-C10) alkoxy (C2-C10) alkynyl, (C1-C10) alkoxycarbonyl (C1-C10) alkyl, (Cl- Cio) alkoxycarbonyl (C2-C10) alkenyl, (Ci-Co) alkoxycarbonyl (C2-C10) alkynyl, halo (C1- Clo) alkoxy (C1-C10) alkyl, halo (Cl-Cio) alkoxy (C2-C10) alkenyl, halo (Ci-Cio) alkoxy (C2- Cio) alkynyl, (C1-C10) alkylthio (Ci-Cio) alkyl, (C1-C10) alkylthio (C2-C10) alkenyl, (C1- Clo) alkylthio (C2-C10) alkynyl, halo (Ci-Cio) alkylthio (C1-C10) alkyl, halo (Ci-

Clo) alkylthio (C2-Cio) alkenyl, halo (Ci-Cio) alkylthio (C2-C10) alkynyl, carboxy (Ci- C2o) alkyl, carboxy (C2-C10) alkenyl, carboxy (C2-Cio) alkynyl, NR3R4, OR3, S (O) jR3, aryl, arylcarbonyloxy (Ci-Cio) alkyl, arylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl (Cl-Cio) alkyl, or aryl, arylcarbonyloxy (Cl-Clo) alkyl, arylcarbonyl (Ci-Cio) alkyl, aroxycarbonyl (C1- Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, thiocyanato, (C1-C10) alkyl, (C1-C10) alkylsulfonyl (C1- Cio) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Cl-Clo) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, ar (C1- Clo) alkyl, ar (Ci-Cio) alkylcarbonyloxy (C1-C10) alkyl, ar (Ci-Cio) alkylcarbonyl (Ci- Cio) alkyl, ar (Ci-Cio) alkoxycarbonyl (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2-Cio) alkynyl, arcyclo (C3-C8) alkyl, aroxy (Ci-Cio) alkyl, or ar (Ci-Cio) alkyl, ar (C1- Clo) alkylcarbonyloxy (C1-C10) alkyl, ar (Ci-Cio) alkylcarbonyl (Ci-Cio) alkyl, ar (Ci- Cio) alkoxycarbonyl (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-C10) alkynyl, arcyclo (C3- (C8) alkyl, aroxy (C1-C10) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, cyclo (C3-C8) alkyl, (C2- Clo) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroarylcarbonyloxy (Ci-Cio) alkyl, heteroarylcarbonyl (Ci-Cio) alkyl, heteroaroxycarbonyl (Cl-Cio) alkyl, or heteroaryl, heteroarylcarbonyloxy (Ci-Cio) alkyl, heteroarylcarbonyl (C1-C10) alkyl, heteroaroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heteroar (Cl-Cio) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl, or heteroar (Ci-Cio) alkyl, heteroar (C-C10) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2- Cio) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4, heterocyclyl, heterocyclylcarbonyloxy (Ci-Cio) alkyl, hetercyclylcarbonyl (C1- Cio) alkyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl, or heterocyclyl, heterocyclylcarbonyloxy (C1-C10)alkyl, heterocyclylcarbonyl (C1-C10)alkyl, heterocyclyloxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, nitro, hydroxy, cyano, (C1-C10) alkyl, (C2-

Clo) alkenyl, (C2-Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-C10) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, S02NR3R4 and NR3R4, wherein j is 0, 1 or 2, Z3 (X3) d is halo, NR3R4, OR3, N (R3)-N=CR3R4, S (O) jR3 or SO2NR3R4 when both d and t'are 0 and j is 0, 1 or 2, (d + q) is 0 or 1, R2 is a hydrogen atom, (C1-C20) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, (Ci- Cio) alkoxy (Ci-Clo) alkyl, (C1-C10) alkoxy (C2-Cio) alkenyl, (C1-C10) alkoxy (C2-C10) alkynyl, (C1-C10) alkylthio (C1-C10) alkyl, (C1-C10) alkylthio (C2-Cio) alkenyl, (Ci-Cio) alkylthio (C2- Cio) alkynyl, carboxy, a carboxylate salt, carboxy (C1-C20) alkyl, carboxy (C2-C2o) alkenyl, carboxy (C2-C20) alkynyl, (C1-C20) alkoxycarbonyl, (Ci-Cio) alkoxycarbonyl (C1-C10)alkyl, (Ci-Cio) alkoxycarbonyl (C2-Cio) alkenyl, (C1-C10)alkoxycarbonyl(C2-C10) alkynyl, (Ci- C2o) alkylcarbonyl, (C2-C2o) alkenylcarbonyl, (C2-C2o) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3-C8) alkyl (C2-10) alkenyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3- C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Cio) alkynyl, or (C1-C20) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, (C1-C10) alkoxy (Ci-Cio) alkyl, (Ci- C10) alkoxy (C2-C10) alkenyl, (Ci-Cio) alkoxy (C2-Cio) alkynyl, (Ci-Clo) alkylthio (C1- C10) alkyl, (Ci-Cio) alkylthio (C2-Cio) alkenyl, (C1-C10) alkylthio (C2-Cio) alkynyl, carboxy (C1-C20) alkyl, carboxy (C2-C10) alkenyl, carboxy (C2-Cio) alkynyl, (Ci- C2o) alkoxycarbonyl, (Ci-Co) alkoxycarbonyl (Ci-Cio) alkyl, (Ci-Cio) alkoxycarbonyl (C2- Clo) alkenyl, (C1-C10) alkoxycarbonyl (C2-Cio) alkynyl, (C1-C20) alkylcarbonyl, (C2- Cio) alkenylcarbonyl, (C2-Cio) alkynylcarbonyl, cyclo (C3-C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (C1-C10) alkyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-C10) alkenyl, heterocyclyl (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, SO2NR3R4 and NR3R4, aryl or aryl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (Cz-Cio) alkenyl, (C2-C10) alkynyl, halo (Cl-Cio) alkyl, halo (C2- Cio) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, carboxy, (C1- C4) alkoxycarbonyl, SO2NR3R4 and NR3R4, ar (Ci-Clo) alkyl, ar (C2-C10) alkenyl, ar (C2-

Cio) alkynyl, or ar (Ci-Cio) alkyl, ar (C2-Cio) alkenyl, ar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, (Ci-Cio) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Clo) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, arylcarbonyl, ar (Ci-Cio) alkylcarbonyl, ar (C2-Cio) alkenylcarbonyl, ar (C2-Cio) alkynylcarbonyl, aroxycarbonyl (Ci-Clo) alkyl, or arylcarbonyl, ar (Cl-Cio) alkylcarbonyl, ar (C2- Cio) alkenylcarbonyl, ar (C2-Cio) alkynylcarbonyl, aroxycarbonyl (Ci-Cio) alkyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-C10) alkenyl, (C2-Cio) alkynyl, halo (C1- Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2-Cio) alkynyl, (C1-C10) alkoxy, halo (Ci-Cio) alkoxy, SO2NR3R4 and NR3R4, heteroaryl, heteroaryl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2- Cio) alkynyl, halo (C1-C10) alkyl, halo (C2-Cio) alkenyl, halo (C2-C10) alkynyl, (Ci- Cio) alkoxy, halo (C1-C10) alkoxy and NR3R4, heteroar (Ci-Clo) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-C10) alkynyl or heteroar (C1-C10) alkyl, heteroar (C2- Cio) alkenyl, heteroar (C2-C10) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (C1-C10) alkoxy, halo (Ci- Cio) alkoxy, SO2NR3R4 and NR3R4, heteroarylcarbonyl, heteroar (C1-C10) alkylcarbonyl, heteroar (C2-C10) alkenylcarbonyl, heteroar (C2-C10) alkynylcarbonyl, heteroaroxycarbonyl (Cl-Cio) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (C1- Cio) alkyl, or heteroarylcarbonyl, heteroar (Ci-Cio) alkylcarbonyl, heteroar (C2- Cio) alkenylcarbonyl, heteroar (C2-C10) alkynylcarbonyl, heteroaroxycarbonyl (Ci- Cio) alkyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl (C1-C10) alkyl substituted with one or more substituents independently selected from halo, cyano, hydroxy, nitro, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-C10) alkynyl, halo (Ci-Cio) alkyl, halo (C2-C10) alkenyl, halo (C2-C10) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, or Rl and R2 taken together with the carbon atom to which they are attached form a 5-7 membered saturated or unsaturated ring, R3, R4 and R5 are each independently a hydrogen atom, (Ci-C2o) alkyl, cyclo (C3- C8) alkyl, cyclo (C3-C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2- Clo) alkenyl, cyclo (C3-C8) alkyl (C2-Cio) alkynyl, cyclo (C3-C8) alkenyl (Ci-Cio) alkyl, cyclo (C3-C8) alkenyl (C2-C10) alkenyl, cyclo (C3-C8) alkenyl (C2-C10) alkynyl, carboxy (C1-

C2o) alkyl, carboxy (C2-Cio) alkenyl, carboxy (C2-Cio) alkynyl, (Ci-Cio) alkoxy (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-C10)alkynyl, or (Ci-Cio) alkyl, cyclo (C3-C8) alkyl, cyclo (C3- C8) alkenyl, cyclo (C3-C8) alkyl (Ci-Cio) alkyl, cyclo (C3-C8) alkyl (C2-Cio) alkenyl, cyclo (C3- C8) alkyl (C2-C10) alkynyl, cyclo (C3-C8) alkenyl (C1-C10) alkyl, cyclo (C3-C8) alkenyl (C2- Clo) alkenyl, cyclo (C3-Cs) alkenyl (C2-C10) alkynyl, carboxy (Ci-C2o) alkyl, carboxy (C2- Cio) alkenyl, carboxy (C2-Cio) alkynyl, (C1-C10) alkoxy (Ci-Cio) alkyl, (C2-Cio) alkenyl or (C2-Clo) alkynyl substituted with one or more halo, aryl, ar (Ci-Cio) alkyl, ar (C2- Clo) alkenyl, ar (C2-C10) alkynyl or aryl, ar (Ci-Cio) alkyl, ar (C2-C10) alkenyl, ar (C2- Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2-C10) alkenyl, (C2-C10) alkynyl, halo (Cl-Clo) alkyl, halo (C2- Clo) alkenyl, halo (C2-Cio) alkynyl, (Ci-Cio) alkoxy and halo (C1-C10) alkoxy, heteroaryl, heteroar (Ci-Cio) alkyl, heteroar (C2-C10) alkenyl, heteroar (C2-Cio) alkynyl or heteroaryl, heteroar (Ci-Clo) alkyl, heteroar (C2-Cio) alkenyl, heteroar (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, (C1-C10) alkyl, (C2- Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci-Cio) alkyl, halo (C2-Cio) alkenyl, halo (C2- Cio) alkynyl, (Ci-Cio) alkoxy and halo (Ci-Cio) alkoxy, heterocyclyl, heterocyclyl (C1- Clo) alkyl, heterocyclyl (C2-Clo) alkenyl, heterocyclyl (C2-Cio) alkynyl, or heterocyclyl, heterocyclyl (Ci-Cio) alkyl, heterocyclyl (C2-Cio) alkenyl, heterocyclyl (C2-Cio) alkynyl substituted with one or more substituents independently selected from halo, hydroxy, cyano, nitro, (Ci-Cio) alkyl, (C2-Cio) alkenyl, (C2-Cio) alkynyl, halo (Ci- Cio) alkyl, halo (C2-C lo) alkenyl, halo (C2-Clo) alkynyl, (Ci-Cio) alkoxy, halo (C1-C10) alkoxy, SO2NR3R4 and NR3R4, or R3 and R4 taken together with the nitrogen atom to which they are attached form a 5-or 6-membered saturated or unsaturated heterocyclic ring, or the pharmaceutically acceptable salts, isomers, tautomers, enantiomers and mixtures thereof Another aspect of this invention relates to pharmaceutical compositions comprising a pharmaceutical compound of this invention and a pharmaceutically acceptable carrier. Preferably, the composition contains from about 0. 1% to about 99% by weight of said pharmaceutical compound depending on the host treated, the disease and the particular mode of administration.

Still another aspect of this invention relates to a method of controlling pain or disease symptoms in a warm-blooded animal exhibiting pain or disease symptoms comprising administering thereto a pharmaceutically effective amount of a compound or a composition comprising a compound of this invention and a pharmaceutically acceptable carrier.

In all embodiments of this invention, the term"alkyl"includes both branched and straight chain alkyl groups. Typical alkyl groups are methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, n-hexyl, n- heptyl, isooctyl, nonyl, decyl, undecyl, dodecyl, tetradecyl, hexadecyl, octadecyl, eicosyl and the like.

The term"halo"refers to fluoro, chloro, bromo or iodo.

The term"haloalkyl"refers to an alkyl group substituted with one or more halo groups, for example chloromethyl, 2-bromoethyl, 3-iodopropyl, trifluoromethyl, perfluoropropyl, 8-chlorononyl and the like.

The term"cycloalkyl"refers to a cyclic aliphatic ring structure, optionally substituted with alkyl, hydroxy and halo, such as cyclopropyl, methylcyclopropyl, cyclobutyl, 2-hydroxycyclopentyl, cyclohexyl, 4-chlorocyclohexyl, cycloheptyl, cyclooctyl and the like.

The term"alkylcarbonyloxyalkyl"refers to an ester moiety, for example acetoxymethyl, ll-butyryloxyethyl and the like.

The term"alkynylcarbonyl"refers to an alkynylketo functionality, for example propynoyl and the like.

The term"hydroxyalkyl"refers to an alkyl group substituted with one or more hydroxy groups, for example hydroxymethyl, 2, 3-dihydroxybutyl and the like.

The term"alkylsulfonylalkyl"refers to an alkyl group substituted with an alkylsulfonyl moiety, for example mesylmethyl, isopropylsulfonylethyl and the like.

The term"alkylsulfonyl"refers to a sulfonyl moiety substituted with an alkyl group, for example mesyl, n-propylsulfonyl and the like.

The term"acetylaminoalkyl"refers to an alkyl group substituted with an amide moiety, for example acetylaminomethyl and the like.

The term"acetylaminoalkenyl"refers to an alkenyl group substituted with an amide moiety, for example 2- (acetylamino) vinyl and the like.

The term"alkenyl"refers to an ethylenically unsaturated hydrocarbon group, straight or branched chain, having 1 or 2 ethylenic bonds, for example vinyl, allyl, 1- butenyl, 2-butenyl, isopropenyl, 2-pentenyl and the like.

The term"haloalkenyl"refers to an alkenyl group substituted with one or more halo groups.

The term"cycloalkenyl"refers to a cyclic aliphatic ring structure, optionally substituted with alkyl, hydroxy and halo, having 1 or 2 ethylenic bonds such as methylcyclopropenyl, trifluoromethylcyclopropenyl, cyclopentenyl, cyclohexenyl, 1, 4- cyclohexadienyl and the like.

The term"alkynyl"refers to an unsaturated hydrocarbon group, straight or branched, having 1 or 2 acetylenic bonds, for example ethynyl, propargyl and the like.

The term"haloalkynyl"refers to an alkynyl group substituted with one or more halo groups.

The term"alkylcarbonyl"refers to an alkylketo functionality, for example acetyl, n-butyryl and the like.

The term"alkenylcarbonyl"refers to an alkenylketo functionality, for example, propenoyl and the like.

The term"aryl"refers to phenyl or naphthyl which may be optionally substituted. Typical aryl substituents include, but are not limited to, phenyl, 4- chlorophenyl, 4-fluorophenyl, 4-bromophenyl, 3-nitrophenyl, 2-methoxyphenyl, 2- methylphenyl, 3-methyphenyl, 4-methylphenyl, 4-ethylphenyl, 2-methyl-3- methoxyphenyl, 2, 4-dibromophenyl, 3, 5-difluorophenyl, 3, 5-dimethylphenyl, 2, 4, 6- trichlorophenyl, 4-methoxyphenyl, naphthyl, 2-chloronaphthyl, 2, 4-dimethoxyphenyl, 4- (trifluoromethyl) phenyl and 2-iodo-4-methylphenyl.

The term"heteroaryl"refers to a substituted or unsubstituted 5 or 6 membered unsaturated ring containing one, two or three heteroatoms, preferably one or two heteroatoms independently selected from oxygen, nitrogen and sulfur or to a bicyclic unsaturated ring system containing up to 10 atoms including one heteroatom selected from oxygen, nitrogen and sulfur. Examples of heteroaryls include, but is not limited to, 2-, 3-or 4-pyridinyl, pyrazinyl, 2-, 4-, or 5-pyrimidinyl, pyridazinyl, triazolyl, imidazolyl, 2-or 3-thienyl, 2-or 3-furyl, pyrrolyl, oxazolyl, isoxazolyl,

thiazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, quinolyl and isoquinolyl. The heterocyclic ring may be optionally substituted with up to two substituents.

The term"aralkyl"is used to describe a group wherein the alkyl chain can be branched or straight chain with the aryl portion, as defined hereinbefore, forming a terminal portion of the aralkyl moiety. Examples of aralkyl groups include, but are not limited to, optionally substituted benzyl, phenethyl, phenpropyl and phenbutyl such as 4-chlorobenzyl, 2, 4-dibromobenzyl, 2-methylbenzyl, 2- (3-fluorophenyl) ethyl, 2- (4-methylphenyl) ethyl, 2- (4- (trifluoromethyl) phenyl) ethyl, 2- (2- methoxyphenyl) ethyl, 2- (3-nitrophenyl) ethyl, 2- (2, 4-dichlorophenyl) ethyl, 2- (3, 5- dimethoxyphenyl) ethyl, 3-phenylpropyl, 3- (3-chlorophenyl) propyl, 3- (2- methylphenyl) propyl, 3- (4-methoxyphenyl) propyl, 3- (4- (trifluoromethyl) phenyl) propyl, 3- (2, 4-dichlorophenyl) propyl, 4-phenylbutyl, 4- (4- chlorophenyl) butyl, 4- (2-methylphenyl) butyl, 4- (2, 4-dichlorophenyl) butyl, 4- (2- methoxphenyl) butyl and 10-phenyldecyl.

The term"arcycloalkyl"is used to describe a group wherein the aryl group is attached to a cycloalkyl group, for example phenylcyclopentyl and the like.

The term"aralkenyl"is used to describe a group wherein the alkenyl chain can be branched or straight chain with the aryl portion, as defined hereinbefore, forming a terminal portion of the aralkenyl moiety, for example styryl (2- phenylvinyl), phenpropenyl and the like.

The term"aralkynyl"is used to describe a group wherein the alkynyl chain can be branched or straight chain with the aryl portion, as defined hereinbefore, forming a terminal portion of the aralkynyl moiety, for example 3-phenyl-1-propynyl and the like.

The term"aroxy"is used to describe an aryl group attached to a terminal oxygen atom. Typical aroxy groups include phenoxy, 3, 4-dichlorophenoxy and the like.

The term"aroxyalkyl"is used to describe a group wherein an alkyl group is substituted with an aroxy group, for example pentafluorophenoxymethyl and the like.

The term"heteroaroxy"is used to describe an heteroaryl group attached to a terminal oxygen atom. Typical heteroaroxy groups include 4, 6-dimethoxypyrimidin- 2-yloxy and the like.

The term"heteroaralkyl"is used to describe a group wherein the alkyl chain can be branched or straight chain with the heteroaryl portion, as defined hereinbefore, forming a terminal portion of the heteroaralkyl moiety, for example 3- furylmethyl, thenyl, furfuryl and the like.

The term"heteroaralkenyl"is used to describe a group wherein the alkenyl chain can be branched or straight chain with the heteroaryl portion, as defined hereinbefore, forming a terminal portion of the heteroaralkenyl moiety, for example 3- (4-pyridyl)-l-propenyl.

The term"heteroaralkynyl"is used to describe a group wherein the alkynyl chain can be branched or straight chain with the heteroaryl portion, as defined hereinbefore, forming a terminal portion of the heteroaralkynyl moiety, for example 4- (2-thienyl)- 1-butynyl.

The term"heterocyclyl"refers to a substituted or unsubstituted 5 or 6 membered saturated ring containing one, two or three heteroatoms, preferably one or two heteroatoms independently selected from oxygen, nitrogen and sulfur or to a bicyclic ring system containing up to 10 atoms including one heteroatom selected from oxygen, nitrogen and sulfur wherein the ring containing the heteroatom is saturated. Examples of heterocyclyls include, but are not limited to, tetrahydrofuryl, pyrrolidinyl, piperidinyl, tetrahydropyranyl, morpholinyl, piperazinyl, dioxolanyl, dioxanyl, indolinyl and 5-methyl-6-chromanyl.

The term"heterocyclylalkyl"is used to describe a group wherein the alkyl chain can be branched or straight chain with the heterocyclyl portion, as defined hereinabove, forming a terminal portion of the heterocyclylalkyl moiety, for example 3-piperidinylmethyl and the like.

The term"heterocyclylalkenyl"is used to describe a group wherein the alkenyl chain can be branched or straight chain with the heterocyclyl portion, as defined hereinbefore, forming a terminal portion of the heterocyclylalkenyl moiety, for example 2-morpholinyl-l-propenyl.

The term"heterocyclylalkynyl"is used to describe a group wherein the alkynyl chain can be branched or straight chain with the heterocyclyl portion, as

defined hereinbefore, forming a terminal portion of the heterocyclylalkynyl moiety, for example 2-pyrrolidinyl-1-butynyl.

The term"carboxyalkyl"includes both branched and straight chain alkyl groups as defined hereinbefore attached to a carboxy (-COOH) group.

The term"carboxyalkenyl"includes both branched and straight chain alkenyl groups as defined hereinbefore attached to a carboxy group.

The term"carboxyalkynyl"includes both branched and straight chain alkynyl groups as defined hereinbefore attached to a carboxy group.

The term"carboxycycloalkyl"refers to a carboxy group attached to a cyclic aliphatic ring structure as defined hereinbefore.

The term"carboxycycloalkenyl"refers to a carboxy group attached to a cyclic aliphatic ring structure having 1 or 2 ethylenic bonds as defined hereinbefore.

The term"cycloalkylalkyl"refers to a cycloalkyl group as defined hereinbefore attached to an alkyl group, for example cyclopropylmethyl, cyclohexylethyl and the like.

The term"cycloalkylalkenyl"refers to a cycloalkyl group as defined hereinbefore attached to an alkenyl group, for example cyclohexylvinyl, cycloheptylallyl and the like.

The term"cycloalkylalkynyl"refers to a cycloalkyl group as defined hereinbefore attached to an alkynyl group, for example cyclopropylpropargyl, 4- cyclopentyl-2-butynyl and the like.

The term"cycloalkenylalkyl"refers to a cycloalkenyl group as defined hereinbefore attached to an alkyl group, for example 2- (cyclopenten-1-yl) ethyl and the like.

The term"cycloalkenylalkenyl"refers to a cycloalkenyl group as defined hereinbefore attached to an alkenyl group, for example 1- (cyclohexen-3-yl) allyl and the like.

The term"cycloalkenylalkynyl"refers to a cycloalkenyl group as defined hereinbefore attached to an alkynyl group, for example 1- (cyclohexen-3-yl) propargyl and the like.

The term"carboxycycloalkylalkyl"refers to a carboxy group attached to the cycloalkyl ring portion of a cycloalkylalkyl group as defined hereinbefore.

The term"carboxycycloalkylalkenyl"refers to a carboxy group attached to the cycloalkyl ring portion of a cycloalkylalkenyl group as defined hereinbefore.

The term"carboxycycloalkylalkynyl"refers to a carboxy group attached to the cycloalkyl ring portion of a cycloalkylalkynyl group as defined hereinbefore.

The term"carboxycycloalkenylalkyl"refers to a carboxy group attached to the cycloalkenyl ring portion of a cycloalkenylalkyl group as defined hereinbefore.

The term"carboxycycloalkenylalkenyl"refers to a carboxy group attached to the cycloalkenyl ring portion of a cycloalkenylalkenyl group as defined hereinbefore.

The term"carboxycycloalkenylalkynyl"refers to a carboxy group attached to the cycloalkenyl ring portion of a cycloalkenylalkynyl group as defined hereinbefore.

The term"alkoxy"includes both branched and straight chain alkyl groups attached to a terminal oxygen atom. Typical alkoxy groups include methoxy, ethoxy, ? t-propoxy, isopropoxy, tert-butoxy and the like.

The term"haloalkoxy"refers to an alkoxy group substituted with one or more halo groups, for example chloromethoxy, trifluoromethoxy, difluoromethoxy, perfluoroisobutoxy and the like.

The term"alkoxyalkoxyalkyl"refers to an alkyl group substituted with an alkoxy moiety which is in turn substituted with a second alkoxy moiety, for example methoxymethoxymethyl, isopropoxymethoxyethyl and the like.

The term"alkylthio"includes both branched and straight chain alkyl groups attached to a terminal sulfur atom, for example methylthio.

The term"haloalkylthio"refers to an alkylthio group substituted with one or more halo groups, for example trifluoromethylthio.

The term"alkoxyalkyl"refers to an alkyl group substituted with an alkoxy group, for example isopropoxymethyl.

The term"alkoxyalkenyl"refers to an alkenyl group substituted with an alkoxy group, for example 3-methoxyallyl.

The term"alkoxyalkynyl"refers to an alkynyl group substituted with an alkoxy group, for example 3-methoxypropargyl.

The term"alkoxycarbonylalkyl"refers to a straight chain or branched alkyl substituted with an alkoxycarbonyl, for example ethoxycarbonylmethyl, 2- (methoxycarbonyl) propyl and the like.

The term"alkoxycarbonylalkenyl"refers to a straight chain or branched alkenyl as defined hereinbefore substituted with an alkoxycarbonyl, for example 4- (ethoxycarbonyl)-2-butenyl and the like.

The term"alkoxycarbonylalkynyl"refers to a straight chain or branched alkynyl as defined hereinbefore substituted with an alkoxycarbonyl, for example 4- (ethoxycarbonyl)-2-butynyl and the like.

The term"haloalkoxyalkyl"refers to a straight chain or branched alkyl as defined hereinbefore substituted with a haloalkoxy, for example 2- chloroethoxymethyl, trifluoromethoxymethyl and the like.

The term"haloalkoxyalkenyl"refers to a straight chain or branched alkenyl as defined hereinbefore substituted with a haloalkoxy, for example 4- (chloromethoxy)-2-butenyl and the like.

The term"haloalkoxyalkynyl"refers to a straight chain or branched alkynyl as defined hereinbefore substituted with a haloalkoxy, for example 4- (2- fluoroethoxy)-2-butynyl and the like.

The term"alkylthioalkyl"refers to a straight chain or branched alkyl as defined hereinbefore substituted with an alkylthio group, for example methylthiomethyl, 3- (isobutylthio) heptyl and the like.

The term"alkylthioalkenyl"refers to a straight chain or branched alkenyl as defined hereinbefore substituted with an alkylthio group, for example 4- (methylthio)- 2-butenyl and the like.

The term"alkylthioalkynyl"refers to a straight chain or branched alkynyl as defined hereinbefore substituted with an alkylthio group, for example 4- (ethylthio)-2- butynyl and the like.

The term"haloalkylthioalkyl"refers to a straight chain or branched alkyl as defined hereinbefore substituted with an haloalkylthio group, for example 2- chloroethylthiomethyl, trifluoromethylthiomethyl and the like.

The term"haloalkylthioalkenyl"refers to a straight chain or branched alkenyl as defined hereinbefore substituted with an haloalkylthio group, for example 4- (chloromethylthio)-2-butenyl and the like.

The term"haloalkylthioalkynyl"refers to a straight chain or branched alkynyl as defined hereinbefore substituted with an haloalkylthio group, for example 4- (2- fluoroethylthio)-2-butynyl and the like.

The term"dialkoxyphosphorvlalkyl"refers to two straight chain or branched alkoxy groups as defined hereinbefore attached to a pentavalent phosphorous atom, containing an oxo substituent, which is in turn attached to an alkyl, for example diethoxyphosphorylmethyl.

The term"oligomer"refers to a low-molecular weight polymer, whose number average molecular weight is typically less than about 5000 g/mol, and whose degree of polymerization (average number of monomer units per chain) is greater than one and typically equal to or less than about 50.

In Schemes 1-20 hereinafter showing how to synthesize compounds of this invention and Tables 1-10 hereinafter listing various representative compounds of this invention, the following abbreviations may be present : Me for methyl, Et for ethyl, Pr or iPr for isopropyl, n-Bu for n-butyl, t-Bu for tert-butyl, Ac for acetyl, Ph for phenyl, 4Cl-Ph or (4Cl) Ph for 4-chlorophenyl, 4Me-Ph or (4Me) Ph for 4- methylphenyl, (p-CH30) Ph for p-methoxyphenyl, (p-N02) Ph for p-nitrophenyl, 4Br- Ph or (4Br) Ph for 4-bromophenyl, 2-CF3-Ph or (2CFs) Ph for 2-trifluoromethylphenyl, Bn for benzyl and the like.

The compounds of Formula I of this invention and the intermediates used in the synthesis of the compounds of this invention can be prepared according to the following methods. Method A can be used when preparing compounds of Formula I- A [compound of Formula I where RI equals C (=G30)- (G31) t, (X3) dZ3] as shown below in Scheme 1 : Method A : Scheme 1 X3dZ3 X3dZ3 I I 30 1 31 30 1 31 G10 G2o Gio G2o i > >"i Zi"Z 2 base > >' i 2"z z Z' (X) m H + Y-C-G G-C (X) qZ Z (X) m C-G G-C-- (X) qZ R2 t solvent Rz t I I III I-A

where ZI (Xl) m-H, Z2 (X2) q, Z3 (X3) d, Z1(X1)m, G10, G11, G20, G21, G30, G31, and R2 are as defined previously for compound of Formula I-A and t = 0 or 1, t'= 0 or 1, q = C or 1, d = 0 or 1, and Y'= halogen such as chlorine.

In a typical preparation, according to Method A, of a compound of Formula I- A [compound of Formula I where R'equals C (=G30)-(G3l) t (X3) dZ3], a compound of Formula II is reacted with a compound of Formula III in a suitable solvent in the presence of a suitable base. Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) or chloroform (CHC13). If desired, mixtures of these solvents may be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates.

Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used. The preferred base is dependent upon the substrates employed and is selected according to the properties of the substrates.

The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C.

The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula II. The compounds of Formula II are generally commercially available or can be prepared according to known procedures.

The compounds of Formula III of Scheme 1 are prepared as shown in Scheme 2.

Scheme 2 (X3) dZ3 (X3) d3 1 31 30 1 31 o 11-halogenating agent R S-C-G G-C- (X) qZ Y-C-G G-C (X) qZ R2 t solvent R2 t

lv lull where Z2 (X'-) q, Z3 (X3) d, G'O, G", G20, G2l G30, G31, and are as defined previously for compound of Formula I-A and t = 0 or 1, t'= 0 or 1, q = 0 or 1, d = 0 or 1, R12 is an alkyl, aralkyl, or aryl group, and yl = halogen such as chlorine.

In a typical preparation of a compound of Formula III, a compound of Formula IV is treated with a suitable halogenating agent in a suitable solvent, where the suitable halogenating agents include chlorine gas, thionyl chloride, and sulfuryl chloride, however, the preferred halogenating agent is sulfuryl chloride.

Suitable solvents for use in the above process include, but are not limited to, hexanes, chlorinated solvents such as methylene chloride, dichloroethane, chloroform, carbon tetrachloride, and the like, however, the reactions are normally run neat. The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C. The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired.

The compounds of Formula IV of Scheme 2 are prepared as shown in Scheme 3 : Scheme 3 (in3) dZ3 (X3) dZ3 30 1 31) t. 30 1 31 po G20 po G2o 12S-11 y2 21-"+ (X2 Z2 base 12S-21-"+ (X2 Z2 solvent Rz vi V IV where Z2(X2)Q[(C=G20)-G21]t-HM, Z2(X2)q, Z3(X3)d, G10, G11, G20, G21, G30, G31, and R2 are as defined previously for compound of Formula I and t = 0 or 1, t'= 0 or 1, q = 0 or 1, d = 0 or 1, Rl2 is an alkyl, aralkyl, or aryl group, and y2 = halogen such as chlorine.

In a typical preparation of a compound of Formula IV, a compound of Formula V is reacted with a compound of Formula VI in a suitable solvent in the presence of a suitable base. Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2Clz) or chloroform (CHC13). If desired, mixtures of these solvents may be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates.

Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used. The preferred base is dependent upon the substrates employed and is selected according to the properties of the substrates.

The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C.

The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula VI. The compounds of Formula VI are generally commercially available or can be prepared according to known procedures.

The compounds of Formula V of Scheme 3 are prepared as shown in Scheme 4 : Scheme 4 (X3) dZ3 (1X3) dZ3 30 1 31 30 1 31 Go Gio Y2 + R2S~H ba R2S-C~G » Y2 10Q10 R2 solvent R2 ,. 2sotvent 2 VIII Vll V

where Z3 (X3) d, Gl°, G", G30, G3l, and R2 are as defined previously for compound of Formula I-A and t'= 0 or 1, d = 0 or 1, R12 = alkyl, aralkyl, or aryl, and Y'and Y2 halogen such as chlorine, bromine, or iodine.

In a typical preparation of a compound of Formula V, a compound of Formula VII is reacted with a compound of Formula VIII in a suitable solvent in the presence of a suitable base. Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, diethyl ether, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) or chloroform (CHC13). If desired, mixtures of these solvents may be used, however, the preferred solvent is diethyl ether. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used, however, the preferred base is sodium hydride.

The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C.

The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula VIII. The compounds of Formula VIII are generally commercially available or can be prepared according to known procedures. Conversion of Y2 from Cl to Br or Cl to I in compound of Formula V can be prepared according to literature procedures. A general description of the synthesis of halogen exchange (Finkelstein reaction) is

described in March, J. Advaitced Orga1lic Chemistry, 4th ed. ; Wiley and Sons : New York, 1992 ; pp 430-431.

The compounds of Formula VII of Scheme 4 are prepared as shown in Scheme 5 : Scheme 5 (IX3) dZ3 Gso (G31) r G30 10 gaz 2 11 G catalyst 1 1l 11 ~y2 G to y solvent R2 G lx X Vil where Z3 (X3) d, Gl°, G", G30, G3l, and R2 are as defined previously for compound of Formula I-A, t'= 0 or 1, d = 0 or 1, and Yl and Y2 = halogen such as chlorine, bromine, or iodine.

In a typical preparation of a compound of Formula VII, a compound of Formula IX is reacted with a compound of Formula X (or a suitable precursor of compound of Formula X) in a suitable solvent in the presence of a suitable base.

Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, diethyl ether, dioxane and the like ; aromatic solvents such as benzene and toluene ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12), carbon tetrachloride (CC14) or chloroform (CHC13). If desired, mixtures of these solvents may be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates. Suitable catalysts for use in the above process include, but are not limited to, pyridine, thioureas and ureas such as tetra-n-butylurea, phosphoramides such as hexamethylphosphotriamide, substituted amides such as dimethylformamide, quaternary ammonium halides such as tetrabutyl or tributylbenzyl ammonium chloride, arylamines such as N, N,- dimethylaminopyridine, N, N-dimethylaniline, tertiary phosphines such as trioctyl phosphine, and alkali metal or alkaline earth metal halides such as cesium or potassium chloride which are used in conjunction with a sequestering agent such as a crown ether (18-crown-6). If desired, mixtures of these catalysts may be used,

however, the preferred catalyst is pyridine. Compound of Formula IX may in some cases exist in a polymeric form. If so, the monomeric form can be achieved via known procedures, one being through thermal depolymerization. Compound of Formula X when GIO = O and Y1 and Y2 = Cl is phosgene, C (=O) CI2. However, other forms of phosgene, phosgene equivalents, can be utilized such as trichloromethyl chloroformate (compound of Formula X in which Gl° = O, Y1 = Cl, and y2 = OCC13) or di (trichloromethyl) carbonate (compound of Formula X in which GIO = O and Y'and y2 = OCCl3). The above process may be carried out at temperatures between about- 78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 100 °C. The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. The catalyst is normally used in lower amounts than that of both compounds of Formula IX and X. The compounds of Formula IX and X are generally commercially available or can be prepared according to known procedures.

The compounds of Formula I-A [compound of Formula I where Ru equals C (=G30)-(G31)t,(X3)dZ3] can be prepared according to Method B as shown in Scheme 6 : Method B : Scheme 6 3 G () dZ' ici G30 G-C (X) G (G), l 10... G G I V) m C-G Yz v Z (X) m C-G » R2 base, solvent R2 t R XI where Z' (xl) m Z2 (X2) q, Z3 (X3) d, G1°, G", G20, G2l, G30, G31, and R2 are as defined previously for compound of Formula I-A and m = 0 or 1, t = 0 or 1, q = 0 or 1, t'= 0 or 1, d = 0 or 1, and y2 = halogen such as chlorine, bromine, or iodine.

In a typical preparation, according to Method B, Scheme 6, of a compound of Formula I-A [compound of Formula I where Ri equals C (=G30)-(G31)t,(X3)dZ3], a compound of Formula XI is reacted with a compound of Formula VI in a suitable

solvent in the presence of a suitable base. Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, diethyl ether, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) or chloroform (CHC13). If desired, mixtures of these solvents may be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used. The preferred base is dependent upon the substrates employed and is selected according to the properties of the substrates. The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C. The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula VI. The compounds of Formula VI are generally commercially available or can be prepared according to known procedures.

The compounds of Formula XI of Scheme 6 are prepared as shown in Scheme 7 : Scheme 7 (in3) dZ3 (1X3) dZ3 30 1 31 30 1 31 Z (X) m H G (G) t, Go go Y,-C-G (G) z (X1) m C G T--Y R2 base, solvent R2 Vil xi

where ZI (XI).-H, Z3 (X3) d, Zl (Xl) m, Gl°, Gll, G30, G31, and R2 are as defined previously for compound of Formula I-A and m = 0 or 1, t'= 0 or 1, d = 0 or 1, and Y'and Y'-~ halogen such as chlorine.

In a typical preparation of a compound of Formula XI, a compound of Formula II is reacted with a compound of Formula VII in a suitable solvent in the presence of a suitable base. Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, diethyl ether, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) or chloroform (CHC13). If desired, mixtures of these solvents may be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used. The preferred base is dependent upon the substrates employed and is selected according to the properties of the substrates.

The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C.

The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula II. The compounds of Formula II are generally commercially available or can be prepared according to known procedures. Conversion of Y2 from Cl to Br or Cl to I in compound of Formula XI can be prepared according to literature procedures. A general description of the synthesis of halogen exchange (Finkelstein reaction) is described in March, J. Adva7lced Organic Chemistry, 4th ed. ; Wiley and Sons : New York, 1992 ; pp 430-431.

The compounds of Formula I-A [compound of Formula I where Ri equals C (=G")- (G31) t, (X3) dZ3] can be prepared according to Method C as shown in Scheme 8 : Method C : Scheme 8 (X3ndZ3 G20 (X) dZ I (G2-C1X2qZ2 Gso Gst, Go zozo Rso ! ventp t () m () q R2 solvent R2 t

Xl l-A (t = 0) where y2 = halogen such of as iodine, bromine, or chlorine, Zl (XI) m, Z3 (X3) d, G'°, G", G30, G31, and RI are as defined previously for compound of Formula I-A and m = 0 or 1, t = 0, q = 0 or 1, t'= 0 or 1, and d = 0 or 1 where Z2 (X2) q = NR3R4, NR3R4R5, or {(NR3R4R5) M} and when q = 0, in compound of Formula VI-A, Z2 can be a tertiary amine where in compound of Formula I-A, Z2 is a quaternary amine salt, and when q = 1, in compound of Formula VI-A, X2Z2 can be a tertiary amine where in compound of Formula I-A, X2Z2 is a quaternary amine salt.

In a typical preparation of a compound of Formula I-A [compound of Formula I where Roi equals C (=G30)-(G3l) t (X3) dZ3], according to Method C, a compound of Formula XI is reacted with a compound of Formula VI-A in a suitable solvent.

Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, diethyl ether, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2Cl2) or chloroform (CHC13). If desired, mixtures of these solvents may be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates.

The above process may be carried out at temperatures between about-78 °C and about 200 °C. Preferably, the reaction is carried out between 0 °C and about 100 °C.

The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of compound of Formula XI is used per equivalent of starting material of compound of Formula VI-A. The compounds of Formula VI-A are generally commercially

available or can be prepared according to known procedures. The compounds of Formula XI can be prepared by the same process as that of Scheme 7.

The compounds of Formula I-B, I-C, and I-A [compounds of Formula I where RI equals C (=G30)-(G31)t'-H, C (=G30)-Yl, and C (=G30)-(G3l) t (X3) dZ3, respectively] can be prepared according to Method D as shown below in Scheme 9 : Method D : Scheme 9 I-C I-A where Zl (XI) m, Z2 (X2) q, Z3 (X3) d, G10, G11, G20, G21, G30, G31, and R2 are as defined above for compound of Formula I-A and m = 0 or 1, t = 0 or 1, t' = 0 or 1, q = 0 or 1, d = 0 or 1, and yl = halogen such as chlorine.

In a typical preparation of a compound of Formula I-B [compound of Formula I where RI equals C (=G30)-(G31)t'-H], a compound of Formula I-A [compound of Formula I where Ri equals C (=G30)-(G31)t'(X3)dZ3] is treated with a suitable solvent under suitable reaction conditions which can successfully transform (G3l) t' (X3) dZ3 to (G3l) t-H via methods known to one skilled in the art. For example, if d = 0, Z3 = benzyl (Bn), t'= 1, and G30 and G31 = oxygen, then typical reaction conditions for the transformation of C (=G30)-G3lZ3 (COzBn) to C (=G30)-G3'H (C02H) would involve the following : suitable solvents include, but are not limited to, ethers such as

tetrahydrofuran (THF), glyme, and the like ; esters such as ethyl acetate ; acetonitrile ; alcohols such as methanol or ethanol ; chlorinated solvents such as methylene chloride (CH2C12) or chloroform (CHC13). If desired, mixtures of these solvents may be used, however, the preferred solvent is ethyl acetate. Suitable catalysts in the presence of at least one equivalent of hydrogen include, palladium, platinum, nickel, rhodium, iridium and ruthenium. The catalysts are normally adsorbed or admixed on an inert support material which includes carbon, alumina, calcium sulfate, or barium sulfate, however, the preferred catalyst and support is palladium on carbon. The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. One skilled in the art would recognize that a hydrogenation reaction to remove a benzyl group as described above would only be utilized when all other functional groups present within compound of Formula I-A are deemed compatible with the reaction conditions. See Greene, T. W. ; Wuts, P. G. M. Protective Groups in Organic Synthesis ; 2nd ed. ; Wiley and Sons : New York, 1991 ; pp 227-265 for additional suitable reaction conditions and appropriate C (=G30)- (G31) t, (X3) dZ3 chemical moieties for the transformation of (G31) t (X3) dZ3 to (G3') t-H.

In a typical preparation of a compound of Formula I-C [compound of Formula I where Ri equals C (=G30)-Yl], a compound of Formula I-B [compound of Formula I where RI equals C (=G30)-(G3l) t-H] is treated with a suitable halo-de-hydroxylation reagent in a suitable solvent, where suitable halo-de-hydroxylation reagents include, but are not limited to, thionyl chloride, oxalyl chloride, oxalyl bromide, triphenyl phosphine in carbon tetrachloride, phosphorus trichloride, and phosphorus pentachloride, however, the preferred halo-de-hydroxylation reagent is thionyl chloride. Suitable solvents for use in the above process include, but are not limited to, hexanes, ethers such as tetrahydrofuran, glyme, and the like ; chlorinated solvents such as methylene chloride, dichloroethane, chloroform, carbon tetrachloride, and the like, however, the reactions are normally run neat with a catalytic amount of dimethylformamide present. The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C. The above process to produce

compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Compounds of Formula I-C [compound of Formula I where RI equals C (=G30)-Yl] can also be synthesized directly from compounds of Formula I-A [compound of Formula I where Ri equals C (=G30)-(G3l) t (X3) dZ3]. In a typical preparation of a compound of Formula I-C, a compound of Formula I-A is treated with a suitable solvent in the presence of suitable reaction conditions which can successfully transform C (=G30)-(G31)t'(X3)dZ3 to C (=G30)-Yy via methods known to one skilled in the art. For example, if d = 0, t'= 1, and Z3 = trimethylsilyl and G30 and G31 = oxygen, then typical reaction conditions for the transformation of C (=G30)- G31Z3 (CO2SiMe3) to C (=G30)-Yl [C (=O)-Cl] would involve treatment of the compound of Formula I-A in which C (=G30)-G3lZ3 is CO2SiMe3 with oxalyl chloride in a suitable solvent such as THF at a temperature ranging from-78 °C and about 100 °C. See Larock, R. C. Comprehensive Organic Transfornta. tions, 2nd ed, New York, 1999 ; p 1968 as well as Greene, T. W. ; Wuts, P. G. M. Protective Groups in Organic Synthesis ; 2nd ed. ; Wiley and Sons : New York, 1991 ; pp 261-262 for additional suitable reaction conditions for the transformation of C (=G30)-(G3l) t (X3) dZ3 to C (=G30)-Yt. One skilled in the art would recognize that a halogenation reaction to convert a silyl ester to an acid chloride as described above would only be utilized when all other functional groups present within compounds of Formula I-A are deemed compatible with the reaction conditions. Compound of Formula I-C in which Yl is chlorine can be interconverted to other halo derivatives via reaction conditions listed in Larock, R.

C. Comprehensive Orgczvic Travsformations, 2nd ed. ; Wiley and Sons : New York, 1999 ; pp 1950-1951.

In a typical preparation of a compound of Formula I-A [compound of Formula I where RI equals C (=G3)- (G31)t'(X3)dZ3] from a compound of Formula I-C [compound of Formula I where Ru equals C (=G30)-Yl], a compound of Formula I-C is reacted with Z3 (X3) d (G3l) t-H in a suitable solvent in the presence of a suitable base. Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2Cl2) or chloroform (CHC13). If desired, mixtures of these solvents may

be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used.

The preferred base is dependent upon the substrates employed and is selected according to the properties of the substrates. The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C. The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula I-C. Suitable reaction conditions for the conversion of C (=G30)-Yl to C (=G30)- (G31) t, (X3) dZ3 can be found in Larock, R. C.

Comprehensive Organic Trawtsformations, 2nd ed. ; Wiley and Sons : New York, 1999 ; pp 1952-1954.

Additionally, a compound of Formula I-A [compound of Formula I where R equals C (=G30)-(G3l) t (X3) dZ3] can be prepared via the reaction of a compound of Formula I-B [compound of Formula I where Ri equals C (=G30)-(G3l) t-H] in a suitable solvent with Z3 (X3) d-H and a suitable coupling reagent. Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) or chloroform (CHC13). If desired, mixtures of these solvents may be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium

carbonate ; or pyridine. If desired, mixtures of these bases may be used. The preferred base is dependent upon the substrates employed and is selected according to the properties of the substrates. The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C. The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or. lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula I-B. Suitable coupling reagents for use in the above process include, but are not limited to, lipases, diazo compounds, anhydrides, acid chlorides, carbodiimides, and carbodiimidazoles. Suitable reaction conditions for the conversion of C (=G30)-(G3l) t-H to C (=G30)-(G3l) t (X3) dZ3 can be found in Larock, R. C. Comprehensiue Organic Transformations, 2nd ed. ; Wiley and Sons : New York, 1999 ; pp 1932-1949.

Alternatively, transformation of a compound of Formula I-B [compound of Formula I where Ru equals C (=G30)- (G3') t,-H] to a compound of Formula I-A [compound of Formula I where Ri equals C (=G30)-(G3l) t (X3) dZ3] can also be accomplished by reaction of a compound of Formula I-B in a suitable solvent with a suitable base in the presence of a suitable commercially available halide, such as an alkyl halide. Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) or chloroform (CHC13). If desired, mixtures of these solvents may be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates.

Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used. The preferred base is dependent upon the substrates employed and is selected according to the properties of the substrates.

Suitable halides include, but are not limited to, alkyl halides such as benzyl chloride, benzyl bromide, methyl iodide, and ethyl iodide. The preferred halide is dependent upon the substrates employed and is selected according to the properties of the substrates. The above process may be carried out at temperatures between about- 78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C. The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula I-B. Suitable reaction conditions for the conversion of C (=G30)-(G3l) t-H to C (=G3°)- (G31) c, (X3) aZ3 can be found in Larock, R. C. Comprehensiue Organic Transformations, 2nd ed. ; Wiley and Sons : New York, 1999 ; pp 1938-1940.

The compounds of Formula I-D of this invention and the intermediates used in the synthesis of the compounds of this invention can be prepared according to the following methods. Method E can be used when preparing compounds of Formula I- D as shown below in Scheme 10 : Method E : Scheme 10

i-c where ZI (XI)., Z3 (X3) d, Gl°, Gll, G20, G21, G30, G3', and R2 are as defined above for compound of Formula I-A, m = 0 or 1, Y'= halogen such as chlorine, and q = 0 and Z2 = CRl3Rl4G32, where G32 is an oxygen atom, a sulfur atom or NR3, and R13 and R14 are independently defined as for R2.

In a typical preparation of a compound of Formula I-D, a compound of Formula I-A [compound of Formula I where RI equals C (=G30)-(G31)t'(X3)dZ3], where the C(=G30)-(G31)t'(X3)dZ3 moiety is reacted intramolecularly with the (X2) qZ2 moiety (where q = 0 and Z2 = CR13Rl4G32) in a suitable solvent in the presence of a suitable base to afford cyclic [-C (=G30)-G32-CR13R14C(=G20)G21C(R2)-]. Suitable solvents include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, and the like ; esters such as ethyl acetate ; acetonitrile ; alcohols such as methanol or ethanol ; chlorinated solvents such as methylene chloride (CH2Cl2) or chloroform (CHC13). The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or

potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used.

The preferred base is dependent upon the substrates employed and is selected according to the properties of the substrates. The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C. The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula I-A.

A compound of Formula I-D can also be prepared via the reaction of a compound of Formula I-B [compound of Formula I where R'equals C (=G30)-(G3l) t where C (=G30)-(G3l) t-H is reacted intramolecularly with (X2) qZ2, where Z2 = CR13Rl4G32, in a suitable solvent in the presence of a suitable base along with a suitable coupling reagent. Suitable reaction conditions would involve the following : suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) or chloroform (CHC13). If desired, mixtures of these solvents may be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used.

The preferred base is dependent upon the substrates employed and is selected according to the properties of the substrates. The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C. The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be

used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula I-B. Suitable coupling reagents for use in the above process include, but are not limited to, lipases, diazo compounds, anhydrides, acid chlorides, carbodiimides, and carbodiimidazoles. Suitable reaction conditions for the conversion of H-(G3l) t-(G30=) C-C (R2)-(G2l [G20=] C) t (X2) qZ2, where Z2 = CRl3Rl4G32, to cyclic [-C (=G30)-G32-CRl3Rl4C (=G20) G2lC (R2)-] can be found in Larock, R. C. Comprehensive Organic Transformations, 2nd ed. ; Wiley and Sons : New York, 1999 ; pp 1932-1949.

In a typical preparation of a compound of Formula I-D, a compound of Formula I-C [compound of Formula I where Ru equals C (=G30)-Yl] where the C (=G30) W moiety is reacted intramolecularly with the (X2) qZ2 moiety (where Z2 = CRl3Rl4G32) in a suitable solvent in the presence of a suitable base. Suitable reaction conditions would involve the following : suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) or chloroform (CHCIs).. If desired, mixtures of these solvents may be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates.

Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used. The preferred base is dependent upon the substrates employed and is selected according to the properties of the substrates.

The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C.

The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula I-C.

Suitable reaction conditions for the conversion of Yl- (G30=) C-C (R2)-

(G21[G20=]C)t(X2)Qz2, where Z2 = CR13R14G32, to cyclic [-C (=G30)- G32CR13Rl4C (=G20) G2'C (R2)-] can be found in Larock, R. C. Compreheitsiue Orgdnic Transformations, 2nd ed. ; Wiley and Sons : New York, 1999 ; pp 1952-1954.

Application of Method A (Scheme 5) as described previously for the synthesis of compound of Formula VII to the synthesis of compound of Formula XIV is described below in Scheme 11. Compound of Formula XII (compound of Formula IX where G"and G30 = O) is reacted with compound of Formula XIII (compound of Formula X where GIO = O) to afford compound of Formula XIV (compound of Formula VII where Gl°, G", and G30 = O) : Scheme 11 (X) dZ R2X0\ (G) t-(X) dZ + Jt catalyst 1 || 4 (G31) to (X3) d3 Gsyt. O O R catalyst o R2 0 () t- 0 0 XII XIII XIV where Z3 (X3) d, d, t', G31, and R2 are as defined previously for compound of Formula I- A, Y'and Y2 = halogen such as chlorine, bromine, or iodine.

Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, diethyl ether, dioxane and the like ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2CI2), carbon tetrachloride (CC14) or chloroform (CHC13). If desired, mixtures of these solvents may be used. The preferred solvent is dependent upon the substrates employed and is selected according to the properties of the substrates. For example, in the reaction of compound of Formula XII, where t'= 1, G31 = O, d = 0, R2 = H, and Z3 = benzyl (Bn), with compound of Formula XIII, where Y'and Y2 = Cl, to afford compound of Formula XIV where t'= 1, G31 = O, d = 0, R2 = H, Z3 = benzyl (Bn), and Y'and Y2 = Cl, then the preferred solvent is carbon tetrachloride. However, in the reaction of compound of Formula XII, where t'= 1, G31 = O, d = 0, R2 = H, and Z3 = ethyl (Et), with compound of Formula XIII, where Y'and Y2 Cl, to afford compound of Formula XIV, where t'= 1, G31= O, d = 0, R2 = H, Z3 = ethyl (Et), and Yl and Y2 = Cl,

then the preferred solvent is tetrahydrofuran. Suitable catalysts for use in the above process include, but are not limited to, pyridine, thioureas and ureas such as tetra-n- butylurea, phosphoramides such as hexamethylphosphotriamide, substituted amides such as dimethylformamide, quaternary ammonium halides such as tetrabutyl or tributylbenzyl ammonium chloride, arylamines such as N, N,- dimethylaminopyridine, N, N-dimethylaniline, tertiary phosphines such as trioctyl phosphine, and alkali metal or alkaline earth metal halides such as cesium or potassium chloride which are used in conjunction with a sequestering agent such as a crown ether (18-crown-6). If desired, mixtures of these catalysts may be used, however, the preferred catalyst is pyridine. Compound of Formula XII may in some cases exist in a polymeric form. If so, the monomeric form can be achieved via known procedures, one being through thermal depolymerization. Compound of Formula XIII in which Y'and Y2 = Cl is phosgene, C (=O) C12. However, other forms of phosgene, phosgene equivalents, can be utilized such as trichloromethyl chloroformate (compound of Formula XIII in which Y'= Cl, and y2 = OCC13) or di (trichloromethyl) carbonate (compound of Formula XIII in which Y'and Y2 = OCCIs). The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 100 °C. The above process to produce compounds of the present invention is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. The catalyst is normally used in lower amounts than that of both compounds of Formula XII and XIII. The compounds of Formula XII and XIII are generally commercially available or can be prepared according to known procedures.

Application of Method A (Scheme 4) as described previously for the synthesis of compound of Formula V to the synthesis of compound of Formula XVI is described below in Scheme 12. Compound of Formula XV (compound of Formula VIII where R12 = Et and Rl2S-H is taken together to equal Et-S-L) is reacted with compound of Formula XIV (compound of Formula VII where G'°, G", and G30 = O) to afford compound of Formula XVI (compound of Formula V where Gl°, G", and G30 = O, and R12 = Et) : Scheme 12

where Z3 (X3) d, d, t', G31 and R2 are as defined previously for compound of Formula I- A, L = metal cation such as Na or K, and Y'and Y2 = halogen such as chlorine, bromine, or iodine.

Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, diethyl ether and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2Clz) or chloroform (CHCl3). If desired, mixtures of these solvents may be used, however, the preferred solvent is diethyl ether. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used, however, the preferred base is sodium hydride.

The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C.

Preparation of the compounds of the present invention by the above process is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula XV except when L = Na or K, then no base is required. The compounds of Formula XV are generally commercially available or can be prepared according to known procedures. For example, R12S-L = EtS-Na, is commercially available.

Conversion of Y2 from Cl to Br or Cl to I in compound of Formula XVI can be

prepared according to literature procedures. A general description of the synthesis of halogen exchange (Finkelstein reaction) is described in March, J. Aducilced Organic Chemistry, 4th ed. ; Wiley and Sons : New York, 1992 ; pp 430-431. Also, see synthesis Example 8 for conversion of Y2 from Cl to I in compound of Formula XVI.

Application of Method A (Scheme 3) as described previously for the synthesis of compound of Formula IV to the synthesis of compound of Formula XVII is described below in Scheme 13. Compound of Formula XVI (compound of Formula V where R12 = Et and G'°, G", and G30 = O) is reacted with compound of Formula VI (where t = 1 and q = 0 or 1) to afford compound of Formula XVII (compound of Formula IV in which t = 1, G'o, G", and G30 = O, R12 = Et, and q = 0 or 1) : Scheme 13 where Z2 (X2) q, Z3 (X3) d, d, t', G20, G21, G31, and R2 are as defined previously for compound of Formula I-A, and Y2 = halogen such as chlorine, bromine, or iodine.

Suitable solvents for use in the above process include, but are not limited to, ethers such as tetrahydrofuran (THF), glyme, diethyl ether and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) or chloroform (CHC13). If desired, mixtures of these solvents may be used, however, the preferred solvent is THF.

Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; or pyridine. If desired, mixtures of these bases may be used, however, the preferred base is diisopropylethylamine. The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out

between 0 °C and about 50 °C. Preparation of the compounds of the present invention by the above process is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula VI. The compounds of Formula VI are generally commercially available or can be prepared according to known procedures.

Application of Method A (Scheme 2) as described previously for the synthesis of compound of Formula III to the synthesis of compound of Formula XVIII is described below in Scheme 14. Compound of Formula XVII (compound of Formula IV where R12 = Et, Gl°, G", and G30 = O, and q = 0 or 1) is reacted with a suitable halogenating agent to afford compound of Formula XVIII (compound of Formula III where Gl°, Gll, and G30 = O, Y'= Cl, and q = 0 or 1) : Scheme 14 XVII XVIII where Z2 (X2) q, Z3 (X3) d, d, t', G20, G2l, G31, and R2 are as defined previously for compound of Formula I-A and t = 1.

Suitable halogenating agents include chlorine gas, thionyl chloride, and sulfuryl chloride, however, the preferred halogenating agent is sulfuryl chloride.

Suitable solvents for use in the above process include, but are not limited to, hexanes, chlorinated solvents such as methylene chloride, dichloroethane, chloroform, carbon tetrachloride and the like, however, the reactions are normally run neat. The above process may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out between 0 °C and about 50 °C. Preparation of the compounds of the present invention by the above process is

preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired.

Application of Method A (Scheme 1) as described previously for the synthesis of compound of Formula I-A to the synthesis of compound of Formula XX is described below in Scheme 15. Compound of Formula XIX (compound of Formula II where m = 1 and Zl (Xl) m-H equals fluoxetine hydrochloride) is reacted with compound of Formula XVIII (compound of Formula III where Yi = Cl, Qio, G", and G30 = O, t = 1, and q = 0 or 1) to afford compound of Formula XX (compound of Formula I-A where m = 1, t = 1, q = 0 or 1, Zl (Xl) m = fluoxetine, and G'°, G", and G30 = O) : Scheme 15 xx where Z2 (X2) q, Z3 (X3) d, d, t', G20, G2l, G31, and R2 are as defined previously for compound of Formula I-A.

In the reaction of a compound of Formula XVIII with a compound of Formula XIX to afford a compound of Formula XX, the following conditions can be used : suitable solvents for use in the above method include ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) and chloroform (CHC13). If desired, mixtures of these solvents may be used, however, the preferred solvent is THF. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; 4-dimethylaminopyridine (DMAP) or pyridine. If desired, mixtures of

these bases may be used, however, the preferred base is DMAP. The above method may be carried out at temperatures between about-78 °C and about i00 °C.

Preferably, the reaction is carried out at 22 °C. Preparation of the compounds of the present invention by the above method is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, two equivalents of base are used per equivalent of starting material of compound of Formula XIX.

Application of Method A (Scheme 1) as described previously for the synthesis of compound of Formula I-A to the synthesis of compound of Formula XXII is described below in Scheme 16. Compound of Formula XXI (compound of Formula II where m = 1 and ZI (Xl) m-H equals fluconazole) is reacted with compound of Formula XVIII (compound of Formula III where Y'= Cl, G1°, G", and G30 0, t = 1, and q = 0 or 1) to afford compound of Formula XXII (compound of Formula I-A where m = 1, t = 1, q = 0 or 1, Zl (Xi) m = fluconazole, and G'°, G", and G30 = O) : Scheme 16 where Z2 (X2) q, Z3 (X3) d, d, t', G20, G21, G3', and R2 are as defined previously for compound of Formula I-A.

In the reaction of a compound of Formula XXI with a compound of Formula XVIII to afford a compound of Formula XXII, the following conditions can be used : suitable solvents for use in the above method include ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) and chloroform (CHC13). If desired, mixtures of these solvents may be used, however, the preferred

solvent is THF. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; 4-dimethylaminopyridine (DMAP), potassium bis (trimethylsilyl) amide (KHMDS) or pyridine. If desired, mixtures of these bases may be used, however, the preferred base is KHMDS. The above method may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out at -78 °C to 0 °C. Preparation of the compounds of the present invention by the above method is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula XXI.

Application of Method A (Scheme 1) as described previously for the synthesis of compound of Formula I-A to the synthesis of compound of Formula XXIV is described below in Scheme 17. Compound of Formula XXIII (compound of Formula II where m = 1 and Zl (Xl) m-H equals nifedipine) is reacted with compound of Formula XVIII (compound of Formula III where Y'= Cl, G'°, G", and G30 = O, t = 1, and q = 0 or 1) to afford compound of Formula XXIV (compound of Formula I-A where m = 1, t = 1, q = 0 or 1, ZI (XI) m = nifedipine, and Gl°, G", and G30 = O) : Scheme 17 xaun mv

where Z2 (X2) q, Z3 (X3) d, d, t', G20, G21, G3', and R2 are as defined previously for compound of Formula I-A.

In the reaction of a compound of Formula XXIII with a compound of Formula XVIII to afford a compound of Formula XXIV, the following conditions can be used : suitable solvents for use in the above method include ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) and chloroform (CHC13). If desired, mixtures of these solvents may be used, however, the preferred solvent is THF. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine or diisopropylethylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; 4-dimethylaminopyridine (DMAP), potassium bis (trimethylsilyl) amide (KHMDS) or pyridine. If desired, mixtures of these bases may be used, however, the preferred base is KHMDS. The above method may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out at -78 °C to 0 °C. Preparation of the compounds of the present invention by the above method is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula XXIII.

Application of. Method A (Scheme 1) as described previously for the synthesis of compound of Formula I-A to the synthesis of compound of Formula XXVI is described below in Scheme 18. Compound of Formula XXV (compound of Formula II where m = 1 and ZXm-H equals norfloxacin) is reacted with compound of Formula XVIII (compound of Formula III where Y = Cl, G'o, G", and G30 = O, t = 1, and q = 0 or 1) to afford compound of Formula XXVI (compound of Formula I-A where m = 1, t = 1, q = 0 or 1, Zl (XI) m = norfloxacin, and Gl°, G", and G30 = O) : Scheme 18

where Z2 (X2) q, Z3 (X3) d, d, t', G20, G21, G3i, and R2 are as defined previously for compound of Formula I-A.

In the reaction of a compound of Formula XXV with a compound of Formula XVIII to afford a compound of Formula XXVI, the following conditions can be used : suitable solvents for use in the above method include ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) and chloroform (CHC13). If desired, mixtures of these solvents may be used, however, the preferred solvent is CH2C12. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine, diisopropylethylamine, or triisopropylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; 4-dimethylaminopyridine (DMAP), potassium bis (trimethylsilyl) amide (KHMDS) or pyridine. If desired, mixtures of these bases may be used, however, the preferred base is triisopropylamine. The above method may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out at 22 °C. Preparation of the compounds of the present invention by the above method is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula XXV.

Application of Method A (Scheme 1) as described previously for the synthesis of compound of Formula I-A to the synthesis of compound of Formula XXVIII is described below in Scheme 19. Compound of Formula XXVII (compound of Formula II where m = 1 and ZXm-H equals 4-acetamidophenol) is reacted with compound of Formula XVIII (compound of Formula III where YI = Cl, G1°, Gm, and G30 = O, t = 1, and q = 0 or 1) to afford compound of Formula XXVIII (compound of Formula I-A where m = 1, t = 1, q = 0 or 1, Z' (X') m = 4-acetamidophenol, and Gl°, G", and G30 = 0) : Scheme 19 XXVIII XXVII where Z2 (X2) q, Z3 (X3) d, d, t', G20, G21, G31, and R2 are as defined previously for compound of Formula I-A.

In the reaction of a compound of Formula XXVII with a compound of Formula XVIII to afford a compound of Formula XXVIII, the following conditions can be used : suitable solvents for use in the above method include ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2Clz) and chloroform (CHC13). If desired, mixtures of these solvents may be used, however, the preferred solvent is CH2C12. Suitable bases for use in the above process include, but are not limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine, diisopropylethylamine, or triisopropylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; 4-dimethylaminopyridine (DMAP), potassium bis (trimethylsilyl) amide (KHMDS) or pyridine. If desired, mixtures of these bases may be used, however, the preferred base is potassium hydroxide. The above method may be carried out at

temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out at 22 °C. Preparation of the compounds of the present invention by the above method is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula XXVII.

Application of Method A (Scheme 1) as described previously for the synthesis of compound of Formula I-A to the synthesis of compound of Formula XXX is described below in Scheme 20. Compound of Formula XXIX (compound of Formula II where m = 1 and Zl (Xl) =-H equals sulfamethoxazole) is reacted with compound of Formula XVIII (compound of Formula III where Y = Cl, G, G", and G30 = O, t = 1, and q = 0 or 1) to afford compound of Formula XXX (compound of Formula I-A where m = 1, t = 1, q = 0 or 1, Z' (Xi) m = sulfamethoxazole, and Gl°, G", and G30 = O) : Scheme 20 XXIX where Z2 (X2) q, Z3 (X3) d, d, t', G20, G2l, G3l, and R2 are as defined previously for compound of Formula I-A.

In the reaction of a compound of Formula XXIX with a compound of Formula XVIII to afford a compound of Formula XXX, the following conditions can be used : suitable solvents for use in the above method include ethers such as tetrahydrofuran (THF), glyme, and the like ; dimethylformamide (DMF) ; dimethylsulfoxide (DMSO) ; acetonitrile ; chlorinated solvents such as methylene chloride (CH2C12) and chloroform (CHC13). If desired, mixtures of these solvents may be used, however, the preferred solvent is CH2C12. Suitable bases for use in the above process include, but are not

limited to, metal hydrides such as sodium or potassium hydride ; metal alkoxides such as sodium or potassium alkoxides ; alkali metal hydroxides such as sodium or potassium hydroxide ; tertiary amines such as triethylamine, diisopropylethylamine, or triisopropylamine ; an alkali metal carbonate such as sodium or potassium carbonate ; 4-dimethylaminopyridine (DMAP), potassium bis (trimethylsilyl) amide (KHMDS) or pyridine. If desired, mixtures of these bases may be used, however, the preferred base is triisopropylamine. The above method may be carried out at temperatures between about-78 °C and about 100 °C. Preferably, the reaction is carried out at 22 °C. Preparation of the compounds of the present invention by the above method is preferably carried out at about atmospheric pressure although higher or lower pressures can be used if desired. Substantially equimolar amounts of reactants are preferably used although higher or lower amounts can be used if desired. Generally, one equivalent of base is used per equivalent of starting material of compound of Formula XXIX.

Following the general methods described hereinbefore, the following compounds of Formula VII (where R2 = H) as listed in Table 1 were prepared.

VII Table 1 : Listing of Compounds of Formula VII Cmpd# Y1 G10 G11 G30 Y2 G31 t' d (X3)dZ3 1-1 Ci O 0 O Ci O 1 0 benzyl 1-2 Ci 0 0 O Ci O 1 0 ethyl 1-3 ci 0 0 O ci O 1 0 methyl 1-4 ci O 0 O ci O 1 0 isopropyl 1-5 ci 0 0 O ci O 1 0 ter-butyl 1-6 C1 0 O O Cl O 1 0 n-butyl The following Examples are provided for guidance to the practitioner in order to practice the invention.

Example 1 : Benzyl 2-chloro-2-[(chlorocarbonyl) oxy] acetate (Compound 1-1 of Table 1) To a 3-neck round-bottom flask, equipped with nitrogen inlet, a thermometer and a solid addition funnel, was added benzyl glyoxylate (50. 9 g, 300 mmol), pyridine (2. 5 mL, 31. 0 mmol) and 1500 mL of carbon tetrachloride. The solution was cooled with dry ice/acetone to-20 °C and triphosgene (230 g, 770 mmol) was added over 5 minutes, maintaining the temperature between-10 °C and-20 °C. The reaction was gradually warmed to room temperature over 2 h, then warmed to 50 °C and was stirred at that temperature for 1 h. The reaction was then cooled and placed in the freezer overnight. The precipitates were filtered by gravity, washing with carbon tetrachloride. The solvent was removed iii vacuo, with low heat, to yield 58 g of the desired benzyl 2-chloro-2-[(chlorocarbonyl) oxy] acetate as a clear colorless oil. 1H- NMR (300 MHz, CDCIs) 8 (ppm) : 5. 24 (s, 2H), 6. 45 (s, 1H), 7. 32 (s, 5H).

Example 2 : Ethyl 2-chloro-2- [ (chlorocarbonyl) oxy] acetate (Compound 1-2 of Table 1) Pyridine (0. 145 mL, 1. 79 mmol) was added to a solution of polymeric ethyl glyoxylate (18. 51 g, 181 mmol) and triphosgene (48. 5 g, 163 mmol) in dry THF at room temperature in a flask fitted with a reflux condenser and connected to a N2 bubbler. After 10 min the flask was placed in a pre-heated 65 °C oil bath. After 21 h, the reaction was allowed to cool to room temperature, and then the mixture was concentrated under vacuum. Ether was added to the residue, the mixture was filtered through Celite, and the filtrate was concentrated, affording 34. 6 g (87% yield) of a yellow oil. lH-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 36 (t, 3H) 4. 36 (q, 2H), 6. 48 (s, 1H).

Example 3 : Methyl 2-chloro-2- [ (chlorocarbonyl) oxy] acetate (Compound 1-3 of Table 1) The title compound was prepared according to the procedure described in Example 2 above, except methyl glyoxylate was substituted for ethyl glyoxylate. 1H- NMR (300 MHz, CDC13) 8 (ppm) : 3. 92 (s, 3H), 6. 52 (s, 1H).

Example 4 : Isopropyl 2-chloro-2- [ (chlorocarbonyl) oxy] acetate (Compound 1-4 of Table 1) The title compound was prepared according to the procedure described in Example 2 above, except isopropyl glyoxylate was substituted for ethyl glyoxylate.

1H-NMR (300 MHz, CDC13) 5 (ppm) : 1. 33 (s, 3H), 1. 35 (s, 3H), 5. 2 (q, 1H), 6. 44 (s, 1H).

Example 5 : tert-Butyl 2-chloro-2- [ (chlorocarbonyl) oxy] acetate (Compound 1-5 of Table 1) The title compound was prepared according to the procedure described in Example 2 above, except ter-butyl glyoxylate was substituted for ethyl glyoxylate.

1H-NMR (300 MHz, CDCIs) 6 (ppm) : 1. 53 (s, 9H), 6. 35 (s, 1H).

Example 6 : n-Butyl 2-chloro-2-[(chlorocarbonyl) oxy] acetate (Compound 1-6 of Table 1) The title compound was prepared according to the procedure described in Example 2 above, except n-butyl glyoxylate was substituted for ethyl glyoxylate.'H- NMR (300 MHz, CDCIs) 6 (ppm) : 0. 94 (t, 3H), 1. 40 (q, 2H), 1. 68 (m, 2H), 4. 28 (m, 2H), 6. 49 (s, 1H).

Following the general methods described hereinbefore, the following compounds of Formula V (where R2 = H) as listed in Table 2 were prepared.

Table 2 : Listing of Compounds of Formula V Cmpd# R12 G10 G11 G30 Y2 G31 t' D (X3)dZ3 2-1 Et O O O C1 O 1 0 ethyl 2-2 Et O O 0 1 O 1 0 ethyl 2-3 Et O O O ci O 1 0 n-butyl 2-4 Et O 0 O 1 O 1 0 n-butyl 2-5 Et O 0 0 ci O 1 0 isopropyl 2-6 Et O 0 0 1 O 1 0 isopropyl The following Examples are provided for guidance to the practitioner in order to practice the invention.

Example 7 : Chloro-ethylsulfanylcarbonyloxy-acetic acid ethyl ester (Compound 2-1 of Table 2) A 1000 mL round bottom flask was charged with sodium ethylthiolate (13. 3 g, 158 mmol) and 500 mL of dry diethyl ether. The mixture was cooled to-70 °C in an acetone dry ice bath. Ethyl 2-chloro-2- [ (chlorocarbonyl) oxy] acetate (32. 8 g, 155 mmol) was added as a solution in 20 mL of diethyl ether over 1. 5 h at such a rate that the reaction temperature did not exceed-65 °C. The reaction was allowed to warm to room temperature and stir for 16 h. The reaction was vacuum filtered, the filtrate dried (MgSO4), gravity filtered, and. concentrated under reduced pressure to yield 33. 5 g of a clear liquid. 1H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 33 (m, 6H), 2. 94 q, 2H), 4. 31 (q, 2H), 6. 65 (s, 1H).

Example 8 : Iodo-ethylsulfanylcarbonyloxy-acetic acid ethyl ester (Compound 2-2 of Table 2) To a stirred solution of chloro-ethylsulfanylcarbonyloxy-acetic acid ethyl ester (33. 5 g, 148 mmol) in 160 mL of dry acetone was added NaI (28. 8. g, 192 mmol). The mixture was stirred at room temperature for 4h. The acetone was removed and the remaining slurry was diluted with 100 mL of diethyl ether. The mixture was filtered through Celite and concentrated under reduced pressure to yield a brown liquid. The liquid was redissolved in 50 mL of diethyl ether and gravity filtered to afford 37. 1 g of a brown liquid.'H-NMR (300 MHz, CDCl3) 8 (ppm) : 1. 33 (m, 6H), 2. 95 (q, 2H), 4. 30 (q, 2H), 7. 21 (s, 1H).

Example 9 : Chloro-ethylsulfanylcarbonyloxy-acetic acid butyl ester (Compound 2-3 of Table 2) The title compound was prepared according to the procedure described in Example 7 above except for the substitution of n-butyl 2-chloro-2- [ (chlorocarbonyl) oxy] acetate for ethyl 2-chloro-2- [ (chlorocarbonyl) oxy] acetate. 1H- NMR (300 MHz, CDCIs) 8 (ppm) : 0. 95 (t, 3H), 1. 33-1. 43 (m, 5H), 1. 67-1. 72 (m, 2H), 2. 93 (q, 2H), 4. 25-4. 30 (m, 2H), 6. 65 (s, 1H).

Example 10 : Iodo-ethylsulfanylcarbonyloxy-acetic acid butyl ester (Compound 2-4 of Table 2) The title compound was prepared according to the procedure described in Example 8 above except for the substitution of chloro-ethylsulfanylcarbonyloxy-acetic acid butyl ester for chloro-ethylsulfanylcarbonyloxy-acetic acid ethyl ester. lH-NMR (300 MHz, CDC13) 8 (ppm) : 0. 95 (t, 3H), 1. 32-1. 43 (m, 5H), 1. 65-1. 70 (m, 2H), 2. 92- 2. 95 (m, 2H), 4. 22-4. 26 (m, 2H), 7. 21 (s, 1H).

Example 11 : Chloro-ethylsulfanylcarbonyloxy-acetic acid isopropyl ester (Compound 2-5 of Table 2) The title compound was prepared according to the procedure described in Example 7 above except for the substitution of isopropyl 2-chloro-2- [ (chlorocarbonyl) oxy] acetate for ethyl 2-chloro-2- [ (chlorocarbonyl) oxy] acetate. 1H- NMR (300 MHz, CDCIs) 8 (ppm) : 1. 30 (t, 9H), 2. 90 (q, 2H), 5. 10 (s, 1H), 6. 60 (s, 1H).

Example 12 : Iodo-ethylsulfanylcarbonyloxy-acetic acid isopropyl ester (Compound 2-6 of Table 2) The title compound was prepared according to the procedure described in Example 8 above except for the substitution of chloro-ethylsulfanylcarbonyloxy-acetic acid isopropyl ester for chloro-ethylsulfanylcarbonyloxy-acetic acid ethyl ester.'H- NMR (300 MHz, CDC13) 8 (ppm) : 1. 30 (t, 9H), 2. 90 (q, 2H), 5. 10 (s, 1H), 7. 15 (s, 1H).

Following the general methods described hereinbefore, the following compounds of Formula IV (where Gic, G", G20, G2l, G30, and G3l = O, and R2 = H) as listed in Table 3 were prepared.

Table 3 : Listing of Compounds of Formula IV Cmpd &num Rl2 t'd (X3) dZ3 t q (X2) qZ2 3-1 Et 1 0 ethyl 1 0 2-propyl 3-2 Et 1 0 ethyl 1 0 t-butyl 3-3 Et 1 0 ethyl 1 0 ethyl 3-4 Et 1 0 ethyl 1 0 2-ethoxyphenyl 3-5 Et 1 0 ethyl 1 0 phenyl 3-6 Et 1 0 ethyl 1 0 2, 4-dichlorophenoxymethyl 3-7 Et 1 0 ethyl 1 0 3- (2, 4-dichlorophenoxy) propyl 3-8 Et 1 0 ethyl 1 0 1- (2, 4-dichlorophenoxy) ethyl 3-9 Et 1 0 ethyl 1 0 2, 5-dichloro-6-methoxyphenyl 3-10 Et 1 0 ethyl 1 0. 2, 4, 6-trimethylphenyl 3-11 Et 1 0 2-propyl 1 0 phenyl 3-12 Et 1 0 2-propyl 1 0 t-butyl 3-13 Et 1 0 2-propyl 1 0 1-methyl-1-cyclopropyl 3-14 Et 1 0 2-propyl 1 0 2-propyl 3-15 Et 1 0 2-propyl 1 0 ethyl 3-16 Et 1 0 2-propyl 1 0 N-acetyl-N-methyl-aminomethyl 3-17 Et 1 0 n-butyl 1 0 (diethoxyphosphoryl) methyl 3-18 Et 1 0 n-butyl 1 0 t-butyl 3-19 Et 1 0 2-propyl 1 0 3, 7-dichloro-8-quinoline The following Examples are provided for guidance to the practitioner in order to practice the invention.

Example 13 : 2-Methylpropanoic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-1 of Table 3) To a stirred ice cold solution of iodo-ethylsulfanylcarbonyloxy-acetic acid ethyl ester (5. 4 g, 17. 0 mmol) in 20 mL of dry THF was added 2-methylpropanoic acid (1. 94 g, 22. 1 mmol) followed by DIEA (2. 85 g, 22. 1 mmol). The reaction was allowed to stir

at room temperature for 16 h. The reaction was diluted with 100 mL of diethyl ether, gravity filtered, and concentrated under reduced pressure. The liquid was suction filtered through a pad of flash grade silica gel and eluted with 20% methylene chloride/hexanes. 1H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 24 (m, 6H), 1. 33 (m, 6H), 2. 66 (m, 1H), 2. 90 (q, 2H), 4. 28 (q, 2H), 5. 92 (s, 1H).

Example 14 : Pivalic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-2 of Table 3) The title compound was prepared according to the procedure described in Example 13 above except for the substitution of pivalic acid for 2-methylpropanoic acid. 1H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 25 (s, 9H), 1. 33 (m, 6H), 2. 88 (q, 2H), 4. 28 (q, 2H), 6. 82 (s, 1H).

Example 15 : Propionic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-3 of Table 3) The title compound was prepared according to the procedure described in Example 13 above except for the substitution of propionic acid for 2-methylpropanoic acid. 1H-NMR (300 MHz, CDC13) 8 (ppm) : 1. 16 (t, 3H), 1. 30 (m, 6H), 2. 47 (q, 2H), 2. 93 (q, 2H), 4. 29 (q, 2H), 6. 94 (s, 1H).

Example 16 : 2-Ethoxybenzoic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-4 of Table 3) The title compound was prepared according to the procedure described in Example 13 above except for the substitution of 2-ethoxybenzoic acid for 2- methylpropanoic acid. 1H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 23 (m, 6H), 1. 44 (t, 3H), 2. 92 (q, 2H), 4. 12 (q, 2H), 4. 31 (q, 2H), 6. 96 (m, 2H), 7. 15 (s, 1H), 7. 43 (t, 1H), 7. 92 (d, 1H).

Example 17 Benzoic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-5 of Table 3) The title compound was prepared according to the procedure described in Example 13 above except for the substitution of benzoic acid for 2-methylpropanoic acid. 1H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 32 (m, 6H), 2. 93 (q, 2H), 4. 35 (q, 2H), 7. 19 (s, 1H), 7. 35 (t, 2H), 7. 48 (t, 1H), 8. 10 (d, 2H).

Example 18 2, 4-Dichlorophenoxyacetic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-6 of Table 3) The title compound was prepared according to the procedure described in Example 13 above except for the substitution of 2, 4-dichlorophenoxyacetic acid for 2- methylpropanoic acid. 1H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 32 (m, 6H), 2. 92 (q, 2H), 4. 29 (q, 2H), 4. 82 (s, 2H), 6. 83 (d, 1H), 6. 95 (s, 1H), 7. 24 (dd, 1H), 7. 38 (s, 1H).

Example 19 : 4- (2, 4-Dichlorophenoxy) butyric acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-7 of Table 3) The title compound was prepared according to the procedure described in Example 13 above except for the substitution of 4- (2, 4-diclorophenoxy) butyric acid for 2-methylpropanoic acid. tH-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 32 (m, 6 H), 2. 18 (m, 2H), 2. 76 (t, 2H), 2. 97 (q, 2H), 4. 02 (q, 2H), 4. 31 (q, 2H), 6. 83 (d, 1H), 6. 86 (s, 1H), 7. 15 (d, 1H), 7. 35 (d, 1H).

Example 20 : 2'- (2, 4-Dichlorophenoxy) propionic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy- methyl ester (Compound 3-8 of Table 3) The title compound was prepared according to the procedure described in Example 13 above except for the substitution of 2'- (2, 4-diclorophenoxy) propionic acid for 2-methylpropanoic acid. 1H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 32 (m, 6H), 1. 74 (m, 3H), 2. 91 (q, 2H), 4. 26 (q, 2H), 4. 88 (m, 1H), 6. 88 (m, 1H), 6. 95 (s, 1H), 7. 18 (d, 1H), 7. 38 (s, 1H).

Example 21 : 2, 5-Dichloro-6-methoxybenzoic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-9 of Table 3) The title compound was prepared according to the procedure described in Example 13 above except for the substitution of 2, 5-dichloro-6-methoxybenzoic acid for 2-methylpropanoic acid. 1H-NMR (300 MHz, CDC13) 8 (ppm) : 1. 34 (m, 6H), 2. 93 ( q, 2H), 3. 94 (s, 3H), 4. 34 (q, 2H), 7. 16 (d, 1H), 7. 18 (s, 1H), 7. 39 (d, 1H).

Example 22 : 2, 4, 6-Trimethylbenzoic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-10 of Table 3) The title compound was prepared according to the procedure described in Example 13 above except for the substitution of 2, 4, 6-trimethylbenzoic acid for 2- methylpropanoic acid. 1H-NMR (300 MHz, CDC13) 8 (ppm) : 1. 33 (m, 6H), 2. 27 (s, 3H), 2. 34 (s, 6H), 2. 90 (q, 2H), 4. 31 (q, 2H), 6. 86 (s, 2H), 7. 16 (s, 1H).

Example 23 : Benzoic acid isopropoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-11 of Table 3) To a stirred ice cold solution of iodo-ethylsulfanylcarbonyloxy-acetic acid isopropyl ester (3. 1 g, 9. 3 mmol) in 40 mL of dry THF was added benzoic acid (1. 5 g, 12. 0 mmol) followed by DIEA (2. 1 mL, 12. 0 mmol). The reaction was allowed to stir at room temperature for 16h. The solvent was removed under reduced pressure.

The residue was dissolved in ether and washed 3 times with a saturated solution of sodium bicarbonate and once with brine. The ether layer was dried over MgSO4 and concentrated to yield 2. 0 g (66%) of the desired product, which was used without further purification. lH-NMR (300 MHz, CDC13) 8 (ppm) : 1. 30 (m, 9H), 2. 90 (q, 2H), 5. 15 (m, 1H), 7. 13 (s, 1H), 7. 55 (m, 3H), 8. 10 (m, 2H).

Example 24 : Pivalic acid isopropoxycarbonyl-ethyl sulfanylcarbonyloxy-methyl ester (Compound 3-12 of Table 3)

The title compound was prepared according to the procedure described in Example 23 above except for the substitution of pivalic acid for benzoic acid. IH- NMR (300 MHz, CDCIs) 8 (ppm) : 1. 30 (m, 18H), 2. 90 (q, 2H), 5. 10 (m, 1H), 6. 85 (s, 1H).

Example 25 : 1-Methyl-1-cyclopropanecarboxylic acid isopropoxycarbonyl- ethylsulfanylcarbonyloxy-methyl ester (Compound 3-13 of Table 3) The title compound was prepared according to the procedure described in Example 23 above except for the substitution of 1-methyl-1-cyclopropanecarboxylic acid for benzoic acid. 1H-NMR (300 MHz, CDCIs) (ppm) : 0. 75 (d, 2H), 1. 35 (m, 14H), 2. 90 (m, 2H), 5. 10 (m, 1H), 6. 85 (s, 1H).

Example 26 : Isobutyric acid isopropoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-14 of Table 3) The title compound was prepared according to the procedure described in Example 23 above except for the substitution of isobutyric acid for benzoic acid.'H- NMR (300 MHz, CDCIs) 8 (ppm) : 1. 25 (m, 15H), 2. 65 (m, 1H), 2. 90 (m, 2H), 5. 10 (m, 1H), 6. 90 (s, 1H).

Example 27 : Propionic acid isopropoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-15 of Table 3) The title compound was prepared according to the procedure described in Example 23 above except for the substitution of propionic acid for benzoic acid. 1H- NMR (300 MHz, CDC13) 8 (ppm) : 1. 15 (t, 3H), 1. 30 (m, 9H), 2. 45 (q, 2H), 2. 90 (q, 2H), 5. 10 (m, 1H), 6. 90 (s, 1H).

Example 28 : Acetyl methyl carbamic acid isopropoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-16 of Table 3)

The title compound was prepared according to the procedure described in Example 23 above except for the substitution of acetyl methyl carbamic acid for benzoic acid. 1H-NMR (300 MHz ; CDCIs) 8 (ppm) : 1. 30 (m, 9H), 2. 10 (d, 3H), 2. 90 (m, 2H), 3. 10 (d, 3H), 4. 20 (m, 2H), 5. 10 (m, 1H), 6. 90 (s, 1H).

Example 29 Diethylphosphonoacetic acid butoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-17 of Table 3) The title compound was prepared according to the procedure described in Example 13 above except for the substitution of diethylphosphonoacetic acid for 2- methylpropanoic acid and iodoethylsulfanylcarbonyloxy-acetic acid butyl ester for iodoethylsulfanylcarbonyloxy-acetic acid ethyl ester. IH-NMR (300 MHz, CD30D) 8 (ppm) : 1. 35 (t, 6H), 2. 89 (q, 2H), 3. 03 (d, 2H), 4. 18 (q, 4H), 5. 84 (s, 2H).

Example 30 Pivalic acid butoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester (Compound 3-18 of Table 3) The title compound was prepared according to the procedure described in Example 13 above except for the substitution of pivalic acid for 2-methylpropanoic acid and iodoethylsulfanylcarbonyloxy-acetic acid butyl ester for iodoethylsulfanylcarbonyloxy-acetic acid ethyl ester. 1H-NMR (300 MHz, CD30D) 8 (ppm) : 1. 25 (s, 9H), 1. 31-1. 45 (m, 8H), 1. 65 (m 2H), 2. 95 (q, 2H), 4. 25 (m, 2H), 6. 92 (s, 1H).

Example 31 : 3, 7-Dichloro-8-quinolinecarboxylic acid isopropoxycarbonyl-ethylsulfanylcarbonyloxy- methyl ester (Compound 3-19 of Table 3) The title compound was prepared according to the procedure described in Example 23 above except for the substitution of 3, 7-dichloro-8-quinolinecarboxylic acid for benzoic acid. 1H-NMR (300 MHz, CDC13) d (ppm) : 1. 35 (m, 9H), 2. 95 (q, 2H), 5. 15 (m, 1H), 7. 25 (s, 1H), 7. 57 (d, 1H), 7. 76 (d, 1H), 8. 14 (s, 1H) 8. 83 (s, 1H).

Following the general methods described hereinbefore, the following compounds of Formula III (where Gt°, G", G20, G2', G30, and G3'= O and R2 = H) as listed in Table 4 were prepared.

Table 4 : Listing of Compounds of Formula III Cmpd &num Y1 t'Cl (X3) dZ3 t q (X2) qZ2 4-1 ci 1 0 ethyl 1 0 2-propyl 4-2 ci 1 0 ethyl 1 0 t-butyl 4-3 Cl 1 0 ethyl 1 0 ethyl 4-4 ci 1 0 ethyl 1 0 2-ethoxyphenyl 4-5 Cl 1 0 ethyl 1 0 phenyl 4-6 Cl 1 0 ethyl 1 0 3- (2, 4-dichlorophenoxy) propyl 4-7 Cl 1 0 ethyl 1 0 1- (2, 4-dichlorophenoxy) ethyl 4-8 Cl 1 0 ethyl 1 0 2, 5-dichloro-6-methoxyphenyl 4-9 Cl 1 0 ethyl 1 0 2, 4, 6-trimethylphenyl 4-10 Cl 1 0 n-butyl 1 0 diethylphosphonomethyl 4-11 Cl 1 0 n-butyl 1 0 t-butyl 4-12 Cl 1 0 2-propyl 1 0 2-propyl 4-13 Cl 1 0 n-butyl 1 0 2-propyl 4-14 Cl 1 0 2-propyl 1 0 phenyl 4-15 Cl 1 0 2-propyl 1 0 undecanyl 4-16 Cl 1 0 2-propyl 1 1 1- [4- (2-methylpropyl) phenyl] ethyl The following Examples are provided for guidance to the practitioner in order to practice the invention.

Example 32 : 2-Methylpropionic acid ethoxycarbonyl-chlorocarbonyloxy-methyl ester (Compound 4- 1 of Table 4) A 100 mL round bottom flask was charged with 2-methylpropionic acid ethoxycarbonyl-ethyl sulfanylcarbonyloxy-methyl ester (4. 4 g, 15. 8 mmol) and cooled to 5 °C. Sulfuryl chloride (2. 70 g, 20. 0 mmol) was added over 1 min. After 30 min of stirring, the cooling bath was removed and the reaction was allowed to stir for 3 h at room temperature and then placed under vacuum. The material was used without

purification. lH-NMR (300 MHz, CDC13) 8 (ppm) : 1. 26 (m, 9H), 2. 58 (m, 1H), 4. 32 (q, 2H), 6. 83 (s, 1H).

Example 33 : Pivalic acid ethoxycarbonyl-chlorocarbonyloxy methyl ester (Compound 4-2 of Table 4) The title compound was prepared according to the procedure described in Example 32 above except for the substitution of pivalic acid ethoxycarbonyl- ethylsulfanylcarbonyloxy methyl ester for isobutyric acid ethoxycarbonyl- ethylsulfanylcarbonyloxy-methyl ester. 1H-NMR (300 MHz, CDC13) 8 (ppm) : 1. 25 (s, 9H), 1. 33 (t, 3H), 4. 32 (q, 2H), 6. 78 (s, 1H).

Example 34 : Propionic acid ethoxycarbonyl-chlorocarbonyloxy-methyl ester (Compound 4-3 of Table 4) The title compound was prepared according to the procedure described in Example 32 above except for the substitution propionic acid ethoxycarbonyl- ethylsulfanylcarbonyloxy-methyl ester for isobutyric acid ethoxycarbonyl- ethylsulfanylcarbonyloxy-methyl ester, using 1. 4 equiv of sulfuryl chloride and starting the reaction at 5 °C. 1H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 21 (t, 3H), 1. 35 (t, 3H), 2. 53 (q, 2H), 4. 32 (q, 2H), 6. 84 (s, 1H).

Example 35 : 2-Ethoxybenzoic acid ethoxycarbonyl-chlorocarbonyloxy-methyl ester (Compound 4-4 of Table 4) The title compound was prepared according to the procedure described in Example 32 above except for the substitution 2-ethoxybenzoic acid ethoxycarbonylethylsulfanyl-carbonyloxy methyl ester for isobutyric acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester, using 1. 4 equiv of sulfuryl chloride and starting the reaction at 5 °C. 1H-NMR (300 MHz, CDC13) 8 (ppm) : 1. 36 (t, 3H), 1. 45 (t, 3H), 4. 13 (q, 2H), 4. 36 (q, 2H), 6. 95 (m, 2H), 7. 02 (s, 1H), 7. 47 (t, 1H), 7. 91 (d, 1H).

Example 36 : Benzoic acid ethoxycarbonyl-chlorocarbonyloxy-methyl ester (Compound 4-5 of Table 4) The title compound was prepared according to the procedure described in Example 32 above except for the substitution benzoic acid ethoxycarbonyl- ethylsulfanylcarbonyloxy-methyl ester for isobutyric acid ethoxycarbonyl- ethylsulfanylcarbonyloxy-methyl ester, using 1. 2 equiv of sulfuryl chloride and starting the reaction at 5 °C. 1H-NMR (300 MHz, CDCIs) 5 (ppm) : 1. 36 (t, 3H), 4. 32 (q, 2H), 7. 09 (s, 1H), 7. 50 (t, 2H), 7. 63 (t, 1H), 8. 10 (d, 2H).

Example 37 : 2, 4-Dichlorophenoxybutyric acid ethoxycarbonyl-chlorocarbonyloxy-methyl ester (Compound 4-6 of Table 4) The title compound was prepared according to the procedure described in Example 32 above except for the substitution 2, 4-dichlorophenoxybutyric acid ethoxycarbonylethyl-sulfanylcarbonyloxy-methyl ester for isobutyric acid ethoxycarbonyl ethylsulfanylcarbonyl-oxy-methyl ester, using 1. 45 equiv of sulfuryl chloride and starting the reaction at 5 °C. 1H-NMR (300 MHz, CDCIs) 6 (ppm) : 1. 34 (t, 3H), 2. 21 (m, 2H), 2. 56 (t, 2H), 4. 07 (t, 2H), 4. 31 (q, 2H), 6. 83 (d, 1H), 6. 86 (s, 1H), 7. 17 (d, 1H), 7. 35 (d, 1H).

Example 38 : 2'- (2, 4-Dichlorophenoxy) propionic acid ethoxycarbonyl-chlorocarbonyloxy-methyl ester (Compound 4-7 of Table 4) The title compound was prepared according to the procedure described in Example 32 above except for the substitution 2'- (2, 4-dichlorophenoxy) propionic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester for isobutyric acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester, using 1. 80 equiv of sulfuryl chloride and starting the reaction at 5 °C.'H-NMR (300 MHz, CDCIs) 5 (ppm) : 1. 37 (t, 3H), 1. 92 (m, 3H), 4. 33 (q, 2H), 4. 83 (m, 1H), 6. 84 (m, 2H), 7. 16 (dd, 1H), 7. 38 (d, 1H).

Example 39 : 2, 5-Dichloro-6-methoxybenzoic acid ethoxycarbonyl-chlorocarbonyloxy-methyl ester (Compound 4-8 of Table 4) The title compound was prepared according to the procedure described in Example 32 above except for the substitution 2, 5-dichloro-6-methoxybenzoic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester for isobutyric acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester, using 1. 45 equiv of sulfuryl chloride and starting the reaction at 5 °C. 1H-NMR (300 MHz, CDCl3) 8 (ppm) : 1. 34 (t, 3H), 3. 95 (s, 3H), 4. 36 (q, 2H), 7. 08 (s, 1H), 7. 18 (d, 1H), 7. 42 (d, 1H).

Example 40 : 2, 4, 6-Trimethylbenzoic acid ethoxycarbonyl-chlorocarbonyloxy-methyl ester (Compound 4-9 of Table 4) The title compound was prepared according to the procedure described in Example 32 above except for the substitution of 2, 4, 6-trimethylbenzoic acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester for isobutyric acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester, using 1. 45 equiv of sulfuryl chloride and starting the reaction at 5 °C.'H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 34 (t, 3H), 2. 28 (s, 3H), 2. 35 (s, 6H), 4. 34 (q, 2H), 6. 89 (s, 1H), 7. 06 (s, 1H), 7. 12 (s, 1H).

Example 41 : Diethylphosphonoacetic acid butoxycarbonyl-chlorocarbonyloxy-methyl ester (Compound 4-10 of Table 4) The title compound was prepared according to the procedure described in Example 32 above except for the substitution diethylphosphonoacetic acid butoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester for isobutyric acid ethoxycarbonyl-ethylsulfanylcarbonyloxy-methyl ester, using 1. 9 equiv of sulfuryl chloride and starting the reaction at 5 °C. 1H-NMR (300 MHz, CDCIs) (ppm) : 0. 96 (t, 3H), 1. 37 (t, 6H), 1. 72 (m, 2H), 2. 01 (m, 2H), 3. 15 (d, 2H), 4. 27 (m, 6H), 6. 85 (s, 1H).

Example 42 : Pivalic acid butoxycarbonyl-chlorocarboryloxy-methyl ester (Compound 4-11 of Table 4) The title compound was prepared according to the procedure described in Example 32 above except for the substitution of pivalic acid butoxycarbonyl- ethylsulfanylcarbonyloxy-methyl ester for isobutyric acid ethoxycarbonyl- ethylsulfanylcarbonyloxy-methyl ester, using 1. 9 equiv of sulfuryl chloride and starting the reaction at 5 °C. 1H-NMR (300 MHz, CDCIs) 8 (ppm) : 0. 95 (t, 3H), 1. 27 (s, 9H), 1. 35-1. 45 (m, 2H), 1. 65-1. 75 (m 2H), 4. 31 (m, 2H), 6. 85 (s, 1H).

Example 43 : 2-Methylpropanoic acid (chlorocarbonyloxy)- [ (l-methylethoxy) carbonyl] methyl ester (Compound 4-12 of Table 4) The title compound was prepared according to the procedure described in Example 32 above except for the substitution of isobutyric acid isobutoxycarbonyl- ethylsulfanylcarbonyloxy-methyl ester for isobutyric acid ethoxycarbonyl- ethylsulfanylcarbonyloxy-methyl ester, using 1. 9 equiv of sulfuryl chloride and starting the reaction at 5 °C. H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 22-1. 30 (m, 6H), 1. 30-1. 40 (m, 6H), 2. 70 (heptet, 1H), 5. 14 (heptet, 1H), 6. 77 (s, 1H). ( Example 44 : 2-Methylpropanoic acid (chlorocarbonyloxy) (butoxycarbonyl) methyl ester (Compound 4-13 of Table 4) Diisopropylethylamine (0. 57g, 4. 41 mmole) was added in three portions 2 min apart to a shaken solution of butyl 2- (ethylthiocarbonyloxy)-2-iodoethanoate (1. 01 g, 2. 92 mmol) and 2-methyl-2-propanoic acid (0. 32 g, 3. 63 mmole) in 1. 11 g anhydrous tetrahydrofuran. One minute later, isobutyric. acid (0. 13 g, 1. 47 mmole) was added to neutralize an accidental amine overcharge. After the mixture stood with occasional shaking for 16 h at room temperature, the slurry was concentrated i7L uacuo to 2. 00 g, and the residue was extracted with three 3. 4-5. 5 g portions of ca. 2/1 w/w diethylether/hexanes. The supernatants were washed with 41. 3 wt. % aqueous potassium carbonate solution and concentrated in uacuo to give 2-methylpropanoic acid (ethylthiocarbonyloxy)- (butoxycarbonyl) methyl ester (0. 79 g, 2. 58 mmol), as a

pale yellow oil. This oil was dissolved in 1. 09 g dichloromethane and 97% sulfuryl chloride (0. 90 g, 6. 67 mmol) was added in three portions 1 min apart at room :. temperature. After the resulting solution stood for another 68 min, it was concentrated in uacuo to constant weight to give 2-methylpropanoic acid (chlorocarbonyloxy)- (butoxycarbonyl) methyl ester (0. 73 g, 2. 60 mmole, 89% overall yield) as a yellow oil. 1H-NMR (300 MHz, CDCIs) 8 (ppm) : 0. 95 (t, 3H), 1. 24 (d, 3H), 1. 25 (d, 2H), 1. 39 (sextet, 2H), 1. 68 (p, 4H), 2. 71 (septet, 1H), 6. 99 (s, 1H).

Example45 : Benzoic acid (chlorocarbonyloxy) (isopropoxycarbonyl) methyl ester (Compound 4-14 of Table 4) Isopropyl 2- (ethylthiocarbonyloxy)-2-iodoethanoate (1. 01 g, 3. 04 mmol) was added to a well-mixed solution of benzoic acid (0. 56 g, 4. 59 mmol) and diisopropylethylamine (0. 55 g, 4. 25 mmol) in 2. 20 g anhydrous tetrahydrofuran. This gave a slight exotherm and slow fading of the red color with precipitation of solid.

After the mixture stood with occasional shaking for 4. 3 h at room temperature, the slurry was concentrated in vacuo to 2. 64 g and the residue was partitioned between 1. 32 g deionized water containing 1. 09 g 41. 3 % potassium carbonate solution and three 1. 6-2. 6 g hexanes extracts. The extracts were concentrated in vacuo to give benzoic acid (ethylthiocarbonyloxy)- (isopropoxycarbonyl)-methyl ester (0. 87g, 2. 67 mmole), as a pale yellow oil. This oil was dissolved in 1. 32 g dichloromethane and 97 % sulfuryl chloride (0. 89 g, 6. 59 mmol) was added in three portions over 3 min at room temperature. The vigorous foaming soon subsided. After the resulting solution stood for another 2. 4 h, it was concentrated in vacuo to constant weight to give benzoic acid (chlorocarbonyloxy)- (isopropoxycarbonyl) methyl ester (0. 85 g, 2. 83 mmole, 93% overall yield) as a yellow oil.'H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 34 (d, 6H), 5. 20 (septet, 1H), 7. 03 (s, 1H), 7. 50 (t, 2H), 7. 66 (t, H), 8. 11 (d, 2H).

Example 46 : Dodecanoic acid (chlorocarbonyloxy) (isopropoxycarbonyl) methyl ester (Compound 4- 15 of Table 4) Isopropyl 2- (ethylthiocarbonyloxy)-2-iodoethanoate (1. 01 g, 3. 04 mmol) was added to a well-mixed solution of dodecanoic acid (0. 91 g, 4. 54 mmol) and

diisopropylethylamine (0. 56 g, 4. 33 rnmol) in 2. 12 g anhydrous tetrahydrofuran.

This gave a slight exotherm and slow fading of the red color with precipitation of solid. After the mixture stood with occasional shaking for 21. 7 h at room temperature, the slurry was concentrated17l uacuo to 2. 9 g and the residue was extracted with four 2. 8-3. 9 g portions of hexanes. The extracts were washed with 0. 94 g 41. 3 % potassium carbonate solution and concentrated i71 vacuo to give dodecanoic acid (ethylthiocarbonyloxy) (isopropoxycarbonyl) methyl ester (0. 77g, 1. 90 mmol), as a pale yellow oil. This oil was dissolved in 1. 42 g dichloromethane and 97 % sulfuryl chloride (0. 73 g, 5. 41 mmol) was added in three portions over 9 min at room temperature. The vigorous foaming soon subsided. After the resulting solution stood for another 3. 6 h, it was concentrated in vacuo to constant weight to give dodecanoic acid (chlorocarbonyloxy)- (isopropoxycarbonyl) methyl ester (0. 75 g, 1. 98 mmole, 65% overall yield) as a yellow oil. tH-NMR (300 MHz, CDCIs) 8 (ppm) : 0. 88 (t, 3H), 1. 26 (bs, 16H), 1. 31 (two equal doublets 1. 3 Hz apart, 6H), 1. 59 (p, 2H), 5. 19 (septet, 1H), 6. 78 (s, 1H).

Example 47 : 2- [4- (2-Methylpropyl) phenyl] propanoic acid (chlorocarbonyloxy) (isopropoxy- carbonyl) methyl ester (Compound 4-16 of Table 4) Five 200 mg ibuprofen (a-methyl-4- (2-methylpropyl) benzeneacetic acid) tablets (total tablet wt. 1. 64 g, 4. 85 mmol) were stirred for 15 min with 3. 56 g dichloromethane containing triisopropylamine (0. 63 g, 4. 87 mmol). Isopropyl 2- (ethylthiocarbonyloxy)-2-iodoethanoate (1. 03 g, 3. 10 mmol) was added with a 0. 90 g dichloromethane pipet rinse, causing a slight exotherm and fading of a red color. After the mixture stood with occasional shaking for 28 h at room temperature, the slurry was concentrated bit vacuo to 3. 88 g and the residue was extracted with five 3. 3-4. 0 g portions of hexanes. The hexanes supernatants were washed with 41. 3 wt. % aqueous potassium carbonate solution and concentrated i71 vacuo to give 2- [4- (2-methylpropyl) phenyl] propanoic acid (ethylthiocarbonyloxy) (isopropoxy- carbonyl) methyl ester (1. 05 g, 2. 56 mmol), as a pale yellow oil. This oil was dissolved in 1. 52 g dichloromethane and 97 % sulfuryl chloride (1. 05 g, 7. 78 mmol) was added in four portions over 5 min at room temperature. After the resulting solution stood for another 120 min, it was concentrated in vacuo to constant weight to give 2- [4- (2-

methylpropyl) phenyl] propanoic acid (chloro-carbonyloxy) (isopropoxy-carbonyl) methyl ester (1. 00 g, 84 % overall yield) as a yellow oil.'H-NMR (300 MHz, CDCl3) 5 (ppm) : 0. 90 ppm (d, 6H), 1. 14-1. 20 (two d, total of 3H), 1. 27 (d, 3H), 1. 55 d (3H), 1. 56 (septet, 1H), 1. 84 (septet, 1H), 2. 45 (dd, 2H), 3. 82 and 3. 84 (two equal q, total of 1H), 5. 04 and 5. 11 (two equal septets, total of 1H), 6. 74 and 6. 76 (two equal s, total of 1H), 7. 11 (d, 2 H), 7. 20 (d, 2H).

Following Method A described hereinbefore, the following compound of Formula XX as listed in Table 5 was prepared.

XX Table 5 : Listing of Compound of Formula XX Cmpd# G20 G21 G31 R2 t' d (X3)dZ3 t q (X2)qZ2 5-1 O O O H 1 0 2-propyl 1 0 2-propyl The following Example is provided for guidance to the practitioner in order to practice the invention.

Example 48 : 2-Methylpropionic acid (N-methyl-3-phenyl-3- [ (4- trifluoromethyl) phenoxy] propylcarbamoyloxy)- (2-propyloxycarbonyl) methyl ester (Compound 5-1 of Table 5) 2-Methylpropanoic acid (chlorocarbonyloxy)- [ (l-methylethoxy) carbonyl] methyl ester (Compound 4-12, 28 pL, 0. 12 mmol) was added via syringe to a solution of w fluoxetine hydrochloride (Sigma Chemical Co., 42. 5 mg, 0. 123 mol) and 4- (dimethylamino) pyridine (30. 0 mg, 0. 246 mmol) in THF (1. 9 mL) at room temperature under N2. The reaction was allowed to stir for 16 h. Then saturated aqueous ammonium chloride was added, the product was extracted into ethyl acetate, the extract was dried over Na2SO4, and the volatiles were removed in vacuo.

The crude product was purified by flash chromatography on silica gel using a

hexanes-ethyl acetate gradient. The title compound was isolated cleanly as a pale yellow oil in 74% yield and consisted of a mixture of diastereomers. lH-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 14-1. 28 (m, 12H), 2. 10-2. 32 (m, 2H), 3. 53-3. 75 (m, 1H), 2. 93- 2. 95 (m, 3H), 3. 51 (t, 2H), 5. 05-5. 17 (m, 1H), 5. 17-5. 27 (m, 1H), 6. 70-6. 75 (four singlets, 1H), 6. 89 (d, 2H), 7. 22-7. 36 (m, 5H), 7. 42 (d, 2H).

Following Method A described hereinbefore, the following compound of Formula XXII as listed in Table 6 was prepared.

XXII Table 6 : Listing of Compound of Formula XXII Cmpd G20 G21 G31 R2 t' d (X3)dZ3 t q (X2)qZ2 6-1 O O O H 1 0 2-propyl 1 0 2-propyl The following Example is provided for guidance to the practitioner in order to practice the invention.

Example 49 : 2-Methylpropionic acid [(2, 4-difluoro-1-phenyl)-bis-(lH-1, 2, 4-triazol-1- ylmethyl)] methyloxycarbonyloxy- (2-propyloxycarbonyl) methyl ester (Compound 6-1 of Table 6) Potassium bis (trimethylsilyl) amide (0. 327 mL of a 0. 5 M solution in toluene, 0. 16 mmol) was added via syringe to a solution of fluconazole (Pfizer, 50. 5 mg, 0. 165 mmol) in THF (1. 5 mL) at-78 °C under N2. The reaction was allowed to stir at -78 °C for 10 min, then at 0 °C for 35 min, at which time 2-methylpropanoic acid (chlorocarbonyloxy)- [ (l-methylethoxy) carbonyl] methyl ester (Compound 4-12, 76 IlL, 0. 16 mmol) was added via syringe. The reaction was allowed to warm slowly to room temperature over 22 h. Then saturated aqueous ammonium chloride was added, the

product was extracted into ethyl acetate, the extract was dried over Na2SO4, and the volatiles were removed in vacuo. The crude product was purified by flash chromatography on silica gel using an ethyl acetate-methanol gradient. The title compound was isolated as a pale yellow oil in 40% yield ; unreacted fluconazole was also recovered (28%). 1H-NMR (300 MHz, CDCIs) (ppm) : 1. 22-1. 25 (m, 6H), 1. 28- 1. 31 (m, 6H), 2. 70 (heptet, 1H), 5. 06-5. 24 (m, 5H), 6. 73 (s, 1H), 6. 73-6. 81 (m, 1H), 6. 82-6. 96 (m, 2H), 7. 85 (s, 1H), 7. 86 (s, 1H), 8. 08 (s, 1H), 8. 12 (s, 1H).

Following Method A described hereinbefore, the following compound of Formula XXIV as listed in Table 7 was prepared.

XXIV Table 7 : Listing of Compound of Formula XXIV Cmpd Go G Gi R2 t'd (X3) dZ3 t q (X2) qZ2 7-1 O O 0 H 1 0 2-propyl 1 0 2-propyl The following Example is provided for guidance to the practitioner in order to practice the invention.

Example 50 : 2-Methylpropionic acid [2, 6-Dimethyl-3, 5-dicarbomethoxy-4- (2-nitrophenyl)-1, 4- dihydropyridin-1-yl] carbonyloxy- (2-propyloxycarbonyl) methyl ester (Compound 7-1 of Table 7) Potassium bis (trimethylsilyl) amide (0. 296 mL of a 0. 5 M solution in toluene, 0. 148 mmol) was added via syringe to a solution of nifedipine (Sigma Chemical Co., 51. 3 mg, 0. 148 mmol) in THF (1. 5 mL) at-78 °C under N2. The reaction was allowed to stir at-78 °C for 15 min, then at 0 °C for 35 min, at which time 2-methylpropanoic acid (chlorocarbonyloxy)- [ (l-methylethoxy) carbonyl] methyl ester (compound 4-12, 33

uL, 0. 15 mmol) was added via syringe. The reaction was allowed to warm slowly to room temperature over 16 h. Then saturated aqueous ammonium chloride was added, the product was extracted into ethyl acetate, the extract was dried over Na2SO4, and the volatiles were removed under reduced pressure. The crude product was purified by flash chromatography on silica gel using a hexanes-ethyl acetate gradient. The title compound was isolated as a pale yellow oil in 12% yield ; unreacted nifedipine was also recovered (54%). 1H-NMR (300 MHz, CDCIs) 8 (ppm) : 1. 20-1. 34 (m, 12 H), 2. 48 (s, 3H), 2. 52 (s, 3H), 2. 67 (heptet, 1H), 3. 72 (s, 3H), 3. 73 (s, 3H), 5. 15 (heptet, 1H), 5. 73 (s, 1H), 6. 86 (s, 1H), 7. 24-7. 35 (m, 2H), 7. 54 (t, 1H), 7. 68 (d, 1H).

Following Method A described hereinbefore, the following compounds of Formula XXVI as listed in Table 8 were prepared.

Table 8 : Listing of Compounds of Formula XXVI Cmpd# G20 G21 G31 R2 t' d (x3)dZ3 t q (X2) qZ2 8-1 O O O H 1 0 n-butyl 1 0 2-propyl 8-2 O O O H 1 0 2-propyl 1 0 phenyl 8-3 O O O H 1 0 n-butyl 1 0 undecyl 8-4 O O 0 H 1 0 2-propyl 1 1 1- [4- (2-methyl- propyl) phenyl] ethyl The following Examples are provided for guidance to the practitioner in order to practice the invention.

Example 51 : 7-(4-[(Butoxycarbonyl) (2-methylpropanoyloxy) methoxycarbonyl]-1-piperazinyl)-1- ethyl-6-fluoro-1, 4-dihydro-4-oxo-3-quinolinecarboxylic acid (Compound 8-1 of Table 8) 2-Methylpropanoic acid (chlorocarbonyloxy) (butoxycarbonyl) methyl ester (0. 22 g, 0. 78 mmol) was added in two portions (0. 19g, 0. 03 g) with shaking 2 min apart to a slurry of norfloxacin (0. 22 g, 0. 69 mmol) and triisopropylamine (0. 15 g, 1. 05 mmol)

in 2. 42 g CH2C12, causing a moderate exotherm and dissolution of much then almost all of the solid. The mixture stood another 10 min at room temperature before it was concentrated in uacuo to 0. 78 g of gum and solid. This residue was repeatedly shaken with small portions of 3-4 : 1 w : w ethyl acetate : hexanes eluant which were added to the top of a 1. 02 g (7. 2 cm x 0. 65 cm ID) silica gel column. Evaporation of the eluate in 3 portions gave a total of 0. 34 g of yellow to white solid crystals. The two colored portions of crystals were washed twice with diethyl ether/hexanes to give 0. 05 g soluble gum and insoluble off-white crystals. The three portions of crystals were combined to give 7- (4- ( (butoxycarbonyl) (2-methylpropanoyloxy)- methoxycarbonyl]-1-piperazinyl)-1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-3-quinoline- carboxylic acid (0. 30 g, 77% yield).'H-NMR (300 MHz, CDC13) 8 (ppm) : 0. 94 (t, 3 H), 1. 23 (d, 3H), 1. 24 (d, 3H), 1. 40 (sextet, 2H), 1. 60 (t, 4H, area may include obscured water peak), 1. 64 (p, 3 H), 2. 67 (septet, 1H), 3. 31 (t, 4H), 3. 77 (s, 4H), 4. 24 (t, 2H), 4. 33 (q, 2H), 6. 85 (s, 1H), 6. 86 (d, 1H)., 8. 09 (d, 1H), and 8. 68 (s, 1H). Mp = 151. 5- 160. 0 °C. Reverse phase LC/electrospray MS gave a predominant LC peak with a positively charged P+1 ion at m/g 563. 8 compared with a calculated m/g of 563. 23 for the C27H34N3OsF parent ion of the assigned structure.

Example 52 : 7- (4- [ (Isopropoxycarbonyl) (benzoyloxy) methoxycarbonyl]-1-piperazinyl)-1-ethyl-6- fluor-1, 4-dihydro-4-oxo-3-quinolinecarboxylic acid (Compound 8-2 of Table 8) The title compound was prepared according to the procedure described in Example 51 above except for the substitution of benzoic acid (chlorocarbonyloxy)- (isopropoxycarbonyl) methyl ester for 2-methylpropanoic acid (chlorocarbonyl- oxy) (butoxycarbonyl) methyl ester. The yield of off-white crystals was 0. 30g (70% after correction for 7 wt. % ethyl acetate). Mp 135-143 °C. Reverse phase LC/electrospray MS gave a predominant LC peak with a positively charged P+1 ion at m/g 583. 7 compared with a calculated m/g of 583. 20 for the CzsHsoNsOsF parent ion of the assigned structure.

Example 53 : 7- (4- [ (Isopropoxycarbonyl) (dodecanoyloxy) methoxycarbonyl]-1-piperazinyl)-1-ethyl-6- fluor-1, 4-dihydro-4-oxo-3-quinolinecarboxylic acid (Compound 8-3 of Table 8)

The title compound was prepared according to the procedure described in Example 51 above except for the substitution of dodecanoic acid (chlorocarbonyl- oxy) (isopropoxycarbonyl) methyl ester for 2-methylpropanoic acid (chlorocarbonyloxy) (butoxycarbonyl) methyl ester. The yield of off-white crystals was 0. 34g (74%). Mp 105. 5-109. 2 °C. Reverse phase LC/electrospray MS gave a predominant LC peak with a positively charged P+1 ion at m/g 661. 8 compared with a calculated m/g of 661. 34 for the C34H48N309F parent ion of the assigned structure.

Example 54 : 7- (4- [ (2- [4- (2-Methylpropyl) phenyl] propanoyloxy) (isopropoxycarbonyl) methoxy- carbonyl]-1-piperazinyl)-1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-3-quinolinecarboxylic acid (Compound 8-4 of Table 8) The title compound was prepared according to the procedure described in Example 51 above except for the substitution of 2- [4- (2-methylpropyl) phenyl]- propanoic acid (chlorocarbonyloxy) (isopropoxycarbonyl) methyl ester for 2- methylpropanoic acid (chlorocarbonyloxy) (butoxycarbonyl) methyl ester. The yield of off-white crystals was 0. 41 g (89%). Mp 88. 0-96. 5 °C. Reverse phase LC/electrospray MS gave a predominant LC peak with a positively charged P+1 ion at m/g 667. 9 compared with a calculated m/g of 667. 29 for the C3sH42N3OsF parent ion of the assigned structure.

Following Method A described hereinbefore, the following compound of Formula XXVIII as listed in Table 9 was prepared.

XXVIII Table 9 : Listing of Compound of Formula XXVIII Cmpd &num G20 G21 G3l R2 t'd % 3) dZ3 t q 2) qZ2 9-1 O O O H 1 0 2-propyl. 1 0 2-propyl

The following Example is provided for guidance to the practitioner in order to practice the invention.

Example 55 2- (2-Methylpropanoyloxy)-2- (4-acetamidophenoxycarbonyloxy) ethanoic acid 1- methylethyl ester (Compound 9-1 of Table 9) 4-Acetamidophenol (0. 15 g, 0. 99 mmol) was stirred for 8 min with 1. 06 g absolute ethanol and fragmented 87. 11 wt. % potassium hydroxide pellets (0. 05 g, 0. 78 meq) to form a homogeneous solution. Ethanol (0. 96 g) was concentrated in vacuo, toluene (0. 50 g) was added, and the mixture was concentrated in uacuo with repeated heating to give an additional 0. 04 g weight loss. Dichloromethane (7. 87 g) and 2- (chlorocarbonyloxy)-2- (2-methylpropanoyloxy) ethanoic acid 1-methylethyl ester (0. 19g, 0. 71 mmol) were added with shaking without dissolving much of the gum.

The mixture stood for 17 h at room temperature, causing solid to form in both the solvent and gum layers. The stirring bar was freed by breaking up the solid and the mixture was stirred for 3. 3 h, forming a finely dispersed slurry. The slurry was concentrated i71 vacuo to a tan opaque gum which was extracted with four portions of ethyl acetate to separate crude (0. 27g, ca. 70% by NMR) 2- (2-methylpropanoyloxy)-2- (4-acetamidophenoxycarbonyloxy) ethanoic acid 1-methylethyl ester from insoluble solid. Short column silica gel chromatography using chloroform eluant gave purified 2- (2-methylpropanoyloxy)-2- (4-acetamidophenoxycarbonyloxy)-ethanoic acid 1- methylethyl ester (0. 17g, 63% yield) as a yellowish tan gum. Reverse phase LC/electrospray MS gave a predominant LC peak with a positively charged P+1 ion at m/g 381. 7 compared with a calculated m/g of 381. 14 for the CisH2sNOs parent ion of the assigned structure.

Following Method A described hereinbefore, the following compound of Formula XXX as listed in Table 10 was prepared.

Table 10 : Listing of Compound of Formula XXX Cmpd &num G20 G21 G31 R2 t'd % 3) dZ3 t q (X2) qz2 10-1 O O O H 1 0 n-butyl 1 0 2-propyl The following Example is provided for guidance to the practitioner in order to practice the invention.

Example 56 4- ( [ (Butoxycarbonyl) (2-methylprop anoyloxy) methoxycarbonyl] amino)-N- (5-methyl-3- isoxazolyl) benzenesulfonamide (Compound 10-1 of Table 10) 2-Methylpropanoic acid (chlorocarbonyloxy) (butoxycarbonyl) methyl ester (0. 21 g, 0. 75 mmol) was added in two portions 2 min apart to a shaken slurry of 4-amino- N- (5-methyl-3-isoxazolyl) benzenesulfonamide (0. 18 g, 0. 71 mmol) in 1. 51 g CH2CI2 containing triisopropylamine (0. 12 g, 0. 84 mmol). This afforded a slightly delayed moderate exotherm and caused most of the solid to dissolve. After 10 min of cooling to room temperature, the mixture was concentrated in vacuo to 0. 70 g, 0. 67 g diethyl ether was added to induce crystallization, and the mixture was concentrated lit vacuo to 0. 65 g of partially crystalline gum. The mixture was repeatedly washed with small portions of diethyl ether, then with ethyl acetate/hexanes eluant and the supernatants were passed through a 1. 14 g (7. 72 cm x 0. 68 cm ID) silica gel column to give six fractions. Five of these fractions, totaling 0. 35 g, appeared by NMR to contain significant amounts of the desired product.

Normal phase preparative HPLC of the non-volatiles from the best of these fractions (0. 13 g) gave high purity 4- ( [ (butoxycarbonyl) (2-methyl- propanoyloxy) methoxycarbonyl] amino)-N- (5-methyl-3-isoxazolyl) benzene- sulfonamide (0. 026 g, 7. 3% yield) as a golden gum, along with an equal quantity of less pure material. Reverse phase LC/electrospray MS gave a predominant LC peak with a positively charged P+1 ion at m/g 497. 7 compared with a calculated m/g of 497. 15 for the C2lH27N3OsS parent ion of the assigned structure.

Table Al describes additional examples of compounds of Formula I which can be made using the procedures described hereinbefore, where R2 is hydrogen, m = 1, q = 0, t = 0 or 1 and the pharmaceutical which defines the pharmaceutical moiety of these examples is Z' (XI) m-H. The following groups, Zl (X1)m-H, X1, G10, G11, R1, G20, G21, t and Z2 are defined within Table Al.

Table Al Cmpd# Z1(X1)m-H X1 G10 G11 R1 G20 G21 t Z2 Al-1 aletamine N O O CO2H O O 1 methyl Al-2 aletamine N O O CO2H O O 1 C(CH3)3 Al-3 aletamine N O O CO2H O O 1 Ph Al-4 aletamine N O O CO2H O O 1 4-Me-Ph <BR> <BR> <BR> A1-5 aletamine N O O CO2H O O 1 2-pyridyl Al-6 aletamine N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-7 aletamine N O O CO2H O O 1 2-furyl Al-8 aletamine N O O CO2H O O 1 2-thienyl Al-9 aletamine N O O CO2H--O Cl Al-10 aletamine N O O CO2H--O {N (Et) 3}+Cl.

Al-11 aletamine N O O CO2H O O 1 CF3CH2 <BR> <BR> A1-12 aletamine N O O COzH 0 O 1 cyclopropyl Al-13 aletamine N O O CO2H O O 1 2-OMe-Ph <BR> <BR> <BR> A1-14 aletamine N O O CO2H O O 1 MeSCH2 Al-15 aletamine N O O CO2H O O 1 MeOCH2 Al-16 aletamine N O O CO2H S S 1 Ph Al-17 aletamine N O O CO2H S S 1 NMe2 Al-18 aletamine N O O CO2H S S 1NBn2 <BR> <BR> Al-19 aletamine N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> Al-20 aletamine N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> A1-21 amphetamine N O O CO2H O O 1 methyl<BR> <BR> <BR> <BR> Al-22amphetamineN00COzH001C (CH3<BR> <BR> <BR> <BR> <BR> A1-23 amphetamine N O O C02H O O 1 Ph Al-24 amphetamine N O O CO2H O O 1 4-Me-Ph Al-25 amphetamine N O O CO2H O O 1 2-pyridyl Al-26 amphetamine N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-27 amphetamine N O O CO2H 0 O 1. 2-furyl<BR> <BR> <BR> <BR> <BR> A1-28 amphetamine N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> A1-29 amphetamine N O O CO2H--O Cl A1-30 amphetamine N O O COzH--0 {N (Et) 3}+Cl.

Al-31 amphetamine N O O CO2H O O 1 CF3CH2 Al-32 amphetamine N O O CO2H O O 1 cyclopropyl <BR> <BR> A1-33 amphetamine N O O CO2H O O 1 2-OMe-Ph Al-39 amphetamine N O O CO2H O O 1 MeSCH2 <BR> <BR> A1-35 amphetamine N O O CO2H O O 1 MeOCH2 Al-36 amphetamine N O O CO2H S S 1 Ph Al-37 amphetamine N O O CO2H S S 1 NMe2 Al-38 amphetamine N O O CO2H S S 1 NBn2 Al-39 amphetamine N O O CO2H O S 1 Ph Al-40 amphetamine N O O CO2H O S 1 Me Al-41 betahistine N O O CO2H O O 1 methyl Al-42 betahistine N O O CO2H O O 1 C(CH3)3 Al-43 betahistine N O O CO2H O O 1 Ph Al-44 betahistine N O O CO2H O O 1 4-Me-Ph <BR> <BR> <BR> A1-45 betahistine N O O COzH 0 O 1 2-pyridyl Al-46 betahistine N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-47 betahistine N O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> <BR> A1-48 betahistine N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> A1-49 betahistine N O O COzH--0 Cl A1-50 betahistine N O O CO2H--0 {N (Et) 3} +Cl- Al-51 betahistine N O O CO2H O O 1 CF3CH2 <BR> <BR> A1-52 betahistine N O O C02H 0 O 1 cyclopropyl Al-53 betahistine N O O CO2H O O 1 2-OMe-Ph <BR> <BR> A1-54 betahistine N O O CO2H O O 1 MeSCH2 Al-55 betahistine N O O CO2H O O 1 MeOCH2 Al-56 betahistine N O O CO2H S S 1 Ph Al-57 betahistine N O O CO2H S S 1 NMe2 Al-58 betahistine N O O CO2H S S 1 NBn2 <BR> <BR> A1-59 betahistine N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> A1-60 betahistine N O O CO2H O S 1 Me Al-61 clonidine N O O CO2H O O 1 methyl Al-62 clonidine N O O CO2H O O 1 C(CH3)3 Al-63 clonidine N O O CO2H O O 1 Ph Al-64 clonidine N O O CO2H O O 1 4-Me-Ph Al-65 clonidine N O O CO2H O O 1 2-pyridyl Al-66 clonidine N O O CO2H O O 1 2-pyridyl <BR> <BR> A1-67 clonidine N O O CO2H O O 1 2-furyl Al-68 clonidine N O O CO2H O O 1 2-thienyl A1-69 clonidine N O O C02H--0 Cl A1-70 clonidine N O O CO2H--O {N (Et) 3} +Cl- Al-71 clonidine N O O CO2H O O 1 CF3CH2 <BR> <BR> A1-72 clonidine N O O CO2H O O 1 cyclopropyl<BR> <BR> <BR> <BR> <BR> A1-73 clonidine N O O CO2H O O 1 2-OMe-Ph Al-74 clonidine N O O CO2H O O 1 MeSCH2 Al-75 clonidine N O O CO2H O O 1 MeOCH2 Al-76 clonidine N O O CO2H S S 1 Ph Al-77 clonidine N O O CO2H S S 1 NMe2 Al-78 clonidine N O O CO2H S S 1 NBn2 A1-79 clonidine N O O C02H O S 1 Ph Al-80clonidineN00C02H0S1Me <BR> <BR> Al-81 etintidine N O O CO2H 0 O 1 methyl<BR> <BR> <BR> <BR> <BR> Al-82 etintidine N O O CO2H O O 1 C(CH3)# Al-83 etintidine N O O CO2H O O 1 Ph Al-84 etintidine N O O CO2H O O 1 4-Me-Ph Al-85 etintidine N O O CO2H O O 1 2-pyridyl Al-86 etintidine N O O CO2H O O 1 4-pyridyl Al-87 etintidine N O O CO2H O O 1 2-furyl Al-88 etintidine N O O CO2H O O 1 2-thienyl A1-89 etintidine N O O CO2H--0 Cl Al-90etintidineN00C02H--0 {N (Et) 3} +Cl- Al-91 etintidine N O O CO2H O O 1 CF3CH2 <BR> <BR> A1-92 etintidine N O O CO2H O O 1 cyclopropyl<BR> <BR> <BR> <BR> A1-93 etintidine N O O CO2H O O 1 2-OMe-Ph<BR> <BR> <BR> <BR> <BR> A1-94 etintidine N O O CO2H O O 1 MeSCH2 Al-95 etintidine N O O CO2H O O 1 MeOCH2 Al-96 etintidine N O O CO2H S S 1 Ph Al-97 etintidine N O O CO2H S S 1 NMe2 Al-98 etintidine N O O CO2H S S 1 NBn2 Al-99 etintidine N O O CO2H O S 1 Ph A1-100 etintidine N O O CO2H O S 1 Me Al-101 fenfluramine N O O CO2H O O 1 methyl <BR> <BR> A1-102 fenfluramine N O O CO2H O O 1 C (CH3) 3<BR> <BR> <BR> <BR> A1-103 fenfluramine N O O CO2H O O 1 Ph Al-104 fenfluramine N O O CO2H O O 1 4-Me-Ph Al-105 fenfluramine N O O CO2H O O 1 2-pyridyl <BR> <BR> Al-106fenauramineN00COH0014-pyridyl<BR> <BR> <BR> <BR> A1-107 fenfluramine N O O CO2H O O 1 2-furyl Al-108 fenfluramine N O O CO2H O O 1 2-thienyl A1-109 fenfluramine N O O CO2H--0 Cl A1-110 fenfluramine N O O CO2H--0 {N (Et) 3} +Cl- Al-111 fenfluramine N O O CO2H O O 1 CF3CH2 Al-112 fenfluramine N O O CO2H O O 1 cyclopropyl <BR> <BR> A1-113 fenfluramine N O O CO2H O O 1 2-OMe-Ph Al-114 fenfluramine N O O CO2H O O 1 MeSCH2 Al-115 fenfluramine N O O CO2H O O 1 MeOCH2 Al-116 fenfluramine N O O CO2H S S 1 Ph Al-117 fenfluramine N O O CO2H S S 1 NMe2 Al-118 fenfluramine N O O CO2H S S 1 NBn2 <BR> <BR> A1-119 fenfluramine N O O C02H O S 1 Ph<BR> <BR> <BR> <BR> A1-120 fenfluramine N O O CO2H O S 1 Me Al-121 fludorex N O O CO2H O O 1 methyl Al-122 fludorex N O O CO2H O O 1 C(CH3)3 Al-123 fludorex N O O CO2H O O 1 Ph Al-124 fludorex N O O CO2H O O 1 4-Me-Ph Al-125 fludorex N O O CO2H O O 1 2-pyridyl Al-126 fludorex N O O CO2H O O 1 4-pyridyl Al-127 fludorex N O O CO2H O O 1 2-furyl <BR> <BR> A1-128 fludorex N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> A1-129 fludorex N O O CO2H--0 Cl A1-130 fludorex N O O CO2H--0 {N (Et) 3} +Cl- <BR> <BR> A1-131 fludorex N O O CO2H O O 1 CF3CH2 Al-132 fludorex N O O CO2H O O 1 cyclopropyl <BR> <BR> A1-133 fludorex N O O CO2H O O 1 2-OMe-Ph Al-134 fludorex N O O CO2H O O 1 MeSCH2 Al-135 fludorex N O O CO2H O O 1 MeOCH2 Al-136 fludorex N O O CO2H S S 1 Ph2 Al-137 fludorex N O O CO2H S S 1 NMe2 Al-138 fludorex N O O CO2H S S 1 NBn2 <BR> <BR> A1-139 fludorex N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-140 fludorex N O O CO2H O S 1 Me Al-141 nifedipine N O O CO2H O O 1 methyl Al-142 nifedipine N O O CO2H O O 1 C(CH3)3 Al-143 nifedipine N O O CO2H O O 1 Ph Al-144 nifedipine N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-145 nifedipine N O O CO2H O O 1 2-pyridyl<BR> <BR> <BR> <BR> <BR> <BR> A1-146 nifedipine N O O CO2H O O 1 4-pyridyl A1-147 nifedipine N O O CO2H O O 1 2-furyl <BR> <BR> A1-148 nifedipine N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> <BR> A1-149 nifedipine N O O CO2H--0 Cl A1-150 nifedipine N O O CO2H--0 {N (Et) 3} +Cl- Al-151 nifedipine N O O CO2H O O 1 CF3CH2 Al-152 nifedipine N O O CO2H O O 1 cyclopropyl Al-153 nifedipine N O O CO2H O O 1 2-OMe-Ph <BR> <BR> A1-154 nifedipine N O O CO2H O O 1 MeSCH2 Al-155 nifedipine N O O CO2H O O 1 MeOCH2 A1-156 nifedipine N O O C02H S S 1 Ph Al-157 nifedipine N O O CO2H S S 1 NMe2 <BR> <BR> Al-158 nifedipine N O O CO2H S S 1 NBnz<BR> <BR> <BR> <BR> <BR> <BR> A1-159 nifedipine N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-160 nifedipine N O O C02H O S 1 Me Al-161 oxmetidine N O O CO2H O O 1 methyl Al-162 oxmetidine N O O CO2H O O 1 C(CH3)3 Al-163 oxmetidine N O O CO2H O O 1 Ph Al-164 oxmetidine N O O CO2H O O 1 4-Me-Ph Al-165 oxmetidine N O O CO2H O O 1 2-pyridyl Al-166 oxmetidine N O O CO2H O O 1 4-pyridyl Al-167 oxmetidine N O O CO2H O O 1 2-furyl Al-168 oxmetidine N O O CO2H O O 1 2-thienyl Al-169 oxmetidine N O O CO2H - - 0 Cl Al-170 oxmetidine N O O CO2H - - 0 {N (Et) 3}+Cl- Al-171 oxmetidine N O O CO2H O O 1 CF3CH2 Al-172 oxmetidine N O O CO2H O O 1 cyclopropyl <BR> <BR> A1-173 oxmetidine N O O CO2H O O 1 2-OMe-Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-174 oxmetidine N O O CO2H O O 1 MeSCH2<BR> <BR> <BR> <BR> <BR> <BR> A1-175 oxmetidine N O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> <BR> <BR> A1-176 oxmetidine N O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-177 oxmetidine N O O C02H S S 1 NMe2 Al-178 oxmetidine N O O CO2H S S 1 NBn2 <BR> <BR> <BR> A1-179 oxmetidine N O O C02H O S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-180 oxmetidine N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> <BR> A1-181 tetrahydrazoline N O O CO2H O O 1 methyl Al-182 tetrahydrazoline N O O CO2H O O 1 C(CH3)3 A1-183 tetrahydrazoline N O O CO2H O O 1 Ph Al-184 tetrahydrazoline N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-185 tetrahydrazoline N O O CO2H O O 1 2-pyridyl Al-186 tetrahydrazoline N O O CO2H O O 1 4-pyridyl Al-187 tetrahydrazoline N O O CO2H O O 1 2-furyl Al-188 tetrahydrazoline N O O CO2H O O 1 2-thienyl A1-189 tetrahydrazoline N O O CO2H--0 C1 A1-190 tetrahydrazoline N O O CO2H--0 {N (Et) 3}+Cl@ Al-191 tetrahydrazoline N O O CO2H O O 1 CF3CH2 Al-192 tetrahydrazoline N O O CO2H O O 1 cyclopropyl Al-193 tetrahydrazoline N O O CO2H O O 1 2-OMe-Ph Al-194 tetrahydrazoline N O O CO2H O O 1 MeSCH2 Al-195 tetrahydrazoline N O O CO2H O O 1 MeOCH2 <BR> <BR> A1-196 tetrahydrazoline N O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-197 tetrahydrazoline N O O CO2H S S 1 NMe2 Al-198 tetrahydrazoline N O O CO2H S S 1 NBn2 <BR> <BR> A1-199 tetrahydrazoline N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-200 tetrahydrazoline N O O CO2H O S 1 Me Al-201 procaine N O O CO2H O O 1 methyl Al-202 procaine N O O CO2H O O 1 C(CH3)3 Al-203 procaine N O O CO2H O O 1 Ph Al-204 procaine N O O CO2H O O 1 4-Me-Ph Al-205 procaine N O O CO2H O O 1 2-pyridyl Al-206 procaine N O O CO2H O O 1 4-pyridyl Al-207 procaine N O O CO2H O O 1 2-furyl Al-208 procaine N O O CO2H O O 1 2-thienyl A1-209 procaine N O O CO2H--0 C1 A1-210 procaine N O O CO2H--0 {N (Et) 3} +Cl- Al-211 procaine N O O CO2H O O 1 CF3CH2 Al-212 procaine N O O CO2H O O 1 cyclopropyl Al-213 procaine N O O CO2H O O 1 2-OMe-Ph Al-214 procaine N O O CO2H O O 1 MeSCH2 Al-215 procaine N O O CO2H O O 1 MeOCH2 Al-216 procaine N O O CO2H S S 1 Ph <BR> <BR> A1-217 procaine N O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> <BR> A1-218 procaine N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> <BR> A1-219 procaine N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-220 procaine N O O CO2H O S 1 Me A1-221 thiabendazole N O O CO2H O O 1 methyl A1-222 thiabendazole N O O CO2H O O 1 C(CH3)3 <BR> <BR> Al-223thiabendazoleN00C02H001Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-224 thiabendazole N O O C02H O O 1 4-Me-Ph A1-225 thiabendazole N O O CO2H O O 1 2-pyridyl Al-226 thiabendazole N O O CO2H O O 1 4-pyridyl Al-227 thiabendazole N O O CO2H O O 1 2-furyl Al-228 thiabendazole N O O CO2H O O 1 2-thienyl A1-229 thiabendazole N O O C02H--0 Cl Al-230 thiabendazole N O O CO2H - - 0 {N (Et) 3} +Cl- Al-231 thiabendazole N O O CO2H O O 1 CF3CH2 Al-232 thiabendazole N O O CO2H O O 1 cyclopropyl Al-233 thiabendazole N O O CO2H O O 1 2-OMe-Ph Al-234 thiabendazole N O O CO2H O O 1 MeSCH2 Al-235 thiabendazole N O O CO2H O O 1 MeOCH2 A1-236 thiabendazole N 0 O C02H S S 1 Ph Al-237 thiabendazole N O O CO2H S S 1 NMe2 <BR> <BR> A1-238 thiabendazole N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> <BR> A1-239 thiabendazole N 0 O C02H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-240 thiabendazole N O O C02H O S 1 Me A1-241 tolazoline N O O CO2H O O 1 methyl A1-242 tolazoline N O O CO2H O O 1 C (CH3) 3 A1-243 tolazoline N O O CO2H O O 1 Ph A1-244 tolazoline N O O CO2H O O 1 4-Me-Ph A1-245 tolazoline N O O COH O O 1 2-pyridyl A1-246 tolazoline N O 0 COH O O 1 4-pyridyl A1-247 tolazoline N O O CO2H O O 1 2-furyl A1-248 tolazoline N O O CO2H O O 1 2-thienyl A1-249 tolazoline N O O CO2H--0 Cl A1-250 tolazoline N O O C02H--0 {N (Et) s} +Cl- A1-251 tolazoline N O O CO2H O O 1 CF3CH2 A1-252 tolazoline N O O CO2H O O 1 cyclopropyl A1-253 tolazoline N O O CO2H O O 1 2-OMe-Ph A1-254 tolazoline N O O CO2H O O 1 MeSCH2 A1-255 tolazoline N O O CO2H O O 1 MeOCH2 A1-256 tolazoline N O O CO2H S S 1 Ph A1-257 tolazoline N O O CO2H S S 1 NMe2 A1-258 tolazoline N O O CO2H S S 1 NBn2 A1-259 tolazoline N O O CO2H O S 1 Ph A1-260 tolazoline N O O CO2H O S 1 Me A1-261 proparacaine N O O CO2H O O 1 methyl A1-262 proparacaine N O O CO2H O O 1 C (CH3) 3 A1-263 proparacaine N O O CO2H O O 1 Ph A1-264 proparacaine N O O CO2H O O 1 4-Me-Ph A1-265 proparacaine N O O CO2H O O 1 2-pyridyl A1-266 proparacaine N O O CO2H O O 1 4-pyridyl A1-267 proparacaine N O O CO2H O O 1 2-furyl A1-268 proparacaine N O O CO2H O O 1 2-thienyl A1-269 proparacaine N O O CO2H--0 Cl A1-270 proparacaine N O O C02H.. + 0 {N (Et) s} Cl A1-271 proparacaine N O O CO2H O O 1 CF3CH2 Al-272 proparacaine N O O CO2H O O 1 cyclopropyl Al-273 proparacaine N O O CO2H O O 1 2-OMe-Ph A1-274 proparacaine N O O CO2H O O 1 MeSCH2 A1-275 proparacaine N O O CO2H O O 1 MeOCH2 A1-276 proparacaine N O O CO2H S S 1 Ph A1-277 proparacaine N O O CO2H S S 1 NMe2 A1-278 proparacaine N O O CO2H S S 1 NBn2 A1-279 proparacaine N O O C02H O S 1 Ph A1-280 proparacaine N O O C02H O S 1 Me A1-281 tocainide N O O CO2H O O 1 methyl A1 282 tocainide N O O C02H O O 1 C (CH3) 3 A1-283 tocainide N O O C02H O O 1 Ph A1-284 tocainide N O O C02H O O 1 4-Me-Ph A1-285 tocainide N O O C02H O O 1 2-pyridyl Al-286tocainideNOOCOzH0014-pyridyl Al-287tocainideNOOCOzH0012-furyl A1-288 tocainide N O O CO2H O O 1 2-thienyl A1-289 tocainide N O O COzH--0 Cl Al-290 tocainide N O O CO2H A1-291 tocainide N O O CO2H O O 1 CF3CH2 A1-292 tocainide N O O CO2H O O 1 cyclopropyl Al-293 tocainide N O O CO2H O O 1 2-OMe-Ph A1-294 tocainide N O O CO2H O O 1 MeSCH2<BR> <BR> <BR> <BR> A1-295 tocainide N O O CO2H O O 1 MeOCH2 Al-296 tocainide N O O CO2H S S 1 Ph <BR> <BR> A1-297 tocainide N O O C02H S S 1 NMe2 Al-298 tocainide N O O CO2H S S 1 NBn2 A1-299 tocainide N O O CO2H O S 1 Ph Al-300 tocainide N O O CO2H O S 1 Me <BR> <BR> A1-301 triamterene N O O CO2H O O 1 methyl Al-302 triamterene N O O CO2H O O 1 C(CH3)3 <BR> <BR> A1-303 triamterene N O O CO2H O O 1 Ph<BR> <BR> <BR> <BR> <BR> A1-304 triamterene N O O CO2H O O 1 4-Me-Ph<BR> <BR> <BR> <BR> <BR> A1-305 triamterene N O O CO2H O O 1 2-pyridyl Al-306 triamterene N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-307 triamterene N O O CO2H O O 1 2-furyl Al-308 triamterene N O O CO2H O O 1 2-thienyl A1-309 triamterene N O O CO2H--0 Cl A1-310 triamterene N O O C02H--0 {N (Et) 3} +Cl- Al-311 triamterene N O O CO2H O O 1 CF3CH2 <BR> <BR> A1-312 triamterene N 0 O C02H O 0 1 cyclopropyl<BR> <BR> <BR> <BR> <BR> A1-313 triamterene N 0 O COzH O 0 1 2-OMe-Ph Al-314 triamterene N O O CO2H O O 1 MeSCH2 Al-315 triamterene N O O CO2H O O 1 MeOCH2 A1-316 triamterene N O O CO2H S S. 1 Ph <BR> <BR> A1-317 triamterene N O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> <BR> A1-318 triamterene N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-319 triamterene N O O CO2H O S 1 Ph A1-320 triamterene N 0 O C02H O S 1 Me Al-321 hydroxyitraconazole O O O CO2H O O 1 methyl Al-322 hydroxyitraconazole O O O CO2H O O 1 C(CH3)3 Al-323 hydroxyitraconazole O O O CO2H O O 1 Ph Al-324 hydroxyitraconazole O O O CO2H O O 1 4-Me-Ph Al-325 hydroxyitraconazole O O O CO2H O O 1 2-pyridyl Al-326 hydroxyitraconazole O O O CO2H O O 1 4-pyridyl Al-327 hydroxyitraconazole O O O CO2H O O 1 2-furyl A1-328 hydroxyitraconazole O O O CO2H O O 1 2-thienyl Al-329 hydroxyitraconazole O O O CO2H - - 0 Cl A1-330 hydroxyitraconazole O 0 O C02H--0 {N (Et) 3} +Cl- Al-331 hydroxyitraconazole O O O CO2H O O 1 CF3CH2 Al-332 hydroxyitraconazole O O O CO2H O O 1 cyclopropyl Al-333 hydroxyitraconazole O O O CO2H O O 1 2-OMe-Ph Al-334 hydroxyitraconazole O O O CO2H O O 1 MeSCH2 Al-335 hydroxyitraconazole O O O CO2H O O 1 MeOCH2 Al-336hydroxyitraconazole000C02HS S 1Ph Al-337 hydroxyitraconazole O O O CO2H S S 1 NMe2 <BR> <BR> Al-338 hydroxyitraconazole 0 0 O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-339 hydroxyitraconazole 0 O O C02H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-340 hydroxyitraconazole 0 O O CO2H O S 1 Me<BR> <BR> <BR> <BR> A1-341 posaconazole O O O CO2H O O 1 methyl Al-342 posaconazole O O O CO2H O O 1 C(CH3)3 Al-343 posaconazole O O O CO2H O O 1 Ph <BR> <BR> A1-344 posaconazole 0 O O CO2H O O 1 4-Me-Ph Al-345 posaconazole O O O CO2H O O 1 2-pyridyl A1-346 posaconazole 0 0 0 COzH O O 1 4-pyridyl A1-347 posaconazole O O O CO2H O O 1 2-furyl A1-348 posaconazole O O O CO2H O O 1 2-thienyl A1-349 posaconazole 0 0 0 COzH--0 Cl A1-350 posaconazole O O O CO2H--0 tN (Et) 3} +Cl- A1-351 posaconazole O O O CO2H O O 1 CF3CH2 A1-352 posaconazole O O O CO2H O O 1 cyclopropyl A1-353 posaconazole O O O CO2H O O 1 2-OMe-Ph A1-364 posaconazole O O O CO2H O O 1 MeSCH2 A1-355 posaconazole O O O C02H O O 1 MeOCH2 A1-356 posaconazole O O O CO2H S S 1 Ph A1-357 posaconazole O O O CO2H S S 1 NMe2 A1-358 posaconazole O O O CO2H S S 1 NBn2 A1-359 posaconazole O O O CO2H O S 1 Ph A1-360 posaconazole O O O C02H O S 1 Me A1-361 voriconazole O O O CO2H O O 1 methyl A1-362 voriconazole O O O CO2H O O 1 C (CH3) 3 Al-363 voriconazole O O O CO2H O O 1 Ph A1-364 voriconazole O O O CO2H O O 1 4-Me-Ph A1-365 voriconazole O O O CO2H O O 1 2-pyridyl A1-366 voriconazole O O O CO2H O O 1 4-pyridyl A1-367 voriconazole O O O COzH 0 O 1 2-furyl A1-368 voriconazole O O 0 CO2H 0 O 1 2-thienyl A1-369 voriconazole O O O CO2H--0 Cl A1-370 voriconazole O O O CO2H--0 {N (Et) 3} +Cl- A1-371 voriconazole O O O CO2H O O 1 CF3CH2 A1-372 voriconazole O O O CO2H O O 1 cyclopropyl Al-373voriconazole000C02H0012-OMe-Ph Al-374voriconazole0 0 0COzH0 0 1MeSCH2 A1-375 voriconazole O O O CO2H O O 1 MeOCH2 A1-376 voriconazole O O O CO2H S S 1 Ph A1-377 voriconazole O 0 O C02H S S 1 NMe2 A1-378 voriconazole O O O CO2H S S 1 NBn2 A1-379 voriconazole O O O CO2H O S 1 Ph A1-380 voriconazole O O O CO2H O S 1 Me Al-381genaconazole000C02H001methyl A1-382 genaconazole O O O CO2H O O 1 C (CH3) 3 A1-383 genaconazole O O O CO2H O O 1 Ph A1-384 genaconazole O 0 0 COaH O O 1 4-Me-Ph A1-385 genaconazole O O O CO2H O O 1 2-pyridyl A1-386 genaconazole O O O CO2H O O 1 4-pyridyl A1-387 genaconazole O O O CO2H O O 1 2-furyl A1-388 genaconazole O O O CO2H O O 1 2-thienyl A1-389 genaconazole O O O CO2H--0 Cl A1-390 genaconazole O O O CO2H--0 {N (Et) s} +Cl- A1-391 genaconazole O O O CO2H O O 1 CF3CH2 A1-392 genaconazole O O O CO2H O O 1 cyclopropyl A1-393 genaconazole O O O CO2H O O 1 2-OMe-Ph A1-394 genaconazole O O O CO2H O O 1 MeSCH2 A1-395 genaconazole O O O CO2H O O 1 MeOCH2 A1-396 genaconazole O O O CO2H S S 1 Ph A1-397 genaconazole O O O CO2H S S 1 NMe2 Al-398 genaconazole O O O CO2H S S 1 NBn2 Al-399 genaconazole O O O CO2H O S 1 Ph Al-400 genaconazole O O O CO2H O S 1 Me Al-401 fluconazole O O O CO2H O O 1 methyl Al-402 fluconazole O O O CO2H O O 1 C(CH3)3 <BR> <BR> A1-403 fluconazole O O O CO2H O O 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-404 fluconazole O O O CO2H O O 1 4-Me-Ph Al-405 fluconazole O O O CO2H O O 1 2-pyridyl A1-406 fluconazole O O O CO2H O O 1 4-pyridyl Al-407 fluconazole O O O CO2H O O 1 2-furyl Al-408 fluconazole O O O CO2H O O 1 2-thienyl A1-409 fluconazole O O O CO2H--0 Cl A1-410 fluconazole 0 O O COzH--0 {N (Et) 3}+Cl# Al-411 fluconazole O O O CO2H O O 1 CF3CH2 Al-412 fluconazole O O O CO2H O O 1 cyclopropyl Al-413 fluconazole O O O CO2H O O 1 2-OMe-Ph Al-414 fluconazole O O O CO2H O O 1 MeSCH2 Al-415 fluconazole O O O CO2H O O 1 MeOCH2 <BR> <BR> <BR> A1-416 fluconazole O O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> Al-417 fluconazole O O 0 CO2H S S 1 NMe2<BR> <BR> <BR> <BR> <BR> <BR> A1-418 fluconazole O 0 O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> <BR> A1-419 fluconazole O 0 O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-420 fluconazole O O 0 C02H O S 1 Me<BR> <BR> <BR> <BR> <BR> <BR> A1-421 metronidazole O O O CO2H O O 1 methyl Al-422 metronidazole O O O CO2H O O 1 C(CH3)3 Al-423 metronidazole O O O CO2H O O 1 Ph <BR> <BR> <BR> A1-424 metronidazole O O O CO2H O O 1 4-Me-Ph<BR> <BR> <BR> <BR> <BR> <BR> <BR> Al-425metronidazole000C02H0 0 12-pyridyl<BR> <BR> <BR> <BR> <BR> Al-426metronidazole000COzH0014-pyridyl Al-427 metronidazole O O O CO2H O O 1 2-furyl Al-428 metronidazole O O O CO2H O O 1 2-thienyl A1-429 metronidazole O 0 O C02H--0 Cl Al-430metronidazole000C02H--0 {N (Et) 3} +Cl- Al-431 metronidazole O O O CO2H O O 1 CF3CH2 Al-432 metronidazole O O O CO2H O O 1 cyclopropyl <BR> <BR> A1-433 metronidazole O O O C02H O O 1 2-OMe-Ph Al-434 metronidazole O O O CO2H O O 1 MeSCH2 Al-435 metronidazole O O O CO2H O O 1 MeOCH2 A1-436 metronidazole 0 O 0 C02H S S 1 Ph Al-437 metronidazole O O O CO2H S S 1 NMe2 <BR> <BR> <BR> A1-438 metronidazole O O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-439 metronidazole O 0 O C02H O S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-440 metronidazole 0 O 0 COzH O S 1 Me Al-441 temazepam O O O CO2H O O 1 methyl Al-442 temazepam O O O CO2H O O 1 C(CH3)3 Al-443 temazepam O O O CO2H O O 1 Ph Al-444 temazepam O O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-445 temazepam O O O C02H O O 1 2-pyridyl<BR> <BR> <BR> <BR> <BR> <BR> Al-446temazepam000C02H0014-pyridyl Al-447 temazepam O O O CO2H O O 1 2-furyl Al-448 temazepam O O O CO2H O O 1 2-thienyl Al-449 temazepam O O O CO2H--0 Cl Al-450 temazepam O O O CO2H - - 0 {N (Et) 3} +Cl- Al-451 temazepam O O O CO2H O O 1 CF3CH2 Al-452 temazepam O O O CO2H O O 1 cyclopropyl Al-453 temazepam O O O CO2H O O 1 2-OMe-Ph Al-454 temazepam O O O CO2H O O 1 MeSCH2 <BR> <BR> A1-455 temazepam O O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> <BR> <BR> A1-456 temazepam O O O CO2H S S 1 Ph Al-457 temazepam O O O CO2H S S 1 NMe2 Al-458 temazepam O O O CO2H S S 1 NBn2 Al-459 temazepam O O O CO2H O S 1 Ph <BR> <BR> A1-460 temazepam O O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> A1-461 buprenorphine O O O CO2H O O 1 methyl Al-462 buprenorphine O O O CO2H O O 1 C(CH3)3 A1-463 buprenorphine O O O CO2H O O 1 Ph Al-464 buprenorphine O O O CO2H O O 1 4-Me-Ph Al-465 buprenorphine O O O CO2H O O 1 2-pyridyl Al-466 buprenorphine O O O CO2H O O 1 4-pyridyl <BR> <BR> A1-467 buprenorphine O O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> <BR> A1-468 buprenorphine O O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> A1-469 buprenorphine O O O CO2H--0 Cl Al-470buprenorphine000C02H-,-0 {N (Et) 3} +Cl- Al-471 buprenorphine O O O CO2H O O 1 CF3CH2 Al-472 buprenorphine O O O CO2H O O 1 cyclopropyl <BR> <BR> A1-473 buprenorphine O O O C02H O 0 1 2-OMe-Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-474 buprenorphine O O O C02H O O 1 MeSCH2<BR> <BR> <BR> <BR> <BR> A1-475 buprenorphine O O O CO2H O O 1 MeOCH2 Al-476 buprenorphine O O O CO2H S S 1 Ph Al-477 buprenorphine O O O CO2H S S 1 NMe2 Al-478 buprenorphine O O O CO2H S S 1 NBn2 <BR> <BR> A1-479 buprenorphine O O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-480 buprenorphine O O O CO2H O S 1 Me Al-481 cafiminol O O O CO2H O O 1 methyl Al-482 cafiminol O O O CO2H O O 1 C(CH3)3 A1-483 cafiminol O O O CO2H O O 1 Ph Al-484 cafiminol O O O CO2H O O 1 4-Me-Ph Al-485 cafiminol O O O CO2H O O 1 2-pyridyl Al-486 cafiminol O O O CO2H O O 1 4-pyridyl <BR> <BR> A1-487 cafiminol O O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> <BR> <BR> A1-488 cafiminol O O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> A1-489 cafiminol O O O CO2H--0 Cl A1-490cafiminol000C02H--0 {N (Et) 3} +Cl- Al-491 cafiminol O O O CO2H O O 1 CF3CH2 Al-492 cafiminol O O O CO2H O O 1 cyclopropyl <BR> <BR> A1-493 cafiminol O O O CO2H O O 1 2-OMe-Ph Al-494 cafiminol O O O CO2H O O 1 MeSCH2 Al-495 cafiminol O O O CO2H O O 1 MeOCH2 Al-496 cafiminol O O O CO2H S S 1 Ph Al-497 cafiminol O O O CO2H S S 1 NMe2 Al-498 cafiminol O O O CO2H S S 1 NBn2 <BR> <BR> A1-499 cafiminol O O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-500 cafiminol O O O CO2H O S 1 Me Al-501 pentazocine O O O CO2H O O 1 methyl Al-502 pentazocine O O O CO2H O O 1 C(CH3)3 Al-503 pentazocine O O O CO2H O O 1 Ph Al-504 pentazocine O O O CO2H O O 1 4-Me-Ph A1-505 pentazocine O O O CO2H O O 1 2-pyridyl Al-506 pentazocine O O O CO2H O O 1 4-pyridyl A1-507 pentazocine O O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> A1-508 pentazocine O O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> A1-509 pentazocine O O O C02H--0 Cl Al-510 pentazocine O O O CO2H - - 0 {N (Et) 3} +Cl- <BR> <BR> A1-511 pentazocine O O O CO2H O O 1 CF3CH2 Al-512 pentazocine O O O CO2H O O 1 cyclopropyl Al-513 pentazocine O O O CO2H O O 1 2-OMe-Ph Al-514 pentazocine O O O CO2H O O 1 MeSCH2 Al-515 pentazocine O O O CO2H O O 1 MeOCH2 <BR> <BR> A1-516 pentazocine O O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-517 pentazocine O O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> A1-518 pentazocine O O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> Al-519 pentazocine O O O C02H O S 1 Ph Al-520 pentazocine O O O CO2H O S 1 Me Al-521 scopolamine O O O CO2H O O 1 methyl Al-522 scopolamine O O O CO2H O O 1 C(CH3)3 Al-523 scopolamine O O O CO2H O O 1 Ph Al-524 scopolamine O O O CO2H O O 1 4-Me-Ph Al-525 scopolamine O O O CO2H O O 1 2-pyridyl Al-526 scopolamine O O O CO2H O O 1 4-pyridyl <BR> <BR> A1-527 scopolamine O 0 O CO2H 0 O 1 2-furyl Al-528 scopolamine O O O CO2H O O 1 2-thienyl Al-529 scopolamine O O O CO2H - - 0 Cl Al-530scopolamine000C02H--0 {N (Et) 3} +Cl- Al-531 scopolamine O O O CO2H O O 1 CF3CH2 <BR> <BR> A1-532 scopolamine O 0 O C02H 0 O 1 cyclopropyl<BR> <BR> <BR> <BR> A1-533 scopolamine O O O CO2H O O 1 2-OMe-Ph Al-534 scopolamine O O O CO2H O O 1 MeSCH2 <BR> <BR> A1-535 scopolamine O O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> A1-536 scopolamine O O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-537 scopolamine O O O C02H S S 1 NMe2<BR> <BR> <BR> <BR> A1-538 scopolamine O O O C02H S S 1 NBn2 Al-539 scopolamine O O O CO2H O S 1 Ph A1-540 scopolamine 0 0 O C02H O S 1 Me Al-541 tramadol O O O CO2H O O 1 methyl Al-542 tramadol O O O CO2H O O 1 C(CH3)3 Al-543 tramadol O O O CO2H O O 1 Ph <BR> <BR> A1-544 tramadol O O O C02H O O 1 4-Me-Ph Al-545 tramadol O O O CO2H O O 1 2-pyridyl Al-546 tramadol O O O CO2H O O 1 4-pyridyl Al-547 tramadol O O O CO2H O O 1 2-furyl Al-548 tramadol O O O CO2H O O 1 2-thienyl A1-549 tramadol O O O CO2H--O Cl Al-550tramadol0 0 0C02H--0 {N (Et) 3}+Cl- Al-551 tramadol O O O CO2H O O 1 CF3CH2 <BR> <BR> Al-552tramadol000C02H0 0 1cyclopropyi<BR> <BR> <BR> <BR> A1-553 tramadol O O O C02H O O 1 2-OMe-Ph Al-554 tramadol O O O CO2H O O 1 MeSCH2 Al-555 tramadol O O O CO2H O O 1 MeOCH2 Al-556 tramadol O O O CO2H S S 1 Ph Al-557 tramadol O O O CO2H S S 1 NMe2 <BR> <BR> A1-558 tramadol O O O CO2H S S 1 NBn2 Al-559 tramadol O O O CO2H O S 1 Ph Al-560 tramadol O O O CO2H O S 1 Me <BR> <BR> Al-561quinidine000C02H0 0 1methyl<BR> <BR> <BR> <BR> Al-562quinidine000C02H0 0 1C (CHs) 3 Al-563 quinidine O O O CO2H O O 1 Ph <BR> <BR> Al-564quinidine000C02H0 0 14-Me-Ph Al-565 quinidine O O O CO2H O O 1 2-pyridyl Al-566 quinidine O O O CO2H O O 1 4-pyridyl Al-567 quinidine O O O CO2H O O 1 2-furyl Al-568 quinidine O O O CO2H O O 1 2-thienyl Al-569 quinidine O O O CO2H - - 0 Cl A1-570 quinidine O O O CO2H--O {N (Et) 3} +Cl- Al-571 quinidine O O O CO2H O O 1 CF3CH2 Al-572 quinidine O O O CO2H O O 1 cyclopropyl <BR> <BR> A1-573 quinidine O O O CO2H O O 1 2-OMe-Ph Al-574 quinidine O O O CO2H O O 1 MeSCH2 <BR> <BR> A1-575 quinidine O O O CO2H O O 1 MeOCH2 Al-576 quinidine O O O CO2H S S 1 Ph <BR> <BR> A1-577 quinidine O O O CO2H S S 1 NMe2 A1-578 quinidine O O O CO2H S S 1 NBn2 Al-579 quinidine O O O CO2H O S 1 Ph <BR> <BR> A1-580 quinidine O O O CO2H O S 1 Me<BR> <BR> <BR> <BR> A1-581 methimazole S-O O CO2H O O 1 methyl Al-582 methimazole S O O CO2H O O 1 C(CH3)3 A1-583 methimazole S O O CO2H O O 1 Ph Al-584 methimazole S O O CO2H O O 1 4-Me-Ph Al-585 methimazole S O O CO2H O O 1 2-pyridyl Al-586 methimazole S O O CO2H O O 1 4-pyridyl Al-587 methimazole S O O CO2H O O 1 2-furyl <BR> <BR> A1-588 methimazole S O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> A1-589 methimazole S O O CO2H--O Cl A1-590 methimazole S O O CO2H--0 {N (Et) 3}+Cl- Al-591 methimazole S O O CO2H O O 1 CF3CH2 Al-592 methimazole S O O CO2H O O 1 cyclopropyl Al-593 methimazole S O O CO2H O O 1 2-OMe-Ph <BR> <BR> A1-594 methimazole S O O CO2H O O 1 MeSCH2 Al-595 methimazole S O O CO2H O O 1 MeOCH2 Al-596methimazoleS00C02HS S 1Ph <BR> <BR> A1-597 methimazole S O O CO2H S S 1 NMe2 Al-598 methimazole S O O CO2H S S 1 NBn2 Al-599 methimazole S O O CO2H O S 1 Ph <BR> <BR> <BR> A1-600 methimazole S O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> <BR> A1-601 haloperidol O O O CO2H O O 1 methyl Al-602 haloperidol O O O CO2H O O 1 C(CH3)3 A1-603 haloperidol O O O CO2H O O 1 Ph Al-604 haloperidol O O O CO2H O O 1 4-Me-Ph Al-605 haloperidol O O O CO2H O O 1 2-pyridyl Al-606 haloperidol O O O CO2H O O 1 4-pyridyl Al-607 haloperidol O O O CO2H O O 1 2-furyl A1-608 haloperidol O O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> A1-609 haloperidol O O O COzH--0 Cl Al-610 haloperidol O O O CO2H - - 0 {N (Et) 3}+Cl- Al-611 haloperidol O O O CO2H O O 1 -CF3CH2 Al-612 haloperidol O O O CO2H O O 1 cyclopropyl A1-613 haloperidol O O O CO2H O O 1 2-OMe-Ph Al-614 haloperidol O O O CO2H O O 1 MeSCH2 Al-615 haloperidol O O O CO2H O O 1 MeOCH2 Al-616 haloperidol O O O CO2H S S 1 Ph A1-617 haloperidol O O O CO2H S S 1 NMe2 Al-618 haloperidol O O O CO2H S S 1 NBn2 <BR> <BR> A1-619 haloperidol O O O C02H O S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-620 haloperidol O O O CO2H O S 1 Me Al-621 hydroxyzine O O O CO2H O O 1 methyl Al-622 hydroxyzine O O O CO2H O O 1 C(CH3)3 Al-623 hydroxyzine O O O CO2H O O 1 Ph <BR> <BR> A1-624 hydroxyzine O O O CO2H O O 1 4-Me-Ph Al-625 hydroxyzine O O O CO2H O O 1 2-pyridyl Al-626 hydroxyzine O O O CO2H O O 1 4-pyridyl A1-627 hydroxyzine O O O CO2H O O 1 2-furyl Al-628 hydroxyzine O O O CO2H O O 1 2-thienyl A1-629 hydroxyzine O O O CO2H--0 Cl Al-630hydroxyzine000C02H--0 {N (Et) 3} +Cl- Al-631 hydroxyzine O O O CO2H O O 1 CF3CH2 Al-632 hydroxyzine O O O CO2H O O 1 cyclopropyl Al-633 hydroxyzine O O O CO2H O O 1 2-OMe-Ph Al-634 hydroxyzine O O O CO2H O O 1 MeSCH2 Al-635 hydroxyzine O O O CO2H O O 1 MeOCH2 <BR> A1-636 hydroxyzine O O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-637 hydroxyzine O O O CO2H S S 1 NMe2 Al-638 hydroxyzine O O O CO2H S S 1 NBn2 <BR> <BR> A1-639 hydroxyzine O O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-640 hydroxyzine O O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> <BR> A1-641 lorazepam O O O CO2H O O 1 methyl Al-642 lorazepam O O O CO2H O O 1 C(CH3)3 Al-643 lorazepam O O O CO2H O O 1 Ph <BR> <BR> A1-644 lorazepam O O O C02H O O 1 4-Me-Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-645 lorazepam O O O CO2H O O 1 2-pyridyl<BR> <BR> <BR> <BR> <BR> <BR> Al-646lorazepam0 0 0C02H0 0 14-pyridyl<BR> <BR> <BR> <BR> <BR> <BR> A1-647 lorazepam O O O C02H O O 1 2-furyl Al-648 lorazepam O O O CO2H O O 1 2-thienyl Al-649 lorazepam O O O CO2H - - 0 Cl Al-650 lorazepam O O O CO2H - - 0 {N (Et) 3} +Cl- Al-651 lorazepam O O O CO2H O O 1 CF3CH2 Al-652 lorazepam O O O CO2H O O 1 cyclopropyl Al-653 lorazepam O O O CO2H O O 1 2-OMe-Ph Al-654 lorazepam O O O CO2H O O 1 MeSCH2 Al-655 lorazepam O O O CO2H O O 1 MeOCH2 <BR> <BR> A1-656 lorazepam O O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-657 lorazepam O O O CO2H S S 1 NMe2 A1-658 lorazepam O O O CO2H S S 1 NBn2 Al-659lorazepam000COzH0S1Ph A1-660 lorazepam O O O CO2H O S 1 Me A1-661 iodoquinol O O O CO2H O O 1 methyl A1-662 iodoquinol O O O CO2H O O 1 C (CH3) 3 A1-663 iodoquinol O O 0 COH O O 1 ph A1-664 iodoquinol O O O CO2H O O 1 4-Me-Ph A1-665 iodoquinol O O O CO2H O O 1 2-pyridyl A1-666 iodoquinol O O O CO2H O O 1 4-pyridyl A1-667 iodoquinol O O O CO2H O O 1 2-furyl A1-668 iodoquinol O O O CO2H O O 1 2-thienyl A1-669 iodoquinol 0 O O CO2H--0 Cl A1-670 iodoquinol O O O CO2H--O {N (Et) 3} +Cl- Al-671iodoquinol000COsH001CFgCH2 A1-672 iodoquinol O O O CO2H O O 1 cyclopropyl A1-673 iodoquinol O O O CO2H O O 1 2-OMe-Ph Al-674 iodoquinol 0 0 0 C02H 0 01MeSCH2 Al-675iodoquinol000C02H001MeOCHs A1-676 iodoquinol 0 O O COzH S S 1 ph Al-677iodoquinol000C02HSSINMe2 A1-678 iodoquinol 0 O O C02H S S 1 NBn2 Al-679iodoquinolOOOCOzHOS1Ph A1-680 iodoquinol 0 O O COzH O S 1 Me A1-681 perphenazine 0 O O CO2H O O 1 methyl A1-682 perphenazine 0 0 O C02H O O 1 C (CHs) s A1-683 perphenazine O O O CO2H O O 1 Ph A1-684 perphenazine O O O CO2H O O 1 4-Me Ph A1-685 perphenazine O O O CO2H O O 1 2-pyrìdyl A1-686 perphenazine 0 O O COH O O 1 4-pyridyl A1-687 perphenazine O O O CO2H O O 1 2-furyl A1-688 perphenazine 0 0 O C02H O O 1 2-thienyl A1-689 perphenazine 0 O O C02H--0 Cl A1-690 perphenazine O O O CO2H-. 0 fN (Et) s} +Cl- A1-691 perphenazine 0 O O COzH O O I CFsCHz Al-692 perphenazine 0 O O CO2H O O 1 cyclopropyl A1-693 perphenazine 0 O O COzH O O 1 2-OMe-Ph A1-694 perphenazine O O O CO2H O O 1 MeSCH2 A1-695 perphenazine O O O CO2H O O 1 MeOCH2 A1-696 perphenazine 0 O O COaH S S 1 Ph A1-697 perphenazine O O O CO2H S S 1 NMe2 Al-698perphenazine000C02HSS1NBn2 Al-699perphenazine000COsHOS1Ph A1-700 perphenazine 0 O O C02H O S 1 Me A1-701 mazindol O O O CO2H O O 1 methyl A1-702 mazindol 0 O O COzH O O 1 C (CHs) s Al-703mazindolO00C02H001Ph Al-704mazindol000C02H0014-Me-Ph A1-705 mazindol 0 O O C02H O O 1 2-pyridyl A1-706 mazindol. 0 O O COH O O 1 4-pyridyl A1-707 mazindol O O O C02H O O 1 2-furyl A1-708 mazindol O O O CO2H O O 1 2-thienyl Al-709mazindol000COzH--0C1 Al-710 mazindol O O O CO2H - - 0 {N (Et) 3} +Cl- Al-711 mazindol O O O CO2H O O 1 CF3CH2 Al-712 mazindol O O O CO2H O O 1 cyclopropyl Al-713 mazindol O O O CO2H O O 1 2-OMe-Ph Al-714 mazindol O O O CO2H O O 1 MeSCH2 Al-715 mazindol O O O CO2H O O 1 MeOCH2 Al-716 mazindol O O O CO2H S S 1 Ph Al-717 mazindol O O O CO2H S S 1 NMe2 Al-718 mazindol O O O CO2H S S 1 NBn2 A1-719 mazindol O O O CO2H O S 1 Ph Al-720 mazindol O O O CO2H O S 1 Me <BR> <BR> <BR> A1-721 astemizole N O O CO2H O O 1 methyl<BR> <BR> <BR> <BR> A1-722 astemizole N O O CO2H O O 1 C (CH3) 3 Al-723 astemizole N O O CO2H O O 1 Ph Al-724 astemizole N O O CO2H O O 1 4-Me-Ph Al-725 astemizole N O O CO2H O O 1 2-pyridyl Al-726 astemizole N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-727 astemizole N O O CO2H O O 1 2-furyl Al-728 astemizole N O O CO2H O O 1 2-thienyl A1-729 astemizole N O O C02H--0 Cl Al-730 astemizole N O O CO2H - - 0 {N (Et) 3}+Cl- Al-731 astemizole N O O CO2H O O 1 CF3CH2 Al-732 astemizole N O O CO2H O O 1 cyclopropyl <BR> <BR> A1-733 astemizole N O O CO2H O O 1 2-OMe-Ph Al-734 astemizole N O O CO2H O O 1 MeSCH2 Al-735 astemizole N O O CO2H O O 1 MeOCH2 Al-736 astemizole N O O CO2H S S 1 Ph Al-737 astemizole N O O CO2H S S 1 NM2 Al-738 astemizole N O O CO2H S S 1 NBn2 Al-739 astemizole N O O CO2H O S 1 Ph A1-740 astemizole N O O CO2H O S 1 Me Al-741 amoxapine N O O CO2H O O 1 methyl Al-742 amoxapine N O O CO2H O O 1 C(CH3)3 A1-743 amoxapine N O O CO2H O O 1 Ph Al-744 amoxapine N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-745 amoxapine N O O CO2H O O 1 2-pyridyl Al-746 amoxapine N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-747 amoxapine N O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> <BR> A1-748 amoxapine N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> Al-749 amoxapine N 0 O C02H--0 Cl A1-750 amoxapine N O O CO2H--O {N (Et) 3} +Cl- <BR> <BR> A1-751 amoxapine N O O CO2H O O 1 CF3CH2<BR> <BR> <BR> <BR> <BR> Al-752amoxapineNOOCOzH001cyclopropyi<BR> <BR> <BR> <BR> <BR> A1-753 amoxapine N O O C02H O O 1 2-OMe-Ph<BR> <BR> <BR> <BR> <BR> A1-754 amoxapine N O O CO2H O O 1 MeSCH2<BR> <BR> <BR> <BR> <BR> A1-755 amoxapine N 0 O CO2H O 0 1 MeOCH2 Al-756 amoxapine N O O CO2H S S 1 Ph Al-757 amoxapine N O O CO2H S S 1 NMe2 Al-758 amoxapine N O O CO2H S S 1 NBn2 <BR> <BR> A1-759 amoxapine N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-760 amoxapine N O O CO2H O S 1 Me Al-761 ciprofloxacin N O O CO2H O O 1 methyl Al-762 ciprofloxacin N O O CO2H O O 1 C(CH3)3 Al-763 ciprofloxacin N O O CO2H O O 1 Ph Al-764 ciprofloxacin N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-765 ciprofloxacin N O O CO2H O O 1 2-pyridyl Al-766 ciprofloxacin N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-767 ciprofloxacin N O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> A1-768 ciprofloxacin N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> A1-769 ciprofloxacin N O O CO2H--O Cl Al-770 ciprofloxacin N O O CO2H - - 0 {N (Et) 3} +Cl- <BR> <BR> A1-771 ciprofloxacin N O O CO2H O O 1 CF3CH2<BR> <BR> <BR> <BR> <BR> A1-772 ciprofloxacin N O O CO2H O O 1 cyclopropyl Al-773 ciprofloxacin N O O CO2H O O 1 2-OMe-Ph <BR> <BR> A1-774 ciprofloxacin N O O CO2H O O 1 MeSCH2<BR> <BR> <BR> <BR> A1-775 ciprofloxacin N O O C02H O O 1 MeOCH2<BR> <BR> <BR> <BR> A1-776 ciprofloxacin N O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-777 ciprofloxacin N O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> A1-778 ciprofloxacin N O O CO2H S S 1 NBn2 Al-779 ciprofloxacin N O O CO2H O S 1 Ph A1-780 ciprofloxacin N O O CO2H O S 1 Me A1-781 chloroquine N O O CO2H O O 1 methyl Al-782 chloroquine N O O CO2H O O 1 C(CH3)3 <BR> <BR> A1-783 chloroquine N O O CO2H O 0 1 Ph<BR> <BR> <BR> <BR> <BR> A1-784 chloroquine N O O CO2H O O 1 4-Me-Ph Al-785 chloroquine N O O CO2H O O 1 2-pyridyl Al-786 chloroquine N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-787 chloroquine N O O CO2H O O 1 2-furyl Al-788 chlroquine N O O CO2H O O 1 2-thienyl A1-789 chloroquine N O O C02H--0 Cl A1-790 chloroquine N O O CO2H--O {N (Et) 3}+Cl- Al-791 chloroquine N O O CO2H O O 1 CF3CH2 Al-792 chloroquine N O O CO2H O O 1 cyclopropyl Al-793 chloroquine N O O CO2H O O 1 2-OMe-Ph Al-794 chloroquine N O O CO2H O O 1 MeSCH2 <BR> <BR> A1-795 chloroquine N O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> A1-796 chloroquine N O O C02H S S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-797 chloroquine N O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> A1-798 chloroquine N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-799 chloroquine N O O C02H O S 1 Ph<BR> <BR> <BR> <BR> A1-800 chloroquine N O O CO2H O S 1 Me Al-801 chlordiazepoxide N O O CO2H O O 1 methyl Al-802 chlordiazepoxide N O O CO2H O O 1 C(CH3)3 Al-803 chlordiazepoxide N O O CO2H O O 1 Ph Al-804 chlordiazepoxide N O O CO2H O O 1 4-Me-Ph Al-805 chlordiazepoxide N O O CO2H O O 1 2-pyridyl Al-806 chlordiazepoxide N O O CO2H O O 1 4-pyridyl Al-807 chlordiazepoxide N O O CO2H O O 1 2-furyl Al-808 chlordiazepoxide N O O CO2H O O 1 2-thienyl Al-809 chlordiazepoxide N O O CO2H - - 0 Cl Al-810 chlordiazepoxide N O O C02H--0 {N (Et) 3}+Cl- Al-811 chlordiazepoxide N O O CO2H O O 1 CF3CH2 Al-812 chlordiazepoxide N O O CO2H O O 1 cyclopropyl Al-813 chlordiazepoxide N O O CO2H O O 1 2-OMe-Ph A1-814 chlordiazepoxide N O O CO2H O O 1 MeSCH2<BR> <BR> <BR> <BR> <BR> A1-815 chlordiazepoxide N O O CO2H O O 1 MeOCH2 Al-816 chlordiazepoxide N O O CO2H S S 1 Ph Al-817 chlordiazepoxide N O O CO2H S S 1 NMe2 Al-818 chlordiazepoxide N O O CO2H S S 1 NBn2 <BR> <BR> A1-819 chlordiazepoxide N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-820 chlordiazepoxide N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> A1-821 clozapine N O O CO2H O O 1 methyl Al-822 clozapine N O O CO2H O O 1 C(CH3)3 A1-823 clozapine N O O CO2H O O 1 Ph Al-824 clozapine N O O CO2H O O 1 4-Me-Ph Al-825 clozapine N O O CO2H O O 1 2-pyridyl Al-826 clozapine N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-827 clozapine N O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> <BR> A1-828 clozapine N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> A1-829 clozapine N O O CO2H--O Cl A1-830 clozapine N O O CO2H--O {N (Et) 3} +Cl- <BR> <BR> A1-831 clozapine N O O C02H O 0 1 CFsCH2<BR> <BR> <BR> <BR> A1-832 clozapine N O O CO2H O O 1 cyclopropyl<BR> <BR> <BR> <BR> <BR> A1-833 clozapine N O O C02H O O 1 2-OMe-Ph Al-834 clozapine N O O CO2H O O 1 MeSCH2 Al-835 clozapine N O O CO2H O O 1 MeOCH2 Al-836 clozapine N O O CO2H S S 1 Ph Al-837 clozapine N O O CO2H S S 1 NMe2 Al-838 clozapine N O O CO2H S S 1 NBn2 <BR> <BR> A1-839 clozapine N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-840 clozapine N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> A1-841 desipramine N O O CO2H O O 1 methyl Al-842 desipramine N O O CO2H O O 1 C(CH3)3 Al-843 desipramine N O O CO2H O O 1 Ph Al-844 desipramine N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-845 desipramine N O O CO2H O O 1 2-pyridyl Al-846 desipramine N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-847 desipramine N O O CO2H O O 1 2-furyl Al-848 desipramine N O O CO2H O O 1 2-thienyl A1-849 desipramine N O O CO2H--O Cl A1-850 desipramine N O O C02H'--0 {N (Et) 3} +Cl- Al-851 desipramine N O O CO2H O O 1 CF3CH2 Al-852 desipramine N O O CO2H O O 1 cyclopropyl Al-853 desipramine N O O CO2H O O 1 2-OMe-Ph Al-854 desipramine N O O CO2H O O 1 MeSCH2 Al-855 desipramine N O O CO2H O O 1 MeOCH2 A1-856 desipramine N O O C02H S S 1 Ph Al-857 desipramine N O O CO2H S S 1 NMe2 Al-858 desipramine N O O CO2H S S 1 NBn2 Al-859 desipramine N O O CO2H O S 1 Ph A1-860 desipramine N O O CO2H O S 1 Me Al-861 enoxacin N O O CO2H O O 1 methyl Al-862 enoxacin N O O CO2H O O 1 C(CH3)3 Al-863 enoxacin N O O CO2H O O 1 Ph Al-864 enoxacin N O O CO2H O O 1 4-Me-ph Al-865 enoxacin N O O CO2H O O 1 2-pyridyl Al-866 enoxacin N O O CO2H O O 1 4-pyridyl Al-867 enoxacin N O O CO2H O O 1 2-furyl Al-868 enoxacin N O O CO2H O O 1 2-thienyl Al-869enoxacinN 0 0C02H--0Cl Al-870enoxacinN 0 0C02H--0 {N (Et) 3} +Cl- Al-871 enoxacin N O O CO2H O O 1 CF3CH2 Al-872 enoxacin N O O CO2H O O 1 cyclopropyl <BR> <BR> A1-873 enoxacin N O O CO2H O O 1 2-OMe-Ph Al-874 enoxacin N O O CO2H O O 1 MeSCH2 <BR> <BR> A1-875 enoxacin N O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> <BR> A1-876 enoxacin N O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> A1-877 enoxacin N O O CO2H S S 1 NMe2 A1-878 enoxacin N O 0 CO2H S S 1 NBn2 <BR> <BR> A1-879 enoxacin N O O C02H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-880 enoxacin N O O CO2H O S 1 Me Al-881 lomefloxacin N O O CO2H O O 1 methyl Al-882 lomefloxacin N O O CO2H O O 1 C(C3)3 Al-883 lomefloxacin N O O CO2H O O 1 Ph Al-884 lomefloxacin N O O CO2H O O 1 4-Me-Ph Al-885 lomefloxacin N O O CO2H O O 1 2-pyridyl Al-886 lomefloxacin N O O CO2H O O 1 4-pyridyl Al-887 lomefloxacin N O O CO2H O O 1 2-furyl Al-888 lomefloxacin N O O CO2H O O 1 2-thienyl A1-889 lomefloxacin N 0 O COzH--0 Cl A1-890 lomefloxacin N O O CO2H--O {N (Et) 3} +Cl- Al-891 lomefloxacin N O O CO2H O O 1 CF3CH2 Al-892 lomefloxacin N O O CO2H O O 1 cyclopropyl Al-893 lomefloxacin N O O CO2H O O 1 2-OMe-Ph <BR> <BR> A1-894 lomefloxacin N O O CO2H O O 1 MeSCH2 Al-895 lomefloxacin N O O CO2H O O 1 MeOCH2 A1-896 lomefloxacin N O O C02H S S 1 Ph Al-897 lomefloxacin N O O CO2H S S 1 NMe2 <BR> <BR> A1-898 lomefloxacin N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-899 lomefloxacin N O O C02H O S 1 Ph Al-900 lomefloxacin N O O CO2H O S 1 Me <BR> <BR> Al-901mepivacaineN 0 0C02H0 0 1methyl Al-902 mepivacaine N O O CO2H O O 1 C(CH3)3 A1-903 mepivacaine N O O CO2H O O 1 Ph Al-904 mepivacaine N O O CO2H O O 1 4-Me-Ph Al-905 mepivacaine N O O CO2H O O 1 2-pyridyl Al-906 mepivacaine N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-907 mepivacaine N O O C02H O O 1 2-furyl Al-908 mepivacaine N O O CO2H O O 1 2-thienyl Al-909mepivacaineN 0 0C02H--0Cl Al-910 mepivacaine N O O CO2H--O {N (Et) 3} +Cl- Al-911 mepivacaine N O O CO2H O O 1 CF3CH2 Al-912 mepivacaine N O O CO2H O O 1 cyclopropyl <BR> <BR> A1-913 mepivacaine N O O CO2H O O 1 2-OMe-Ph Al-914 mepivacaine N O O CO2H O O 1 MeSCH2 Al-915 mepivacaine N O O CO2H O O 1 MeOCH2 <BR> <BR> A1-916 mepivacaine N O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-917 mepivacaine N O O CO2H S S 1-NMe2 Al-918 mepivacaine N O O CO2H S S 1 NBn2 <BR> <BR> A1-919 mepivacaine N O. O CO2H O S 1 Ph<BR> <BR> <BR> <BR> A1-920 mepivacaine N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> A1-921 molindone N O O CO2H O O 1 methyl<BR> <BR> <BR> <BR> <BR> Al-922 molindone N O O COzH O 0 1 C (CH3) s Al-923 molindone N O O CO2H O O 1 Ph Al-924 molindone N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-925 molindone N O O CO2H O O 1 2-pyridyl Al-926 molindone N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-927 molindone N O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> <BR> A1-928 molindone N O O C02H 0 O 1 2-thienyl Al-929 molindone N O O CO2H - - 0 Cl A1-930 molindone N O O CO2H--O {N (Et) 3} +Cl- Al-931 molindone N O O CO2H O O 1 CF3CH2 <BR> <BR> A1-932 molindone N O O CO2H O O 1 cyclopropyl<BR> <BR> <BR> <BR> <BR> A1-933 molindone N O O C02H 0 O 1 2-OMe-Ph Al-934 molindone N O O CO2H O O 1 MeSCH2 Al-935 molindone N O O CO2H O O 1 MeOCH2 A1-936 molindone N O O C02H S S 1 Ph Al-937 molindone N O O CO2H S S 1 NMe2 Al-938 molindone N O O CO2H S S 1 NBn2 Al-939 molindone N O O CO2H O S 1 Ph <BR> <BR> <BR> A1-940 molindone N O O C02H O S 1 Me<BR> <BR> <BR> <BR> <BR> A1-941 naphazoline N O O CO2H O O 1 methyl Al-942 naphazoline N O O CO2H O O 1 C(CH3)3 A1-943 naphazoline N O O COzH 0 O 1 Ph Al-944 naphazoline N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-945 naphazoline N O O CO2H O O 1 2-pyridyl Al-946 naphazoline N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-947 naphazoline N O O CO2H O O 1 2-furyl Al-948 naphazoline N O O CO2H O O 1 2-thienyl A1-949 naphazoline N O O CO2H--O Cl A1-950 naphazoline N O O CO2H--O {N (Et) 3} +Cl- Al-951 naphazoline N O O CO2H O O 1 CF3CH2 Al-952 naphazoline N O O CO2H O O 1 cyclopropyl Al-953 naphazoline N O O CO2H O O 1 2-OMe-Ph Al-954 naphazoline N O O CO2H O O 1 MeSCH2 Al-955 naphazoline N O O CO2H O O 1 MeOCH2 A1-956 naphazoline N O O C02H S S 1 Ph Al-957 naphazoline N O O CO2H S S 1 NMe2 Al-958 naphazoline N O O CO2H S S 1 NBn2 <BR> <BR> A1-959 naphazoline N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> A1-960 naphazoline N O O C02H O S 1 Me Al-961 norfloxacin N O O CO2H O O 1 methyl Al-962 norfloxacin N O O CO2H O O 1 C(CH3)3 Al-963 norfloxacin N O O CO2H O O 1 Ph Al-964 norfloxacin N O O CO2H O O 1 4-Me-Ph Al-965 norfloxacin N O O CO2H O O 1 2-pyridyl Al-966 norfloxacin N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-967 norfloxacin N O O COzH O 0 1 2-furyl Al-968 norfloxacin N O O CO2H O O 1 2-thienyl A1-969 norfloxacin N O O CO2H--O Cl Al-970 norfloxacin N O O CO2H - - 0 {N (Et) 3} +Cl- <BR> <BR> A1-971 norfloxacin N O O CO2H O O 1 CF3CH2 Al-972 norfloxacin N O O CO2H O O 1 cyclopropyl Al-973 norfloxacin N O O CO2H O O 1 2-OMe-Ph Al-974 norfloxacin N O O CO2H O O 1 MeSCH2 Al-975 norfloxacin N O O CO2H O O 1 MeOCH2 Al-976 norfloxacin N O O CO2H S S 1 Ph Al-977 norfloxacin N O O CO2H S S 1 NMe2 Al-978 norfloxacin N O O CO2H S S 1 NBn2 <BR> <BR> A1-979 norfloxacin N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> A1-980 norfloxacin N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> A1-981 pimozide N O O CO2H O O 1 methyl<BR> <BR> <BR> <BR> A1-982 pimozide N O O CO2H O O 1 C (CH3) 3<BR> <BR> <BR> A1-983 pimozide N O O CO2H O O 1 Ph Al-984 pimozide N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-985 pimozide N O O CO2H O O 1 2-pyridyl Al-986 pimozide N O O CO2H O O 1 4-pyridyl Al-987 pimozide N O O CO2H O O 1 2-furyl Al-988 pimozide N O O CO2H O O 1 2-thienyl Al-989 pimozide N O O CO2H - - 0 Cl A1-990 pimozide N O O CO2H-0 {N (Et) 3} +Cl- <BR> <BR> A1-991 pimozide N O O CO2H O O 1 CF3CH2 Al-992 pimozide N O O CO2H O O 1 cyclopropyl Al-993 pimozide N O O CO2H O O 1 2-OMe-Ph Al-994 pimozide N O O CO2H O O 1 MeSCH2 Al-995 pimozide N O O CO2H O O 1 MeOCH2 Al-996 pimozide N O O CO2H S S 1 Ph Al-997 pimozide N O O CO2H S S 1 NMe2 Al-998 pimozide N O O CO2H S S 1 NBn2 <BR> <BR> A1-999 pimozide N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> A1-1000 pimozide N O O CO2H O S 1 Me Al-1001 prazosin N O O CO2H O O 1 methyl Al-1002 prazosin N O O CO2H O O 1 C(CH3)3 A1-1003 prazosin N O O CO2H O O 1 Ph Al-1004 prazosin N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1005 prazosin N O O CO2H O O 1 2-pyridyl Al-1006 prazosin N O O CO2H O O 1 4-Pyridyl Al-1007 prazosin N O O CO2H O O 1 2-furyl <BR> <BR> A1-1008 prazosin N O O CO2H O O 1 2-thienyl Al-1009 prazosin N O O CO2H - - 0 Cl A1-1010 prazosin N O O CO2H--0 {N (Et) 3} +Cl- Al-1011 prazosin N O O CO2H O O 1 CF3CH2 <BR> <BR> A1-1012 prazosin N O O CO2H O O 1 cyclopropyl<BR> <BR> <BR> <BR> A1-1013 prazosin N O O CO2H O O 1 2-OMe-Ph Al-1014 prazosin N O O CO2H O O 1 MeSCH2 Al-1015 prazosin N O O CO2H O O 1 MeOCH2 Al-1016 prazosin N O O CO2H S S 1 Ph Al-1017 prazosin N O O CO2H S S 1 NMe2 Al-1018 prazosin N O O CO2H S S 1 NBn2 <BR> <BR> A1-1019 prazosin N O O C02H O S 1 Ph<BR> <BR> <BR> <BR> A1-1020 prazosin N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> A1-1021 sulfamethizolee N O O CO2H O O 1 methyl Al-1022 sulfamethizolee N O O CO2H O O 1 C(CH3)3 <BR> <BR> A1-1023 sulfamethizolee N O O CO2H O O 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1024 sulfamethizolee N O O CO2H O O 1 4-Me-Ph Al-1025 sulfamethizolee N O O CO2H O O 1 2-pyridyl Al-1026 sulfamethizolee N O O CO2H O O 1 4-pyridyl Al-1027 sulfamethizolee N O O CO2H O O 1 2-furyl Al-1028 sulfamethizolee N O O CO2H O O 1 2-thienyl A1-1029 sulfamethizolee N O O CO2H--0 Cl A1-1030 sulfamethizolee N O O CO2H--0 {N (Et) 3} +Cl- <BR> <BR> A1-1031 sulfamethizolee N O O CO2H O O 1 CF3CH2 Al-1032 sulfamethizolee N O O CO2H O O 1 cyclopropyl Al-1033 sulfamethizolee N O O CO2H O O 1 2-OMe-Ph Al-1034 sulfamethizolee N O O CO2H O O 1 MeSCH2 Al-1035 sulfamethizolee N O O CO2H O O 1 MeOCH2 <BR> <BR> A1-1036 sulfamethizolee N O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> A1-1037 sulfamethizolee N O O C02H S S 1 NMe2<BR> <BR> <BR> <BR> A1-1038 sulfamethizolee N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> A1-1039 sulfamethizolee N O O C02H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1040 sulfamethizolee N O 0 C02H O S 1 Me<BR> <BR> <BR> <BR> A1-1041 tacrine N O O CO2H O O 1 methyl Al-1042 tacrine N O O CO2H O O 1 C(CH3)3 Al-1043 tacrine N O O CO2H O O 1 Ph <BR> <BR> A1-1044 tacrine N O O CO2H O O 1 4-Me-Ph Al-1045 tacrine N O O CO2H O O 1 2-pyridyl <BR> <BR> Al-1046tacrineNOOCOsH0014-pyridyl Al-1047 tacrine N O O CO2H O O 1 2-furyl Al-1048 tacrine N O O CO2H O O 1 2-thienyl A1-1049 tacrine N O O CO2H--0 Cl Al-1050 tacrine N O O C02H--0 {N (Et) 3)'Cl- Al-1051 tacrine N O O CO2H O O 1 CF3CH2 Al-1052 tacrine N O O CO2H O O 1 cyclopropyl Al-1053 tacrine N O O CO2H O O 1 2-OMe-Ph Al-1054 tacrine N O O CO2H O O 1 MeSCH2 Al-1055 tacrine N O O CO2H O O 1 MeOCH2 A1-1056 tacrine N O O CO2H S S 1 Ph <BR> <BR> A1-1057 tacrine N O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> A1-1058 tacrine N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> A1-1059 tacrine N O O CO2H O S 1 Ph Al-1060 tacrine N O O CO2H O S 1 Me Al-1061 terazosin N O O CO2H O O 1 methyl Al-1062 terazosin N O O CO2H O O 1 C(CH3)3 Al-1063 terazosin N O O CO2H O O 1 Ph <BR> <BR> Al-1064terazosinNOOC02H0014-Me-Ph Al-1065 terazosin N O O CO2H O O 1 2-pyridyl Al-1066 terazosin N O O CO2H O O 1 4-pyridyl Al-1067 terazosin N O O CO2H O O 1 2-furyl Al-1068 terazosin N O O CO2H O O 1 2-thienyl A1-1069 terazosin N O O CO2H--0 Cl Al-1070terazosinN00C02H--0 {N (Et) 3} +Cl- Al-1071 terazosin N O O CO2H O O 1 CF3CH2 Al-1072 terazosin N O O CO2H O O 1 cyclopropyl Al-1073 terazosin N O O CO2H O O 1 2-OMe-Ph Al-1074 terazosin N O O CO2H O O 1 MeSCH2 A1-1075 terazosin N O O CO2H O O 1 MeOCH2 Al-1076 terazosin N O O CO2H S S 1 Ph <BR> <BR> A1-1077 terazosin N O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> <BR> A1-1078 terazosin N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-1079 terazosin N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1080 terazosin N O O CO2H O S 1 Me Al-1081 timolol N O O CO2H O O 1 methyl Al-1082 timolol N O O CO2H O O 1 C(CH3)3 Al-1083 timolol N O O CO2H O O 1 Ph A1-1084 timolol N O O CO2H O O 1 4-Me-Ph<BR> <BR> <BR> <BR> <BR> A1-1085 timolol N O O CO2H O O 1 2-pyridyl Al-1086 timolol N O O CO2H O O 1 4-pyrdiyl A1-1087 timolol N O O CO2H O O 1 2-furyl Al-1088 timolol N O O CO2H O O 1 2-thienyl A1-1089 timolol N O O CO2H--0 C1 Al-1090timololN 0 0C02H--0 {N (Et) 3} +Cl Al-1091 timolol N O O CO2H O O 1 CF3CH2 Al-1092 timolol N O O CO2H O O 1 cyclopropyl A1-1093 timolol N O O CO2H O O 1 2-OMe-Ph<BR> <BR> <BR> <BR> <BR> A1-1094 timolol N O O CO2H O O 1 MeSCH2 Al-1095 timolol N O O CO2H O O 1 MeOCH2 Al-1096 timolol N O O CO2H S S 1 Ph A1-1097 timolol N O 0 COzH S S 1 NMe2<BR> <BR> <BR> <BR> <BR> A1-1098 timolol N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-1099 timolol N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1100 timolol N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> A1-1121 xylometazoline N O O CO2H O O 1 methyl Al-1122 xylometazoline N O O CO2H O O 1 C(CH3)3 Al-1123 xylometazoline N O O CO2H O O 1 Ph Al-1124xylometazolineN00C02H0014-Me-Ph Al-1125 xylometazoline N O O CO2H O O 1 2-pyridyl Al-1126 xylometazoline N O O CO2H O O 1 4-pyridyl Al-1127 xylometazoline N O O CO2H O O 1 2-furyl Al-1128 xylometazoline N O O CO2H O O 1 2-thienyl Al-1129 xylometazoline N O O CO2H - - 0 Cl A1-1130 xylometazoline N O O CO2H--0 {N (Et) 3} +Cl- A1-1131 xylometazoline N O O CO2H O O 1 CF3CH2 Al-1132 xylometazoline N O O CO2H O O 1 cyclopropyl Al-1133 xylometazoline N O O CO2H O O 1 2-OMe-Ph Al-1134 xylometazoline N O O CO2H O O 1 MeSCH2 Al-1135 xylometazoline N O O CO2H O O 1 MeOCH2 A1-1136 xylometazoline N O O CO2H S S 1 Ph Al-1137 xylometazoline N O O CO2H S S 1 NMe2 Al-1138 xylometazoline N O O CO2H S S 1 NBn2 Al-1139 xylometazoline N O O CO2H O S 1 Ph A1-1140 xylometazoline N O O CO2H O S 1 Me Al-1141 lovastatin O O O CO2H O O 1 methyl Al-1142 lovastatin O O O CO2H O O 1 C(CH3)3 Al-1143 lovastatin O O O CO2H O O 1 Ph Al-1144 lovastatin O O O CO2H O O 1 4-Me-Ph Al-1145 lovastatin O O O CO2H O O 1 2-pyridyl Al-1146 lovastatin O O O CO2H O O 1 4-pyridyl Al-1147 lovastatin O O O CO2H O O 1 2-furyl <BR> <BR> A1-1148 lovastatin O O O CO2H O O 1 2-thienyl Al-1149 lovastatin O O O CO2H - - 0 Cl Al-1150 lovastatin 0 O O CO2H--0 {N (Et) 3} +Cl- Al-1151 lovastatin O O O CO2H O O 1 CF3CH2 Al-1152 lovastatin O O O CO2H O O 1 cyclopropyl A1-1153 lovastatin O O O CO2H O O 1 2-OMe-Ph Al-1154 lovastatin O O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1155 lovastatin O O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> <BR> <BR> Al-1156 lovastatin 0 O O COzH S S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1157 lovastatin O O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> <BR> A1-1158 lovastatin O O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-1159 lovastatin 0 O O C02H O S 1 Ph Al-1160 lovastatin O O O CO2H O S 1 Me Al-1161 warfarin O O O CO2H O O 1 methyl Al-1162 warfarin O O O CO2H O O 1 C(CH3)3 <BR> <BR> A1-1163 warfarin O O O CO2H O O 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1164 warfarin O O O CO2H O O 1 4-Me-Ph Al-1165 warfarin O O O CO2H O O 1 2-pyridyl <BR> <BR> A1-1166 warfarin O O O CO2H O O 1 4-pyridyl Al-1167 warfarin O O O CO2H O O 1 2-furyl Al-1168 warfarin O O O CO2H O O 1 2-thienyl Al-1169 warfarin O O O CO2H - - 0 Cl A1-1170 warfarin 0 O O COzH--0 {N (Et) 3} +Cl- Al-1171 warfarin O O O CO2H O O 1 CF3CH2 Al-1172 warfarin O O O CO2H O O 1 cyclopropyl Al-1173 warfarin O O O CO2H O O 1 2-OMe-Ph Al-1174 warfarin O O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1175 warfarin O O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> <BR> A1-1176 warfarin O O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> Al-1177 warfarin O O O C02H S S 1 NMe2<BR> <BR> <BR> <BR> <BR> A1-1178 warfarin O O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-1179 warfarin 0 O O C02H O S 1 Ph Al-1180 warfarin O O O CO2H O S 1 Me Al-1181 atorvastatin O O O CO2H O O 1 Me Al-1182 atorvastatin O O O CO2H O O 1 C(CH3)3 Al-1183 atorvastatin O O O CO2H O O 1 Ph <BR> <BR> A1-1184 atorvastatin O O O C02H O O 1 4-Me-Ph Al-1185 atorvastatin O O O CO2H O O 1 2-pyridyl Al-1186 atorvastatin O O O CO2H O O 1 4-pyridyl Al-1187 atorvastatin O O O CO2H O O 1 2-furyl Al-1188 atorvastatin O O O CO2H O O 1 2-thienyl A1-1189 atorvastatin O O O CO2H--0 C1 Al-1190 atorvastatin O O O CO2H - - 0 {N (Et) 3} +Cl- Al-1191 atorvastatin O O O CO2H O O 1 CF3CH2 Al-1192 atorvastatin O O O CO2H O O 1 cyclopropyl Al-1193 atorvastatin O O O CO2H O O 1 2-OMe-Ph Al-1194 atorvastatin O O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1195 atorvastatin O O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> <BR> A1-1196 atorvastatin O O O CO2H S S 1 Ph Al-1197 atorvastatin O O O CO2H S S 1 NMe2 Al-1198 atorvastatin O O O CO2H S S 1 NBn2 Al-1199atorvastatin00 0C02H0S1Ph Al-1200 atorvastatin O O O CO2H O S 1 Me Al-1201 atropine O O O CO2H O O 1 methyl Al-1202 atropine O O O CO2H O O 1 C(CH3)3 Al-1203 atropine O O O CO2H O O 1 Ph Al-1204 atropine O O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1205 atropine O O O CO2H O O 1 2-pyridyl Al-1206 atropine O O O CO2H O O 1 4-pyridyl Al-1207 atropine O O O CO2H O O 1 2-furyl Al-1208 atropine O O O CO2H O O 1 2-thienyl Al-1209 atropine O O O CO2H - - 0 Cl Al-1210 atropine O O O CO2H - - 0 {N (Et) 3} +Cl- Al-1211 atropine O O O CO2H O O 1 CF3CH2 <BR> <BR> A1-1212 atropine O O O CO2H O O 1 cyclopropyl<BR> <BR> <BR> <BR> <BR> <BR> A1-1213 atropine O O O CO2H O O 1 2-OMe-Ph Al-1214 atropine O O O CO2H O O 1 MeSCH2 Al-1215 atropine O O O CO2H O O 1 MeOCH2 Al-1216atropine00 0C02HSS1Ph Al-1217 atropine O O O CO2H S S 1 NMe2 Al-1218 atropine O O O CO2H S S 1 NBn2 A1-1219 atropine O O O CO2H O S 1 Ph Al-1220 atropine O O O CO2H O S 1 Me <BR> <BR> A1-1221 bicalutamide O O O CO2H O O 1 methyl Al-1222 bicalutamide O O O CO2H O O 1 C(CH3)3 Al-1223 bicalutamide O O O CO2H O O 1 Ph <BR> <BR> <BR> Al-1224bicalutamide00 0C02H0014-Me-Ph<BR> <BR> <BR> <BR> <BR> <BR> <BR> A1-1225 bicalutamide O 0 O C02H O O 1 2-pyridyl<BR> <BR> <BR> <BR> <BR> <BR> Al-1226bicalutamide000C02H0014-pyridyl<BR> <BR> <BR> <BR> <BR> A1-1227 bicalutamide O O O CO2H O O 1 2-furyl Al-1228 bicalutamide O O O CO2H O O 1 2-thienyl Al-1229bicalutamide00 0C02H--0C1 Al-1230 bicalutamide O O O CO2H - - 0 {N (Et) 3}+Cl <BR> <BR> A1-1231 bicalutamide O O O CO2H O O 1 CF3CH2 Al-1232 bicalutamide O O O CO2H O O 1 cyclopropyl Al-1233 bicalutamide O O O CO2H O O 1 2-OMe-Ph Al-1234 bicalutamide O O O CO2H O O 1 MeSCH2 Al-1235 bicalutamide O O O CO2H O O 1 MeOCH2 Al-1236bicalutamide00 0C02HSS1Ph Al-1237 bicalutamide O O O CO2H S S 1 NMe2 Al-1238 bicalutamide O O O CO2H S S 1 NBn2 A1-1239 bicalutamide O O O CO2H O S 1 Ph Al-1240bicalutamide00 0C02H0SIMe Al-1241 clobesol O O O CO2H O O 1 methyl <BR> <BR> Al-1242clobesolO0 0COzHOOIC (CHg) 3 Al-1243 clobesol O O O CO2H O O 1 Ph Al-1244 clobesol O O O CO2H O O 1 4-Me-Ph Al-1245 clobesol O O O CO2H O O 1 2-pyridyl Al-1246 clobesol O O O CO2H O O 1 4-pyridyl Al-1247 clobesol O O O CO2H O O 1 2-furyl <BR> <BR> Al-1248clobesol00 0C02H0012-thienyl Al-1249 clobesol O O O CO2H - - 0 Cl Al-1250 clobesol O 0 O CO2H--0 {N (Et) 3} +Cl- Al-1251 clobesol O O O C02H O 0 1 CF3CH2 Al-1252 clobesol O O O CO2H O O 1 cyclopropyl Al-1253 clobesol O O O C02H O O 1 2-OMe-Ph Al-1254 clobesol O O O C02H O O 1 MeSCH2 Al-1255 clobesol O O O C02H O O 1 MeOCH2 Al-1256 clobesol O O O C02H S S 1 Ph Al-1257 clobesol O O O C02H S S 1 NMe2 Al-1258 clobesol O O O C02H S S 1 NBn2 Al-1259 clobesol O O O C02H O S 1 Ph Al-1260 clobesol O O O C02H O S 1 Me Al-1261 fluticasone O O O CO2H 0 O 1 methyl propionate Al-1262 fluticasone O O O CO2H 0 O 1 C (CH3) 3 propionate Al-1263 fluticasone O O O C02H O O 1 Ph propionate Al-1264 fluticasone O O O CO2H 0 O 1 4-Me-Ph propionate Al-1265 fluticasone O O O CO2H O O 1 2-pyridyl propionate Al-1266 fluticasone O O O CO2H O O 1 4-pyridyl propionate Al-1267 fluticasone 0 O O CO2H 0 O 1 2-furyl propionate Al-1268 fluticasone O O O CO2H O O 1 2-thienyl propionate Al-1269 fluticasone O O O C02H--0 ci propionate Al-1270 fluticasone O O O CO2H--0 {N (Et) 3}+Cl propionate Al-1271 fluticasone O O O CO2H O O 1 CF3CH2 propionate Al-1272 fluticasone O O O CO2H O O 1 cyclopropyl propionate Al-1273 fluticasone O O O C02H O O 1 2-OMe-Ph propionate Al-1274 fluticasone O O O CO2H O 0 1 MeSCH2 propionate Al-1275 fluticasone O 0 O C02H 0 O 1 MeOCH2 propionate Al-1276 fluticasone O O O C02H S S 1 Ph propionate Al-1277 fluticasone O O O C02H S S 1 NMe2 propionate Al-1278 fluticasone O O O C02H S S 1 NBn2 propionate Al-1279 fluticasone O O O C02H 0 S 1 Ph propionate Al-1280 fluticasone 0 O O C02H O S 1 Me propionate Al-1301 loperidine HCl O O O CO2H O O 1 methyl Al-1302 loperidine HCl O O O CO2H O O 1 C(CH3)3 Al-1303 loperidine HCl O O O CO2H O O 1 Ph Al-1304 loperidine HCl O O O CO2H O O 1 4-Me-Ph Al-1305 loperidine HCl O O O CO2H O O 1 2-pyridyl Al-1306 loperidine HCl O O O CO2H O O 1 4-pyridyl A1-1307 loperidine HC1 O O O CO2H O O 1 2-furyl Al-1308 loperidine HCl O O O CO2H O O 1 2-thienyl Al-1309 loperidine HCl O O O CO2H - - 0 Cl Al-1310 loperidine HCl O O O CO2H - - 0 {N (Et) 3}+Cl Al-1311 loperidine HCl O O O CO2H O O 1 CF3CH2 Al-1312 loperidine HCl O O O CO2H O O 1 cyclopropyl Al-1313 loperidine HCl O O O CO2H O O 1 2-OMe-Ph Al-1314 loperidine HCl O O O CO2H O O 1 MeSCH2 Al-1315 loperidine HCl O O O CO2H O O 1 MeOCH2 A1-1316 loperidine HC1 O O O CO2H S S 1 Ph Al-1317 loperidine HCl O O O CO2H S S 1 NMe2 Al-1318 loperidine HCl O O O CO2H S S 1 NBn2 Al-1319 loperidine HCl O O O CO2H O S 1 Ph <BR> <BR> A1-1320 loperidine HC1 O O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> A1-1321 monozid O O O CO2H O O 1 methyl Al-1322 monozid O O O CO2H O O 1 C(CH3)3 Al-1323 monozid O O O CO2H O O 1 Ph <BR> <BR> A1-1324 monozid O O O CO2H O O 1 4-Me-Ph<BR> <BR> <BR> <BR> <BR> A1-1325 monozid O O O CO2H O O 1 2-pyridyl Al-1326 monozid O O O CO2H O O 1 4-pyridyl Al-1327 monozid O O O CO2H O O 1 2-furyl Al-1328 monozid O O O CO2H O O 1 2-thienyl A1-1329 monozid O O O CO2H--0 C1 A1-1330 monozid O O O CO2H--0 {N (Et) 3} +Cl- <BR> <BR> A1-1331 monozid O 0 O C02H 0 0 1 CF3CH2 Al-1332 monozid O O O CO2H O O 1 cyclopropyl <BR> <BR> A1-1333 monozid O O O COzH O O 1 2-OMe-Ph<BR> <BR> <BR> <BR> <BR> A1-1334 monozid O O O CO2H O O 1 MeSCH2 Al-1335 monozid O O O CO2H O O 1 MeOCH2 <BR> <BR> A1-1336 monozid O O O C02H S S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1337 monozid O O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> A1-1338 monozid O 0 O C02H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-1339 monozid O O O C02H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1340 monozid O O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> A1-1341 oxybutynin HCl O 0 O C02H O 0 1 methyl Al-1342 oxybutynin HCl O O O CO2H O O 1 C(CH3)3 Al-1343 oxybutynin HCl O O O CO2H O O 1 Ph <BR> <BR> A1-1344oxybutyninHCl000C02H0014-Me-Ph Al-1345 oxybutynin HCl O O O CO2H O O 1 2-pyridyl <BR> <BR> A1-1346oxybutyninHCl000C02H0014-pyridyl Al-1347 oxybutynin HCl O O O CO2H O O 1 2-furyl Al-1348 oxybutynin HCl O O O CO2H O O 1 2-thienyl Al-1349 oxybutynin HCl O O O CO2H - - 0 Cl A1-1350 oxybutynin HCl O 0 O C02H--0 {N (Et) 3} +Cl- Al-1351 oxybutynin HCl O O O CO2H O O 1 CF3CH2 Al-1352 oxybutynin HCl O O O CO2H O O 1 cycloporpyl Al-1353 oxybutynin HCl O O O CO2H O O 1 2-OMe-Ph A1-1354 oxybutynin HC1 O O O CO2H O O 1 MeSCH2 Al-1355 oxybutynin HCl O O O CH2H O O 1 MeOCH2 Al-1356 oxybutynin HCl O O O CH2H S S 1 Ph Al-1357 oxybutynin HCl O O O CH2H S S 1 NMe2 Al-1358 oxybutynin HCl O O O CH2H S S 1 NMe2 Al-1359 oxybutynin HCl O O O CH2H O S 1 Ph Al-1360 oxybutynin HCl O O O CH2H O S 1 Me <BR> <BR> A1-1361 oxycodone O O O CO2H O O 1 methyl Al-1362 oxycodone O O O CO2H O O 1 C(CH3)3 Al-1363 oxycodone O O O CO2H O O 1 Ph Al-1364 oxycodone O O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1365 oxycodone O O O CO2H O O 1 2-pyridyl Al-1366 oxycodone O O O CO2H O O 1 4 - pyridyl <BR> <BR> A1-1367 oxycodone O O O CO2H O O 1 2-furyl Al-1368 oxycodone O O O CO2H O O 1 2-thienyl Al-1369 oxycodone O O O CO2H - - 0 Cl A1-1370 oxycodone O O O CO2H--0 {N (Et) 3} +Cl- Al-1371 oxycodone O O O CO2H O O 1 CF3CH2 Al-1372 oxycodone O O O CO2H O O 1 cyclopropyl <BR> <BR> A1-1373 oxycodone O O O CO2H O O 1 2-OMe-Ph<BR> <BR> <BR> <BR> <BR> A1-1374 oxycodone O O O CO2H O O 1 MeSCH2 Al-1375 oxycodone O O O CO2H O O 1 MeOCH2 Al-1376oxycodoneO 0 0C02HS S 1Ph <BR> <BR> A1-1377 oxycodone O O O CO2H S S 1 NMe2 Al-1378 oxycodone O O O CO2H S S 1 NBn2 A1-1379 oxycodone O 0 O C02H O S 1 Ph Al-1380 oxycodone O O O CO2H O S 1 Me <BR> <BR> A1-1381 piroxicam O O O CO2H O O 1 methyl<BR> <BR> <BR> <BR> Al-1382piroxicamO 0 0C02H0 0 1C (CHs) 3<BR> <BR> <BR> <BR> A1-1383 piroxicam O O O CO2H O O 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1384 piroxicam O O O CO2H O O 1 4-Me-Ph Al-1385 piroxicam O O O CO2H O O 1 2-pyridyl Al-1386 piroxicam O O O CO2H O O 1 4-pyridyl Al-1387 piroxicam O O O CO2H O O 1 2-furyl Al-1388 piroxicam O O O CO2H O O 1 2-thienyl A1-1389 piroxicam 0 O O CO2H--0 C1 A1-1390 piroxicam O 0 O C02H--0 {N (Et) 3} +Cl- Al-1391 piroxicam O O O CO2H O O 1 CF3CH2 Al-1392 piroxicam O O O CO2H O O 1 cyclopropyl <BR> <BR> A1-1393 piroxicam O O O CO2H O O 1 2-OMe-Ph Al-1394 piroxicam O O O CO2H O O 1 MeSCH2 Al-1395 piroxicam O O O CO2H O O 1 MeOCH2 Al-1396piroxicamO 0 0C02HS S 1Ph <BR> <BR> A1-1397 piroxicam O O O CO2H S S 1 NMe2 Al-1398 piroxicam O O O CO2H S S 1 NBn2 <BR> <BR> A1-1399 piroxicam O O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> A1-1400 piroxicam O O O C02H O S 1 Me<BR> <BR> <BR> <BR> <BR> Al-1401simvastatin000C02H001methyl Al-1402 simvastatin O O O CO2H O O 1 C(CH3)3 Al-1403 simvastatin O O O CO2H O O 1 Ph <BR> <BR> Al-1404simvastatin000C02H0014-Me-Ph Al-1405 simvastatin O O O CO2H O O 1 2-pyrdyl Al-1406 simvastatin O O O CO2H O O 1 4-pyridyl <BR> <BR> A1-1407 simvastatin O O O C02H O O 1 2-furyl Al-1408 simvastatin O O O CO2H O O 1 2-thienyl Al-1409 simvastatin O O O CO2H - - 0 Cl A1-1410 simvastatin O O O CO2H--0 {N (Et) 3} +Cl- Al-1411 simvastatin O O O CO2H O O 1 CF3CH2 Al-1412 simvastatin O O O CO2H O O 1 cyclopropyl <BR> <BR> A1-1413 simvastatin O O O CO2H O O 1 2-OMe-Ph<BR> <BR> <BR> <BR> <BR> A1-1414 simvastatin O O O CO2H O O 1 MeSCH2<BR> <BR> <BR> <BR> <BR> A1-1415 simvastatin O O O CO2H O O 1 MeOCH2 Al-1416simvastatin0 0 0C02HS S 1Ph <BR> <BR> A1-1417 simvastatin O O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> <BR> A1-1418 simvastatin O O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-1419 simvastatin O 0 O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1420 simvastatin O O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> A1-1421 troglitazone O O O CO2H O O 1 methyl Al-1422 troglitazone O O O CO2H O O 1 C(CH3)3 A1-1423 troglitazone O O O CO2H O O 1 Ph Al-1424 troglitazone O O O CO2H O O 1 4-Me-Ph Al-1425 troglitazone O O O CO2H O O 1 2-pyridyl Al-1426 troglitazone O O O CO2H O O 1 4-pyridyl Al-1427 troglitazone O O O CO2H O O 1 2-furyl Al-1428 troglitazone O O O CO2H O O 1 2-thienyl Al-1429troglitazone0 0 0C02H--0C1 Al-1430troglitazone000C02H--0 {N (Et) 31+Cl- <BR> <BR> A1-1431 troglitazone O O O CO2H O O 1 CF3CH2 Al-1432 troglitazone O O O CO2H O O 1 cyclopropyl <BR> <BR> A1-1433 troglitazone O O O CO2H O O 1 2-OMe-Ph Al-1434 troglitazone O O O CO2H O O 1 MeSCH2 Al-1435 troglitazone O O O CO2H O O 1 MeOCH2 A1-1436 troglitazone O O O CO2H S S 1 Ph Al-1437 troglitazone O O O CO2H S S 1 NMe2 Al-1438 troglitazone O O O CO2H S S 1 NBn2 <BR> <BR> A1-1439 troglitazone O O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1440 troglitazone O O O C02H O S 1 Me Al-1441 carbamazepam N O O CO2H O O 1 methyl Al-1442 carbamazepam N O O CO2H O O 1 C(CH3)3 A1-1443 carbamazepam N O O CO2H O O 1 Ph Al-1444 carbamazepam N O O CO2H O O 1 4-Me-Ph Al-1445 carbamazepam N O O CO2H O O 1 2-pyridyl <BR> <BR> A1-1446 carbamazepam N O O C02H O O 1 4-pyridyl Al-1447 carbamazepam N O O CO2H O O 1 2-furyl Al-1448 carbamazepam N O O CO2H O O 1 2-thienyl A1-1449 carbamazepam N O O C02H--0 C1 Al-1450carbamazepamN00C02H--0 {N (Et) 3}+Cl- Al-1451 carbamazepam N O O CO2H O O 1 CF3CH2 Al-1452 carbamazepam N O O CO2H O O 1 cyclopropyl Al-1453 carbamazepam N O O CO2H O O 1 2-OMe-Ph A1-1454 carbamazepam N O O CO2H O O 1 MeSCH2<BR> <BR> <BR> <BR> <BR> A1-1455 carbamazepam N O O CO2H O O 1 MeOCH2 Al-1456 carbamazepam N O O CO2H S S 1 Ph <BR> <BR> A1-1457 carbamazepam N O O CO2H S S 1 NMe2 Al-1458 carbamazepam N O O CO2H S S 1 NBn2 Al-1459 carbamazepam N O O CO2H O S 1 Ph <BR> <BR> A1-1460 carbamazepam N O O C02H O S I Me<BR> <BR> <BR> <BR> A1-1461 amoxicillin N O O C02H O O 1 methyl Al-1462 amoxicillin N O O CO2H O O 1 C(CH3)3 Al-1463 amoxicillin N O O CO2H O O 1 Ph Al-1464 amoxicillin N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1465 amoxicillin N O O C02H O O 1 2-pyridyl Al-1466 amoxicillin N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-1467 amoxicillin N O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> A1-1468 amoxicillin N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> A1-1469 amoxicillin N O O COzH--0 Cl A1-1470 amoxicillin N O O CO2H--0 {N (Et) 3}+Cl- Al-1471 amoxicillin N O O CO2H O O 1 CF3CH2 <BR> <BR> A1-1472 amoxicillin N O O CO2H O O 1 cyclopropyl Al-1473 amoxicillin N O O CO2H O O 1 2-OMe-Ph <BR> <BR> A1-1474 amoxicillin N O O CO2H O O 1 MeSCH2 Al-1475 amoxicillin N O O CO2H O O 1 MeOCH2 Al-1476 amoxicillin N O O CO2H S S 1 Ph Al-1477 amoxicillin N O O CO2H S S 1 NMe2 Al-1478 0 0COsHSS1NBn2 <BR> <BR> A1-1479 amoxicillin N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> A1-1480 amoxicillin N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> A1-1481 benazepril N O O C02H 0 O 1 methyl Al-1482 benzepril N O O CO2H O O 1 C(CH3)3 A1-1483 benazepril N O O CO2H O O 1 Ph Al-1484 benzepril N O O CO2H O O 1 4-Me-Ph Al-1485 benzepril N O O CO2H O O 1 2-pyridyl Al-1486 benzepril N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-1487 benazepril N O O CO2H O O 1 2-furyl Al-1488 benzepril N O O CO2H O O 1 2-thienyl Al-1489 benzepril N O O CO2H - - 0 Cl Al-1490benazeprilN00C02H--0 {N (Et) 3} +Cl- Al-1491 benzepril N O O CO2H O O 1 CF3CH2 Al-1492 benzepril N O O CO2H O O 1 cyclopropyl <BR> <BR> A1-1493 benazepril N O O C02H O O 1 2-OMe-Ph Al-1494 benzepril N O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1495 benazepril N O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> Al-1496benazeprilN 0 0COzHSS1Ph Al-1497 benzepril N O O CO2H S S 1 NMe2 Al-1498 benzepril N O O CO2H S S 1 NBn2 <BR> <BR> A1-1499 benazepril N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> A1-1500 benazepril N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> A1-1501 cefachlor N O O CO2H O O 1 methyl Al-1502 cafachlor N O O CO2H O O 1 C(CH3)3 A1-1503 cefachlor N O O CO2H O O 1 Ph Al-1504 cafachlor N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1505 cefachlor N O O CO2H O O 1 2-pyridyl Al-1506 cafachlor N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-1507 cefachlor N O O CO2H O O 1 2-furyl Al-1508 cafachlor N O O CO2H O O 1 2-thienyl Al-1509 cafachlor N O O CO2H - - 0 Cl Al-1510 cafachlor N O O CO2H - - 0 {N(Et)3}+Cl- Al-1511 cafachlor N O O CO2H O O 1 CF3AH2 Al-1512 cafachlor N O O CO2H O O 1 cyclopropyl Al-1513 cafachlor N O O CO2H O O 1 2-OMe-Ph <BR> <BR> A1-1514 cefachlor N O O CO2H O O 1 MeSCH2<BR> <BR> <BR> <BR> <BR> A1-1515 cefachlor N O O CO2H O O 1 MeOCH2 Al-1516 cafachlor N O O CO2H O O 1 Ph Al-1517 cafachlor N O O CO2H O O 1 NMe2 Al-1518 cafachlor N O O CO2H O O 1 NBn2 <BR> <BR> A1-1519 cefachlor N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1520 cefachlor N O O CO2H O S 1 Me Al-1521 cetirizine N O O CO2H O O 1 methyl Al-1522 cetirizine N O O CO2H O O 1 C(CH3)3 Al-1523 cetirizine N O O CO2H O O 1 Ph Al-1524 cetirizine N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1525 cetirizine N O O CO2H O O 1 2-pyridyl Al-1526 cetirizine N O O CO2H O O 1 4-pyridyl Al-1527 cetirizine N O O CO2H O O 1 2-furyl <BR> <BR> A1-1528 cetirizine N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> A1-1529 cetirizinec N O O CO2H--0 C1 A1-1530 cetirizine N O O CO2H--0 {N (Et) 3}+Cl- <BR> <BR> A1-1531 cetirizine N O O CO2H O O 1 CF3CH2<BR> <BR> <BR> <BR> <BR> <BR> A1-1532 cetirizine N O O CO2H O O 1 cyclopropyl Al-1533 cetirizine N O O CO2H O O 1 2-OMe-Ph Al-1534 cetirizine N O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1535 cetirizine N O O CO2H O O 1 MeOCH2 Al-1536 cetirizine N O O CO2H S S 1 Ph Al-1537 cetirizine N O O CO2H S S 1 NMe2 Al-1538 cetirizine N O O CO2H S S 1 NBn2 <BR> <BR> A1-1539 cetirizine N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1540 cetirizine N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> A1-1541 cefadroxil N O O CO2H O O 1 methyl<BR> <BR> <BR> <BR> A1-1542 cefadroxil N O O CO2H O O 1 C (CH3) 3<BR> <BR> <BR> <BR> <BR> A1-1543 cefadroxil N O O CO2H O O 1 Ph Al-1544 cafadroxil N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1545 cefadroxil N O O CO2H O O 1 2-pyridyl Al-1546 cafadroxil N O O CO2H O O 1 4-pyridyl Al-1547 cafadroxil N O O CO2H O O 1 2-furyl Al-1548 cafadroxil N O O CO2H O O 1 2-thienyl Al-1549 cafadroxil N O O CO2H O O 1 Cl Al-1550 cefadroxil N O O CO2H--0 {N (Et) 3} +Cl- <BR> <BR> A1-1551 cefadroxil N O O CO2H O O 1 CF3CH2 Al-1552 cafadroxil N O O CO2H O O 1 cyclopropyl <BR> <BR> A1-1553 cefadroxil N O O CO2H O O 1 2-OMe-Ph Al-1554 cafadroxil N O O CO2H O O 1 MeSCH2 Al-1555 cafadroxil N O O CO2H O O 1 MeOCH2 Al-1556 cafadroxil N O O CO2H S S 1 Ph Al-1557 cafadroxil N O O CO2H O S 1 NMe2 Al-1558 cafadroxil N O O CO2H S S 1 NBn2 Al-1559 cafadroxil N O O CO2H S S 1 Ph A1-1560 cefadroxil N O O CO2H O S 1 Me Al-1561 clonazepam N O O CO2H O O 1 methyl Al-1562 clonazepam N O O CO2H O O 1 C(CH3)3 Al-1563 clonazepam N O O CO2H O O 1 Ph Al-1564 clonazepam N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1565 clonazepam N O O CO2H O O 1 2-pyridyl Al-1566 clonazepam N O O CO2H O O 1 4-pyridyl Al-1567 clonazepam N O O CO2H O O 1 2-furyl <BR> <BR> A1-1568 clonazepam N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> <BR> A1-1569 clonazepam N O O CO2H--0 C1 A1-1570 clonazepam N O O CO2H--0 {N (Et) 3)'Cl- <BR> <BR> A1-1571 clonazepam N O O CO2H O O 1 CF3CH2 Al-1572 clonazepam N O O CO2H O O 1 cyclopropyl Al-1573 clonazepam N O O CO2H O O 1 2-OMe-Ph Al-1574 clonazepam N O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1575 clonazepam N O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> <BR> <BR> A1-1576 clonazepam N O O CO2H S S 1 Ph A1-1577 clonazepam N O O CO2H S S 1 NMe2 <BR> <BR> A1-1578 clonazepam N O O CO2H S S 1 NBn2 Al-1579 clonazepam N O O CO2H O S 1 Ph A1-1580 clonazepam N O O C02H 0 S 1 Me Al-1581 demethylimipramine N O O CO2H O O 1 methyl Al-1582 demethylimipramine N O O CO2H O O 1 C(CH3)3 Al-1583 demethylimipramine N O O CO2H O O 1 Ph Al-1584 demethylimipramine N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1585 demethylimipramine N O O CO2H O O 1 2-pyridyl Al-1586 demethylimipramine N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-1587 demethylimipramine N O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> <BR> <BR> A1-1588 demethylimipramine N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> <BR> A1-1589 demethylimipramine N O O CO2H--0 C1 A1-1590 demethylimipramine N O O CO2H--0 {N (Et) 3} +Cl- <BR> <BR> A1-1591 demethylimipramine N O O CO2H O O 1 CF3CH2<BR> <BR> <BR> <BR> <BR> <BR> A1-1592 demethylimipramine N O O CO2H O O 1 cyclopropyl<BR> <BR> <BR> <BR> <BR> <BR> A1-1593 demethylimipramine N O O CO2H O O 1 2-OMe-Ph Al-1594 demethylimipramine N O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1595 demethylimipramine N O O CO2H O O 1 MeOCH2 Al-1596 demethylimipramine N O O CO2H S S 1 Ph <BR> <BR> A1-1597 demethylimipramine N O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> <BR> <BR> A1-1598 demethylimipramine N O O CO2H S S 1 NBn2 Al-1599 demethylimipramine N O O CO2H O S 1 Ph Al-1600 demethylimipramine N O O CO2H O S 1 Me Al-1601 deprenil O O O CO2H O O 1 methyl Al-1602 deprenil O O O CO2H O O 1 C(CH3)3 Al-1603 deprenil O O O CO2H O O 1 Ph Al-1604 deprenil O O O CO2H O O 1 4-Me-Ph Al-1605 deprenil O O O CO2H O O 1 2-pyridyl Al-1606 deprenil O O O CO2H O O 1 4-pyridyl Al-1607 deprenil O O O CO2H O O 1 2-furyl Al-1608 deprenil O O O CO2H O O 1 2-thienyl A1-1609 deprenil O O O CO2H--0 C1 A1-1610 deprenil O O O C02H--0 {N (Et) 3} +Cl- Al-1611 deprenil O O O CO2H O O 1 CF3CH2 Al-1612 deprenil O O O CO2H O O 1 cyclopropyl Al-1613 deprenil O O O CO2H O O 1 2-OMe-Ph Al-1614 deprenil O O O CO2H O O 1 MeSCH2 Al-1615 deprenil O O O CO2H O O 1 MeOCH2 A1-1616 deprenil O O O C02H S S 1 Ph Al-1617 deprenil O O O CO2H O O 1 NMe2 Al-1618 deprenil O O O CO2H S S 1 NMn2 <BR> <BR> A1-1619 deprenil 0 O O C02H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1620 deprenil O O 0 COzH O S 1 Me Al-1621 doxazosin O O O CO2H O O 1 methyl <BR> <BR> Al-1622doxazosin0 0 0C02H0 0 1C (CHs) 3<BR> <BR> <BR> <BR> <BR> A1-1623 doxazosin O O O C02H O O 1 Ph Al-1624 doxazosin O O O CO2H O O 1 4-Me-Ph Al-1625 doxazosin O O O CO2H O O 1 2-pyridyl Al-1626doxazosin000COzH0014-pyridyl Al-1627 doxazosin O O O CO2H O O 1 2-furyl Al-1628 doxazosin O O O CO2H O O 1 2-thienyl Al-1629 doxazosin O O O CO2H - - 0 Cl A1-1630 doxazosin O O O CO2H--0 {N (Et) 3}+Cl- Al-1631 doxazosin O O O CO2H O O 1 CF3CH2 Al-1632 doxazosin O O O CO2H O O 1 cyclopropyl A1-1633 doxazosin O O O CO2H O O 1 2-OMe-Ph<BR> <BR> <BR> <BR> <BR> A1-1634 doxazosin O O O CO2H O O 1 MeSCH2 Al-1635 doxazosin O O O CO2H O O 1 MeOCH2 Al-1636 doxazosin O O O CO2H S S 1 Ph Al-1637 doxazosin O O O CO2H S S 1 NMe2 Al-1638 doxazosin O O O CO2H S S 1 NBn2 <BR> <BR> Al-1639 doxazosin O 0 O COzH O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1640 doxazosin O O O CO2H O S 1 Me<BR> <BR> <BR> <BR> <BR> A1-1641 enalapril O O 0 C02H 0 O 1 methyl Al-1642 enalapril O O O CO2H O O 1 C(CH3)3 Al-1643 enalapril O O O CO2H O O 1 Ph <BR> <BR> A1-1644 enalapril O O O CO2H O O 1 4-Me-Ph Al-1645 enalapril O O O CO2H O O 1 2-pyridyl <BR> <BR> Al-1646enalapril000COzH0014-pyridyl<BR> <BR> <BR> <BR> A1-1647 enalapril O O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> <BR> A1-1648 enalapril O O O C02H O O 1 2-thienyl Al-1649 enalapril O O O CO2H - - 0 Cl Al-1650 enalapril 0 O O COzH--0 {N (Et) 3} +Cl- Al-1651 enalapril O O O CO2H O O 1 CF3CH2 Al-1652 enalapril O O O CO2H O O 1 cyclopropyl A1-1653 enalapril O O O CO2H O O 1 2-OMe-Ph Al-1654 enalapril O O O CO2H O O 1 MeSCH2 Al-1655 enalapril O O O CO2H O O 1 MeOCH2 A1-1656 enalapril O O O C02H S S 1 Ph Al-1657 enalapril O O O CO2H S S 1 NMe2 Al-1658 enalapril O O O CO2H S s 1 NBn2 A1-1659 enalapril 0 O O COzH O S 1 Ph Al-1660 enalapril O O O CO2H O S 1 Me <BR> <BR> A1-1661 famciclovir O 0 0 COzH O O 1 methyl<BR> <BR> <BR> <BR> <BR> A1-1662 famciclovir O O O CO2H O O 1 C (CH3) 3<BR> <BR> <BR> <BR> A1-1663 famciclovir O O O CO2H O O 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1664 famciclovir O O O CO2H O O 1 4-Me-Ph Al-1665 famciclovir O O O CO2H O O 1 2-pyridyl Al-1666 famciclovir O O O CO2H O O 1 4-pyridyl <BR> <BR> A1-1667 famciclovir O O O C02H O O 1 2-furyl Al-1668 famciclovir O O O CO2H O O 1 2-thienyl Al-1669famciclovir0 0 0C02H--0C1 A1-1670 famciclovir 0 O 0 C02H--0 {N (Et) 3}+Cl- <BR> <BR> Al-1671famciclovir0 0 0C02H0 0 1CFgCHs Al-1672 famciclovir O O O CO2H O O 1 cyclopropyl Al-1673 famciclovir O O O CO2H O O 1 2-OMe-Ph Al-1674 famciclovir O O O CO2H O O 1 MeSCH2 Al-1675 famciclovir O O O CO2H O O 1 MeOCH2 <BR> <BR> A1-1676 famciclovir O O O C02H S S 1 Ph<BR> <BR> <BR> <BR> A1-1677 famciclovir O O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> A1-1678 famciclovir O 0 O C02H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-1679 famciclovir O O O C02H O S 1 Ph<BR> <BR> <BR> <BR> A1-1680 famciclovir O O O CO2H O S 1 Me Al-1681 fluoxetine HCl N O O CO2H O O 1 methyl Al-1682 fluoxetine HCl N O O CO2H O O 1 C(CH3)3 Al-1683 fluoxetine HCl N O O CO2H O O 1 Ph <BR> <BR> Al-1684 fluoxetine HCl N 0 O CO2H O O 1 4-Me-Ph<BR> <BR> <BR> <BR> A1-1685 fluoxetine HCl N 0 O C02H O O 1 2-pyridyl Al-1686 fluoxetine HCl N O O CO2H O O 1 4-pyridyl Al-1687 fluoxetine HCl N O O CO2H O O 1 2-furyl Al-1688 fluoxetine HCl N O O CO2H O O 1 2-thienyl A1-1689 fluoxetine HC1 N O O C02H--0 C1 Al-1690 fluoxetine HCl N 0 O COzH--0 {N (Et) 3} +Cl- Al-1691 fluoxetine HCl N O O CO2H O O 1 CF3CH2 Al-1692 fluoxetine HCl N O O CO2H O O 1 cyclopropyl Al-1693 fluoxetine HCl N O O CO2H O O 1 2-OMe-Ph Al-1694 fluoxetine HCl N O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1695 fluoxetine HC1 N O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> <BR> A1-1696 fluoxetine HC1 N O O CO2H S S 1 Ph Al-1697 fluoxetine HCl N O O CO2H S S 1 NMe2 <BR> <BR> A1-1698 fluoxetine HC1 N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-1699 fluoxetine HC1 N O O C02H O S 1 Ph Al-1700 fluoxetine HCl N O O CO2H O S 1 Me Al-1701 gabapentin N O O CO2H O O 1 methyl Al-1702 gabapentin N O O CO2H O O 1 C(CH3)3 Al-1703 gabapentin N O O CO2H O O 1 Ph Al-1704 gabapentin N O O CO2H O O 1 4-Me-Ph Al-1705 gabapentin N O O CO2H O O 1 2-pyridyl Al-1706 gabapentin N O O CO2H O O 1 4-pyridyl Al-1707 gabapentin N O O CO2H O O 1 2-furyl Al-1708 gabapentin N O O CO2H O O 1 2-thienyl A1-1709 gabapentin N O O C02H--0 C1 A1-1710 gabapentin N O O CO2H--0 {N (Et) 3}+Cl- <BR> <BR> A1-1711 gabapentin N O O CO2H O O 1 CF3CH2 Al-1712 gabapentin N O O CO2H O O 1 cyclopropyl Al-1713 gabapentin N O O CO2H O O 1 2-OMe-Ph Al-1714 gabapentin N O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1715 gabapentin N O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> <BR> A1-1716 gabapentin N O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> A1-1717 gabapentin N O O CO2H S S 1 NMe2 Al-1718 gabapentin N O O CO2H S S 1 NBn2 Al-1719 gabapentin N O O CO2H O S 1 Ph A1-1720 gabapentin N O O C02H O S 1 Me Al-1721 methylphenidate N O O CO2H O O 1 methyl Al-1722 methylphenidate N O O CO2H O O 1 C(CO3)3 Al-1723 methylphenidate N O O CO2H O O 1 Ph <BR> <BR> A1-1724 methylphenidate N O O C02H O O 1 4-Me-Ph<BR> <BR> <BR> <BR> <BR> A1-1725 methylphenidate N O O CO2H O O 1 2-pyridyl Al-1726 methylphenidate N O O CO2H O O 1 4-pyridyl A1-1727 methylphenidate N O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> <BR> Al-1728 methylphenidate N O O CO2H 0 O 1 2-thienyl<BR> <BR> <BR> <BR> A1-1729 methylphenidate N 0 O CO2H--0 Cl Al-1730 methylphenidate N O O CO2H - - 0 {N (Et) 3} +Cl- Al-1731 methylphenidate N O O CO2H O O 1 CF3CH2 Al-1782 methylphenidate N O O CO2H O O 1 cyclopropyl Al-1733 methylphenidate N O O CO2H O O 1 2-OMe-Ph <BR> <BR> A1-1734 methylphenidate N O O CO2H O O 1 MeSCH2<BR> <BR> <BR> <BR> <BR> A1-1735 methylphenidate N O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> <BR> A1-1736 methylphenidate N O O C02H S S 1 Ph Al-1737 methylphenidate N O O CO2H S S 1 NMe2 <BR> <BR> A1-1738 methylphenidate N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> A1-1739 methylphenidate N O O C02H O S 1 Ph Al-1740 methylphenidate N O O CO2H O S 1 Me Al-1741 olanzapine N O O CO2H O O 1 methyl Al-1742 olanzapine N O O CO2H O O 1 C(CH3)3 Al-1743 olanzapine N O O CO2H O O 1 Ph Al-1744 olanzapine N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1745 olanzapine N O O CO2H O O 1 2-pyridyl Al-1746 olanzapine N O O CO2H O O 1 4-pyridyl Al-1747 olanzapine N O O CO2H O O 1 2-furyl A1-1748 olanzapine N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> A1-1749 olanzapine N O O CO2H--0 C1 A1-1750 olanzapine N O O CO2H--0 {N (Et) 3} +Cl- Al-1751 olanzapine N O O CO2H O O 1 CF3CH2 Al-1752 olanzapine N O O CO2H O O 1 cyclopropyl A1-1753 olanzapine N O O CO2H O O 1 2-OMe-Ph Al-1754 olanzapine N O O CO2H O O 1 MeSCH2 Al-1755 olanzapine N O O CO2H O O 1 MeOCH2 <BR> <BR> A1-1756 olanzapine N O O CO2H S S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1757 olanzapine N O O CO2H S S 1 NMe2<BR> <BR> <BR> <BR> <BR> A1-1758 olanzapine N O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> A1-1759 olanzapine N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1760 olanzapine N O O CO2H O S 1 Me Al-1761 lansoprazole N O O CO2H O O 1 methyl Al-1762 lansoprazole N O O CO2H O O 1 C(CH2)3 Al-1763 lansoprazole N O O CO2H O O 1 Ph Al-1764 lansoprazole N O O CO2H O O 1 4-Me-Ph Al-1765 lansoprazole N O O CO2H O O 1 2-pyridyl Al-1766lansoprazoleNOOC02H0014-pyridyl Al-1767 lansoprazole N O O CO2H O O 1 2-furyl Al-1768 lansoprazole N O O CO2H O O 1 2-thienyl A1-1769 lansoprazole N O O CO2H--0 Cl Al-1770 lansoprazole N O O CO2H - - 0 {N (Et) 3} +Cl- Al-1771 lansoprazole N O O CO2H O O 1 CF3CH2 Al-1772 lansoprazole N O O CO2H O O 1 cyclopropyl <BR> <BR> A1-1773 lansoprazole N O O CO2H O O 1 2-OMe-Ph Al-1774 lansoprazole N O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1775 lansoprazole N O O CO2H O O 1 MeOCH2 Al-1776 lansoprazole N O O CO2H S S 1 Ph Al-1777 lansoprazole N O O CO2H S S 1 NMe2 Al-1778 lansoprazole N O O CO2H S S 1 NBn2 <BR> <BR> A1-1779 lansoprazole N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1780 lansoprazole N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> A1-1781 omeprazole N O O CO2H O O 1 methyl Al-1782 omeprazole N O O CO2H O O 1 C(CH3)3 A1-1783 omeprazole N O O CO2H O O 1 Ph Al-1784 omeprazole N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1785 omeprazole N O O C02H 0 O 1 2-pyridyl Al-1786 omeprazole N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-1787 omeprazole N O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> A1-1788 omeprazole N O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> A1-1789 omeprazole N O O CO2H--0 C1 A1-1790 omeprazole N O O CO2H--0 {N (Et) 3} +Cl- Al-1791 omeprazole N O O CO2H O O 1 CF3CH2 Al-1792 omeprazole N O O CO2H O O 1 cyclopropyl <BR> <BR> A1-1793 omeprazole N O O CO2H O O 1 2-OMe-Ph<BR> <BR> <BR> <BR> A1-1794 omeprazole N O O CO2H O O 1 MeSCH2 Al-1795 omeprazole N O O CO2H O O 1 MeOCH2 Al-1796 omeprazole N O O CO2H S S 1 Ph Al-1797 omeprazole N O O CO2H S S 1 NMe2 Al-1798 omeprazole N O O CO2H S S 1 NBn2 <BR> <BR> A1-1799 omeprazole N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1800 omeprazole N O O CO2H O S 1 Me<BR> <BR> <BR> <BR> A1-1801 omeprazole O O O C02H O O 1 methyl Al-1802 omeprazol O O O CO2H O O 1 C(CH3)3 Al-1803 0 0C02H001Ph Al-1804 omeprazole O O O CO2H O O 1 4-Me-Ph Al-1805 omeprazole O O O CO2H O O 1 2-pyridyl A 1-1806 omeprazole O O O CO2H O O 1 4-pyridyl Al-1807 omeprazole O O O CO2H O O 1 2-furyl <BR> <BR> A1-1808 omeprazole O O O C02H O O 1 2-thienyl Al-1809 omeprazole O O O CO2H - - 0 Cl Al-1810 omeprazole O O O CO2H - - 0 {N (Et) 3} +Cl- Al-1811 omeprazole O O O CO2H O O 1 CF3CH2 Al-1812 omeprazole O O O CO2H O O 1 cyclopropyl <BR> <BR> A1-1813 omeprazole O O O C02H O O 1 2-OMe-Ph Al-1814 omeprazole O O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1815 omeprazole O O O CO2H O O 1 MeOCH2 Al-1816 omeprazole O O O CO2H S S 1 Ph Al-1817 omeprazole O O O CO2H S S 1 NMe2 Al-1818 omeprazole O O O CO2H S S 1 NBn2 <BR> <BR> A1-1819 omeprazole O O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1820 omeprazole O O O CO2H O S 1 Me Al-1821 phentermine O O O CO2H O O 1 methyl Al-1822 phentermine O O O CO2H O O 1 C(CH3)3 Al-1823 phentermine O O O CO2H O O 1 Ph Al-1824 phentermine O O O CO2H O O 1 4-Me-Ph Al-1825 phentermine O O O CO2H O O 1 2-pyridyl Al-1826 phentermine O O O CO2H O O 1 4-pyridyl <BR> <BR> A1-1827 phentermine O O O CO2H O O 1 2-furyl<BR> <BR> <BR> <BR> <BR> A1-1828 phentermine O O O CO2H O O 1 2-thienyl<BR> <BR> <BR> <BR> A1-1829 phentermine O O O C02H--0 C1 A1-1830 phentermine O O O CO2H--0 {N (Et) 3} +Cl- Al-1831 phentermine O O O CO2H O O 1 CF3CH2 Al-1832 phentermine O O O CO2H O O 1 cyclopropyl <BR> <BR> A1-1833 phentermine O O O CO2H O O 1 2-OMe-Ph<BR> <BR> <BR> <BR> A1-1834 phentermine O O O CO2H O O 1 MeSCH2<BR> <BR> <BR> <BR> <BR> A1-1835 phentermine O O O CO2H O O 1 MeOCH2 Al-1836phentermine0 0 0C02HS S 1Ph Al-1837 phentermine O O O CO2H S S 1 NMe2 <BR> <BR> A1-1838 phentermine O O O CO2H S S 1 NBn2<BR> <BR> <BR> <BR> <BR> A1-1839 phentermine O O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1840 phentermine O O 0 COzH O S 1 Me Al-1841 paroxetine N O O CO2H O O 1 methyl Al-1842 paroxetine N O O CO2H O O 1 C(CH3)3 Al-1843 paroxetine N O O CO2H O O 1 Ph Al-1844 paroxetine N O O CO2H O O 1 4-Me-Ph Al-1845 paroxetine N O O CO2H O O 1 2-pyridyl <BR> <BR> Al-1846paroxetineN00C02H0014-pyridyl Al-1847 paroxetine N O O CO2H O O 1 2-furyl Al-1848 paroxetine N O O CO2H O O 1 2-thienyl A1-1849 paroxetine N O O CO2H--0 C1 Al-1850 paroxetine N O O CO2H - - 0 {N (Et) 3} +Cl- Al-1851 paroxetine N O O CO2H O O 1 CF3CH2 <BR> <BR> A1-1852 paroxetine N O O CO2H O O 1 cyclopropyl<BR> <BR> <BR> <BR> <BR> A1-1853 paroxetine N O O CO2H O O 1 2-OMe-Ph Al-1854 paroxetine N O O CO2H O O 1 MeSCH2 <BR> <BR> A1-1855 paroxetine N O O CO2H O O 1 MeOCH2<BR> <BR> <BR> <BR> <BR> A1-1856 paroxetine N O O C02H S S 1 Ph<BR> <BR> <BR> <BR> <BR> A1-1857 paroxetine N O O CO2H S S 1 NMe2 Al-1858 paroxetine N O O CO2H S S 1 NBn2 A1-1859 paroxetine N O O CO2H O S 1 Ph Al-1860 paroxetine N O O CO2H O S 1 Me Al-1861 quinapril N O O CO2H O O 1 methyl Al-1862 quinapril N O O CO2H O O 1 C(CH3)3 Al-1863 quinapril N O O CO2H O O 1 Ph <BR> <BR> A1-1864 quinapril N O O CO2H O O 1 4-Me-Ph Al-1865 quinapril N O O CO2H O O 1 2-pyridyl Al-1866 quinapril N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-1867 quinapril N O O CO2H O O 1 2-furyl A1-1868 quinapril. N O O CO2H O O 1 2-thienyl Al-1869quinaprilN 0 0C02H--0C1 A1-1870 quinapril N 0 O COzH--0 {N (Et) 3} +Cl- Al-1871 quinapril N O O CO2H O O 1 CF3CH2 Al-1872 quinapril N O O CO2H O O 1 cyclopropyl Al-1873 quinapril N O O CO2H O O 1 2-OMe-Ph A1-1874 quinapril N O O CO2H O O 1 MeSCH2<BR> <BR> <BR> <BR> <BR> <BR> A1-1875 quinapril N O O CO2H O O 1 MeOCH2 Al-1876 quinapril N O O CO2H S S 1 Ph Al-1877 quinapril N O O CO2H S S 1 NMe2 Al-1878 quinapril N O O CO2H S S 1 NBn2 <BR> <BR> A1-1879 quinapril N O O CO2H O S 1 Ph<BR> <BR> <BR> <BR> <BR> <BR> A1-1880 quinapril N O O CO2H O S 1 Me Al-1881 sertraline N O O CO2H O O 1 methyl Al-1882 sertraline N O O CO2H O O 1 C(CH3)3 A1-1883 sertraline N O O CO2H O O 1 Ph Al-1884 sertraline N O O CO2H O O 1 4-Me-Ph <BR> <BR> <BR> A1-1885 sertraline N O O CO2H O O 1 2-pyridyl Al-1886 sertraline N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-1887 sertraline N O O C02H 0 O 1 2-furyl Al-1888 sertraline N O O CO2H O O 1 2-thienyl Al-1889 sertraline N O O CO2H - - 0 Cl Al-1890 sertraline N O O CO2H - - 0 {N (Et) 3)'Cl- <BR> <BR> A1-1891 sertraline N O O CO2H O O 1 CF3CH2<BR> <BR> <BR> <BR> <BR> <BR> A1-1892 sertraline N O O CO2H O O 1 cyclopropyl<BR> <BR> <BR> <BR> <BR> <BR> A1-1893 sertraline N O O CO2H O O 1 2-OMe-Ph<BR> <BR> <BR> <BR> <BR> A1-1894 sertraline N O O CO2H O O 1 MeSCH2 Al-1895 sertraline N O O CO2H O O 1 MeOCH2 Al-1896 sertraline N O O CO2H S S 1 Ph Al-1897 sertraline N O O CO2H S S 1 NMe2 Al-1898 sertraline N O O CO2H S S 1 NBn2 A1-1899 sertraline N O O CO2H O S 1 Ph Al-1900 sertraline N O O CO2H O S 1 Me Al-1901 bupropion N O O CO2H O O 1 methyl <BR> <BR> A1-1902 bupropion N O O CO2H O O 1 C (CH3) 3<BR> <BR> <BR> <BR> <BR> <BR> A1-1903 bupropion N O O CO2H O O 1 Ph Al-1904 bupropion N O O CO2H O O 1 4-Me-Ph <BR> <BR> A1-1905 bupropion N O O C02H O O 1 2-pyridyl Al-1906 bupropion N O O CO2H O O 1 4-pyridyl <BR> <BR> A1-1907 bupropion N O O C02H O O 1 2-furyl<BR> <BR> <BR> <BR> <BR> <BR> A1-1908 bupropion N O O C02H O O 1 2-thienyl<BR> <BR> <BR> <BR> <BR> <BR> A1-1909 bupropion N O O C02H--0 C1 A1-1910 bupropion N O O CO2H--0 {N (Et) 3)'Cl- Al-1911 bupropion N O O CO2H O O 1 CF3CH2 Al-1912 bupropion N O O CO2H O O 1 cyclopropyl Al-1913 bupropion N O O CO2H O O 1 2-OMe-Ph Al-1914 bupropion N O O CO2H O O 1 MeSCH2 Al-1915 bupropion N O O CO2H O O 1 MeOCH2 Al-1916 bupropion N O O CO2H S S 1 Ph Al-1917 bupropion N O O CO2H S S 1 NMe2 Al-1918 bupropion N O O CO2H S S 1 NBn2 Al-1919 bupropion N O O CO2H O S 1 Ph A1-1920 bupropion N O O CO2H O S 1 Me

Table A2 : Compounds (A2-1)-(A2-1920) are compounds of Formula I where XI, Z' (X1)m-H, G10,G11, G2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ri which equals C02Me.

Table A3 : Compounds (A3-1)- (A3-1920) are compounds of Formula I where XI, Zl (X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R'which equals CO2Et.

Table A4 : Compounds (A4-1)- (A4-1920) are compounds of Formula I where XI, Z' (X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for RI which equals CO2n-Pr, Table A5 : Compounds (A5-1)- (A5-1920) are compounds of Formula I where XI, Z1 (X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R1 which equals C02t-Bu.

Table A6 : Compounds (A6-1)- (A6-1920) are compounds of Formula I where X1, Z1 (X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ru which equals C02cyclopropyl.

Table A7 : Compounds (A7-1)- (A7-1920) are compounds of Formula I where X1, Z1 (X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R'which equals COzBn.

Table A8 : Compounds (A8-1)-(A8-1920) are compounds of Formula I where Xl, ZI (XI).-H, GIO, G", R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ru which equals CO2CH2CH2Ph.

Table A9 : Compoudns (A9-1)-(A9-1920) are compounds of Formula I where X1, Z' (X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ru which equals C02CH2CFs.

Table A10 : Compounds (A10-1)-(A10-1920) are compounds of Formula I where XI, Z1(X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for RI which equals CO2CH2OMe.

Table All : Compounds (All-l)- (All-1920) are compounds of Formula I where XI, ZI (XI) m-H, G'°, G", R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ru which equals CO2allyl.

Table A12 : Compounds (A12-1)-(A12-1920) are compounds of Formula I where X1, Z1(X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R1 which equals C02Ph.

Table A13 : Compounds (A13-1)-(A13-1920) are compounds of Formula I where XI, ZI (Xl) m-H, Gl°, G", R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for RI which equals CO2-2 (OMe) Ph.

Table A14 : Compounds (A14-1)-(A14-1920) are compounds of Formula I where Xl, Z1 (Xl) m-H, Gl°, G", R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R'which equals C02-3- (OMe) Ph.

Table A15 : Compounds (A15-1)-(A15-1920) are compounds of Formula I where Xl, Z1(X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R'which equals C02-4- (OMe)-Ph.

Table A16 : Compounds (A16-1)-(A16-1920) are compounds of Formula I where X1, Z' (Xl) m-H, G'°, G", R2, G20, G21, m t, q and Z2 are identical to those in Table Al except for R1 which equals CO20-2 (Me) Ph.

Table A17 : Compounds (A17-1)-(A17-1920) are compounds of Formula I where X1, Z1(X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ri which equals CO2-3 (Me) Ph.

Table A18 : Compounds (A18-1)-(A18-1920) are compounds of Formula I where XI, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R'which equals CO2-4 (Me) Ph.

Table A19 : Compounds (A19-1)-(A19-1920) are compounds of Formula I where XI, Zl (X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R1 which equals C02-4 (NO2) Ph.

Table A20 : Compounds (A20-1)- (A20-1920) are compounds of Formula I where X1, ZI (XI) m-H, Gl°, G", R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for RI which equals CO2SiMe3.

Table A21 : Compounds (A21-1)- (A21-1920) are compounds of Formula I where XI, Zl (X1) m-H, Gl°, G", R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ru which equals C (=O) N (H) Me.

Table A22 : Compounds (A22-1)- (A22-1920) are compounds of Formula I where Xi, Z' (Xl) m-H, Gl°, G", R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ri which equals C (=O) NMe2.

Table A23 : Compounds (A23-1)- (A23-1920) are compounds of Formula I where Xi, Z1(X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R1 which equals C (=O) NBn2.

Table A24 : Compounds (A24-1)- (A24-1920) are compounds of Formula I where XI, Z1 (X') m-H, Gl°, Gll, R2, G20o G1, m, t, q and Z2 are identical to those in Table Al except for RI which equals C (=O) N (Me) Bn.

Table A25 : Compounds (A25-1)- (A25-1920) are compounds of Formula I where Xi, Z' (X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for RI which equals C (=O) N (Me) Ph.

Table A26 : Compounds (A26-1)- (A26-1920) are compounds of Formula I where XI, ZI (Xljm-H, G1°, G", R2, G2o, G21, m, t, q and Z2 are identical to those in Table Al except for RI which equals C (=O) N (H) Ph.

Table A27 : Compounds (A27-1)- (A27-1920) are compounds of Formula I where XI, Z1(X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for RI which equals C (=O) N (H) NMe2.

Table A28 : Compounds (A28-1)- (A28-1920) are compounds of Formula I where XI, Z1 (X') m-H, G'°, G", R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ri which equals CO2n-octyl.

Table A29 : Compounds (A29-1)- (A29-1920) are compounds of Formula I where XI, Z1(X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R1 which equals C (=O) N (H) n-Bu.

Table A30 : Compounds (A30-1)- (A30-1920) are compounds of Formula I where X1, Z1(X1)m-H, G10, G11, R2, G20, m, t, q and Z2 are identical to those in Table Al except for R'which equals C (=O) N (H) N (H) CO2Et.

Table A31 : Compounds (A31-1)- (A31-1920) are compounds of Formula I where Xl, ZI (X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ru which equals C (=O) N (H) N (H) CO2t-Bu.

Table A32 : Compounds (A32-1)- (A32-1920) are compounds of Formula I where Xl, Z1(X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ri which equals C (=O) N (H) N=CHMe.

Table A33 : Compounds (A33-1)- (A33-1920) are compounds of Formula I where XI, Zl (X1)m-H, G10, G11, R2, G20,G 21, m, t, q and Z2 are identical to those in Table Al except for R'which equals C (=O) N (H) N=CMe2.

Table A34 : Compounds (A34-1)- (A34-1920) are compounds of Formula I where XI, Z' (X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for RI which equals C (=O) N (H) N=CHPh.

Table A35 : Compounds (A35-1)- (A35-1920) are compounds of Formula I where X', Z1 (Xl) m-H, Gl° G", R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R'which equals C (=O) SPh.

Table A36 : Compounds (A36-1)- (A36-1920) are compounds of Formula I where XI, ZI (Xl) m-H, G10, G", R2, G20, G2l, m, t, q and Z2 are identical to those in Table Al except for Ri which equals C (=O) SEt.

Table A37 : Compounds (A37-1)- (A37-1920) are compounds of Formula I where Xl, Z1 (X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for Ri which equals C (=O) Sn-Bu.

Table A38 : Compounds (A38-1)- (A38-1920) are compounds of Formula I where Xl, Z1 (XI) m-H, Gl°, G", R2, G2o, G21, m, t, q and Z2 are identical to those in Table Al except for R'which equals C (=O) N (H) OMe.

Table A39 : Compounds (A39-1)- (A39-1920) are compounds of Formula I where XI, Z1(X1)m-H, G10, G11, R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for R'which equals C (=O) N (H) OBn.

Table A40 : Compounds (A40-1)- (A40-1920) are compounds of Formula I where XI, Z1 (X') m-H, G'°, G", R2, G2o, G21, m, t, q and Z2 are identical to those in Table Al except for Ru which equals C (=O) N (H) NH2.

Table A41 : Compounds (A41-1)- (A41-1920) are compounds of Formula I where XI, Zl (Xl) m-H, Gl°, G", R2, G20, G21, m, t, q and Z2 are identical to those in Table Al except for RI which equals C (=O) N (H) OH.

Table B1 describes additional examples of compounds of Formula I which can be made using the procedures described hereinbefore, where R2 is hydrogen, m = 0, q = 1, t = 0 or 1 and the pharmaceutical which defines the pharmaceutical moiety of these examples is Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2). The following groups, Z1, G10 Qii, Rl, G20, G21, t, x2 and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2(X2) are defined within Table B1.

Table B1 Cmpd# Z1 G10 G11 R1 G20 G21 t X2 Z2(X2)q-[(C=G20)- G21]t-H or when t = 0, Z2 (X2) q or Z2 (X2) q-H <BR> <BR> B 1-1 Me O O CO2H--0 N bisacodyl<BR> <BR> <BR> <BR> <BR> Bl-2 cyclohexyl O O COzH--0 N bisacodyl<BR> <BR> <BR> <BR> <BR> B 1-3 t-Bu O O CO2H--0 N bisacodyl B1-4 CF3CH2 O O CO2H - - 0 N bisacodyl B 1-5 allyl O O CO2H--0 N bisacodyl B1-6 4-(NO2)Ph O O CO2H - - 0 N bisacodyl B1-7 PhS O O C02H--0 N bisacodyl B 1-8 N (Me) Ph O O CO2H - - 0 N bisacodyl B 1-9 N (H) OMe O O CO2H - - 0 N bisacodyl B1-10 N (H) CO2Et O O CO2H - - 0 N bisacodyl B1-11 Me O O CO2H - - 0 N bupivacaine B1-12 cyclohexyl O O CO2H - - 0 N bupivacine B1-13 t-Bu O O C02H--0 N bupivacaine B1-14 CF3CH2 O O CO2H - - 0 N bupivacine B1-15 allyl O O CO2H - - 0 N bupivacaine B1-16 4-(NO2)Ph O O CO2H - - 0 N bupivacaine B1-17 PhS O O CO2H - - 0 N bupivacaine B1-18-N (Me) Ph O O C02H--0 N bupivacaine B 1-19 N (H) OMe O O C02H-0 N bupivacaine B 1-20 N (H) CO2Et O O CO2H - - 0 N pupivacaine Bl-21 Me O O CO2H--0 N chloroprocaine B1-22 cyclohexyl O O CO2H - - 0 n chloroprocaine Bl-23 t-Bu O O C02H--0 N chloroprocaine B1-24 CF3CH2 O O CO2H - - 0 N chloroprocaine B 1-25 allyl O O C02H--0 N chloroprocaine B1-26 4-(NO2)Ph O O CO2H - - 0 N chloroprocaine Bl-27 PhS O O C02H--0 N chloroprocaine B1-28 N (Me) Ph O O CO2H - - 0 N chloroprocaine B1-29 N (H) OMe O O CO2H - - 0 N chloroprocaine B1-30 N (H) C02Et00C02H--ONchloroprocaine B1-31 Me O O CO2H - - 0 N tetracaine Bl-32cyclohexyl00C02H-0 Ntetracaine <BR> <BR> B 1-33 t-Bu O 0 COzH-0 N tetracaine<BR> <BR> <BR> <BR> <BR> Bl-34 CF3CH2 0 0 CO2H--0 N tetracaine Bl-35 allyl O O CO2H - - 0 N tetracaine Bl-36 4-(NO2)Ph O O CO2H - - 0 N tetracaine <BR> <BR> B 1-37 PhS O O CO2H-0 N tetracaine Bl-38 N (Me) Ph O O CO2H - - 0 N tetracaine Bl-39 N (H) OMe O O CO2H-0 N tetracaine B 1-40 N (H) CO2Et O O CO2H - - 0 N tetracaine Bl-41 Me O O CO2H - - 0 N acrivistine Bl-42 cyclohexyl O O CO2H - - 0 N acrivistine <BR> <BR> Bl-43 t-Bu O 0 CO2H--0 N acrivistine Bl-44 CF3CH2 O O CO2H - - 0 N acrivistine Bl-45 allyl O O CO2H - - 0 N acrivistine Bl-46 4-(NO2)Ph O O CO2H - - 0 N acrivistine Bl-47 PhS O O CO2H - - 0 N acrivistine Bl-48 N (Me) Ph O O CO2H - - 0 N acrivistine Bl-49 N (H) OMe O O CO2H - - 0 N acrivistine Bl-50 N (H) CO2Et O O CO2H - - 0 N acrivistine <BR> <BR> B1-51 Me O 0 CO2H--0 N amiodarone Bl-52 cyclohexyl O O CO2H - - 0 N amiodarone Bl-53 t-Bu O O CO2H - - 0 N amiodarone Bl-54 CF3CH2 0 0 CO2H - - 0 N amiodarone <BR> <BR> B1-55 allyl O O CO2H--0 N amiodarone Bl-56 4-(NO2)Ph O O CO2H - - 0 N amiodarone Bl-57 PhS O O CO2H - - 0 N amiodarone Bl-58 N (Me) Ph O O CO2H - - 0 N amiodarone Bl-59 N (H) OMe O O CO2H - - 0 N amiodarone Bl-60 N (H) CO2Et O O CO2H - - 0 N amiodarone <BR> <BR> B1-61 Me O O CO2H--0 N amitriptyline<BR> <BR> <BR> <BR> <BR> Bl-62 cyclohexyl O 0 C02H--0 N amitriptyline<BR> <BR> <BR> <BR> <BR> B1-63 t-Bu O O C02H--0 N amitriptyline Bl-64CF3CH200C02H-0 Namitriptyline Bl-65 Allyl O O CO2H - - 0 N amitriptyline Bl-66 4-(NO2)PH O O CO2H - - 0 N amitriptyline Bl-67 PhS O O CO2H - - 0 N amitriptyline B 1-68 N (Me) Ph 0 O C02H--0 N amitriptyline B 1-69 N (H) OMe 0 O CO2H-0 N amitriptyline Bl-70 N (H) C02Et00C02H--ONamitriptyline Bl-71 Me O O CO2H - - 0 N amrinone Bl-72 cyclohexyl O O CO2H - - 0 N amrinone Bl-73 t-Bu O O CO2H - - 0 N amrinone Bl-74 CF3CH2 O O CO2H - - 0 N amrinone <BR> <BR> <BR> B 1-75 allyl O O CO2H--0 N amrinone Bl-76 4- (NO2) Ph 0 0 C02H 0 N amrinone B1-77 PhS O O CO2H - - 0 N amrinone Bl-78 N (Me) Ph O 0 C02H--0 N amrinone B 1-79 N (H) OMe O 0 C02H 0 N amrinone B1-80 N (H) CO2Et O O CO2H - - 0 N amrinone <BR> <BR> B1-81 Me O O CO2H--0 N atropine<BR> <BR> <BR> <BR> B 1-82 cyclohexyl 0 O C02H-0 N atropine Bl-83 t-Bu O 0 C02H--0 N atropine Bl-84 CF3CH2 O O CO2H - - 0 N atropine B 1-85 allyl O O CO2H--0 N atropine B 1-86 4- (NO2) Ph0 0 C02H 0 N atropine Bl-87 Phs O O CO2H - - 0 N atropine B 1-88 N (Me) Ph O O CO2H - - 0 N atropine Bl-89 N (H) OMe O 0 COzH--0 N atropine B 1-90 N (H) CO2Et O O CO2H - - 0 N atropine <BR> <BR> Bl-91 Me O 0 CO2H--0 N benzphetamine Bl-92 cyclohexyl O O CO2H - - 0 N benzphetamine <BR> <BR> Bl-93 t-Bu O 0 CO2H--0 N benzphetamine<BR> <BR> <BR> <BR> Bl-94 CF3CH2 O 0 CO2H--0 N benzphetamine Bl-95 allyl O O CO2H - - 0 N benzphetamine Bl-96 4-(NO2)Ph O O CO2H - - 0 N benzphetamine Bl-97 PhS O O CO2H - - 0 N benzphetamine Bl-98 N (Me) Ph O O CO2H - - 0 N benzphetamine Bl-99 N (H) OMe O 0 CO2H--0 N benzphetamine Bl-100 N(H)CO2Et O O CO2H - - 0 N benzphetamine Bl-101 Me O O CO2H - - 0 N beperiden Bl-102 cyclohexyl O O CO2H - - 0 N beperiden Bl-103 t-Bu O O C02H--0 N beperiden Bl-104 CF3CH2 O O CO2H - - 0 N beperiden Bl-105 allyl O O CO2H - - 0 N beperiden <BR> <BR> B1-106 4- (NO2) Ph O 0 CO2H--0 N beperiden<BR> <BR> <BR> <BR> <BR> B 1-107 PhS O O CO2H--0 N beperiden B 1-108 N (Me) Ph O O CO2H - - 0 N beperiden B 1-109 N (H) OMe00C02H-- 0 Nbeperiden Bl-110 N (H) CO2Et O O CO2H - - 90 N beperiden Bl-111 Me O O CO2H - - 0 N bromopheniramine Bl-112 cyclohexyl O O CO2H - - 0 N bromopheniramine Bl-113 t-Bu O O CO2H - - 0 N bromopheniramine Bl-114 CF3CH2 O O CO2H - - 0 N bromopheniramine <BR> <BR> B 1-115 allyl O 0 COzH--0 N bromopheniramine Bl-116 4-(NO2)Ph O O CO2H - - 0 N bromopheniramine Bl-117 PhS O O CO2H - - 0 N bromopheniramine Bl-118 N(Me)Ph O O CO2H - - 0 N bromopheniramine <BR> <BR> B1-119 N (H) OMe O O C02H--0 N bromopheniramine Bl-120 N(H)CO2Et O O CO2H - - 0 N bromopheniramine B 1-121 Me O 0 CO2H--0 N clemastine Bl-122 cyclohexyl O O CO2H - - 0 N clemastine Bl-123 t-Bu O O CO2H - - 0 N clemastine Bl-124 CF3CH2 O O CO2H - - 0 N clemastine Bl-125 allyl O O CO2H - - 0 N clemastine Bl-126 4- (NO2) Ph O 0 COzH--0 N clemastine Bl-127 PhS O O CO2H - - 0 N clemastine Bl-128 N (Me) Ph O O COzH--0 N clemastine Bl-129 N (H) OMe O O COzH--0 N clemastine B 1-130 N (H) CO2Et O O CO2H - - 0 N clemastine B1-131 Me O 0 C02H--0 N clomiphene B1-132 cyclohexyl O O CO2H - - 0 N clomiphene Bl-133 t-Bu O O CO2H - - 0 N clompiphene Bl-134 CF3CH2 O O CO2H - - 0 N clomiphene Bl-135 allyl O O CO2H - - 0 N clomiphene Bl-136 4-(NO2Ph) O O CO2H - - 0 N clomiphene <BR> <BR> B1-137 PhS O O CO2H--0 N clomiphene Bl-138 N(Me)Ph O O CO2H - - 0 N clomiphene B 1-139 N (H) OMe O O CO2H-0 N clomiphene B 1-140 N (H) CO2Et O O CO2H - - 0 N clomiphene <BR> <BR> B1-141 Me O O CO2H--0 N cyclobenzaprine<BR> <BR> <BR> <BR> <BR> <BR> B 1-142 cyclohexyl O O CO2H--0 N cyclobenzaprine<BR> <BR> <BR> <BR> <BR> B 1-143 t-Bu O O CO2H--0 N cyclobenzaprine Bl-144 CF3CH2 O O CO2H - - 0 N cyclobenzaprine Bl-145 allyl O O CO2H - - 0 N cyclobenzaprine Bl-146 4-(NO2)Ph O O CO2H - - 0 N cyclobenzaprine <BR> B1-147 PhS O O CO2H--0 N cyclobenzaprine Bl-148 N (Me) Ph O O CO2H - - 0 N cyclobenzaprine Bl-149 N(H)OMe O O CO2H - - 0 N cyclobenzaprine B1-150 N (H) CO2Et 0 O C02H--0 N cyclobenzaprine<BR> <BR> <BR> <BR> <BR> B1-151 Me O O CO2H--0 N cyclopentolate<BR> <BR> <BR> <BR> <BR> <BR> B 1-152 cyclohexyl O O CO2H--0 N cyclopentolate Bl-153 t-Bu O O CO2H - - 0 N cyclopentolate Bl-154 CF3CH2 O O CO2H - - 0 N cyclopentolate Bl-155 allyl O O CO2H - - 0 N cyclopentolate Bl-156 4-(NO2)Ph O O CO2H - - 0 N cyclopentolate Bl-157 PhS O 0 C02H--0 N cyclopentolate Bl-158 N (Me) Ph O O CO2H - - 0 N cyclopentolate B1-159 N (H) OMe O 0 C02H--0 N cyclopentolate Bl-160 N(H)CO2Et O O CO2H - - 0 N cyclopentolate B 1-161 Me O O CO2H--0 N dicyclomine Bl-162 cyclohexyl O O CO2H - - 0 N dicyclomine B1-163 t-Bu O 0 CO2H--0 N dicyclomine Bl-164 CF3CH2 O O CO2H - - 0 N dicyclomine B 1-165 allyl O O CO2H--0 N dicyclomine Bl-166 4-(NO2)Ph O O CO2H - - 0 N dicyclomine B 1-167 PhS O O CO2H--0 N dicyclomine B 1-168 N (Me) Ph O O CO2H - - 0 N dicyclomine B1-169 N (H) Ome O O CO2H - - 0 N dicyclomine B1-170 N (H) CO2Et O O CO2H - - 0 N dicyclomine B 1-171 Me O O CO2H--0 N diethylproprion<BR> <BR> <BR> <BR> <BR> <BR> B1-172 cyclohexyl O O C02H--0 N diethylproprion<BR> <BR> <BR> <BR> <BR> <BR> B1-173 t-Bu O O CO2H--0 N diethylproprion<BR> <BR> <BR> <BR> <BR> <BR> B1-174 CFsCH2 O O C02H--0 N diethylproprion<BR> <BR> <BR> <BR> <BR> B1-175 allyl O O CO2H--0 N diethylproprion B1-176 4-(NO2)Ph O O CO2H - - 0 N diethylproprion B1-177 PhS O O CO2H--0 N diethylproprion B1-178 N(Me)Ph O O CO2H - - 0 N diethylproprion B1-179 N(H)OMe O O CO2H - - 0 N diethylproprion B1-180 N(H)CO2Et O O CO2H - - 0 N diethylproprion Bl-181 Me O O CO2H - - 0 N diltizem Bl-182 cyclohexyl O O CO2H - - 0 N diltizem B 1-183 t-Bu O O CO2H--0 N diltiazem Bl-184 CF3CH2 O O CO2H - - 0 N diltizem Bl-185 allyl O O CO2H - - 0 N diltizem B 1-186 4- (NO2) Ph O O CO2H-0 N diltiazem Bl-187 PhS O O CO2H - - 0 N diltizem B 1-188 N (Me) Ph O O CO2H - - 0 N diltizem Bl-189 N (H) OMe O O C02H--0 N diltiazem B 1-190 N (H) CO2Et O O CO2H - - 0 N diltizem B1-191 Me O O CO2H--0 N diphenhydramine Bl-192 cyclohexyl O O CO2H - - 0 N diphenhydramine Bl-193 t-Bu O O CO2H - - 0 N diphenhydramine Bl-194 CF3CH2 O O CO2H - - 0 N diphenhydramine Bl-195 allyl O O CO2H - - 0 N diphenhydramine Bl-196 4-(NO2)Ph O O CO2H - - 0 N diphenhydramine Bl-197 PhS O O CO2H - - 0 N diphenhydramine B 1-198 N (Me) Ph 0 O CO2H--0 N diphenhydramine Bl-199 N(H)OMe O O CO2H - - 0 N diphenhydramine B 1-200 N (H) C02Et 0 O CO2H--0 N diphenhydramine<BR> <BR> <BR> <BR> <BR> <BR> Bl-201 Me 0 O CO2H--0 N diphenidol Bl-202 cyclohexyl O O CO2H - - 0 N diphenidol Bl-203 t-Bu O O CO2H - - 0 N diphenidol Bl-204 CF3CH2 O O CO2H - - 0 N diphenidol Bl-205 allyl 0 O CO2H--0 N diphenidol Bl-206 4-(NO2)Ph O O CO2H - - 0 N diphenidol Bl-207 PhS 0 O C02H--0 N diphenidol Bl-208 N (Me) Ph O O CO2H--0 N diphenidol B 1-209 N (H) OMe O O CO2H-0 N diphenidol Bl-210 N (H) CO2Et O O CO2H - - 0 N diphenidol Bl-211 Me 0 0 C02H-0 N diphenoxylate Bl-212 cyclohexyl O O CO2H - 0 N diphenoxylate B1-213 t-Bu O O CO2H--0 N diphenoxylate B l-214 CF3CH2 O O CO2H - - 0 N diphenoxylate Bl-215 allyl O O CO2H--0 N diphenoxylate Bl-216 4-(NO2)Ph O O CO2H - - 0 N diphenoxylate B1-217 PhS O 0 COzH--0 N diphenoxylate B l-218 N(Me)Ph O O CO2H - - 0 N diphenoxylate Bl-219 N(H)OMe O O CO2H - - 0 N diphenoxylate Bl-220 N (H) C02Et00C02H-- 0 Ndiphenoxylate Bl-221 Me O O CO2H--0 N doxapram B 1-222 cyclohexyl O O CO2H - - N doxapram B 1-223 t-Bu O O CO2H--0 N doxapram Bl-224 CF3CH2 O O CO2H - - 0 N doxapram Bl-225 allyl O O CO2H - - 0 N doxapram Bl-226 4-(NO2)Ph O O CO2H - - 0 N doxapram Bl-227 PhS O O CO2H - - 0 N doxapram Bl-228 N (Me) Ph00C02H-- 0 Ndoxapram Bl-229 N (H) OMe O O CO2H - - 0 N doxapram B 1-230 N (H) CO2Et O O CO2H - - 0 N doxapram Bl-231 Me O O CO2H - - 0 N doxepin Bl-232 cyclohexyl O O CO2H--0 N doxepin Bl-233 t-Bu O O CO2H - - 0 N doxepin B 1-234 CF3CH2 O O C02H--0 N doxepin Bl-235 allyl O O CO2H - - 0 N doxepin Bl-236 4-(NO2)Ph O O CO2H 0 N dxoepin Bl-237 PhS O O CO2H 0 N dxoepin Bl-238 N (Me) Ph O O C02H 0 N doxepin Bl-239 N (H) OMe O O CO2H-0 N doxepin Bl-240 N (H) CO2Et O O CO2H-0 N doxepin Bl-241 Me O O CO2H - 0 N fentanyl <BR> <BR> B 1-242 cyclohexyl O O CO2H-0 N fentanyl Bl-243 t-Bu O O CO2H - 0 N fentanyl Bl-244 CF3CH2 O O CO2H - 0 N fentanyl Bl-245 allyl O O CO2H - 0 N fentanyl Bl-246 4-(NO2)Ph O O CO2H - - 0 N fentanyl <BR> <BR> B 1-247 PhS O O CO2H--0 N fentanyl Bl-248 N (Me) Ph O O CO2H - - 0 N fentanyl Bl-249 N (H) OMe O O CO2H - - 0 N fentanyl Bl-250 N (H) CO2Et O O CO2H--0 N fentanyl <BR> <BR> B 1-251 Me O O CO2H--0 N flavoxate Bl-252 cyclohexyl O O CO2H - - 0 N flavoxate Bl-253 b-Bu O O CO2H - - 0 N flavoxate Bl-254 CF3-CH2 O O CO2H - - 0 N flavoxate <BR> <BR> B 1-255 allyl O O CO2H--0 N flavoxate Bl-256 4-(NO2)Ph O O CO2H - - 0 N flavoxate <BR> <BR> B 1-257 PhS O O CO2H--0 N flavoxate Bl-258 N (Me) Ph O O CO2H - - 0 N flavoxate Bl-259 N (H) OMe O O CO2H - - 0 N flavoxate B1-260 N (H) CO2Et O O CO2H - - 0 N flavoxate <BR> <BR> B1-261 Me O O CO2H--0 N flurazepam<BR> <BR> <BR> <BR> <BR> <BR> B 1-262 cyclohexyl O O CO2H--0 N flurazepam Bl-263 t-Bu O O CO2H - - 0 N flurazepam Bl-264 CF3CH2 O O CO2H - 0 N flurazepam <BR> <BR> B 1-265 allyl O O CO2H--0 N flurazepam Bl-266 4-(NO2)Ph O O CO2H - - 0 N flurazepam <BR> <BR> B1-267 PhS O O CO2H--0 N flurazepam Bl-268 N (Me) Ph O O CO2H - - 0 N flurazepam B1-269 N (H) Ome O O CO2H - - 0 N flurazepam Bl-270 N (H) CO2Et O O CO2H - - 0 N flurazepam B1-271 Me O O CO2H--0 N levomethadyl Bl-272 cyclohexyl O 0 CO2H--0 N levomethadyl Bl-273 t-Bu O O CO2H - - 0 N levomethadyl Bl-274 CF3CH2 O O CO2H - - 0 N levomethadyl Bl-275 allyl O O CO2H - - 0 N levomethadyl Bl-276 4-(NO2)Ph O O CO2H - - 0 N levomethadyl B 1-277 PhS O O CO2H--0 N levomethadyl Bl-278 N (Me) Ph O O CO2H - - 0 N levomethadyl B1-279 N (H) OMe O 0 CO2H--0 N levomethadyl B 1-280 N (H) CO2Et O O CO2H - - 0 N levomethadyl Bl-281 Me O O CO2H - - 0 N loratadine Bl-282 cyclohexyl O O CO2H - - 0 N loratadine Bl-283 t-Bu O O CO2H - - 0 N loratadine Bl-284 CF3CH2 O O CO2H - - 0 N loratadine Bl-285 allyl O O CO2H - - 0 N loratadine Bl-286 4-(NO2)Ph O O CO2H - - 0 N loratadine Bl-287 PhS O O COzH--0 N loratadine Bl-288 N (Me) Ph O O CO2H - - 0 N loratadine Bl-289 N (H) OMe O O CO2H - - 0 N loratadine Bl-290 N (H) C02Et 0 O COzH--0 N loratadine <BR> <BR> B1-291 Me O O CO2H--0 N mechlorethamine Bl-292 cyclohexyl O O CO2H - - 0 N mechlorethamine Bl-293 t-Bu O O CO2H - - 0 N mechlorethamine Bl-294 CF3CH2 O O CO2H - - 0 N mechlorethamine Bl-295 allyl O O CO2H - - 0 N mechlorethamine Bl-296 4- (NO2) Ph0 0 C02H 0 N mechlorethamine Bl-297 Phs O O CO2H - - 0 N mechlorethamine B 1-298 N (Me) Ph O O CO2H - - 0 N mechlorethamine B 1-299 N (H) Ome O O CO2H - - 0 N mechlorethamine B 1-300 N (H) CO2Et O O CO2H - - 0 N mechlorethamine Bl-301 Me O O CO2H - - 0 N meperidine <BR> <BR> B 1-302 cyclohexyl O O CO2H--0 N meperidine<BR> <BR> <BR> <BR> <BR> B1-303 t-Bu O O CO2H--0 N meperidine<BR> <BR> <BR> <BR> <BR> B1-304 CF3CH2 O O CO2H-0 N meperidine<BR> <BR> <BR> <BR> B1-305 allyl O O CO2H--0 N meperidine Bl-306 4-(NO2)Ph Me O O CO2H - - 0 N meperidine <BR> <BR> B1-307 PhS O O C02H--0 N meperidine Bl-308 N (Me) Ph Me O O CO2H - - 0 N meperidine Bl-309 N (H) OMe O O CO2H--0 N meperidine Bl-310 N(H)CO2Et Me O O CO2H - - 0 N meperidine Bl-311 Me O O CO2H - - 0 N mepivacaine B cyclohexyl O O CO2H - - 0 N mepivacaine <BR> <BR> Bl-313 t-Bu O O CO2H--0 N mepivacaine<BR> <BR> <BR> <BR> <BR> B1-314 CF3CH2 O O CO2H--0 N mepivacaine<BR> <BR> <BR> <BR> <BR> B1-315 allyl O O CO2H--0 N mepivacaine Bl-316 4-(NO2)Ph O O CO2H - - 0 N mepivacaine <BR> <BR> B1-317 PhS O O CO2H--0 N mepivacaine Bl-318 N (Me) Ph O O CO2H-0 N mepivacaine Bl-319 N (H) OMe O O CO2H-0 N mepivacaine Bl-320 N(H)CO2Et O O CO2H - - 0 N mepivacaine Bl-321 Me O O CO2H - - 0 N methadone Bl-322 cyclohexyl O O CO2H - - 0 N methadone <BR> <BR> Bl-323 t-Bu O O CO2H--0 N methadone Bl-324 CF3CH2 O O CO2H - - 0 N methadone Bl-325 allyl O O CO2H - - 0 N methadone Bl-326 4-(NO2)Ph O O CO2H - - 0 N methadone Bl-327 PhS O O CO2H - - 0 N methadone Bl-328 N (Me) Ph O O CO2H - - 0 N methadone Bl-329 N (H) OMe O O CO2H - - 0 N methadone Bl-330 N (H) CO2Et O O C02H-0 N methadone Bl-331 Me O O CO2H - - 0 N minoxidil <BR> <BR> B1-332 cyclohexyl O O C02H--0 N minoxidil<BR> <BR> <BR> <BR> <BR> B1-333 t-Bu O O C02H--0 N minoxidil<BR> <BR> <BR> <BR> <BR> B 1-334 CFsCH2 O 0 COzH--0 N minoxidil Bl-335 allyl O O CO2H - - 0 N minoxidil Bl-336 4-(NO2)Ph O O CO2H - - 0 N minoxidil Bl-337 PhS O O CO2H - - 0 N minoxidil Bl-338 N (Me) Ph O O CO2H-O N minoxidil Bl-339 N (H) OMe O O CO2H-0 N minoxidil Bl-340 N (H) CO2Et O O CO2H - - 0 N minoxidil Bl-341 Me O O CO2H - - 0 N naftifine B1-342 cyclohexyl O 0 C02H--0 N naftifine Bl-343 t-Bu O O CO2H - - 0 N naftifine Bl-344 CF3CH2 O O CO2H - - 0 N naftifine Bl-345 allyl O O CO2H - - 0 N naftifine Bl-346 4-(NO2)Ph O O CO2H - - 0 N naftifine Bl-347 PhS 0 O CO2H--0 N naftifine B 1-348 N (Me) Ph O O CO2H--0 N naftifine Bl-349 N (H) OMe 0 O CO2H-0 N naftifine B 1-350 N (H) CO2Et O O CO2H - - 0 N naftifine B 1-351 Me O O CO2H--0 N orphenadrine B 1-352 cyclohexyl O O CO2H - - 0 N orphenadrine Bl-353 t-Bu O O CO2H - - 0 N orphenadrine Bl-354 CF3CH2 O O CO2H - - 0 N orphenadrine B 1-355 allyl O O CO2H--0 N orphenadrine<BR> <BR> <BR> <BR> <BR> B 1-356 4-(NO2) Ph O O CO2H-0 N orphenadrine Bl-357 PhS O O CO2H - - 0 N orphenadrine Bl-358 N (Me) Ph O O CO2H-0 N orphenadrine B 1-359 N (H) OMe O O C02H--0 N orphenadrine Bl-360 N (H) C02Et O O CO2H-0 N orphenadrine B 1-361 Me O O CO2H--0 N oxybutynin Bl-362 cyclohexyl O O CO2H - - 0 N oxybutynin Bl-363 t-Bu O O CO2H - - 0 N oxybutynin Bl-364 CF3CH2 O O CO2H - - 0 N oxybutynin Bl-365allyl00C02H--0 Noxybutynin Bl-366 4-(NO2)Ph O O CO2H - - 0 N oxybutynin Bl-367 PhS O O CO2H - - 0 N oxybutynin Bl-368 N (Me) Ph O O CO2H - - 0 N oxybutynin Bl-369 N (H) OMe O O CO2H-0 N oxybutynin Bl-370 N (H) CO2Et O O CO2H-0 N oxybutynin Bl-371 Me O O CO2H - - 0 N oxymetazoline Bl-372 cyclohexyl O O CO2H - - 0 N oxymetazoline Bl-373 t-Bu O O CO2H - - 0 N oxymetazoline Bl-374 CF3CH2 O O CO2H - - 0 N oxymetazoline Bl-375 allyl O O CO2H - - 0 N oxymetazoline Bl-376 4-(NO2)Ph O O CO2H - - 0 N oxymetazoline Bl-377 PhS 0 0 C02H-0 N oxymetazoline Bl-378 N (Me) Ph O O CO2H - - 0 N oxymetazoline B1-379 N (H) OMe O O C02H--0 N oxymetazoline<BR> <BR> <BR> <BR> <BR> B1-380 N (H) CO2Et O O CO2H-0 N oxymetazoline Bl-381 Me O O CO2H--0 N phenoxybenzamine B1-382 cyclohexyl O 0 C02H--0 N phenoxybenzamine Bl-383 t-Bu O O CO2H - - 0 N phenoxybenzamine B1-384 CH3CH2 O O CO2H - - 0 N phenoxybenzamine B 1-385 allyl O O C02H--0 N phenoxybenzamine Bl-386 4-(NO2)Ph O O CO2H - - 0 N phenoxybenzamine B1-387 PhS O O C02H-0 N phenoxybenzamine Bl-388 N (Me) Ph O 0 C02H--0 N phenoxybenzamine Bl-389 N(H)OMe O O CO2H - - 0 N phenoxybenzamine Bl-390 N(H)CO2Et O O CO2H - - 0 N phenoxybenzamine Bl-391 Me O O CO2H - - 0 N pilocarpine <BR> <BR> B1-392 cyclohexyl O O C02H--0 N pilocarpine<BR> <BR> <BR> <BR> <BR> B 1-393 t-Bu O O CO2H--0 N pilocarpine Bl-394 CF3CH2 O O CO2H - - 0 N pilocarpine <BR> <BR> B1-395 allyl O O CO2H--0 N pilocarpine<BR> <BR> <BR> <BR> <BR> Bl-396 4- (NO2) Ph O O CO2H--0 N pilocarpine<BR> <BR> <BR> <BR> <BR> B1-397 PhS O O CO2H--0 N pilocarpine Bl-398 N (Me) PH O O CO2H - - 0 N pilocarpine Bl-399 N (H) OMe00C02H-- 0 Npilocarpine B 1-400 N (H) CO2Et O O CO2H - - 0 N pilocarpine <BR> <BR> B 1-401 Me O O CO2H--0 N pyrazinamide<BR> <BR> <BR> <BR> <BR> B 1-402 cyclohexyl O O CO2H--0 N pyrazinamide<BR> <BR> <BR> <BR> <BR> B 1-403 t-Bu O O CO2H--0 N pyrazinamide<BR> <BR> <BR> <BR> <BR> B 1-404 CF3CH2 O O CO2H--0 N pyrazinamide B 1-405 allyl O O CO2H--0 N pyrazinamide Bl-406 4-(NO2)Ph O O CO2H - - 0 N pyrazinamide Bl-407 PhS O O CO2H - - 0 N pyrazinamide Bl-408 N (Me) Ph O O CO2H - - 0 N pyrazinamide <BR> <BR> B 1-409 N (H) OMe 0 O CO2H--0 N pyrazinamide Bl-410 N (H) C02Et O O CO2H--0 N pyrazinamide Bl-411 Me O O CO2H - - 0 N pyroxidine Bl-412 cyclohexyl O O CO2H - - 0 N pyroxidine B1-413 t-Bu O O CO2H--0 N pyroxidine Bl-414 CF3CH2 O O CO2H - - 0 N pyroxidine <BR> <BR> B1-415 allyl O O CO2H--0 N pyroxidine<BR> <BR> <BR> <BR> <BR> B 1-416 4- (NO2) Ph 0'0 C02H-0 N pyroxidine<BR> <BR> <BR> <BR> <BR> Bl-417PhS00C02H--0 Npyroxidine B 1-418 N (Me) Ph O O CO2H - - 0 N pyroxidine Bl-419 N (H) OMe O O CO2H - - 0 N pyroxidine Bl-420 N (H) CO2Et O O CO2H - - 0 N pyroxidine Bl-421 Me O O CO2H - - 0 N risperidone Bl-422 cyclohexyl O O CO2H - - 0 N risperidone Bl-423 t-Bu O O CO2H - - 0 N risperidone Bl-424 CF3CH2 O O CO2H - - 0 N risperidone Bl-425 allyl O O CO2H - - 0 N risperidone Bl-426 4-(NO2)Ph O O CO2H - - 0 N risperidone B 1-427 PhS O O CO2H--0 N risperidone Bl-428 N(Me)Ph O O CO2H - - 0 N risperidone B 1-429 N (H) OMe O O CO2H-0 N risperidone Bl-430 N(H)CO2Et O O CO2H - - 0 N risperidone Bl-431 Me O O CO2H - - 0 N sufentanil B 1-432 cyclohexyl O O CO2H-0 N sufentanil Bl-433 t-Bu O O CO2H - - 0 N sufentanil Bl-434 CF3CH2 O O CO2H - - 0 N sufentanil Bl-435 allyl O O CO2H - - 0 N sufentanil Bl-436 4-(NO2)Ph O O CO2H - - 0 N sufentanil Bl-437 PhS O O CO2H - - 0 N sufentanil Bl-438 N (Me) Ph O O CO2H-0 N sufentanil Bl-439 N (H) OMe O O CO2H - - 0 N sufentanil B 1-440 N (H) C02Et O O CO2H-0 N surentanil Bl-441 Me O O CO2H - - 0 N tamoxifen Bl-442 cyclohexyl O O CO2H - - 0 N tamoxifen <BR> <BR> B 1-443 t-Bu O O CO2H--0 N tamoxifen Bl-444 CF3CH2 O O CO2H - - 0 N tamoxifen Bl-445 allyl O O CO2H - - 0 N tamoxifen Bl-446 4-(NO2)Ph O O CO2H - - 0 N tamoxifen Bl-447 PhS O O CO2H - - 0 N tamoxifen B 1-448 N (Me) Ph O O CO2H - - 0 N tamoxifen B 1-449 N (H) OMe O 0 C02H--0 N tamoxifen Bl-450 N (H) CO2Et O 0 C02H--0 N tamoxifen <BR> <BR> B1-451 Me O O C02H--0 N terbinafine Bl-452 cyclohexyl O O CO2H - - 0 N terbinafine <BR> <BR> Bl-453 t-Bu O O CO2H--0 N terbinafine Bl-454 CF3CH2 O O CO2H - - 0 N terbinafine <BR> <BR> B 1-455 allyl O O CO2H--0 N terbinafine Bl-456 4-(NO2)Ph O O CO2H - - 0 N terbinafine Bl-457 PhS O O CO2H - - 0 N terbinafine B 1-458 N (Me) Ph O O C02H--0 N terbinafine B 1-459 N (H) OMe O O CO2H--0 N terbinafine B 1-460 N (H) CO2Et O O CO2H-0 N terbinafine Bl-461 Me O O CO2H - - 0 N trihexyphenidyl B 1-462 cyclohexyl O O C02H--0 N trihexyphenidyl Bl-463 t-Bu O O CO2H - - 0 N trihexyphenidyl Bl-464 CF3CH2 O O CO2H - - 0 N trihexyphenidyl Bl-465 allyl O O CO2H - - 0 N trihexyphenidyl Bl-466 4-(NO2)Ph O O CO2H - - 0 N trihexyphenidyl Bl-467 PhS O O CO2H - - 0 N trihexyphenidyl <BR> <BR> B1-468. N (Me) Ph O 0 C02H--0 N trihexyphenidyl B 1-469 N (H) OMe O O CO2H - - 0 N trihexyphenidyl Bl-470 N (H) CO2Et O O CO2H - - 0 N trihexyphenidyl <BR> <BR> Bl-471 Me O O C02H--0 N troleandomycin B 1-472 cyclohexyl O O CO2H--0 N troleandomycin Bl-473 t-Bu O O CO2H - - 0 N troleandomycin B 1-474 CF3CH2 O O CO2H - - 0 N troleandomycin B 1-475 allyl O O CO2H--0 N troleandomycin Bl-476 4-(NO2)Ph O O CO2H - - 0 N troleandomycin Bl-477 PhS O O CO2H - - 0 N troleandomycin B 1-478 N (Me) Ph00C02H--0Ntroleandomycin B 1-479 N (H) OMe O O CO2H - - 0 N troleandomycin Bl-480 N(H)CO2Et O O CO2H - - 0 N troleandomycin Bl-481 Me O O CO2H - - 0 N verapamil Bl-482 cyclohexyl O O CO2H - - 0 N verapamil <BR> <BR> Bl-483 t-Bu O O CO2H--0 N verapamil<BR> <BR> <BR> <BR> <BR> B 1-484 CF3CH2 O O CO2H--0 N verapamil<BR> <BR> <BR> <BR> <BR> B 1-485 allyl O O CO2H--0 N verapamil<BR> <BR> <BR> <BR> <BR> <BR> B 1-486 4-(NO2) Ph O O CO2H--0 N verapamil<BR> <BR> <BR> <BR> <BR> B 1-487 PhS O O CO2H--0 N verapamil Bl-488 N (Me) Ph O O C02H--0 N verapamil B 1-489 N (H) OMe O O CO2H--0 N verapamil B 1-490 N (H) CO2Et O O CO2H - - 0 N verapamil B 1-491 Me O O CO2H-0 N caffeine<BR> <BR> <BR> <BR> <BR> <BR> B 1-492 cyclohexyl O O CO2H-0 N caffeine Bl-493 t-Bu O O CO2H - - 0 N caffeine Bl-494 CF3CH2 O O CO2H - - 0 N caffeine Bl-495 allyl O O CO2H - - 0 N caffeine Bl-496 4-(NO2)Ph O O CO2H - - 0 N caffeine Bl-497. PhS00C02H--0Ncaffeine Bl-498 N (Me) Ph O O C02H-. 0 N caffeine B 1-499 N (H) OMe O O C02H--0 N caffeine Bl-500 N (H) CO2Et O O CO2H - - 0 N caffeine <BR> <BR> B1-501 Me O O CO2H--0 N cyproheptadine Bl-502 cyclohexyl O O CO2H - - 0 N cyproheptadine Bl-503 t-Bu O O CO2H - - 0 N cyproheptadine Bl-504 CF3CH2 O O CO2H - - 0 N cyproheptadine Bl-505 allyl O O CO2H - 0 N cyproheptadine Bl-506 4-(NO2)Ph O O CO2H - 0 N cyproheptadine Bl-507 PhS O O CO2H - 0 N cyproheptadine Bl-508 N (Me) Ph O O CO2H-0 N cyproheptadine Bl-509 N (H) OMe O 0 C02H-0 N cyproheptadine Bl-510 N (H) CO2Et O O CO2H--0 N cyproheptadine Bl-511 Me O O CO2H - 0 N pramoxine B1-512 cyclohexyl O O CO2H--0 N pramoxine Bl-513 t-Bu O O CO2H - 0 N pramoxine Bl-514 CF3CH2 O O CO2H - 0 N pramoxine Bl-515 allyl O O CO2H - - 0 N pramoxine Bl-516 4-(NO2)Ph O O CO2H - - 0 N pramoxine Bl-517 PhS O O CO2H - 0 N pramoxine Bl-518 N (Me) Ph00C02H--0Npramoxine Bl-519 N (H) OMe O O CO2H - - 0 N pramoxine Bl-520 N (H) C02Et00C02H--0Npramoxine <BR> B1-521 Me O O CO2H--0 O iodoquinol Bl-522 cyclohexyl O O CO2H - - 0 O iodoquinol Bl-523 t-Bu O O CO2H - - 0 O iodoquinol B1-524CF3CH200C02H--00iodoquinol Bl-525 allyl O O CO2H - - 0 O iodoquinol Bl-526 4-(NO2)Ph O O CO2H - - O N iodoquinol <BR> B 1-527 PhS O O CO2H-0 O iodoquinol Bl-528 N (Me) Ph00C02H--00iodoquinol <BR> B 1-529 N (H) OMe O O CO2H--0 O iodoquinol Bl-530 N (H) CO2Et O O C02H--0 O iodoquinol Bl-531 Me O O CO2H - - 0 O metronidazole <BR> <BR> B 1-532 cyclohexyl O O CO2H--0 O metronidazole Bl-533 t-Bu O O CO2H - - 0 O metronidazole B 1-534 CF3CH2 O O CO2H-0 O metronidazole <BR> <BR> Bl-535 allyl O O C02H-0 0 metronidazole Bl-536 4-(NO2)Ph O O CO2H - - 0 O metronidazole <BR> <BR> B1-537 PhS O O CO2H--0 O metronidazole Bl-538 N (Me) Ph O O CO2H--0 O metronidazole Bl-539 N (H) OMe O O CO2H--0 O metronidazole <BR> <BR> B1-540 N (H) CO2Et O O CO2H--0 O metronidazole B1-541 Me O O CO2H - - 0 N papaverine Bl-542 cyclohexyl O O CO2H - 0 N papaverine Bl-543 t-Bu O O CO2H - - 0 N papaverine Bl-544 CF3CH2 O O CO2H - - 0 N papaverine Bl-545 allyl O O CO2H - - 0 N papaverine <BR> <BR> B1-546 4-(NO2) Ph O O CO2H 0 N papaverine<BR> <BR> <BR> <BR> <BR> <BR> B 1-547 PhS O O CO2H--0 N papaverine Bl-548 N (Me) Ph O O C02H--0 N papaverine Bl-549 N (H) OMe O O CO2H - - 0 N papaverine Bl-550 N (H) CO2Et O O CO2H--0 N papaverine Bl-551 Me O O CO2H - - 0 N tropicamide Bl-552 cyclohexyl O 0 C02H--0 N tropicamide Bl-553 t-Bu O O CO2H - 0 N tropicamide B1-554 CF3CH2 O O CO2H-0 N tropicamide Bl-555 allyl O O CO2H - - 0 N tropicamide <BR> <BR> B1-556 4-(NO2) Ph O O CO2H-0 N tropicamide<BR> <BR> <BR> <BR> <BR> B1-557 PhS O O C02H--0 N tropicamide Bl-558 N (Me) Ph00C02H--0Ntropicamide Bl-559 N (H) OMe00C02H--0Ntropicamide Bl-560 N (H) CO2Et O O CO2H - - 0 N tropicamide B1-561 Me O O CO2H--0 N halazepam<BR> <BR> <BR> <BR> <BR> B1-562 cyclohexyl O O CO2H--0 N halazepam<BR> <BR> <BR> <BR> <BR> B1-563 t-Bu O 0 C02H--0 N halazepam Bl-564 CF3CH2 O O CO2H - - 0 N halazepam Bl-565 allyl O O CO2H - - 0 N halazepam Bl-566 4-(NO2)Ph O O CO2H - 0 N halazepam Bl-567 PhS O O CO2H - 0 N halazepam B 1-568 N (Me) Ph O 0 C02H-0 N halazepam B 1-569 N (H) OMe O O CO2H--0 N halazepam B 1-570 N (H) CO2Et O O CO2H-0 N halazepam B1-571 Me O O CO2H--0 O mazindol Bl-572 cyclohexyl O O CO2H - - 0 O mazindol B 1-573 t-Bu O O CO2H--0 O mazindol Bl-574 CF3CH2 O O CO2H - - 0 O mazindol Bl-575 allyl O O CO2H - 0 O mazindol Bl-576 4-(NO2)Ph O O CO2H - 0 O mazindol Bl-577 PhS O O CO2H - 0 O mazindol Bl-578 N (Me) Ph O O CO2H - 0 O mazindol Bl-579 N (H) OMe O O CO2H--0 O mazindol Bl-580 N (H) C02Et00C02H--00mazindol Bl-581 Me O O CO2H - - 0 O hydroxyitraconazole <BR> <BR> B 1-582 cyclohexyl O O CO2H--0 O hydroxyitraconazole Bl-583 t-Bu O O CO2H - - 0 O hydroxyitraconazole Bl-584 CF3CH2 O O CO2H - - 0 O hydroxyitraconazole Bl-585 allyl O O CO2H - - 0 O hydroxyitraconazole <BR> <BR> B1-586 4- (NO2) Ph 0 O CO2H--0 O hydroxyitraconazole Bl-587 PhS O O CO2H - - 0 O hydroxyitraconazole Bl-588 N (Me) Ph 0 O CO2H--0 O hydroxyitraconazole Bl-589 N (H) OMe O O COzH--0 O hydroxyitraconazole Bl-590 N (H) C02Et O O CO2H--0 O hydroxyitraconazole Bl-591 Me O O CO2H - - 0 O posaconazole Bl-592 cyclohexyl O O CO2H - - 0 O posaconazole B 1-593 t-Bu O O CO2H--0 O posaconazele Bl-594 CF3CH2 O O CO2H - - 0 O posaconazole <BR> <BR> B1-595 allyl O O CO2H--0 O posaconazole<BR> <BR> <BR> <BR> B1-596 4-(NO2) Ph O O CO2H--0 O posaconazole<BR> <BR> <BR> <BR> <BR> B 1-597 PhS O O CO2H--0 O posaconazole B 1-598 N (Me) Ph O O CO2H--0 O posaconazole Bl-599 N (H) OMe O O CO2H - - 0 O posaconazole <BR> <BR> B 1-600 N (H) CO2Et O O C02H--0 O posaconazole<BR> <BR> <BR> <BR> <BR> B1-601 Me O O CO2H--0 O voriconazole Bl-602 cyclohexyl O O CO2H - - 0 O voriconazole <BR> <BR> B 1-603 t-Bu O O CO2H--0 O voriconazole Bl-604 CF3CH2 O O CO2H - - 0 O voriconazole Bl-605 allyl O O CO2H - - 0 O voriconazole Bl-606 4-(NO2)Ph O O CO2H - - 0 O voriconazole Bl-607 PhS O O CO2H - - 0 O voriconazole B 1-608 N (Me) Ph O O CO2H - - 0 O voriconazole B 1-609 N (H) OMe O O CO2H--0 O voriconazole Bl-610 N (H) CO2Et O O CO2H - - 0 O voriconazole <BR> <BR> B 1-611 Me O O CO2H--0 O fluconazole Bl-612 cyclohexyl O O CO2H - - 0 O fluconazole Bl-613 t-Bu O O CO2H - - 0 O fluconazole B1-614 CF3CH2 O O CO2H - - 0 O fluconazole Bl-615 allyl O O CO2H - - 0 O fluconazole Bl-616 4-(NO2)Ph O O CO2H - - 0 O fluconazole <BR> <BR> B1-617 PhS O O CO2H--0 O fluconazole Bl-618 N(Me)Ph O O CO2H - - 0 O fluconazole Bl-619 N (H) OMe00C02H--00fluconazole B 1-620 N (H) CO2Et O O C02H--0 O fluconazole Bl-621 Me O O CO2H - - 0 O genaconazole Bl-622 cyclohexyl O O CO2H - - 0 O genaconazole Bl-623 t-Bu O O CO2H - - 0 O genaconazole Bl-624 CF3CH2 O O CO2H - - 0 O genaconazole Bl-625 allyl O O CO2H - - 0 O genaconazole Bl-626 4-(NO2)Ph O O CO2H - - 0 O genaconazole Bl-627 PhS O O CO2H - - 0 O genaconazole B 1-628 N (Me) Ph00C02H--00genaconazole B 1-629 N (H) OMe00C02H--00genaconazole Bl-630 N (H) CO2Et O 0 C02H--0 O genaconazole Bl-631 Me O O CO2H - - 0 N aliconazole B 1-632 cyclohexyl O O CO2H - - 0 N aliconazole <BR> <BR> B 1-633 t-Bu O O CO2H--0 N aliconazole Bl-634 CF3CH2 O O CO2H - - 0 N aliconazole Bl-635 allyl O O CO2 H - - 0 N aliconazole Bl-636 4-(NO2)Ph O O CO2H - - 0 N aliconazole B 1-637 PhS O O CO2H - - 0 N aliconazole B 1-638 N (Me) Ph O O CO2H--0 N aliconazole Bl-639 N (H) OMe O O CO2H-0 N aliconazole Bl-640 N (H) C02Et00C02H--0Naliconazole Bl-641 Me O O CO2H - - 0 N becliconazole B 1-642 cyclohexyl O O CO2H - - 0 N becliconazole Bl-643 t-Bu O O CO2H - - 0 N becliconazole Bl-644 CF3CH2 O O CO2H - 0 N becliconazole <BR> <BR> B 1-645 allyl O O CO2H--0 N becliconazole Bl-646 4-(NO2)Ph O O CO2H - - 0 N becliconazole Bl-647 PhS O O CO2H - - 0 N becliconazole B 1-648 N (Me) Ph O O CO2H - - 0 N becliconazole Bl-649 N (H) OMe O O CO2H - - 0 N becliconazole Bl-650 N(H)CO2Et O O CO2H - - 0 N becliconazole <BR> <BR> B 1-651 Me O O C02H--0 N brolaconazole B l-652 cyclohexyl O O CO2H - - 0 N brolaconazole <BR> <BR> B1-653 t-Bu O O C02H--0 N brolaconazole B l-654 CF3CH2 O O CO2H - - 0 N brolaconazole <BR> <BR> B 1-655 allyl O O CO2H--0 N brolaconazole B 1-656 4- (NO2) Ph O O C02H--0 N brolaconazole <BR> <BR> B 1-657 PhS O O CO2H--0 N brolaconazole Bl-658 N (Me) Ph O O CO2H - - 0 N brolaconazole Bl-659 N(H)OMe O O CO2H - - 0 N brolaconazole Bl-660 N(H)CO2Et O O CO2H - - 0 N brolaconazole Bl-661 Me O O CO2H - - 0 N butaconazole B 1-662 cyclohexyl O O CO2H--0 N butaconazole <BR> <BR> Bl-663 t-Bu O O CO2H--0 N butaconazole<BR> <BR> <BR> <BR> <BR> <BR> B 1-664 CF3CH2 O O CO2H--0 N butaconazole Bl-665 allyl O O CO2H - - 0 N butaconazole Bl-666 4-(NO2)Ph O O CO2H - - 0 N butaconazole <BR> <BR> B 1-667 PhS O O CO2H--0 N butaconazole B 1-668 N (Me) Ph O O CO2H - - 0 N butaconazole Bl-669 N (H) OMe O O CO2H--0 N butaconazole B 1-670 N (H) CO2Et O O CO2H - - 0 N butaconazole <BR> <BR> Bl-671 Me O O C02H--0 N clotrimazole B 1-672 cyclohexyl O O CO2H--0 N clotrimazole <BR> <BR> B 1-673 t-Bu O O CO2H--0 N clotrimazole Bl-674 CF3CH2 O O CO2H - - 0 N clotrimazole B 1-675 allyl O O CO2H--0 N clotrimazole B l-676 4-(NO2)Ph O O CO2H - - 0 N clotrimazole <BR> <BR> B 1-677 PhS O O CO2H--0 N clotrimazole Bl-678 N (Me) Ph O O CO2H - - 0 N clotrimazole Bl-679 N (H) OMe O O CO2H - - 0 N clotrimazole Bl-680 N(H)CO2Et O O CO2H - - 0 N clotrimazole Bl-681 Me O O CO2H - - 0 N croconazole B 1-682 cyclohexyl O O CO2H--0 N croconazole <BR> <BR> B 1-683 t-Bu O O CO2H--0 N croconazole Bl-684 CF3CH2 O O CO2H - - 0 N croconazole <BR> <BR> <BR> B 1-685 allyl O O CO2H--0 N croconazole Bl-686 4-(NO2)Ph O O CO2H - - 0 N croconazole <BR> <BR> B 1-687 PhS O O CO2H--0 N croconazole B 1-688 N (Me) Ph O O CO2H - - 0 N croconazole B 1-689 N (H) OMe O O CO2H - - 0 N croconazole <BR> <BR> B 1-690 N (H) C02Et O O C02H--0 N croconazole Bl-691 Me O O CO2H - - 0 N econazole B 1-692 cyclohexyl O O CO2H--0 N econazole Bl-693 t-Bu O O CO2H - - 0 N econazole Bl-694 CF3CH2 O O CO2H - - 0 N econazole B 1-695 allyl O O CO2H--0 N econazole Bl-696 4-(NO2)Ph O O CO2H - - 0 N econazole <BR> <BR> B 1-697 PhS O O CO2H--0 N econazole B 1-698 N (Me) Ph O O CO2H--0 N econazole B 1-699 N (H) OMe O O CO2H - - 0 N econazole Bl-700 N (H) CO2Et O O CO2H - - 0 N econazole <BR> <BR> B1-701 Me O O CO2H--0 N democonazole<BR> <BR> <BR> <BR> <BR> <BR> B 1-702 cyclohexyl O O CO2H--0 N democonazole Bl-703 t-Bu O O CO2H - - 0 N democonazole Bl-704 CF3CH2 O O CO2H - - 0 N democonazole <BR> <BR> <BR> B1-705 allyl O O CO2H--0 N democonazole Bl-706 4-(NO2)Ph O O CO2H - - 0 N democonazole <BR> <BR> Bl-707 PhS O O C02H--0 N democonazole Bl-708 N (Me) Ph O O CO2H - - 0 N democonazole Bl-709 N (H) Ome O O CO2H - - 0 N democonazole Bl-710 N (H) CO2Et O O CO2H - - 0 N democonazole <BR> <BR> B1-711 Me O O CO2H--0 N doconazole<BR> <BR> <BR> <BR> <BR> B1-712 cyclohexyl O O CO2H--0 N doconazole Bl-713 t-Bu O O CO2H - - 0 N doconazole Bl-714 CF3CH2 O O CO2H - - 0 N doconazole Bl-715 allyl O O CO2H - - 0 N doconazole <BR> <BR> Bl-716 4- (NO2) Ph O 0 C02H--0 N doconazole Bl-717 PhS O O CO2H - - 0 N doconazole Bl-718 N (Me) Ph O O CO2H - - 0 N doconazole Bl-719 N (H) OMe O O CO2H - - 0 N doconazole Bl-720 N (H) CO2Et O O CO2H--0 N doconazole <BR> <BR> B1-721 Me O O CO2H--0 N fenticonazole<BR> <BR> <BR> <BR> <BR> <BR> B 1-722 cyclohexyl O O CO2H--0 N fenticonazole<BR> <BR> <BR> <BR> B 1-723 t-Bu O O CO2H--0 N fenticonazole<BR> <BR> <BR> <BR> <BR> B 1-724 CF3CH2 O O C02H--0 N fenticonazole Bl-725 allyl O O CO2H - - 0 N fenticonazole Bl-726 4-(NO2)Ph O O CO2H - - 0 N fenticonazole <BR> <BR> B1-727 PhS O O C02H--0 N fenticonazole Bl-728 N (Me) Ph O O C02H--0 N fenticonazole Bl-729 N (H) OMe O O CO2H - - 0 N fenticonazole <BR> <BR> B1-730 N (H) CO2Et O O CO2H-0 N fenticonazole Bl-731 Me O O CO2H - - 0 N eberconazole B 1-732 cyclohexyl O O CO2H--0 N eberconazole Bl-733 t-Bu O O CO2H - - 0 N eberconazole Bl-734 CF3CH2 O O CO2H - - 0 N eberconazole <BR> <BR> B 1-735 allyl O O CO2H--0 N eberconazole Bl-736 4-(NO2)Ph O O CO2H - - 0 N eberconazole Bl-737 PhS O O CO2H - - 0 N eberconazole Bl-738 N (Me) Ph O O CO2H - - 0 N eberconazole Bl-739 N (H) OMe00C02H--0Neberconazole Bl-740 N (H) CO2Et O O CO2H - - 0 N eberconazole Bl-741 Me O O CO2H - - 0 N isoconazole <BR> <BR> <BR> B1-742 cyclohexyl O O C02H--0 N isoconazole<BR> <BR> <BR> <BR> B 1-743 t-Bu O O C02H--0 N isoconazole Bl-744 CF3CH2 O O CO2H - - 0 N isoconazole Bl-745 allyl O O CO2H - - 0 N isoconazole Bl-746 4-(NO2)Ph O O CO2H - - 0 N isoconazole <BR> <BR> B 1-747 PhS O O CO2H--0 N isoconazole Bl-748 N (Me) Ph O O CO2H--0 N isoconazole Bl-749 N (H) OMe O O CO2H--0 N isoconazole Bl-750 N (H) CO2Et O O CO2H - - 0 N isoconazole <BR> <BR> B1-751 Me O O CO2H--0 N miconazole<BR> <BR> <BR> <BR> <BR> <BR> B 1-752 cyclohexyl O O CO2H--0 N miconazole Bl-753 t-Bu O O CO2H - - 0 N miconazole Bl-754 CF3CH2 O O CO2H - - 0 N miconazole <BR> <BR> <BR> B 1-755 allyl O 0 C02H--0 N miconazole Bl-756 4-(NO2)Ph O O CO2H - - 0 N miconazole Bl-757 Phs O O CO2H - - 0 N miconazole Bl-758 N (Me) Ph O O CO2H-0 N miconazole Bl-759 N (H) OMe O O CO2H - - 0 N miconazole Bl-760 N (H) CO2Et O O CO2H-0 N miconazole <BR> <BR> B1-761 Me O O CO2H--0 N neticonazole<BR> <BR> <BR> <BR> <BR> <BR> B 1-762 cyclohexyl O O CO2H--0 N neticonazole Bl-763 t-Bu O O CO2H - - 0 N neticonazole Bl-764 CF3CH2 O O CO2H - - 0 N neticonazole <BR> <BR> <BR> B 1-765 allyl O O CO2H--0 N neticonazole Bl-766 4-(NO2)Ph O O CO2H - - 0 N neticonazole Bl-767 PhS O O CO2H - - 0 N neticonazole Bl-768 N (Me) Ph O O CO2H - - 0 N neticonazole B1-79 N (H) Ome O O CO2H - - 0 N neticonazole B1-770 N (H) C02Et00COzH--0Nneticonazole Bl-771 Me O O CO2H - - 0 N omoconazole <BR> <BR> <BR> B 1-772 cyclohexyl O O CO2H--0 N omoconazole<BR> <BR> <BR> <BR> <BR> B 1-773 t-Bu 0 O C02H-0 N omoconazole Bl-774 CF3CH2 O O CO2H - - 0 N omoconazole <BR> <BR> <BR> B 1-775 allyl O O CO2H-0 N omoconazole Bl-776 4-(NO2)Ph O O CO2H - - 0 N omoconazole <BR> <BR> B1-777 PhS O O CO2H-0 N omoconazole Bl-778 N (Me) Ph O 0 C02H-0 N omoconazole B 1-779 N (H) OMe O O C02H-0 N omoconazole Bl-780 N (H) C02Et00COzH-0Nomoconazole Bl-781 Me O O CO2H - - 0 N orconazole B l-782 cyclohexyl O O CO2H - - 0 N orconazole <BR> <BR> B 1-783 t-Bu O O CO2H--0 N orconazole Bl-784 CF3CH2 O O CO2H - - 0 N orconazole Bl-785 allyl 0 0 C02H-0 N orconazole Bl-786 4-(NO2)Ph O O CO2H - - 0 N orconazole Bl-787 PhS O O CO2H - - 0 N orconazole B 1-788 N (Me) Ph O O CO2H - - 0 N iorconazole B 1-789 N (H) OMe O O CO2H - - 0 N orconazole Bl-790 N (H) C02Et0 0 C02H-0 N orconazole Bl-791 Me O O CO2H - - 0 N oxiconazole B 1-792 cyclohexyl O 0 COzH--0 N oxiconazole <BR> <BR> Bl-793 t-Bu O 0 COzH-0 N oxiconazole Bl-794 CF3CH2 O O CO2H - - 0 N oxiconazole Bl-795 allyl O 0 CO2H--0 N oxiconazole Bl-796 4-(NO2)Ph O O CO2H - - 0 N oxiconazole Bl-797 PhS O O CO2H - - 0 N oxiconazole Bl-798 N (Me) Ph O O CO2H - - 0 N oxiconazole Bl-799 N (H) OMe O O CO2H - - 0 N oxiconazole Bl-800 N (H) C02Et O O CO2H-0 N oxiconazole Bl-801 Me O O CO2H - - 0 N parconazole B 1-802 cyclohexyl0 0 C02H-0 N parconazole Bl-803 t-Bu O O CO2H - - 0 N parconazole Bl-804 CF3CH2 O O CO2H - - 0 N parconazole Bl-805 allyl O O CO2H - - 0 N parconazole Bl-806 4-(NO2)Ph O O CO2H - - 0 N parconazole <BR> <BR> B 1-807 PhS O O CO2H--0 N parconazole B 1-808 N (Me) Ph O O CO2H - - 0 N parconazole B 1-809 N (H) OMe O O C02H-0 N parconazole Bl-810N (H) C02Et O O CO2H-0 N parconazole <BR> <BR> B 1-811 Me O O CO2H--0 N ravuconazole<BR> <BR> <BR> <BR> <BR> B 1-812 cyclohexyl O O CO2H--0 N ravuconazole Bl-813 t-Bu O O CO2H - - 0 N ravuconazole <BR> <BR> <BR> B 1-814 CF3CH2 O O CO2H--0 N ravuconazole<BR> <BR> <BR> <BR> <BR> B1-815 allyl O O CO2H--0 N ravuconazole Bl-816 4-(NO2)Ph O O CO2H - - 0 N ravuconazole Bl-817 PhS O O CO2H - - 0 N ravuconazole B 1-818 N (Me) Ph O O CO2H - - 0 N ravuconazole Bl-819 N (H) OMe O O CO2H - - 0 N ravuconazole <BR> <BR> B 1-820 N (H) C02Et O O CO2H--0 N ravuconazole Bl-821 Me O O CO2H - - 0 N sertaconazole B l-822 cyclohexyl O O CO2H - - 0 N sertaconazole <BR> <BR> B 1-823 t-Bu O O CO2H--0 N sertaconazole Bl-824 CF3CH2 O O C02H--0 N sertaconazole <BR> <BR> B 1-825 allyl O O CO2H--0 N sertaconazole Bl-826 4-(NO2)Ph O O CO2H - - 0 N sertaconazole <BR> <BR> B 1-827 PhS O O CO2H--0 N sertaconazole B 1-828 N (Me) Ph O O C02H--0 N sertaconazole Bl-829 N(H)OMe O O CO2H - - 0 N sertaconazole <BR> <BR> B 1-830 N (H) CO2Et 0 O C02H--0 N sertaconazole Bl-831 Me O O CO2H - - 0 N sulconazole <BR> <BR> B 1-832 cyclohexyl O O CO2H--0 N sulconazole Bl-833 t-Bu O O CO2H - - 0 N sulconazole Bl-834 CF3CH2 O O CO2H - - 0 N sulconazole <BR> <BR> Bl-835 allyl O O C02H--0 N sulconazole<BR> <BR> <BR> <BR> <BR> B1-836 4- (NO2) Ph O 0 C02H--0 N sulconazole Bl-837 PhS O O CO2H - - 0 N sulconazole Bl-838 N (Me) Ph 0 O C02H-0 N sulconazole Bl-839 N (H) OMe 0 O CO2H-0 N sulconazole Bl-840 N (H) CO2Et O O CO2H - - 0 N sulconazole Bl-841 Me O O CO2H - - 0 N tioconazole Bl-842 cyclohexyl O O CO2H - - 0 N tioconazole Bl-843 t-Bu O O CO2H - - 0 N tioconazole Bl-844 CF3Ch2 O O CO2H - - 0 N tioconazole <BR> <BR> B 1-845 allyl O O C02H--0 N tioconazole Bl-846 4-(NO2)Ph O O CO2H - - 0 N tioconazole Bl-847 PhS O O CO2H - - 0 N tioconazole Bl-848 N (Me) Ph O 0 C02H--0 N tioconazole B 1-849 N (H) OMe O O CO2H - - 0 N tioconazole Bl-850 N (H) C02Et00C02H--0Ntioconazole <BR> <BR> B 1-851 Me O O CO2H--0 N valconazole Bl-852 Cyclohexyl O O CO2H - - 0 N valconazole Bl-853 t-Bu O O CO2H - - 0 N valconazole <BR> <BR> Bl-854 CF3CH2 0 O CO2H--0 N valconazole Bl-855 allyl O O CO2H - - 0 N valconazole <BR> <BR> B1-856 4-(NO2) Ph O O CO2H-0 N valconazole Bl-857 PhS O O CO2H - - 0 N valconazole Bl-858 N (Me) Ph O O CO2H - - 0 N valconazole B 1-859 N (H) OMe O O CO2H - - 0 N valconazole Bl-860 N (H) CO2Et O O CO2H-0 N valconazole Bl-861 Me O O CO2H - - 0 N zinoconazole Bl-862 cyclohexyl O O CO2H - - 0 N zinoconazole <BR> <BR> B 1-863 t-Bu O O CO2H--0 N zinoconazole Bl-864 CF3CH3 O O CO2H - - 0 N zinoconazole <BR> <BR> B 1-865 allyl O O CO2H--0 N zinoconazole<BR> <BR> <BR> <BR> B1-866 4-(NO2) Ph O O CO2H-0 N zinoconazole Bl-867 PhS O O CO2H - - 0 N zinoconazole B 1-868 N (Me) Ph O O CO2H--0 N zinoconazole B 1-869 N (H) OMe O O CO2H-0 N zinoconazole B 1-870 N (H) CO2Et O O CO2H--0 N zinoconazole <BR> <BR> B 1-871 Me O O C02H 0 O 1 C cloxacillin B 1-872 cyclohexyl O O C02H 0 O 1 C cloxacillin <BR> <BR> B 1-873 t-Bu O O CO2H O O 1 C cloxacillin Bl-874 CF3CH2 O O CO2H O O 1 C clooxacillin Bl-875 allyl O O CO2H O O 1 C clooxacillin Bl-876 4-(NO2)Ph O O CO2H O O 1 C clooxacillin Bl-877 PhS O O CO2H O O 1 C clooxacillin] Bl-878 N (Me) Ph O O CO2H O O 1 C cloxacillin Bl-879 N (H) OMe O O CO2H O O 1 C cloxacillin Bl-880 N(H)CO2Et O O CO2H O O 1 C cloxacillin <BR> <BR> B1-881 Me O O CO2H O O 1 C valproic acid<BR> <BR> <BR> <BR> <BR> B1-882 cyclohexyl O O C02H O O 1 C valproic acid Bl-883 t-Bu O O CO2H O O 1 C valproic acid Bl-884 CF3CH2 O O CO2H O O 1 C valproic acid <BR> <BR> B1-885 allyl O O CO2H O O 1 C valproic acid Bl-886 4-(NO2)Ph O O CO2H O O 1 C valproic acid Bl-887 PhS O O CO2H O O 1 C valproic acid B 1-888 N (Me) Ph O O CO2H O O 1 C valproic acid B 1-889 N (H) OMe O O CO2H O O 1 C valproic acid B1-890 N (H) C02Et00C02H001Cvalproicacid Bl-891 Me O O CO2H O O 1 C retinoic acid Bl-892 cyclohexyl O O CO2H O O 1 C retinoic acid Bl-893 t-Bu O O CO2H O O 1 C retinoic acid Bl-894 CF3CH2 O O CO2H O O 1 C retinoic acid Bl-895 allyl O O CO2H O O 1 C retinoic acid Bl-896 4-(NO2)Ph O O CO2H O O 1 C retinoic acid Bl-897 PhS O O CO2H O O 1 C retinoic acid Bl-898 N (Me) Ph O O CO2H O O 1 C retinoic acid Bl-899 N (H) OMe O O CO2H OO 1 C retinoic scid Bl-900 N (H) CO2Et O 0 CO2H 0 O 1 C retinoic acid Bl-901 Me O O CO2H O O 1 C oxaprozin <BR> <BR> Bl-902 cyclohexyl O O COzH 0 O 1 C oxaprozin<BR> <BR> <BR> <BR> <BR> B 1-903 t-Bu O O C02H 0 O 1 C oxaprozin<BR> <BR> <BR> <BR> <BR> <BR> Bl-904CF3CH200C02H001Coxaprozin Bl-905 allyl O O CO2H O O 1 C oxaprozin Bl-906 4-(NO2)Ph O O CO2H O O 1 C oxaprozin Bl-907 PhS O O CO2H O O 1 C oxaprozin Bl-908 N (Me) Ph O O CO2H O O 1 C oxaprozin Bl-909 N (H) OMe O O CO2H 0 O 1 C oxaprozin Bl-910 N (H) CO2Et O O CO2H O O 1 C oxaprozin <BR> <BR> B 1-911 Me O O CO2H O O 1 C naproxen Bl-912 cyclohexyl O O CO2H O O 1C naproxen <BR> <BR> B1-913 t-Bu O O C02H O O 1 C naproxen Bl-914 CF3CH2 O O CO2H O O 1 C naproxen Bl-915 allyl O O CO2H O O 1 C naproxen Bl-916 4-(NO2)Ph O O CO2H O O 1 C naproxen Bl-917 PhS O O CO2H O O 1 C naproxen Bl-918 N (Me) Ph O O CO2H O O 1 C naproxen Bl-919 N (H) OMe O O CO2H O O 1 C naproxen Bl-920 N(H)CO2Et O O CO2H O O 1 C naproxen Bl-921 Me O O CO2H O O 1 C monopril <BR> <BR> B1-922 cyclohexyl O O CO2H 0 O 1 C monopril Bl-923 t-Bu O O CO2H O O 1 C monopril Bl-924 CF3CH2 O O CO2H O O 1 C monopril <BR> <BR> B1-925 allyl O O CO2H 0 O 1 C monopril Bl-926 4-(NO2)Ph O O CO2H O O 1 C monopril Bl-927 PhS O O CO2H O O 1 C monopril B 1-928 N (Me) Ph O O CO2H O O 1 C monopril B 1-929 N (H) OMe O O CO2H O O 1 C monopril Bl-930 N (H) C02Et O O CO2H O 0 1 C monopril <BR> <BR> B1-931 Me O 0 CO2H O 0 1 C ketorolac<BR> <BR> <BR> <BR> <BR> <BR> Bl-932 cyclohexyl O O CO2H 0 O 1 C ketorolac Bl-933 t-Bu O O CO2H O O 1 C ketorolac Bl-934 CF3CH2 O O CO2H O O 1 C ketorolac Bl-935 ally O O CO2H O O 1 C ketorolac <BR> <BR> Bl-936 4- (NO2) Ph O 0 CO2H 0 O 1 C ketorolac Bl-937 PhS O O CO2H O O 1 C ketorolac Bl-938 N (Me) Ph O O CO2H O O 1 C ketorolac Bl-939 N (H) OMe O O CO2H O O 1 C ketorolac Bl-940 N (H) CO2Et O O CO2H O O 1 C ketorolac Bl-941 Me O O CO2H O O 1 C ketoprofen Bl-942 cyclohexyl O O CO2H O O 1 C ketoprofen <BR> <BR> Bl-943 t-Bu O O CO2H 0 O 1 C ketoprofen<BR> <BR> <BR> <BR> <BR> B1-944CF3CH200C02H001Cketoprofen Bl-945 allyl O O CO2H O O 1 C ketoprofen Bl-946 4-(NO2)Ph O O CO2H O O 1 C ketoprofen Bl-947 PhS O O CO2H O O 1 C ketoprofen B 1-948 N (Me) Ph O O CO2H O O 1 C ketoprofen B 1-949 N (H) OMe O O CO2H O O 1 C ketoprofen B 1-950 N (H) CO2Et O O CO2H O O 1 C ketoprofen Bl-951 Me O O CO2H O O 1 C indomethacin B 1-952 cyclohexyl O O CO2H O O 1 C indomethacin <BR> <BR> B 1-953 t-Bu O O CO2H O O 1 C indomethacin Bl-954 CF3CH2 O O CO2H O O 1 C indomethacin Bl-955 allyl O O CO2H O O 1 C indomethacin Bl-956 4-(NO2)Ph O O CO2H O O 1 C indomethacin <BR> <BR> B 1-957 PhS O O CO2H O O 1 C indomethacin Bl-958 N (Me) Ph O O CO2H O O 1 C indomethacin Bl-959 N (H) OMe O O CO2H O O 1 C indomethacin Bl-960 N(H)CO2Et O O CO2H O O 1 C indomethacin Bl-961 Me O O CO2H O O 1 C ibuprofen <BR> <BR> B1-962 cyclohexyl O 0 C02H O O 1 C ibuprofen Bl-963 t-Bu O O CO2H O O 1 C ibuprofen Bl-964 CF3CH2 O O CO2H O O 1 C ibuprofen Bl-965 allyl O O CO2H O O 1 C ibuprofen Bl-966 4-(NO2)Ph O O CO2H O O 1 C ibuprofen <BR> <BR> B 1-967 PhS O O CO2H O O 1 C ibuprofen Bl-968 N (Me) Ph O O CO2H O O 1 C ibuprofen B 1-969 N (H) OMe O O CO2H O O 1 C ibuprofen B 1-970 N (H) CO2Et O O CO2H O O 1 C ibuprofen Bl-971 Me O O CO2H O O 1 C gemfibrozil <BR> <BR> B 1-972 cyclohexyl O O CO2H O O 1 C gemfibrozil Bl-973 t-Bu O O CO2H O O 1 C gemfibrozi Bl-974 CF3CH2 O O CO2H O O 1 C gemfibrozil Bl-975 allyl O O CO2H O O 1 C gemfibrozil Bl-976 4-(NO2)Ph O O CO2H O O 1 C gemfibrozil Bl-977 PhS O O CO2H O O 1 C gemfibrozil B 1-978 N (Me) Ph O O CO2H O O 1 C gemfibrozil Bl-979 N (H) OMe O O CO2H O O 1 C gemfibrozil Bl-980 N (H) CO2Et O O CO2H O O 1 C gemfibrozil Bl-981 Me O O CO2H O O 1 C flurbiprofen Bl-982 cyclohexyl O O CO2H O O 1 C flurbiprofen Bl-983 t-Bu O O CO2H O O 1 C flurbiprofen Bl-984 CF3CH2 O O CO2H O O 1 C flurbiprofen Bl-985 allyl O O CO2H O O 1 C flurbiprofen Bl-986 4-(NO2)Ph O O CO2H O O 1 C flurbiprofen Bl-987 PhS O O CO2H O O 1 C flurbiprofen Bl-988 N (Me) Ph O O CO2H O O 1 C flurbiprofen B 1-989 N (H) OMe O O CO2H O O 1 C flurbiprofen Bl-990 N (H) CO2Et O O CO2H O O 1 C flurbiprofen Bl-991 Me O O CO2H O O 1 C arthrocine B 1-992 cyclohexyl O O CO2H O O 1 C arthrocine <BR> <BR> B 1-993 t-Bu O O C02H O O 1 C arthrocine<BR> <BR> <BR> <BR> B1-994 CF3CH2 O O CO2H O 0 1 C arthrocine Bl-995 allyl O O CO2H O O 1 C arthrocine <BR> <BR> Bl-9964- (N02) Ph00C02H001Carthrocine Bl-997 PhS O O CO2H O O 1 C arthrocine Bl-998 N (Me) Ph O O CO2H O O 1 C arthrocine B 1-999 N (H) OMe00C02H001Carthrocine Bl-1000 N (H) CO2Et O O CO2H O O 1 C arthrocine Bl-1001 Me O O CO2H O O 1 C adapalene <BR> <BR> B 1-1002 cyclohexyl O O CO2H O O 1 C adapalene Bl-1003 t-Bu O O CO2H O O 1 C adapalene Bl-1004 CF3CH2 O O CO2H O O 1 C adapalene Bl-1005 allyl O O CO2H O O 1 C adapalene Bl-1006 4-(NO2)Ph O O CO2H O O 1 C adapalene Bl-1007 PhS O O CO2H O O 1 C adapalene B 1-1008 N (Me) Ph O O CO2H O O 1 C adapalene B 1-1009 N (H) OMe O O CO2H O O 1 C adapalene Bl-1010 N (H) CO2Et O O CO2H O O 1 C adapalene Bl-1011 Me O O CO2H O O 1 C lansoprazole <BR> <BR> B 1-1012 cyclohexyl O O CO2H O O 1 C lansoprazole<BR> <BR> <BR> <BR> <BR> B 1-1013 t-Bu O O CO2H O O 1 C lansoprazole<BR> <BR> <BR> <BR> B 1-1014CFsCH200C02H001Clansoprazole Bl-1015 allyl O O CO2H O O 1 C lansoprazole Bl-1016 4-(NO2)Ph O O CO2H O O 1 C lansoprazole <BR> <BR> B1-1017 PhS O O CO2H O O 1 C lansoprazole Bl-1018 N (Me) Ph O O CO2H O O 1 C lansoprazole Bl-1019 N (H) OMe O O CO2H O O 1 C lansoprazole <BR> <BR> B 1-1020 N (H) CO2Et O O CO2H O O 1 C lansoprazole<BR> <BR> <BR> <BR> B 1-1021 Me O O CO2H O O 1 C lovastatin<BR> <BR> <BR> <BR> B 1-1022 cyclohexyl O O CO2H O O 1 C lovastatin Bl-1023 t-Bu O O CO2H O O 1 C lovastatin Bl-1024 CF3CH2 O O CO2H O O 1 C lovastatin Bl-1025 allyl O O CO2H O O 1 C lovastatin Bl-1026 4-(NO2)Ph O O CO2H O O 1 C lovastatin Bl-1027 PhS O O CO2H O O 1 C lovastatin Bl-1028 N(Me)Ph O O CO2H O O 1 C lovastatin Bl-1029 N(H)OMe O O CO2H O O 1 C lovastain Bl-1030 N(H)CO2Et O O CO2H O O 1 C lovastatin <BR> <BR> B 1-1031 Me 0 O C02H O 0 1 C warfarin Bl-1032 cyclohexyl O O CO2H O O 1 C warfarin Bl-1033 t-Bu O O CO2H O O 1 C warfarin Bl-1034 CF3CH2 O O CO2H O O 1 C warfarin Bl-1035 . allyl O O CO2H O O 1 C warfarin Bl-1036 4-(NO2)Ph O O CO2H O O 1 C warfarin Bl-1037 PhS O O CO2H O O 1 C warfarin Bl-1038 N (Me) Ph O O CO2H O O 1 C warfarin B 1-1039 N (H) OMe O O CO2H O O 1 C warfarin B 1-1040 N (H) CO2Et O O CO2H O O 1 C warfarin Bl-1041 Me O O CO2H - - 0 N tolteridine Bl-1042 cyclohexyl O O CO2H - - 0 N tolteridine <BR> <BR> B 1-1043 t-Bu O O CO2H--0 N tolteridine BL-1044 CF3CH2 O O CO2H - - 0 N tolteridine <BR> <BR> B 1-1045 allyl O O CO2H--0 N tolteridine Bl-1046 4-(NO2)Ph O O CO2H - - 0 N tolteridine Bl-1047 PhS O O CO2H - - 0 N tolteridine B 1-1048 N (Me) Ph O O CO2H - - 0 N tolteridine B 1-1049 N (H) OMe 0 O C02H--0 N tolteridine Bl--1050 N(H)CO2Et O O CO2H - - 0 N tolteridine Bl-1051 Me O O CO2H - - 0 N ticlopidine B 1-1052 cyclohexyl O O CO2H--0 N ticlopidine Bl-1053 t-Bu O O CO2H - - 0 N ticlopidine Bl-1054 CF3CH2 O O CO2H - - 0 N ticlopidine Bl-1055 allyl O O CO2H - - 0 N ticlopidine Bl-1056 4-(NO2)Ph O O CO2H - - 0 N ticlopidine <BR> <BR> B 1-1057 PhS O O CO2H--0 N ticlopidine B 1-1058 N (Me) Ph O O CO2H - - 0 N ticlopidine Bl-1059 N (H) OMe O O C02H--0 N ticlopidine Bl-1060 N(H)CO2Et O O CO2H - - 0 N ticlopidine <BR> <BR> B1-1061 Me O O CO2H--0 N sibutramine B 1-1062 cyclohexyl O O CO2H--0 N sibutramine <BR> <BR> B1-1063 t-Bu O O CO2H--0 N sibutramine Bl-1064 CF3CH2 O O CO2H - - 0 N sibutramine <BR> <BR> Bl-1065 allyl O O CO2H--0 N sibutramine Bl-1066 4-(NO2)Ph O O CO2H - - 0 N sibutramine <BR> <BR> B 1-1067 PhS O O CO2H--0 N sibutramine B 1-1068 N (Me) Ph O O CO2H - - 0 N sibutramine B 1-1069 N (H) OMe O O CO2H--0 N sibutramine <BR> <BR> B 1-1070 N (H) C02Et O O CO2H--0 N sibutramine Bl-1071 Me O O CO2H - - 0 N propoxyphene <BR> <BR> B 1-1072 cyclohexyl O O CO2H--0 N propoxyphene<BR> <BR> <BR> <BR> <BR> Bl-1073 t-Bu O O CO2H--0 N propoxyphene Bl-1074 CF3CH2 O O CO2H - - 0 N propoxyphene <BR> <BR> Bl-1075 allyl O O C02H--0 N propoxyphene Bl-1076 4-(NO2)Ph O O CO2H - - 0 N propoxyphene <BR> <BR> Bl-1077 PhS O O C02H--0 N propoxyphene Bl-1078 N (Me) Ph O O CO2H - - 0 N propoxyphene Bl-1079 N (H) OMe O O CO2H - - 0 N propoxyphene Bl-1080 N(H)CO2Et O O CO2H - - 0 N propoxyphene <BR> <BR> B 1-1081 Me O O CO2H--0 N nifurantin Bl-1082 cyclohexyl O O CO2H - - 0 N nifurantin Bl-0183 t-Bu O O CO2H - - 0 N nifurantin Bl-1084 CF3CH2 O O CO2H - - 0 N nifurantin Bl-1085 allyl O O CO2H - - 0 N nifurantin Bl-1086 4-(NO2)Ph O O CO2H - - 0 N nifurantin Bl-1087 PhS O O CO2H - - 0 N nifurantin Bl-1088 N (Me) Ph O O CO2H - - 0 N nifurantin Bl-1089 N (H) OMe O O CO2H - - 0 N nifurantin Bl-1090 N (H) C02Et O O CO2H--0 N nifurantin Bl-1091 Me O O CO2H - - 0 N nefazodone Bl-1092 cyclohexyl O O CO2H - - 0 N nefazodone Bl-193 t-Bu O O CO2H - - 0 N nefazodone Bl-1094 CF3CH2 O O CO2H - - 0 N nefazodone <BR> <BR> B 1-1095 allyl O O C02H--0 N nefazodone Bl-1096 4-(NO2)Ph O O CO2H - - 0 N nefazodone <BR> <BR> B 1-1097 PhS O O CO2H--0 N nefazodone Bl-1098 N (Me) Ph O O CO2H - - 0 N nefazodone Bl-1099 N (H) OMe O O C02H--0 N nefazodone Bl-1100 N (H) CO2Et O O CO2H--0 N nefazodone <BR> <BR> B 1-1101 Me O O CO2H--0 N donezapil<BR> <BR> <BR> <BR> <BR> Bl-1102 cyclohexyl O O CO2H--0 N donezapil Bl-1103 t-Bu O O CO2H - - 0 N donezapil Bl-1104 CF3CH2 O O CO2H - - 0 N donezapil <BR> <BR> Bl-1105 allyl O O CO2H--0 N donezapil<BR> <BR> <BR> <BR> <BR> B 1-1106 4-(NO2) Ph O O CO2H-0 N donezapil Bl-1107 PhS O O CO2H - - 0 donezapil Bl-1108N (Me) Ph O O CO2H--0 N donezapil Bl-1109 N (H) OMe O O C02H-0 N donezapil Bl-1110 N (H) CO2Et O O CO2H--0 N donezapil Bl-1111 Me O O CO2H - - 0 N dicodid Bl-1112 cyclohexyl O O CO2H - - 0 N dicodid <BR> <BR> Bl-1113 t-Bu O O CO2H--0 N dicodid Bl-1114 CF3CH2 O O CO2H - - 0 N dicodid <BR> <BR> <BR> B1-1115 allyl O O C02H--0 N dicodid Bl-1116 4-(NO2)Ph O O CO2H - - 0 N dicodid <BR> <BR> B1-1117 PhS O O CO2H-0 N dicodid Bl-1118 N (Me) Ph O O CO2H - - 0 N dicodid Bl-1119 N (H) OMe O O CO2H--0 N dicodid Bl-1120 N (H) CO2Et O O CO2H - - 0 N dicodid <BR> <BR> B 1-1121 Me O O CO2H--0 N colchicine Bl-1122 cyclohexyl O O CO2H - - 0 N colchicine Bl-1123 t-Bu O O CO2H - - 0 N colchicine Bl-1124 CF3CH2 O O CO2H - - 0 N colchicine <BR> <BR> <BR> B 1-1125 allyl O O CO2H--0 N colchicine Bl-1126 4-(NO2)Ph O O CO2H - - 0 N colchicine Bl-1127 PhS O O CO2H - - 0 N colchicine B 1-1128 N (Me) Ph O O CO2H--0 N colchicine Bl-1129 N (H) OMe O O CO2H - - 0 N colchicine Bl-1130 N (H) CO2Et O O CO2H - - 0 N colchicine <BR> <BR> B1-1131 Me O O CO2H--0 N citalopram<BR> <BR> <BR> <BR> <BR> <BR> B1-1132 cyclohexyl O O CO2H--0 N citalopram Bl-1133 t-Bu O O CO2H - - 0 N citalopram Bl-1134 CF3CH2 O O CO2H - - 0 N citalopram Bl-1135 ally O O CO2H O O CO2H - - N citalopram Bl-1136 4-(NO2)Ph O O CO2H - - N citalopram <BR> <BR> Bl-1137 PhS O O CO2H--0 N citalopram B 1-1138 N (Me) Ph O O CO2H - - 0 N citalopram Bl-1139 N (H) OMe O O CO2H - - 0 N citalopram Bl-1140 (NH)CO2Et O O CO2H - - 0 N citalopram Bl-1141 Me O O CO2H - - 0 N benzatropine <BR> <BR> B 1-1142 cyclohexyl O O CO2H--0 N benzatropine<BR> <BR> <BR> <BR> <BR> <BR> B 1-1143 t-Bu O O CO2H--0 N benzatropine Bl-1144 CF3CH2 O O CO2H - - 0 N benzatropine Bl-1145 allyl O O CO2H - - 0 N benzatropine Bl-1146 4-(NO2)Ph O O CO2H - - 0 N benzatropine Bl-1147 PhS O O CO2H - - 0 N benzatropine Bl-1148 N(Me)Ph O O CO2H - - 0 N benzatropine Bl-1149 N(H)OMe O O CO2H - - 0 N benzatropine Bl-1150 N(H)CO2Et O O CO2H - - 0 N benzatropine Bl-1151 O O CO2H - - 0 N bISACODYL Bl-1152 EtO O O C02H--0 N bisacodyl Bl-1153 t-BuO O O CO2H - - 0 N bisacodyl B1-1154 cyclohexylO O O CO2H - - 0 N bisacodyl <BR> <BR> B1-1155 iPrO O O CO2H--0 N bisacodyl<BR> <BR> <BR> <BR> <BR> <BR> B1-1156 PhO O 0 C02H--0 N bisacodyl B1-1157 (HOCH2- O O CO2H - - 0 N biasacodyl CH2) 2N B 1-1158 N (H) NMe2 O O CO2H--0 N bisacodyl B1-1159 4-(OH)Ph O O CO2H - - 0 N bisacodyl B1-1160 4-(NH2)Ph O O CO2H - - 0 N bisacdyl B1-1161 EtS O O CO2H - - 0 N bupivacaine B1-1162 EtO O O CO2H - - 0 N bupivacaine B1-1163 t-BuO O O CO2H - - 0 N bupivacaine <BR> <BR> B 1-1164 cyclohexyl0 O 0 C02H--0 N bupivacaine Bl-1165iPrO00C02H--0 Nbupivacaine B1-1166 PhO O O CO2H - - 0 N bupivacaine B1-1167 (HOCH2- O O CO2H - - 0 N bupivacaine <BR> <BR> CH2) 2N<BR> <BR> <BR> <BR> <BR> <BR> B 1-1168N (H) NMe200COzH--ONbupivacaine B1-1169 4-(OH)Ph O O CO2H - - 0 N bupivacaine <BR> <BR> B1-1170 4- (NH2) Ph 0 O CO2H--0 N bupivacaine B1-1171 EtS O O CO2H - - 0 N chloroprocaine <BR> <BR> B1-1172 EtO O 0 CO2H--0 N chloroprocaine<BR> <BR> <BR> <BR> <BR> Bl-1173 t-BuO 0 O CO2H--0 N chloroprocaine B1-1174 cyclohexylO O O CO2H - - 0 N choroprocaine <BR> <BR> B1-1175 iPrO O 0 C02H--0 N chloroprocaine<BR> <BR> <BR> <BR> <BR> B1-1176 PhO 0 O C02H--0 N chloroprocaine<BR> <BR> <BR> <BR> <BR> B 1-1177 (HOCH2-0 O CO2H--0 N chloroprocaine<BR> <BR> <BR> <BR> <BR> <BR> CH2) 2N<BR> <BR> <BR> <BR> <BR> B1-1178 N (H) NMe2 O 0 C02H--0 N chloroprocaine<BR> <BR> <BR> <BR> <BR> B 1-1179 4- (OH) Ph 0 O CO2H--0 N chloroprocaine<BR> <BR> <BR> <BR> <BR> <BR> Bl-1180 4- (NH2) Ph O O C02H--0 N chloroprocaine B1-1181 EtS O O CO2H - - 0 N tetracaine B1-1182 EtO O O CO2H - - 0 N tetracaine B1-1183 t-BuO O O CO2H - - 0 N tetracaine B1-1184 cyclohexylO O O CO2H - - 0 N tetracaine <BR> <BR> Bl-1185 iPrO 0 O C02H--0 N tetracaine B1-1186 PhO O O CO2H - - 0 N tetracaine B1-1187 (HOCH2- O O CO2H - - 0 N tetracaine CH2) 2N B1-1188 N(H)NMe2 O O CO2H - - 0 N tetracaine B1-1189 4-(OH)Ph O O CO2H - - 0 N tetracaine Bl-11904- (NH2) Ph00C02H-- 0 Ntetracaine B1-1191 EtS O O CO2H - - 0 N acrivistine B1-1192 EtO O O CO2H - - 0 N acrivistine <BR> <BR> Bl-1193 t-BuO 0 O C02H--0 N acrivistine B1-1194 cyclohexylO O O CO2H - - 0 N acrivistine <BR> <BR> B1-1195 iPrO O 0 C02H--0 N acrivistine B1-1196 PhO O O CO2H - - 0 N acrivistine B1-1197 (HOCH2- O O CO2H - - 0 N acrivistine CH2) 2N B1-1198 N(H)NMe2 O O CO2H - - 0 N acrivistine <BR> <BR> B1-1199 4- (OH) Ph 0 O C02H--0 N acrivistine Bl-12004- (NH2) Ph00C02H-- 0 Nacrivistine B1-1201 EtS O O CO2H - - 0 N amiodarone <BR> <BR> B 1-1202 EtO O O CO2H--0 N amiodarone<BR> <BR> <BR> <BR> <BR> B 1-1203 t-BuO O O CO2H--0 N amiodarone B1-1204 cyclohexylO O O CO2H - - 0 N amiodarone <BR> <BR> Bl-1205 iPrO O O CO2H--0 N amiodarone B1-1206 PhO O O CO2H - - 0 N amiodarone B1-1207 (HOCH2- O O CO2H - - 0 N amiodarone CH2) 2N B1-1208 N(H)NMe2 O O CO2H - 0 N amiodarone <BR> <BR> B 1-12094- (OH) Ph00C02H- 0 Namiodarone<BR> <BR> <BR> <BR> <BR> B1-1210 4-(NH2) Ph O O CO2H 0 N amiodarone<BR> <BR> <BR> <BR> B 1-1211 EtS O O CO2H--0 N amitriptyline B1-1212 EtO O O CO2H - - 0 N amitriptyline B1-1213 t-BuO O O CO2H - - 0 N amitriptyline B1-1214 cyclohexylO O O CO2H - - 0 N amitriptyline <BR> <BR> B1-1215 iPrO O O CO2H--0 N amitriptyline B1-1216 PhO O CO2H - - 0 N amitriptyline B1-1217 (HOCH2- O O CO2H - - 0 N amitriptyline CH2) 2N B1-1218 N(H)NMe2 O O CO2H - - 0 N amitriptyline B1-1219 4-(OH)Ph OO CO2H - - 0 N amitriptyline B1-1220 4-(NH2)Ph O O CO2H - - 0 N amitriptyline B1-1221 EtS O O CO2H - - 0 N amrinone B1-1222 EtO O O CO2H - 0 N amrinone B1-1223 t-BuO O O CO2H - - 0 N amrinone B1-1224 cyclohexylO O O CO2H - - 0 N amrinone Bl-1225iPrO00C02H--0 Namrinone B1-1226 PhO O O CO2H - - 0 N amrinone B1-1227 (HOCH2- O O CO2H - - 0 N amrinone CH2) 2N B 1-1228 N (H) NMe2 O O CO2H - 0 N amrinone B1-1229 4-(OH)Ph O O CO2H - - 0 N amrinone <BR> <BR> Bl-1230 4- (NH2) Ph O 0 CO2H--0 N amrinone<BR> <BR> <BR> <BR> B1-1231 EtS O O CO2H--0 N atropine B1-1232 EtO O O CO2H - - 0 N atropine B1-1233 t-BuO O O CO2H - - 0 N atropine B1-1234 cyclohexylO O O CO2H - - 0 N atropine B 1-1235 iPrO O O CO2H--0 N atropine B1-1236 PhO O O CO2H - - 0 N atropine B1-1237 (HOCH2- O O CO2H - - 0 N atropine CH2) 2N Bl-1238 N (H) NMe2 O O CO2H - - 0 N atropine B1-1239 4-(OH)Ph O O CO2H - 0 N atropine <BR> <BR> B 1-1240 4-(NH2) Ph O O C02H-0 N atropine<BR> <BR> <BR> <BR> B1-1241 EtS O O CO2H--0 N benzphetamine B1-1242 EtO O O CO2H - - 0 N benzphetamine <BR> <BR> Bl-1243 t-BuO O 0 C02H--0 N benzphetamine B1-1244 cyclohexylO O O CO2H - - 0 N benzphetamine <BR> <BR> B 1-1245 iPrO O O CO2H--0 N benzphetamine B1-1246 PhO O O CO2H - - 0 N benzphetamine B 1-1247 (HOCH2-O 0 C02H-0 N benzphetamine CH2) 2N B1-1248 N(H)NMe2 O O CO2H - 0 N benzphetamine <BR> <BR> B 1-1249 4-(OH) Ph O O CO2H-0 N benzphetamine<BR> <BR> <BR> <BR> B1-1250 4-(NH2) Ph O O CO2H-0 N benzphetamine<BR> <BR> <BR> <BR> <BR> B 1-1251 EtS O O CO2H--0 N beperiden B1-1252 EtO O O CO2H - - 0 N beperiden Bl-1253 t-BuO O O CO2H--0 N beperiden B1-1254 cyclohexylO O O CO2H - - 0 N beperiden <BR> <BR> B 1-1255 iPrO O 0 C02H--0 N beperiden<BR> <BR> <BR> <BR> <BR> B1-1256 PhO 0 O CO2H--0 N beperiden B1-1257 (HOCH2- O O CO2H - - 0 N beperiden CH2) 2N B1-1258 N(H)NMe2 O O CO2H - - 0 N beperiden B1-1259 4-(OH) Ph O O CO2H--0 N beperiden B1-1260 4-(NH2)Ph O O CO2H - - 0 N beperiden B1-1261 EtS O O CO2H - - 0 N bromopheniramine B1-1262 EtO O O CO2H - - 0 N bromopheniramine B1-1263 t-BoU O O CO2H - - 0 N bromopheniramine B1-1264 cyclohexylO O O CO2H - - 0 N brompheniramine B1-1265 iPrO O O CO2H - - 0 N bromopheniramine B1-1266 PhO O O CO2H - - 0 N bromopheniramine B1-1267 (HOCH2- O O CO2H - - 0 N brromopheniramine CH2) 2N B1-1268 N(H)NMe2 O O CO2H - - 0 N brompheniramine B1-1269 4-(OH)Ph O O CO2H - - 0 N bromopheniramine <BR> <BR> B 1-1270 4-(NH2) Ph O O CO2H--0 N bromopheniramine<BR> <BR> <BR> <BR> <BR> B1-1271 EtS 0 O CO2H--0 N clemastine B1-1272 EtO O O CO2H - - 0 N clemastine B1-1273 t-BuO O O CO2H - - 0 N clemastine B1-1274 cyclohexylO O O CO2H - - 0 N clemastine B1-1275 iPrO O O CO2H - - 0 N clemastine B1-1276 PhO O O CO2H - - 0 N clemastine B1-1277 (HOCH2- O O CO2H - - 0 N celastine CH2) 2N <BR> <BR> B 1-1278 N (H) NMe2 O O CO2H-0 N clemastine<BR> <BR> <BR> <BR> B 1-1279 4-(OH) Ph O O CO2H-0 N clemastine<BR> <BR> <BR> <BR> <BR> B1-1280 4-(NH2) Ph O O CO2H-0 N clemastine B1-1281 EtS O O CO2H - 0 N clomiphen B1-1282 EtO O O CO2H - - 0 N clomiphene B1-1283 t-BuO O O CO2H - - 0 N clomiphene B1-1284 cyclohexylO O O CO2H - - 0 N clomiphene <BR> <BR> B 1-1285 iPrO O O CO2H--0 N clomiphene<BR> <BR> <BR> <BR> B 1-1286PhO00COzH--ONclomiphene B1-1287 (HOCH2- O O CO2H - - 0 N clomiphene CH2) 2N b1-1288 N(H)NMe2 O O CO2H - - 0 N clomiphen <BR> <BR> B 1-1289 4- (OH) Ph O O COzH--0 N clomiphene<BR> <BR> <BR> <BR> B 1-1290 4-(NH2) Ph O O CO2H-0 N clomiphene<BR> <BR> <BR> <BR> <BR> B1-1291 EtS O O CO2H--0 N cyclobenzaprine B1-1292 EtO O O CO2H - - 0 N cyclobenzaprine B1-1293 t-BuO O 0 CO2H--0 N cyclobenzaprine B1-1294 cyclohexylO O O CO2H - - 0 N cyclobenzaprine <BR> <BR> B1-1295 iPrO O O C02H--0 N cyclobenzaprine B1-1296 PhO O O CO2H - - 0 N cyclobenzprine <BR> <BR> B 1-1297 (HOCH2-O 0 CO2H--0 N cyclobenzaprine CH2) 2N <BR> <BR> B 1-1298 N (H) NMe2 O O CO2H--0 N cyclobenzaprine<BR> <BR> <BR> <BR> B1-1299 4- (OH) Ph O 0 CO2H--0 N cyclobenzaprine B1-1300 4(NH2)Ph O O CO2H - - 0 N cyclobenzyprine B1-1301 EtS O O CO2H - - 0 N cyclopentolate B1-1302 EtO O O CO2H - - 0 N cyclopentolate B1-1303 t-BuO O O CHO2H - - 0 N cyclpentolate B1-1304 cyclohexylO O O CO2H - - 0 N cyclopentolate <BR> <BR> B1-1305 iPrO O O CO2H--0 N cyclopentolate B1-1306 PhO O O CO2H - - 0 N cyclopentolate B1-1307 (HOCH2- O O CO2H - - 0 N cyclopentolate CH2) 2N B1-1308 N(H)NMe2 O O CO2H - - 0 N cyclopentolate B1-1309 4-(OH)Ph O O CO2H - - 0 N cyclopentolate <BR> <BR> B1-1310 4- (NH2) Ph O 0 C02H--0 N cyclopentolate<BR> <BR> <BR> <BR> <BR> B1-1311 EtS O O CO2H--0 N dicyclomine B1-1312 EtO O O CO2H - - 0 N dicyclomine B1-1313 t-BuO O O CO2H - - 0 N dicyclomine B1-1314 cyclohexylO O O CO2H - - 0 N dicyclomine <BR> <BR> B1-1315 iPrO O O CO2H--0 N dicyclomine B1-1316 PhO O O CO2H - - 0 N dicyclomine B 1-1317 (HOCH2-0 O CO2H--0 N dicyclomine CH2) 2N B1-1318 N(H)NMe2 O O CO2H - - 0 N dicyclomine <BR> <BR> B1-1319 4-(OH) Ph O O CO2H-0 N dicyclomine B1-1320 4-(NH2)Ph O O CO2H - - 0 N dicyclomine <BR> <BR> B1-1321 EtS O O CO2H--0 N diethylproprion B1-1322 EtO O O CO2H - - 0 N diethylproprion <BR> <BR> B1-1323 t-BuO O O C02H--0 N diethylproprion B1-1324 cyclohexylO O O CO2H - - 0 N diethylproprion B1-1325 iPrO O O CO2H - - 0 N diethylproprion <BR> <BR> B 1-1326 PhO 0 O C02H--0 N diethylproprion<BR> <BR> <BR> <BR> <BR> B1-1327 (HOCH2-0 O C02H--0 N diethylproprion CH2) 2N B1-1328 N(H)NMe2 O O CO2H - - 0 N diethylproprion B1-1329 4-(OH)Ph O O CO2H - - 0 N diethylproprion <BR> <BR> B 1-1330 4- (NH2) Ph 0 O CO2H--0 N diethylproprion<BR> <BR> <BR> <BR> <BR> B1-1331 EtS 0 O C02H--0 N diltiazem B1-1332 EtO O O CO2H - - 0 N diltiazem B1-1333 t-BuO O O CO2H - - 0 N diltiazem B1-1334 cyclohexylO O O CO2H - - 0 N diltiazem B1-1335 iPrO O O CO2H - - 0 N diltiazem B1-1336 Pho O O CO2H - - 0 N diltiazem B1-1337 (HOCH2- O O CO2H - - 0 N diltiazem CH2) 2N B 1-1338 N (H) NMe2 O O CO2H--0 N diltiazem B1-1339 4-(OH) Ph O O CO2H-0 N diltiazem B1-1340 4-(NH2)Ph O O CO2H - - 0 N diltiazem B1-1341 Ets O O CO2H - - 0 N diphenhydramine B1-1342 EtO O O CO2H--0 N diphenhydramine B1-1343 t-BuO O O CO2H - - 0 N diphenhydramine B1-1344 cyclohexylO O O CO2H - - 0 N diphenhydramine B1-1345 iPrO O O C02H--0 N diphenhydramine B1-1346 PhO O O CO2H - - 0 N diphenhydramine B1-1347 (HOCH2- O O CO2H - - 0 N diphenhydramine CH2) 2N<BR> <BR> <BR> <BR> <BR> B 1-1348 N (H) NMe2 O O CO2H--0 N diphenhydramine<BR> <BR> <BR> <BR> B1-1349 4-(OH) Ph O O CO2H-0 N diphenhydramine<BR> <BR> <BR> <BR> <BR> B 1-1350 4-(NH2) Ph O O CO2H--0 N diphenhydramine<BR> <BR> <BR> <BR> B1-1351 EtS O O CO2H--0 N diphenidol B1-1352 EtO O O CO2H - - 0 N diphenidol B1-1353 t-BuO O O CO2H - - 0 N diphenidol B1-1354 cyclohexyl0 O O C02H--0 N diphenidol<BR> <BR> <BR> <BR> <BR> B1-1355 iPrO O O C02H--0 N diphenidol B1-1356 PhO O O CO2H - - 0 N diphenidol B1-1357 (HOCH2- O O CO2H - - 0 N diphenidol CH2) 2N B1-1358 N (H) NMe2 O O CO2H - - 0 N diphenidol B1-1359 4-(OH) Ph O O CO2H-0 N diphenidol B1-1360 4-(NH2)Ph O O CO2H - - 0 N diphenidol Bl-1361 EtS O O C02H--0 N diphenoxylate B1-1362 EtO O O CO2H - - 0 N diphenoxylate B1-1363 t-BuO O O CO2H - - 0 N diphenoxylate B1-1364 cyclohexylO O O CO2H - - 0 N diphenoxylate B1-1365 iPrO O O CO2H - - 0 N diphenoxylate B1-1366 PhO O O CO2H - - 0 N diphenoxylate B1-1367 (HOCH2- O O CO2H - - 0 N diphenoxylate CH2) 2N<BR> <BR> <BR> <BR> <BR> B1-1368 N (H) NMe2 O O CO2H--0 N diphenoxylate B1-1369 4-(OH)PH O O CO2H - - 0 N diphenoxylate B1-1370 4-(NH2) Ph O O CO2H-0 N diphenoxylate B1-1371 EtS O O CO2H - - 0 N doxapram B1-1372 EtO O O CO2H - - 0 N doxapram B1-1373 t-BuO O O CO2H - - 0 N doxapram B1-1374 cyclohexylO O O CO2H - - 0 N doxapram B1-1375 iPrO O O CO2H--0 N doxapram B1-1376 PhO O O CO2H - - 0 N doxapram B1-1377 (HOCH2- O O CO2H - - 0 N doxapram <BR> <BR> CH2) 2N<BR> <BR> <BR> <BR> <BR> B1-1378 N (H) NMe2 O O CO2H-0 N doxapram B1-1379 4-(OH)Ph O O CO2H - - 0 N doxapram B1-1380 4-(NH2)Ph O O CO2H - - 0 N doxapram B1-1381 EtS O O C02H--0 N doxepin B1-1382 EtO O O CO2H - - 0 N doxepin B1-1383 t-BuO O O CO2H - - 0 N doxepin B1-1384 cyclohexylO O O CO2H - - 0 N doxepin B1-1385 iPrO O O C02H--0 N doxepin Bl-1386 PhO O O CO2H - 0 N doxepin Bl-1387 (HOCH2- O O CO2H - 0 N doxepin CH2) 2N Bl-1388 N(H)NMe2 O O CO2H 0 N doxepin Bl-1389 4-(OH)Ph O O CO2H 0 N doxepin B 1-13904- (NH2) Ph00C02H0 Ndoxepin <BR> <BR> B1-1391 EtS O O CO2H 0 N fentanyl Bl-1392 EtO O O CO2H - - 0 N fentanyl <BR> <BR> B1-1393 t-BuO 0 O CO2H--0 N fentanyl Bl-1394 cyclohexylO O O CO2H - - 0 N fentanyl Bl-1395 iPrO O O CO2H - - 0 N fentanyl Bl-1396 PhO O O CO2H - 0 N fentanyl Bl-1397 (HOCH2-0 O CO2H-0 N fentanyl CH2) 2N B 1-1398 N (H) NMe2 O O CO2H - 0 N fentanyl <BR> <BR> B 1-1399 4-(OH) Ph O O CO2H-0 N fentanyl<BR> <BR> <BR> <BR> <BR> <BR> B 1-1400 4-(NH2) Ph O O CO2H-0 N fentanyl<BR> <BR> <BR> <BR> <BR> <BR> <BR> B1-1401 EtS O O CO2H-0 N flavoxate Bl-1402 EtO O O CO2H 0 N flavoxate Bl-1403 t-BuO O O CO2H - - 0 N flavoxate Bl-1404 cyclohexylO O O CO2H - 0 N flavoxate <BR> <BR> B 1-1405 iPrO O O CO2H--0 N flavoxate Bl-1406 PhO O O CO2H - - 0 N flavoxate Bl-1407 (HOCH2- O O CO2H - - 0 N flavoxate CH2) 2N Bl-1408 N(H)NMe2 O O CO2H - 0 N flavoxate Bl-1409 4-(OH)Ph O O CO2H - 0 N flavoxate <BR> <BR> B1-1410 4-(NH2) Ph O O CO2H 0 N flavoxate<BR> <BR> <BR> <BR> <BR> <BR> <BR> B1-1411 EtS O O CO2H-0 N flurazepam Bl-1412 EtO O O CO2H - 0 N flurazepam <BR> <BR> Bl-1413 t-BuO 0 O CO2H-0 N flurazepam Bl-1414 cyclohexylO O O CO2H - - 0 N flurazepam <BR> <BR> B1-1415 iPrO O O CO2H--0 N flurazepam Bl-1416 PhO O O CO2H - - 0 N flurazepam Bl-1417 (HOCH2- O O CO2H - - 0 N flurazepam <BR> <BR> CH2) 2N<BR> <BR> <BR> <BR> <BR> <BR> <BR> B 1-1418 N (H) NMe2 O O CO2H-0 N flurazepam<BR> <BR> <BR> <BR> <BR> <BR> B1-1419 4-(OH) Ph O O C02H 0 N flurazepam<BR> <BR> <BR> <BR> <BR> <BR> <BR> B1-1420 4-(NH2) Ph O O CO2H 0 N flurazepam Bl-1421 EtS O O CO2H - 0 N levomethadyl Bl-1422 EtO O O CO2H - - 0 N levomethadyl <BR> <BR> Bl-1423 t-BuO 0 O C02H-0 N levomethadyl Bl-1424 cyclohexylO O O CO2H - 0 N levomethadyl <BR> <BR> B 1-1425 iPrO 0 O C02H-0 N levomethadyl Bl-1426PhO00C02H--0 Nlevomethadyl Bl-1427 (HOCH2- O O CO2H - - 0 N levomethadyl CH2) 2N <BR> <BR> B 1-1428 N (H) NMe2 O O CO2H-0 N levomethadyl Bl-1429 4-(OH)Ph O O CO2H - - 0 N levomethadyl Bl-1430 4-(NH2)Ph O O CO2H 0 N levomethadyl Bl-1431 EtS O O CO2H - - 0 N loratadine Bl-1432 EtO O O CO2H - - 0 N loratadine Bl-1433 t-BuO O O CO2H - - 0 N loratadine Bl-1434 cyclohexylO O O CO2H - - 0 N loratadine <BR> <BR> B 1-1435 iPrO O O CO2H--0 N loratadine<BR> <BR> <BR> <BR> <BR> B 1-1436 PhO O O CO2H--0 N loratadine<BR> <BR> <BR> <BR> <BR> Bl-1437 (HOCH2-O 0 CO2H-0 N loratadine<BR> <BR> <BR> <BR> <BR> <BR> CH2) 2N Bl-1438 N(H)NMe2 O O CO2H - 0 N loratadine Bl-1439 4-(OH)Ph O O CO2H - - 0 N loratadine <BR> <BR> B1-1440 4- (NH2) Ph 0 O CO2H--0 N loratadine<BR> <BR> <BR> <BR> <BR> B1-1441 EtS O O CO2H--0 N mechlorethamine<BR> <BR> <BR> <BR> <BR> B1-1442 EtO O O CO2H--0 N mechlorethamine Bl-1443 t-BuO O O CO2H - - 0 N mechlorethamine Bl-1444 cyclohexylO O O CO2H - - 0 N mechlorethamine <BR> <BR> B 1-1445 iPrO O O CO2H--0 N mechlorethamine Bl-1446 PhO O O CO2H - - 0 N mechlorethamine Bl-1447 (HOCH2- O O CO2H - - 0 N mechlorethamine CH2) 2N Bl-1448 N(H)NMe2 O O CO2H - - 0 N mechlorethamine <BR> <BR> B1-1449 4-(OH) Ph O O CO2H--0 N mechlorethamine<BR> <BR> <BR> <BR> <BR> B1-1450 4-(NH2) Ph O O CO2H-0 N mechlorethamine<BR> <BR> <BR> <BR> <BR> B 1-1451 EtS O O CO2H--0 N meperidine Bl-1452 EtO O O CO2H - - 0 N meperidine Bl-1453 t-BuO O O CO2H - - 0 N meperidine Bl-1454 cyclohexylO O O CO2H - - 0 N meperidine <BR> <BR> Bl-1455 iPrO O O CO2H--0 N meperidine Bl-1456PhO00C02H-0 Nmeperidine Bl-1457 (HOCH2- O O CO2H - 0 N meperidine CH2) 2N B 1-1458 N (H) NMe2 O O CO2H - - 0 N meperidine <BR> <BR> B1-1459 4- (OH) Ph O 0 CO2H--0 N meperidine Bl-1460 4-(NH2)Ph O O CO2H - - 0 N meperidine Bl-1461 EtS O 0 C02H--0 N mepivacaine Bl-1462 EtO O O CO2H - - 0 N mepivacaine Bl-1463 t-BuIO O O CO2H - - 0 N mepivacaine Bl-1464 cyclohexylO O O CO2H - - 0 N mepivacaine <BR> <BR> B1-1465 iPrO 0 O C02H--0 N mepivacaine Bl-1466 PhO O O CO2H - - 0 N mepivacaine Bl-1467 (HOCH2- O O CO2H - 0 N mepivacaine CH2)2N <BR> <BR> B 1-1468 N (H) NMe2 O O CO2H-0 N mepivacaine Bl-1469 4-(OH)Ph O O CO2H - 0 N mepivacaine B 1-14704- (NH2) Ph00C02H-0 Nmepivacaine Bl-1471 EtS O O CO2H - 0 N methadone Bl-1472 EtO O O CO2H - - 0 N methadone Bl-1473 t-BuO O O CO2H - - 0 N methadone Bl-1474 cyclohexylO O O CO2H - - 0 N methadone <BR> <BR> Bl-1475 iPrO O O CO2H--0 N methadone Bl-1476 PhO O O CO2H - - 0 N methadone <BR> <BR> Bl-1477 (HOCH2-O O CO2H--0 N methadone CH2) 2N B 1-1478 N (H) NMe200COzH-0 Nmethadone Bl-141479 4-(OH)Ph O O CO2H - 0 N methadone <BR> <BR> Bl-1480 4- (NH2) Ph O 0 CO2H-0 N methadone Bl-1481 EtS O O CO2H - 0 N minoxidil Bl-1482EtO00C02H--0 Nminoxidil Bl-1483 t-BuO O O CO2H - - 0 N minoxidil B1-1484 cyclohexylO O O CO2H - 0 N minoxidil Bl-1485 iPrO O O CO2H - - 0 N minoxidil Bl-1486PhO00C02H--0 Nminoxidil Bl-1487 (HOCH2- O O CO2H - - 0 N minoxidil CH2) 2N Bl-1488 N(H)NMe2 O O CO2H - 0 N minoxidil Bl-1489 4-(OH)Ph O O CO2H - - 0 N minoxidil Bl-1490 4-(NH2)Ph O O CO2H - - 0 N minoxidil Bl-1491 EtS O O CO2H - - 0 N naftifine Bl-1492 EtO O O CO2H - - 0 N naftifine Bl-1493 t-BuO O O CO2H - - 0 N naftifine Bl-1494 cyclohexylO O O CO2H - - 0 N naftifine <BR> <BR> Bl-1495 iPrO O O CO2H--0 N naftifine Bl-1496 PhO O O CO2H - - 0 N naftifine Bl-1497 (HOCH2- O O CO2H - - 0 N naftifine CH2) 2N Bl-1498 N (H) NMe2 O O CO2H - - 0 N naftifine <BR> <BR> B1-1499 4-(OH) Ph O O CO2H-0 N naftifine Bl-1500 4-(NH2)Ph O O CO2H - - 0 N naftifine B1-1501 EtS O 0 CO2H--0 N orphenadrine Bl-1502 EtO O O CO2H - - 0 N orphenadrine Bl-1503 t-BuO O O CO2H - - 0 N orphenadrine B1-1504 cyclohexylO O O CO2H - 0 N orphenadrine <BR> <BR> B1-1505 iPrO O O CO2H 0 N orphenadrine Bl-1506 PhO O O CO2H - 0 N orphenadrine <BR> <BR> B1-1507 (HOCH2-O O CO2H-0 N orphenadrine CH2) 2N Bl-1508N (H) NMe200C02H-- 0 Norphenadrine <BR> <BR> Bl-15094- (OH) Ph00C02H-- 0 Norphenadrine<BR> <BR> <BR> <BR> <BR> B1-1510 4- (NH2) Ph O 0 CO2H--0 N orphenadrine Bl-1511 EtS O O CO2H - - 0 N oxybutynin Bl-1512 EtO O O CO2H - - 0 N oxybutynin <BR> <BR> B1-1513 t-BuO O 0 C02H--0 N oxybutynin B1-1514 cyclohexylO O O CO2H - 0 N oxybutynin Bl-1515 iPrO O O CO2H - - 0 N oxybutynin <BR> <BR> B1-1516 PhO O 0 C02H-0 N oxybutynin<BR> <BR> <BR> <BR> <BR> B1-1517 (HOCH2-0 0 C02H-0 N oxybutynin CH2) 2N Bl-1518 N(H)NMe2 O O CO2H - 0 N oxybutynin Bl-1519 4-(OH)Ph O O CO2H - - 0 N oxybutynin <BR> <BR> B1-1520 4-(NH2) Ph O O CO2H-0 N oxybutynin Bl-1521EtS00C02H--0 Noxymetazoline Bl-1522EtO00C02H--0 Noxymetazoline Bl-1523 t-BuO O O CO2H - - 0 N oxymetazoline Bl-1524 cyclohexylO O O CO2H - - 0 N oxymetazoline Bl-1525 iPrO O O C02H--0 N oxymetazoline<BR> <BR> <BR> B 1-1526 PhO O O CO2H--0 N oxymetazoline B 1-1527 (HOCH2- O O CO2H - - 0 N oxymetazoline CH2) 2N Bl-1528 N(H)NMe2 O O CO2H - 0 N oxymetazoline B1-1529 4-(OH) Ph O O CO2H-0 N oxymetazoline<BR> <BR> <BR> B1-1530 4- (NH2) Ph 0 O CO2H--0 N oxymetazoline<BR> <BR> <BR> <BR> B1-1531 EtS O O CO2H--0 N phenoxybenzamine<BR> <BR> <BR> <BR> B1-1532 EtO O O C02H--0 N phenoxybenzamine Bl-1533 t-BuO O O CO2H - - 0 N phenoxybenzamine B1-1534 cyclohexyl0 O O CO2H--0 N phenoxybenzamine<BR> <BR> <BR> B1-1535 iPrO O O CO2H--0 N phenoxybenzamine Bl-1536 PhO O O CO2H - - 0 N phenoxybenzamine Bl-1537 (HOCH2- O O CO2H - - 0 N phenoxybenzamine CH2) 2N Bl-1538 N(H)NMe2 O O CO2H - - 0 N phenoxybenzamine B 1-1539 4-(OH) Ph O O CO2H-0 N phenoxybenzamine<BR> <BR> <BR> <BR> B1-1540 4-(NH2) Ph O O CO2H-0 N phenoxybenzamine<BR> <BR> <BR> Bl-1541 EtS O O CO2H - - 0 N pilocarpine<BR> <BR> <BR> Bl-1542 EtO O O CO2H - - 0 N pilocarpine Bl-1543 t-BuO O O CO2H - - 0 N pilocarpine Bl-1544 cyclohexylO O O CO2H - - 0 N pilocarpine Bl-1545 iPrO 0 0 C02H-0 N pilocarpine Bl-1546 PhO O O CO2H - - 0 N pilocarpine Bl-1547 (HOCH2- O O CO2H - - 0 N pilocarpine CH2) 2N Bl-1548 N (H) NMe2 O O CO2H--0 N pilocarpine B1-1549 4- (OH) Ph O O C02H--0 N pilocarpine Bl-1550 4-(NH2)Ph O O CO2H - - 0 N pilocarpine B1-1551 EtS O O C02H--0 N pyrazinamide Bl-1552 EtO O O CO2H - - 0 N pyrazinamide Bl-1553 t-BuO O O CO2H - - 0 N pyrazinamide Bl-1554 cyclohexylO O O CO2H - - 0 N pyrazinamide Bl-1555 iPrO O O CO2H - - 0 N pyrazinamide Bl-1556 PhO O O CO2H - - 0 N pyrazinamide Bl-1557 (HOCH2- O O CO2H - - 0 N pyrazinamide CH2) 2N Bl-1558 N (H) NMe2 O O CO2H - - 0 N pyrazinamide Bl-1559 4-(OH)Ph O O CO2H - - 0 N pyrazinamide B 1-1560 4- (NH2) Ph 0 O C02H--0 N pyrazinamide Bl-1561 EtS O O CO2H - - 0 N pyroxidine Bl-1562 EtO O O CO2H - - 0 N pyroxidine Bl-1563 t-BuO O O CO2H - - 0 N pyroxidine Bl-1564 cyclohexylO O O CO2H - - 0 N pyroxidine B1-1565 iPrO O O CO2H--0 N pyroxidine Bl-1566 PhO O O CO2H - - 0 N pyroxidine Bl-1567 (HOCH2- O O CO2H - - 0 N pyroxidine CH2) 2N Bl-1568N (H) NMe2 O O CO2H - - 0 N pyroxidine Bl-1569 4-(OH)Ph O O CO2H - - 0 N pyroxidine Bl-1570 4-(NH2)Ph O O CO2H - - 0 N pyroxidine B1-1571 EtS O O CO2H-0 N risperidone Bl-1572 EtO O O CO2H - - 0 N risperidone Bl-1573 t-BuO O O CO2H - - 0 N risperidone Bl-1574 cyclohexylO O O CO2H - - 0 N risperidone Bl-1575 iPrO O O C02H--0 N risperidone Bl-1576 PhO O O CO2H - - 0 N risperidone Bl-1577 (HOCH2- O O CO2H - - 0 N risperidone CH2) 2N <BR> <BR> B 1-1578 N (H) NMe2 O O CO2H--0 N risperidone Bl-1579 4-(OH)Ph O O CO2H - - 0 N risperidone <BR> <BR> B 1-1580 4-(NH2) Ph O O CO2H-0 N risperidone<BR> <BR> <BR> <BR> B1-1581 EtS O O CO2H--0 N sufentanil Bl-1582 EtO O O CO2H - - 0 N sufentanil Bl-1583 t-BuO O O CO2H - - 0 N sufentanil Bl-1584 cyclohexylO O O CO2H - - 0 N sufentanil <BR> <BR> B1-1585 iPrO O O CO2H--0 N sufentanil Bl-1586 PhO O O CO2H - - 0 N sufentanil Bl-1587 (HOCH2- O O CO2H - - 0 N sufentanil CH2) 2N B1-1588 N (H) NMe2 O O CO2H - - 0 N sufentanil <BR> <BR> B 1-1589 4-(OH) Ph O O CO2H-0 N sufentanil<BR> <BR> <BR> <BR> B 1-1590 4-(NH2) Ph O O CO2H--0 N sufentanil<BR> <BR> <BR> <BR> B1-1591 EtS O O CO2H--0 N tamoxifen Bl-1592 EtO O O CO2H - - 0 N tamoxifen Bl-1593 t-BuO O O CO2H - - 0 N tamoxifen Bl-1594 cyclohexylO O O CO2H - - 0 N tamoxifen <BR> <BR> B1-1595 iPrO O O CO2H--0 N tamoxifen Bl-1596 PhO O O CO2H - - 0 N tamoxifen Bl-1597 (HOCH2- O O CO2H - - 0 N tamoxifen CH2) 2N B1-1598 N (H) NMe2 O O CO2H - - 0 N tamoxifen Bl-1559 (OH) Ph O O C02H--0 N tamoxifen <BR> <BR> B1-1600 4-(NH2) Ph O O CO2H-0 N tamoxifen Bl-1601 EtS O O CO2H - - 0 N terbinafine Bl-1602 EtO O O CO2H - - 0 N terbinafine Bl-1603 t-BuO O O CO2H - - 0 N terbinafine Bl-1604 cyclohexylO O O CO2H - - 0 N terbinafine <BR> <BR> B 1-1605 iPrO O 0 CO2H--0 N terbinafine Bl-1606 PhO O O CO2H - - 0 N terbinafine <BR> <BR> B 1-1607 (HOCH2-0 O CO2H--0 N terbinafine<BR> <BR> <BR> <BR> <BR> CH2) 2N Bl-1608 N(H)NMe2 O O CO2H - 0 N terbinafine Bl-1609 4-(OH)Ph O O CO2H - - 0 N terbinafine <BR> <BR> B1-1610 4-(NH2) Ph O O CO2H-0 N terbinafine<BR> <BR> <BR> B 1-1611 EtS O O C02H--0 N trihexyphenidyl Bl-1612 EtO O O CO2H - - 0 N trihexyphenidyl Bl-1613 t-BuO O O CO2H - - 0 N trihexyphenidyl <BR> <BR> B 1-1614 cyclohexyl0 O O C02H--0 N trihexyphenidyl Bl-1615 iPrO O O CO2H - - 0 N trihexyphenidyl Bl-1616 PhO O O CO2H - - 0 N trihexyphenidyl Bl.-1617 (HOCH2-O O CO2H--0 N trihexyphenidyl <BR> <BR> CH2) 2N<BR> <BR> <BR> <BR> <BR> B 1-1618 N (H) NMe2 O O CO2H--0 N trihexyphenidyl<BR> <BR> <BR> <BR> <BR> <BR> B 1-1619 4- (OH) Ph O O C02H--0 N trihexyphenidyl<BR> <BR> <BR> <BR> <BR> <BR> B1-1620 4-(NH2) Ph O O CO2H-0 N trihexyphenidyl<BR> <BR> <BR> <BR> <BR> <BR> B 1-1621 EtS O O CO2H--0 N troleandomycin Bl-1622 EtO O O CO2H - - 0 N troleandomycin Bl-1623 t-BuO O O CO2H - - 0 N troleandomycin Bl-1624 cyclohexylO O O CO2H - - 0 N troleandomycin <BR> <BR> B 1-1625 iPrO O O CO2H--0 N troleandomycin Bl-1626 PhO O O CO2H - - 0 N troleandomycin Bl-1627 (HCH2- O O CO2H - - 0 N troleandomycin CH2) 2N <BR> <BR> B 1-1628 N (H) NMe2 O O CO2H--0 N troleandomycin Bl-1629 4-(OH)Ph O O CO2H - - 0 N troleandomycin <BR> <BR> B 1-1630 4-(NH2) Ph O O CO2H-0 N troleandomycin<BR> <BR> <BR> <BR> <BR> B 1-1631 EtS O O CO2H--0 N verapamil Bl-1632 EtO O O CO2H - - 0 N verapamil Bl-1633 t-BuO O O CO2H - - 0 N verapamil Bl-1634 cyclohexylO O O CO2H - - 0 N verapamil <BR> <BR> B 1-1635 iPrO O O CO2H--0 N verapamil Bl-1636 PhO O O CO2H - - 0 N verapamil Bl-1637 (HOCH2- O O CO2H - - 0 N verapamil CH2) 2N Bl-1638 N(H)NMe2 O O CO2H - - 0 N verapamil Bl-1639 4-(OH)Ph O O CO2H - - 0 N verapamil <BR> <BR> B 1-1640 4- (NH2) Ph O 0 CO2H--0 N verapamil<BR> <BR> <BR> <BR> <BR> <BR> B 1-1641 EtS O O CO2H--0 N caffeine Bl-1642 EtO O O CO2H - - 0 N caffeine Bl-1643 t-BuO O O CO2H - - 0 N caffeine Bl-1644 cyclohexylO O CO2H - - 0 N caffeine B 1-1645 iPrO O O CO2H--0 N caffeine Bl-1646 PhO O O CO2H - - 0 N caffeine Bl-1647 (HOCH2- O O CO2H - - 0 N caffeine CH2) 2N B 1-1648 N (H) NMe2 O O CO2H - - 0 N caffeine <BR> <BR> Bl-16494- (OH) Ph00C02H-- 0 Ncaffeine<BR> <BR> <BR> <BR> <BR> <BR> B1-1650 4-(NH2) Ph O O CO2H-0 N caffeine<BR> <BR> <BR> <BR> <BR> <BR> B 1-1651 EtS O 0 C02H--0 N cyproheptadine Bl-1652 EtO O O CO2H - - 0 N cyproheptadine Bl-1653 t-BuO O O CO2H - - 0 N cyproheptadine Bl-1654 cyclohexylO O O CO2H - - 0 N cyproheptadine B 1-1655 iPrO O O C02H--0 N cyproheptadine Bl-1656 PhO O O CO2H - - 0 N cyproheptadine <BR> <BR> B 1-1657 (HOCH2-O 0 C02H--0 N cyproheptadine CH2) 2N Bl-1658 N(H)NMe2 O O CO2H - - 0 N cyproheptadine Bl-1659 4-(OH)Ph O O CO2H - - 0 N cyproheptadine <BR> <BR> B 1-1660 4-(NH2) Ph O O C02H--0 N cyproheptadine Bl-1661 EtS O O CO2H - - 0 N pramoxine Bl-1662 EtO O O CO2H - - 0 N pramoxine Bl-1663 t-BuO O O CO2H - - 0 N pramoxine Bl-1664 cyclohexylO O O CO2H - - 0 N pramoxine <BR> <BR> B 1-1665 iPrO O O CO2H--0 N pramoxine Bl-1666 PhO O O CO2H - - 0 N pramoxine Bl-1667 (HOCH2- O O CO2H - 0 N pramoxine CH2) 2N B 1-1668 N (H) NMe200C02H-- 0 Npramoxine Bl-1669 4-(OH)Ph O O CO2H - - 0 N pramoxine <BR> <BR> B1-1670 4- (NH2) Ph O 0 CO2H--0 N pramoxine Bl-1671 EtS O O CO2H - - 0 O iodoquinol <BR> <BR> B 1-1672 EtO O O CO2H--0 O iodoquinol Bl-1673 t-BuO O O CO2H - - 0 O iodoquinol B1-1674 CyclohexylO O O CO2H - - 0 O iodoquinol Bl-1675 iPrO O O CO2H - - 0 O iodoquinol Bl-1676 PhO O O CO2H - - 0 O iodoquinol Bl-1677 (HOCH2- O O CO2H - - 0 O iodoquinol CH2) 2N B 1-1678 N (H) NMe2 O O CO2H - - 0 O iodoquinol Bl-1679 4-(OH)Ph O O CO2H - - 0 O iodoquinol <BR> <BR> B1-1680 4- (NH2) Ph O 0 CO2H--0 O iodoquinol Bl-1681 EtS O O CO2H - - 0 O metronidazole <BR> <BR> B 1-1682 EtO O 0 CO2H--0 O metronidazole<BR> <BR> <BR> <BR> <BR> B 1-1683 t-BuO O O CO2H--0 O metronidazole Bl-1684 cyclohexylO O O CO2H - - 0 O metronidazole <BR> <BR> Bl-1685 iPrO 0 O C02H--0 O metronidazole<BR> <BR> <BR> <BR> B 1-1686 PhO O 0 CO2H--0 O metronidazole Bl-1687 (HOCH2- O O CO2H - - 0 O metroidazole CH2) 2N <BR> <BR> B 1-1688 N (H) NMe2 O 0 CO2H--0 O metronidazole<BR> <BR> <BR> <BR> B 1-1689 4- (OH) Ph O 0 CO2H--0 O metronidazole Bl-1690 4-(NH2)Ph O O CO2H - - 0 O metronidazole <BR> <BR> B 1-1691 EtS O O CO2H--0 N papaverine Bl-1692 EtO O O CO2H - - 0 N papaverine Bl-1693 t-BuO O O CO2H - - 0 N papaverine Bl-1694 cyclohexylO O O CO2H - - 0 N papaverine <BR> <BR> B 1-1695 iPrO O O C02H--0 N papaverine Bl-1696 PhO O O CO2H - - 0 N papaverine Bl-1697 (HOCH2- O O CO2H - - 0 N papaverine CH2) 2N B 1-1698 N (H) NMe2 O O CO2H - - 0 N papaverine Bl-1699 4-(OH)Ph O O CO2H - - 0 N papaverine Bl-1700 4-(NH2)Ph O O CO2H - - 0 N papaverine <BR> <BR> B1-1701 EtS O 0 C02H--0 N tropicamide Bl-1702 EtO O O CO2H - - 0 N tropicamide Bl-1703 t-BuO O O CO2H - - 0 N tropicamide Bl-1704 cyclohexylO O O CO2H - - 0 N tropicamide <BR> <BR> B1-1705 iPrO O O CO2H--0 N tropicamide Bl-1706 PhO O O CO2H - - 0 N tropicamide Bl-1706 (HOCH2- O O CO2H - - 0 N tropicamide CH2) 2N B1-1708 N (H) NMe2 O O CO2H - - 0 N tropicamide Bl-1709 4-(OH)Ph O O CO2H - - 0 N tropicamide B1-1710 4-(NH2) Ph O O CO2H-0 N tropicamide Bl-1711 EtS O O CO2H - - 0 N halazepam Bl-1712 EtO O O CO2H - - 0 N halazepam Bl-1713 t-BuO 0 O CO2H--0 N halazepam Bl-1714 CyclohexylO O O CO2H - - 0 N halazepam B1-1715 iPrO O O C02H--0 N halazepam Bl-1716 PhO O O CO2H - - 0 N halazepam Bl-1717 (HOCH2- O O CO2H - - 0 N halazepam CH2) 2N B1-1718 N (H) NMe2 O O CO2H--0 N halazepam <BR> <BR> B1-1719 4-(OH) Ph O O CO2H--0 N halazepam<BR> <BR> <BR> <BR> B 1-1720 4-(NH2) Ph O O CO2H--0 N halazepam<BR> <BR> <BR> <BR> <BR> B1-1721 EtS O O CO2H--0 O mazindol Bl-1722 EtO O O CO2H - - 0 O mazindol Bl-1723 t-BuO O O CO2H - - 0 O mazindol B1-1724 cyclohexyl0 0 O CO2H--0 O mazindol Bl-1725 iPrO O O CO2H - - 0 O mazindol Bl-1726 PhO O O CO2H - - 0 O mazindol Bl-1727 (HOCH2- O O CO2H - - 0 O mazindol CH2) 2N Bl-1728 N (H) NMe2 O O CO2H - - 0 O mazindol Bl-1729 4-(OH)Ph O O CO2H - - 0 O mazindol Bl-1730 4-(NH2)Ph O O CO2H - - 0 O mazindol <BR> <BR> B1-1731 EtS 0 O CO2H--0 O hydroxyitraconazole B 1-1732 EtO O O CO2H - - 0 O hydroxyitraconazole Bl-1733 t-BuO O O CO2H - - 0 O hydroxyitraconazole Bl-1734 cyclohexylO O O CO2H - - 0 O, hydroxyitraconazole <BR> <BR> B1-1735 iPrO O O CO2H--0 O hydroxyitraconazole<BR> <BR> <BR> <BR> <BR> B1-1736 PhO O O CO2H--0 O hydroxyitraconazole B1-1737 (HOCH2- O O CO2H - - 0 O hydroxyitraconazole CH2) 2N Bl-1738 N (H) NMe2 O O CO2H - - 0 O hydroxyitraconazole Bl-1739 4-(OH)Ph O O CO2H - - 0 O hydroxyitraconazole Bl-1740 4-(NH2)Ph O O CO2H - - 0 O hydroxyitraconazole Bl-1741 EtS O O CO2H - - 0 O posaconazole Bl-1742 EtO O O CO2H - - 0 O posaconazole Bl-1743 t-BuO O O CO2H - - 0 O posaconazole Bl-1744 cyclohexylO O O CO2H - - 0 O posaconazole Bl-1745 iPrO O O CO2H - - 0 O posaconazole Bl-1746 PhO O O CO2H - - 0 O posaconazole Bl-1747 (HOCH2- O O CO2H - - 0 O posaconazole CH2))2N B1-1748 N (H) NMe2 0 O C02H-0 0 posaconazole Bl-1749 4-(OH)Ph O O CO2H - - 0 O posaconazole B 1-1750 4-(NH2) Ph O O CO2H--0 O posaconazole Bl-1751 EtS O O CO2H - - 0 O voriconazole Bl-1752 EtO O O CO2H - - 0 O voriconazole Bl-1753 t-BuO O O CO2H - - 0 O voriconazole B1-1754 cyclohexyl0 O 0 C02H--0 O voriconazole Bl-1755 iPrO O O CO2H - - 0 O voriconazole Bl-1756PhO00COzH--0 0voriconazole Bl-1757 (HOCH2- O O CO2H - - 0 O voriconazole CH2) 2N <BR> <BR> B 1-1758 N (H) NMe2 O O CO2H--0 O voriconazole<BR> <BR> <BR> <BR> <BR> B1-1759 4- (OH) Ph O 0 C02H--0 O voriconazole Bl-1760 4-(NH2)Ph O O CO2H - - 0 O voriconazole <BR> <BR> B1-1761 EtS O 0 C02H--0 O fluconazole Bl-1762 EtO O O CO2H - - 0 O fluconazole Bl-1763 t-BuO O O CO2H - - 0 O fluconazole Bl-1764 cyclohexylO O O CO2H - - 0 O fluconazole Bl-1765 iPrO O O CO2H - - 0 O fluconazole Bl-1766PhO00C02H--0 0fluconazole <BR> <BR> B 1-1767 (HOCH2-O O CO2H--0 O fluconazole CH2) 2N Bl-1768 N(H)NMe2 O O CO2H - - 0 O fluconazole <BR> <BR> B 1-17694- (OH) Ph00C02H-- 0 0fluconazole B 1-1770 4- (NH2) Ph 0 O C02H--0 O fluconazole Bl-1771 EtS O O CO2H - - 0 O genaconazole <BR> <BR> B 1-1772 EtO O 0 C02H--0 0 genaconazole Bl-1773 t-BuO O O CO2 H - - 0 O genaconazole <BR> <BR> B1-1774 cyclohexyl0 O O CO2H--0 O genaconazole<BR> <BR> <BR> <BR> <BR> B1-1775 iPrO O O CO2H--0 O genaconazole Bl-1776 PhO O O CO2H - - 0 O genaconazole B1-1777 (HOCH2- O O CO2H - - 0 O genaconazole CH2) 2N B 1-1778 N (H) NMe2 O O CO2H - - 0 O genaconazole <BR> <BR> B 1-1779 4- (OH) Ph O 0 C02H--0 O genaconazole Bl-1780 4-(NH2)Ph O O CO2H - - 0 O genaconazole <BR> <BR> B1-1781 EtS O O CO2H--0 N aliconazole Bl-1782 EtO O O CO2H - - 0 N aliconazole Bl-1783 t-BuO O O CO2H - - 0 N aliconazole Bl-1784 cyclohexylO O O CO2H - - 0 N aliconazole Bl-1785 iPrO O O CO2H - - 0 N aliconazole Bl-1786 PhO O O CO2H - - 0 N aliconazole Bl-1787 (HOCH2- O O CO2H - - 0 N aliconazole CH2) 2N Bl-1788 N(H)NMe2 O O CO2H - - 0 N aliconazole <BR> <BR> B1-1789 4-(OH) Ph O O C02H--0 N aliconazole Bl-1790 4-(NH2)Ph O O CO2H - - 0 N aliconazole <BR> <BR> B1-1791 EtS O O C02H--0 N becliconazole Bl-1792 EtO O O CO2H - - 0 N becliconazole <BR> <BR> B1-1793 t-BuO O O CO2H--0 N becliconazole Bl-1794 cyclohexylO O O CO2H - - 0 N becliconazole <BR> <BR> B1-1795 iPrO 0 O C02H--0 N becliconazole Bl-1796 PhO O O CO2H - - 0 N becliconazole Bl-1797 (HOCH2- O O CO2H - - 0 N becliconazole CH2) 2N <BR> <BR> B 1-1798 N (H) NMe2 O 0 C02H--0 N becliconazole Bl-1799 4-(OH)Ph O O CO2H - - 0 N becliconazole Bl-1800 4-(NH2)Ph O O CO2H - - 0 N becliconazole B1-1801 EtS O O CO2H-0 N brolaconazole<BR> <BR> <BR> <BR> B 1-1802 EtO O O CO2H-0 N brolaconazole Bl-1803 t-BuO O O CO2H - - 0 N brolaconazole Bl-1804 cyclohexylO O O CO2H - - 0 N brolaconazole <BR> <BR> B 1-1805 iPrO O O CO2H--0 N brolaconazole Bl-1806 PhO O O CO2H - - 0 N brolaconazole Bl-1807 (HOCH2- O O CO2H - - 0 N brolaconazole CH2) 2N <BR> <BR> B 1-1808 N (H) NMe2 O 0 C02H--0 N brolaconazole Bl-1809 4-(OH)Ph O O CO2H - - 0 N brolaconazole <BR> <BR> B 1-1810 4-(NH2) Ph O O CO2H-0 N brolaconazole<BR> <BR> <BR> <BR> B 1-1811 EtS O O CO2H--0 N butaconazole Bl-1812 EtO O O CO2H - - 0 N butaconazole Bl-1813 t-BuO O O CO2H - - 0 N butaconazole Bl-1814 cyclohexylO O O CO2H - - 0 N butaconazole <BR> <BR> B1-1815 iPrO O O CO2H-0 N butaconazole Bl-1816 PhO O O CO2H - - 0 N butaconazole Bl-1817 (HOCH2- O O CO2H - - 0 N butaconazole CH2) 2N Bl-1818 N(H)NMe2 O O CO2H - 0 N butaconazole <BR> <BR> B1-1819 4-(OH) Ph O O CO2H-0 N butaconazole<BR> <BR> <BR> <BR> <BR> B 1-1820 4-(NH2) Ph O O CO2H--0 N butaconazole<BR> <BR> <BR> <BR> B 1-1821 EtS O O CO2H--0 N clotrimazole Bl-1822 EtO O O CO2H - - 0 N clotrimazole Bl-1823 t-BuO O O CO2H - - 0 N clotrimazole Bl-1824 cycohexylO O O CO2H - - 0 N clotrimazole <BR> <BR> B 1-1825 iPrO O O CO2H-0 N clotrimazole Bl-1826 PHO O O CO2H - - 0 N Clotrimazole Bl-1827 (HOCH2- O O CO2H - - 0 N clotrimazole <BR> <BR> CH2) 2N<BR> <BR> <BR> <BR> <BR> B 1-1828 N (H) NMe2 O O C02H--0 N clotrimazole Bl-1829 4-(OH)Ph O O CO2H - - 0 N clotrimazole <BR> <BR> B 1-1830 4-(NH2) Ph O O CO2H-0 N clotrimazole<BR> <BR> <BR> <BR> B 1-1831 EtS O O CO2H-0 N croconazole Bl-1832 EtO O O CO2H - - 0 N croconazole Bl-1833 t-BuO O O CO2H - - 0 N croconazole Bl-1834 cyclohexylO O O CO2H - - 0 N croconazole <BR> <BR> B 1-1835 iPrO O O CO2H-0 N croconazole Bl-1836 PhO O O CO2H - 0 N croconazole <BR> <BR> <BR> B1-1837 (HOCH2-0 O C02H-0 N croconazole<BR> <BR> <BR> <BR> <BR> CH2) 2N Bl-1838 N (H) NMe2 O O CO2H - - 0 N croconazole <BR> <BR> B1-1839 4-(OH) Ph O O CO2H-0 N croconazole<BR> <BR> <BR> <BR> <BR> B 1-1840 4-(NH2) Ph O O CO2H-0 N croconazole Bl-1841 EtS O O CO2H - - 0 N econazole Bl-1842 EtO O O CO2H - - 0 N econazole Bl-1843 t-BuO O O CO2H - - 0 N econazole Bl-1844 cyclohexylO O O CO2H - - 0 N econazole Bl-1845 iPrO O O CO2H - 0 N econazole B 1-1846 PhO O O CO2H - 0 N econazole B1-1847 (HOCH2- O O CO2 H - - 0 N econazole CH2) 2N B 1-1848 N (H) NMe2 0 O C02H--0 N econazole <BR> <BR> B 1-1849 4-(OH) Ph O O CO2H--0 N econazole<BR> <BR> <BR> <BR> <BR> B 1-1850 4-(NH2) Ph O O CO2H-0 N econazole<BR> <BR> <BR> <BR> <BR> B 1-1851 EtS O O CO2H--0 N democonazole B1-1852 EtO O O CO2H - - 0 N democonazole B1-1853 t-BuO O O CO2H - - 0 N democonazole B1-1854 cyclohexylO O O CO2H - - 0 N democonazole <BR> <BR> Bl-1855 iPrO O O CO2H--0 N democonazole B1-1856 PhO O O CO2H - - 0 N democonazole B1-1857 (HOCH2- O O CO2H - - 0 N democonazole <BR> <BR> CH2) 2N<BR> <BR> <BR> <BR> <BR> B 1-1858 N (H) NMez O O CO2H-0 N democonazole<BR> <BR> <BR> <BR> <BR> B 1-1859 4-(OH) Ph O O CO2H-0 N democonazole<BR> <BR> <BR> <BR> <BR> B1-1860 4-(NH2) Ph O O CO2H-0 N democonazole<BR> <BR> <BR> <BR> <BR> B 1-1861 EtS O O CO2H--0 N doconazole B1-1862 EtO O O CO2H - - 0 N doconazole <BR> <BR> <BR> Bl-1863 t-BuO 0 O CO2H--0 N doconazole B1-1864 cyclohexylO O O CO2H - - 0 N doconazole <BR> <BR> B 1-1865 iPrO O O CO2H--0 N doconazole B1-1866 PhO O O CO2H - - 0 N doconazole B1-1867 (HOCH2- O O CO2H - - 0 N doconazole CH2) 2N <BR> <BR> B 1-1868 N (H) NMez O O CO2H-0 N doconazole B1-1869 4-(OH)Ph O O CO2H - - 0 N doconazole B1-1870 4-(NH2)Ph O O CO2H - - 0 N doconazole <BR> <BR> B 1-1871 EtS O O CO2H--0 N fenticonazole B1-1872 EtO O O CO2H - - 0 N fenticonazole B1-1873 t-BuO O O CO2H - - 0 N fenticonazole B1-1874 cyclohexylO O O CO2H - - 0 N fenticonazole <BR> <BR> B 1-1875 iPrO O O CO2H--0. N fenticonazole B1-1876 PhO O O CO2H - - 0 N fenticonazole <BR> <BR> <BR> Bl-1877 (HOCH2-0 O COzH--0 N fenticonazole CH2) 2N <BR> <BR> B 1-1878 N (H) NMez O O CO2H--0 N fenticonazole B1-1879 4-(OH)Ph O O CO2H - - 0 N fenticonazole B1-1880 4-(NH2)Ph O O CO2H - - O N fenticonazole <BR> <BR> B1-1881 EtS O O CO2H--0 N eberconazole B1-1882 EtO O O CO2H - - 0 N eberconazole B1-1883 t-BuO O O CO2H - - 0 N eberconazole B1-1884 cyclohexylO O O CO2H - - 0 N eberconazole <BR> <BR> Bl-1885 iPrO O O CO2H--0 N eberconazole B1-1886 PhO O O CO2H - - 0 N EBERCONAZOLE B1-1887 (HOCH2- O O CO2H - - 0 N eberconazole CH2) 2N B 1-1888 N (H) NMe2 O O CO2H - - 0 N eberconazole B1-1889 4-(OH)Ph O O CO2H - - 0 N eberconazole <BR> <BR> B 1-1890 4- (NH2) Ph O O COzH--0 N eberconazole B1-1891 EtS O O CO2H - 0 N isoconazole B1-1892 EtO O O CO2H - - 0 N isoconazole <BR> <BR> Bl-1893 t-BuO 0 O CO2H--0 N isoconazole B1-1894 cyclohexylO O O CO2H - - 0 N isoconazole B1-1895 iPrO O O CO2H - - 0 N isoconazole <BR> <BR> B 1-1896 PhO O O CO2H--0 N isoconazole Bl-1897 (HOCH2-00C02H-- 0 Nisoconazole CH2) 2N <BR> <BR> Bl-1898 N (H) NMe2 0 O C02H-0 N isoconazole<BR> <BR> <BR> <BR> B 1-1899 4- (OH) Ph 0 O CO2H-0 N isoconazole<BR> <BR> <BR> <BR> B1-1900 4-(NH2) Ph O O CO2H-0 N isoconazole B1-1901 EtS O O CO2H - - 0 N miconazole B1-1902 EtO O O CO2H - - 0 N miconazole B1-1903 t-BuO O O CO2H - - 0 N miconazole B1-1904 cyclohexylO O O CO2H - - 0 N miconazole <BR> <BR> B 1-1905 iPrO O O CO2H--0 N miconazole B1-1906 PhO O O CO2H - - 0 N miconazole B-1-1907 (HOCH2- O O CO2H - - 0 N miconazole CH2) 2N B1-1908 N(H)NMe2 O O CO2H - - 0 N miconazole B1-1909 4-(OH)Ph O O CO2H - - 0 N miconazole B1-1910 4-(NH2)Ph O O CO2H - - 0 N miconazole B1-1911 EtS O O CO2H - - 0 N neticonazole B1-1912 EtO O O CO2H - - 0 N neticonazole <BR> <BR> B1-1913 t-BuO 0 O C02H--0 N neticonazole B1-1914 cyclohexylO O O CO2H - - 0 N neticonazole B1-1915 iPrO O O CO2H 0 N neticonazole Bl-1916PhO00C02H0 Nneticonazole <BR> <BR> B1-1917 (HOCH2-O O CO2H 0 N neticonazole CH2) 2N B1-1918 N(H)NMe2 O O CO2H - 0 N neticonazole <BR> <BR> B1-1919 4- (OH) Ph O O C02H-0 N neticonazole<BR> <BR> <BR> <BR> B1-1920 4- (NH2) Ph 0 O CO2H-0 N neticonazole B 1-1921EtS00C02H-0 Nomoconazole B 1-1922EtO00C02H-0 Nomoconazole B1-1923 t-BuO O O CO2H - 0 N omoconazole <BR> <BR> B 1-1924 cyclohexyl0 O 0 C02H--0 N omoconazole B1-1925 iPrO O O CO2H - - 0 N omoconazole B1-1926 PhO O O CO2H - - 0 N omoconazole Bl-1927 (HOCH2-00C02H-- 0 Nomoconazole CH2) 2N B1-1928 N(H)NMe2 O O CO2H - 0 N omoconazole B1-1929 4-(OH)Ph O O CO2H - 0 N omoconazole <BR> <BR> B1-1930 4-(NH2) Ph O O CO2H-0 N omoconazole B1-1931 EtS O O CO2H - - 0 N orconazole B1-1932 EtO O O CO2H - - 0 N orconazole <BR> <BR> Bl-1933<-BuO00C02H--0 Norconazole B1-1934 cyclohexylO O O CO2H - - 0 N orconazole B1-1935 iPrO O O CO2H - - 0 N orconazole Bl-1936PhO00C02H--0 Norconazole <BR> <BR> B 1-1937 (HOCH2-0 O CO2H--0 N orconazole CH2) 2N B1-1938 N (H) NMe2 O O CO2H--0 N orconazole B1-1939 4-(OH)Ph O O CO2H - - 0 N orconazole <BR> <BR> B 1-1940 4- (NH2) Ph O O CO2H--0 N orconazole<BR> <BR> <BR> <BR> <BR> B1-1941 EtS O O CO2H--0 N oxiconazole<BR> <BR> <BR> <BR> <BR> B 1-1942 EtO O O CO2H--0 N oxiconazole B1-1943 t-BuO O O CO2H - - 0 N oxiconazole B1-1944 cyclohexylO O O CO2H - - 0 N oxiconazole B1-1945 iPrO O O CO2H - - 0 N oxiconazole B1-1946 PhO O O CO2H - - 0 N oxiconazole B1-1947 (HOCH2- O O CO2H - - 0 N oxiconazole CH2) 2N B 1-1948 N (H) NMe2 O O C02H--0 N oxiconazole B1-1949 4-(OH)Ph O O CO2H - - 0 N oxiconazole <BR> <BR> B 1-1950 4-(NH2) Ph O O CO2H--0 N oxiconazole B1-1951 EtS O O CO2H - - 0 N parconazole <BR> <BR> B 1-1952 EtO O O CO2H--0 N parconazole B1-1953 t-BuO O O CO2H - - 0 N parconazole B1-1954 cyclohexylO O O CO2H - - 0 N parconazole <BR> <BR> Bl-1955 iPrO O O C02H--0 N parconazole B1-1956 PhO O O CO2H - - 0 N parconazole B1-1957 (HOCH2- O O CO2H - - 0 N parconazole CH2) 2N B1-1958 N (H) NMe2 O O CO2H - - 0 N parconazole <BR> <BR> B1-1959 4-(OH) Ph O O CO2H 0 N parconazole<BR> <BR> <BR> <BR> <BR> B1-1960 4-(NH2) Ph O O CO2H-0 N parconazole<BR> <BR> <BR> <BR> B 1-1961 EtS O O CO2H--0 N ravuconazole B1-1962 EtO O O CO2H - - 0 N ravuconazole B1-1963 t-BuO O O CO2H - - 0 N ravuconazole B1-1964 cyclohexylO O O CO2H - - 0 N ravuconazole B1-1965 iPrO O O CO2H - - 0 N ravuconazole B1-1966 PhO O O CO2H - - 0 N ravuconazole B1-1967 (HOCH2- O O CO2H - - 0 N ravuconazole CH2) 2N B1-1968 N(H)NMe2 O O CO2H - - 0 N ravuconazole B1-1969 4-(OH)Ph O O CO2H - - 0 N ravuconazole <BR> <BR> B1-1970 4-(NH2) Ph O O CO2H-0 N ravuconazole<BR> <BR> <BR> <BR> <BR> Bl-1971EtS00C02H--0 Nsertaconazole B1-1972 EtO O O CO2H - - 0 N sertaconazole B1-1973 t-BuO O O CO2H - - 0 N sertaconazole B1-1974 cyclohexylO O O CO2H - - 0 N sertaconazole B1-1975 iPrO O O CO2H - - 0 N sertaconazole B1-1976 PhO O O CO2H - - 0 N sertaconazole B1-1977 (HOCH2- O O CO2H - - 0 N sertaconazole CH2) 2N B1-1978 N(H)NMe2 O O CO2H - 0 N sertaconazole <BR> <BR> B1-1979 4- (OH) Ph O 0 C02H-0 N sertaconazole<BR> <BR> <BR> <BR> <BR> B1-1980 4- (NH2) Ph O O CO2H--0 N sertaconazole<BR> <BR> <BR> <BR> <BR> B1-1981 EtS O 0 C02H--0 N sulconazole B1-1982 EtO O O CO2H - - 0 N sulconazole B1-1983 t-BuO O O CO2H - - 0 N sulconazole B1-1984 cyclohexylO O O CO2H - - 0 N sulconazole Bl.-1985 iPrO O O CO2H-0 N sulconazole B1-1986 PhO O O CO2H - - 0 N sulconazole B1-1987 (HOCH2- O O CO2H - - 0 N sulconazole CH2) 2N B 1-1988 N (H) NMe2 O O CO2H - - 0 N sulconazole B1-1989 4-(OH)Ph O O CO2H - - 0 N sulconazole <BR> <BR> B 1-1990 4-(NH2) Ph O O CO2H-0 N sulconazole<BR> <BR> <BR> <BR> B 1-1991 EtS O O CO2H--0 N tioconazole B1-1992 EtO O O CO2H - - 0 N tioconazole B1-1993 t-BuO O O CO2H - - 0 N tioconazole B1-1994 cyclohexylO O O CO2H - - 0 N tioconazole <BR> <BR> B 1-1995 iPrO O O CO2H--0 N tioconazole B1-1996 PhO O O CO2H - - 0 N tioconazole B1-1997 (HOCH2- O O CO2H - - 0 N tioconazole CH2) 2N B1-1998 N(H)NMe2 O O CO2H - - 0 N tioconazole B1-1999 4-(OH)Ph O O CO2H - - 0 N tioconazole <BR> <BR> B1-2000 4-(NH2) Ph O O CO2H-0 N tioconazole Bl-2001EtS00C02H--0 Nvalconazole B1-2002 EtO O O CO2H - - 0 N valconazole B1-2003 t-BuO O O CO2H - - 0 N valconazole B 2-2004 cyclohexylO O O CO2H - - 0 N valconazole <BR> <BR> B 1-2005 iPrO O O CO2H--0 N valconazole B1-2006 PhO O O CO2H - - 0 N valconazole B1-2007 (HOCH2- O O CO2H - - 0 N valconazole CH2) 2N Bl-2008N (H) NMe2 O O CO2H--0 N valconazole B1-2009 4-(OH)Ph O O CO2H - - 0 N valconazole <BR> <BR> B 1-2010 4-(NH2) Ph O O CO2H-0 N valconazole<BR> <BR> <BR> <BR> <BR> B1-2011 EtS O O CO2H--0 N zinoconazole B1-2012 EtO O O CO2H - - 0 N zinoconazole B1-2013 t-BuO O O CO2H - - 0 N zinoconazole B1-2014 cyclohexylO O O CO2H - - 0 N zinoconazole B1-2015 iPrO O O CO2H - - 0 N zinoconazole B1-2016 PhO O O CO2H - - 0 N zinoconazole B1-2017 (HOCH2- O O CO2H - - 0 N zinoconazole CH2) 2N B1-2018 N (H) NMe2 O O CO2H - - 0 N zinoconazole <BR> <BR> B 1-2019 4-(OH) Ph O O CO2H-0 N zinoconazole B1-2020 4-(NH2)Ph O O CO2H - - 0 N zinoconazole B1-2021 EtS O O C02H O 0 1 C cloxacillin B1-2022 EtO O O CO2H O O 1 C cloxacillin B1-2023 t-BuO O O CO2H O O 1 C cloxacillin B 1-2024cyclohexylO00C02H00 1 C cloxacillin B1-2025 iPrO O O CO2H O O 1 C cloxacillin B1-2026 PhO O O CO2H O O 1 C cloxacillin B1-2027 (HOCH2- O O CO2H O O 1 C cloxacillin CH2) 2N Bl-2028N (H) NMe2 O O CO2H O O 1 C cloxacillin B1-2029 4-(OH)Ph O O CO2H O O 1 C cloxacillin B1-2030 4-(NH2)Ph O O CO2H O O 1 C cloxacilin B1-2031 EtS O O CO2H O O 1 C valproic acid B1-2032 EtO O O CO2H O O 1 C valproic acid B1-2033 t-BuO O O CO2H O O 1 C valproic acid <BR> <BR> B 1-2034cyclohexylO00COzH001Cvalproicacid B1-2035 iPrO O O CO2H O O 1 C valproic acid B1-2036 PhO O O CO2H O O 1 C valproic acid B1-2037 (HOCH2- O O CO2H O O 1 C valproic acid CH2) 2N B1-2038 N (H) NMe2 O O CO2H O O 1 C valproic acid B1-2039 4-(OH)Ph O O CO2H O O 1 C valproic acid B1-2040 4-(NH2)Ph O O CO2H O O 1 C valproic acid <BR> <BR> B1-2041 EtS O O CO2H O O 1 C retinoic acid<BR> <BR> <BR> <BR> <BR> Bl-2042EtO00COzH001Cretinoicacid<BR> <BR> <BR> <BR> <BR> B1-2043 t-BuO O O CO2H O O 1 C retinoic acid B1-2044 cyclohexylO O O CO2H O O 1 C retinoic acid <BR> <BR> B1-2045 iPrO O O CO2H O O 1 C retinoic acid B1-2046 PhO O O CO2H O O 1 C retinoic acid B1-2047 (HOCH2- O O CO2H O O 1 C retinoic acid CH2) 2N B 1-2048 N (H) NMe2 O O CO2H O O 1 C retinoic acid <BR> <BR> B1-2049 4-(OH) Ph O O CO2H O O 1 C retinoic acid B1-2050 4-(NH2)Ph O O CO2H O O 1 C retinoic acid <BR> <BR> B1-2051 EtS O O CO2H O O 1 C oxaprozin B1-2052 EtO O O CO2H O O 1 C oxaprozin B1-2053 t-BuO O O CO2H O O 1 C oxaprozin <BR> <BR> B1-2054 cyclohexyl0 0 O C02H O 0 1 C oxaprozin<BR> <BR> <BR> <BR> <BR> B1-2055 iPrO 0 O C02H O 0 1 C oxaprozin B1-2056 PhO O O CO2H O O 1 C oxaprozin B1-2057 (HOCH2- O O CO2H O O 1 C oxaprozin CH2) 2N Bl-2058 N (H) NMe200C02H001Coxaprozin B1-2059 4-(OH)Ph O O CO2H O O 1 C oxaprozin B 1-2060 4-(NH2)Ph O O CO2H O O 1 C oxaprozin B1-2061 EtS O O CO2H O O 1 C naproxen B1-2062 EtO O O CO2H O O 1 C naproxen B1-2063 t-BuO O O CO2H O O 1 C naproxen <BR> <BR> B 1-2064cyclohexylO00C02H001Cnaproxen B1-2065 iPrO O O CO2H O O 1 C naproxen B1-2066 PhO O O CO2H O O 1 C naproxen B1-2067 (HOCH2- O O CO2H O O 1 C naproxen CH2) 2N B1-2068 N(H)NME2 O O CO2H O O 1 C naproxen B1-2069 4-(OH)Ph O O CO2H O O 1 C naproxen B1-2070 4-(NH2)Ph O O CO2H O O 1 C naproxen <BR> <BR> Bl-2071EtS00C02H001Cmonopril<BR> <BR> <BR> <BR> <BR> Bl-2072EtO00C02H001Cmonopril B1-2073 t-BuO O O CO2H O O 1 C monopril B1-2074 cyclohexylO O O CO2H O O 1 C monopril B1-2075 iPrO O O CO2H O O 1 C monopril B1-2076 PhO O O CO2H O O 1 C monopril Bl-2077 (HOCH2- O O CO2H O O 1 C monopril CH2) 2N Bl-2078 N (H) NMe2 O O CO2H O O 1 C monopril Bl-2079 4-(OH)Ph O O CO2H O O 1 C monopril <BR> <BR> Bl-20804- (NH2) Ph00C02H001Cmonopril.<BR> <BR> <BR> <BR> <BR> <P>B1-2081 EtS O O CO2H O O 1 C ketorolac Bl-2082 EtO O O CO2H O O 1 C ketorolac Bl-2083 t-BuO O O CO2H O O 1 C ketorolac B 1-2084 cyclohexylO O O CO2H O O 1 C ketorolac <BR> <BR> B 1-2085 iPrO O O CO2H O O 1 C ketorolac Bl-2086 PhO O O CO2H O O 1 C ketorolac Bl-2087 (HOCH2- O O CO2H O O 1 C ketorolac CH2) 2N B 1-2088 N (H) NMe200C02H001Cketorolac Bl-2089 4-(OH)Ph O O CO2H O O 1 C ketorolac <BR> <BR> Bl-20904- (NH2) Ph00C02H001Cketorolac<BR> <BR> <BR> <BR> <BR> <BR> B1-2091 EtS O O CO2H O O 1 C ketoprofen Bl-2092 EtO O O CO2H O O 1 C ketoprofen Bl-2093 t-BuO O O CO2H O O 1 C ketoprofen Bl-2094 cyclohexylO O O CO2H O O 1 C ketoprofen Bl-2095 iPrO O O CO2H O O 1 C ketoprofen Bl-2096 PhO O O CO2H O O 1 C ketoprofen Bl-2097 (HOCH2- O O CO2H O O 1 C ketoprofen CH2) 2N Bl-2098 N (H) NMe200C02H001Cketoprofen Bl-2099 4-(OH)Ph O O CO2H O O 1 C ketoprofen Bl-2100 4-(NH2)Ph O O CO2H O O 1 C ketoprofen <BR> <BR> B 1-2101 EtS O O CO2H O O 1 C indomethacin Bl-2102 EtO O O CO2H O O 1 C indomethacin Bl-2103 t-BuO O O CO2H O O 1 C indomethacin Bl-2104 cyclohexylO O O CO2H O O 1 C indomethacin Bl-2105 iPrO O O CO2H O O 1 C indomethacin Bl-2106 PhO O O CO2H O O 1 C indomethacin Bl-2107 (HOCH2- O O CO2H O O 1 C indomethacin CH2) 2N B 1-2108 N (H) NMe200C02H001Cindomethacin Bl-2109 4-(OH)Ph O O CO2H O O 1 C indomethacin Bl-2110 4-(NH2)Ph O O CO2H O O 1 C indomethacin Bl-2111 EtS O O CO2H O O 1 C ibuprofen Bl-2112 EtO O O CO2H O O 1 C ibuprofen Bl-2113 t-BuO O O CO2H O O 1 C ibuprofen Bl-2114 cyclohexylO O O CO2H O O 1 C ibuprofen <BR> <BR> Bl-2115 iPrO O O CO2H 0 O 1 C ibuprofen<BR> <BR> <BR> <BR> <BR> <BR> Bl-2116PhO00C02H001Cibuprofen Bl-2117 (HOCH2- O O CO2H O O 1 C ibuprofen CH2) 2N B 1-2118 N (H) NMe2 O O CO2H O O 1 C ibuprofen <BR> <BR> B 1-2119 4-(OH) Ph O O CO2H O O 1 C ibuprofen Bl-2120 4-(NH2)Ph O O CO2H O O 1 C ibuprofen B1-2121 EtS O O CO2H O O 1 C gemfibrozil Bl-2122 EtO O O CO2H O O 1 C gemfibrozil Bl-2123 t-BuO O O CO2H O O 1 C gemfibrozil Bl-2124 cyclohexylO O O CO2H O O 1 C gemfibrozil <BR> <BR> B1-2125 iPrO O O CO2H O O 1 C gemfibrozil Bl-2126 PhO O O CO2H O O 1 C gemfibrozil Bl-2127 (HOCH2- O O CO2H O O 1 C gemfibrozil CH2) 2N B 1-2128 N (H) NMe200C02H001Cgem6brozil <BR> <BR> Bl-21294. (OH) Ph00C02H001Cgemfibrozil Bl-2130 4-(NH2)Ph O O CO2H O O 1 C gemfibrozil Bl-2131 EtS O O CO2H O O 1 C flurbiprofen Bl-2132 EtO O O CO2H O O 1 C flurbiprofen Bl-2133 t-Buo O O CO2H O O 1 C flurbiprofen Bl-2134 cyclohexylO O O CO2H O O 1 C flurbiprofen Bl-2135 iPrO O O CO2H O O 1 C flurbiprofen Bl-2136 PhO O O CO2H O O 1 C flurbiprofen <BR> <BR> B1-2137 (HOCH2-O O CO2H O O 1 C flurbiprofen CH2) 2N B1-2138 N (H) NMe200COsH001Cflurbiprofen Bl-2139 4-(OH)Ph O O CO2H O O 1 C flurbiprofen <BR> <BR> B1-2140 4- (NH2) Ph O O CO2H 0 O 1 C flurbiprofen Bl-2141 EtS O O CO2H O O 1 C arthrocine Bl-2142 EtO O O CO2H O O 1 C arthrocine Bl-2143 t-BuO O O CO2H O O 1 C arthrocine Bl-2144 cyclohexylO O O CO2H O O 1 C arthrocine Bl-2145 iPrO O O CO2H O O 1 C arthrocine Bl-2146 PhO O O CO2H O O 1 C arthrocine Bl-2147 (HOCH2- O O CO2H O O 1 C arthrocine CH2) 2N B 1-2148 N (H) NMe200C02H001Carthrocine Bl-2149 4-(OH)Ph O O CO2H O O 1 C arthrocine Bl-2150 4-(NH2)Ph O O CO2H O O 1 C arthrocine <BR> <BR> B1-2151 EtS O O CO2H O O 1 C adapalene Bl-2152 EtO O O CO2H O O 1 C adapalene Bl-2153 t-BuO O O CO2H O O 1 C adapalene B1-2154 cyclohexylO O O CO2H O O 1 C adapalene <BR> <BR> Bl-2155 iPrO O O CO2H 0 O 1 C adapalene Bl-2156 PhO O O CO2H O O 1 C adapalene B1-2157 (HOCH2- O O CO2H O O 1 C adapalene CH2) 2N Bl-2158 N (H) NMe200COH001Cadapalene Bl-2159 4-(OH)Ph O O CO2H O O 1 C adapalene Bl-2160 4-(NH2)Ph O O CO2H O O 1 C adapalene <BR> <BR> Bl-2161 EtS O O CO2H 0 O 1 C lansoprazole Bl-2162 EtO O O CO2H O O 1 C lansoprazole Bl-2163 t-BuO O O CO2H O O 1 C lansoprazole Bl-2164 cyclohexylO O O CO2H O O 1 C lansoprazole <BR> <BR> B 1-2165 iPrO O O CO2H O O 1 C lansoprazole Bl-2166 PhO O O CO2H O O 1 C lansoprazole Bl-2167 (HOCH2- O O CO2H O O 1 C lansoprazole CH2) 2N B 1-2168 N (H) NMe200C02H00 1 C lansoprazole Bl-2169 4-(OH)Ph O O CO2H O O 1 C lansoprazole B l-2170 4-(NH2)PH O O CO2H O O 1 C lansoprazole B l-2171 EtS O O CO2H O O 1 C lovastatin Bl-2172 EtO O O CO2H O O 1 C lovastatin B 1-2173 t-BuO O O CO2H O O 1 C lovastatin B 1-2174cyclohexylO00C02H00 1 C lovastatin B1-2175 iPrO O O C02H O O 1 C lovastatin Bl-2176 PhO O O CO2H O O 1 C lovastatin Bl-2177 (HOCH2- O O CO2H O O 1 C lovastatin CH2) 2N Bl-2178 N (H) NMe200C02H00 1 C lovastatin B l-2179 4-(OH)Ph O O CO2H O O 1 C lovastatin B l-2180 4-(NH2)Ph O O CO2H O O 1 C lovastatin B l-2181 EtS O O CO2H O O 1 C warfarin Bl-2182 EtO O O CO2H O O 1 C warfarin Bl-2183 t-BuO O O CO2H O O 1 C warfarin B l-2184 cyclohexylO O O CO2H O O 1 C warfarin B l-2185 iPrO O O CO2H O O 1 C warfarin B l-2186 O O CO2H O O 1 C warfarin B 1-2187 (HOCH2- O O CO2H O O 1 C warfarin CH2) 2N B 1-2188 N (H) NMe200C02H00 1 C warfarin B 1-21894- (OH) Ph00C02H00 1 C warfarin B l-2190 4-(NH2)Ph O O CO2H O O 1 C warfarin B 1-2191 EtS O 0 C02H--0 N tolteridine B l-2192 EtO O O CO2H - - 0 N tolteridine B l-2193 t-BuO O O CO2H - - 0 N tolteridine Bl-2194 cyclohexylO O O CO2H - - 0 N tolteridine B l-2195 iPrO O O CO2H - - 0 N tolteridine B 1-2196 PhO O 0 C02H--0 N tolteridine B 1-2197 (HOCH2- O O CO2H - - 0 N tolteridine CH2) 2N B 1-2198 N (H) NMe2 O O CO2H - - 0 N tolteridine Bl-2199 4-(OH)Ph O O CO2H - - 0 N tolteridine Bl-2200 4-(NH2)Ph O O CO2H - - 0 N tolteridine B l-2201 EtS O O CO2H - - 0 N tolteridine Bl-2202 EtO O O CO2H - - 0 N tolteridine <BR> <BR> B 1-2203 t-BuO 0 O C02H--0 N ticlopidine B 1-2204 cyclohexylO O O CO2H - - 0 N tolteridine B 1-2205 iPrO 0 O C02H--0 N ticlopidine B l-2206 PhO O O CO2H - - 0 N tolteridine B 1-2207 (HOCH2- O O CO2H - - 0 N tolteridine CH2) 2N B 1-2208 N (H) NMe2 0 O C02H--0 N ticlopidine B l-2209 4-(OH)Ph O O CO2H - - 0 N tolteridine <BR> <BR> B1-2210 4- (NH2) Ph O O COzH--0 N ticlopidine Bl-2211 EtS O O CO2H - - 0 N sibutramine <BR> <BR> B 1-2212 EtO O 0 CO2H--0 N sibutramine<BR> <BR> <BR> <BR> <BR> B 1-2213 t-BuO 0 O C02H--0 N sibutramine Bl-2214 cyclhexylO O O CO2H - - 0 N sibutramine Bl-2215 iPrO O O CO2H - 0 N sibutramine Bl-2216PhO00C02H--0 Nsibutramine <BR> <BR> <BR> B1-2217 (HOCH2-0 O CO2H 0 N sibutramine<BR> <BR> <BR> <BR> <BR> <BR> CH2) 2N Bl-2218 N (H) NMe2 O O CO2H - - 0 N sibutramine Bl-2219 4-(OH)Ph O O CO2H - - 0 N sibutramine <BR> <BR> B1-2220 4-(NH2) Ph O O CO2H--0 N sibutramine<BR> <BR> <BR> <BR> <BR> Bl-2221EtS00C02H--0 Npropoxyphene Bl-2222 EtO O O CO2H - - 0 N propoxyphene Bl-2223 t-BuO O O CO2H - - 0 N propoxyphene <BR> <BR> B 1-2224 cyclohexylO O O CO2H--0 N propoxyphene Bl-2225 iPrO O O CO2H - - 0 N propoxyphene Bl-2226 PhO O O CO2H - - 0 N propoxyphene <BR> <BR> B 1-2227 (HOCH2-0 O CO2H--0 N propoxyphene CH2) 2N Bl-2228 N(H)NMe2 O O CO2H - - 0 N propoxyphene Bl-2229 4-(OH)Ph O O CO2H - - 0 N propoxyphene B 1-2230 4-(NH2) Ph O O CO2H--0 N propoxyphene <BR> <BR> Bl-2231 EtS O O C02H--0 N nifurantin B l-2232 EtO O O CO2H - - 0 N nifurantin Bl-2233 t-BuO O O CO2H - - 0 N nifurantin B l-2234 cyclohexylO O O CO2H - - 0 N nifurantin <BR> <BR> B1-2235 iPrO O O C02H--0 N nifurantin Bl-2236 PhO O O CO2H - - 0 N nifurantin Bl-2237 (HOCH2-00C02H-- 0 Nnifurantin CH2) 2N B 1-2238 N (H) NMe200C02H-0 Nnifurantin Bl-2239 4-(OH)Ph O O CO2H - - 0 N nifurantin B 1-22404- (NH2) Ph00C02H-0 Nnifurantin Bl-2241 EtS O O CO2H - - 0 N nefazodone Bl-2242 EtO O O CO2H - - 0 N nefazodone Bl-2243 t-BuO O O CO2H - - 0 N nefazodone B 1-2244 cyclohexyl0 O 0 C02H-0 N nefazodone Bl-2245 iPrO O O CO2H - - 0 N nefazodone Bl-2246 PhO O O CO2H - - 0 N nefazodone Bl-2247 (HOCH2- O O CO2H - - 0 N nefazodone CH2) 2N Bl-2248 N (H) NMe200C02H-- 0 Nnefazodone Bl-2249 4-(OH)Ph O O CO2H - - 0 N nefazodone <BR> <BR> B1-2250 4-(NH2) Ph O O CO2H-0 N nefazodone Bl-2251 EtS O O CO2H - - 0 N donezapil Bl-2252 EtO O O CO2H - - 0 N donezapil Bl-2253 t-BuO O O CO2H - - 0 N donezapil <BR> <BR> B1-2254 cyclohexyl0 0 O C02H--0 N donezapil Bl-2255 iPrO O O CO2H - - 0 N donezapil Bl-2256 PhO O O CO2H - - 0 N donezapil Bl-2257 (HOCH2- O O CO2H - - 0 N donezapil CH2) 2N Bl-2258 N(H)NMe2 O O CO2H - - 0 N donezapil B 1-2259 4- (OH) Ph 0 O C02H--0 N donezapil B l-2260 4-(NH2)Ph O O CO2H - - 0 N donezapil

B1-2261 EtS O O CO2H--0 N dicodid Bl-2262 EtO O O CO2H - - 0 N dicodid Bl-2263 t-BuO O O CO2H - - 0 N dicodid Bl-2264 cyclohexylO O O CO2H - - 0 N dicodid B 1-2265 iPrO O O CO2H--0 N dicodid Bl-2266 PhO O O CO2H - - 0 N dicodid B 1-2267 (HOCH2-0 O CO2H--0 N dicodid CH2) 2N B 1-2268 N (H) NMe2 O O CO2H--0 N dicodid Bl-2269 4-(OH)Ph O O CO2H - - 0 N dicodid Bl-2270 4-(NH2)Ph O O CO2H - - 0 N dicodid Bl-2271 EtS O O CO2H - - 0 N colchicine Bl-2272 EtO O O CO2H - - 0 N colchicine Bl-2273 t-BuO O O CO2H - - 0 N colchicine Bl-2274 cyclohexylO O O CO2H - - 0 N colchicine B 1-2275 iPrO O O CO2H--0 N colchicine Bl-2276 PhO O O CO2H - - 0 N colchicine <BR> <BR> B 1-2277 (HOCH2-O O CO2H--0 N colchicine<BR> <BR> <BR> <BR> CH2) 2N B 1-2278 N (H) NMe2 O O CO2H - - 0 N colchicine Bl-2279 4-(OH)Ph O O CO2H - - 0 N colchicine Bl-2280 4-(NH2)Ph O O CO2H - - 0 N colchicine B 1-2281 EtS O O CO2H--0 N citalopram Bl-2282 EtO O O CO2H - - 0 N citalopram Bl-2283 t-BuO O O CO2H - - 0 N citalopram B 1-2284 cyclohexyO O O CO2H - - 0 N citalopram Bl-2285 iPrO O O CO2H - - 0 N citalopram Bl-2286 PhO O O CO2H - - 0 N citalopram Bl-2287 (HOCH2- O O CO2H - - 0 N citalopram CH2) 2N B 1-2288 N (H) NMe200C02H--0 Ncitalopram Bl-2289 4-(OH)Ph O O CO2H - - 0 N citalopram Bl-2290 4-(NH2)Ph O O CO2H - - 0 N citalopram Bl-2291 EtS O O CO2H - - 0 N benzatropine Bl-2292 EtO O O CO2H - - 0 N benzatropine Bl-2293 t-BuO 0 O CO2H--0 N benzatropine Bl-2294 cyclohexylO O O CO2H - - 0 N benzatropine Bl-2295 iPrO O O CO2H - - 0 N benzatropine Bl-2296 PhO O O CO2H - - 0 N benzatropine Bl-2297 (HOCH2- O O CO2H - - 0 N benzatropine CH2) 2N B 1-2298 N (H) NMe2 0 O C02H--0 N benzatropine <BR> <BR> B 1-22994- (OH) Ph00C02H--ONbenzatropine<BR> <BR> <BR> <BR> B 1-2300 4-(NH2) Ph O O C02H-0 N benzatropine Table B2 : Compounds (B2-1)- (B2-2300) are compounds of Formula I where X2, Z1, G10, G", R2, G20, Gay m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for RI which equals CO2Me.

Table B3 : Compounds (B3-1)- (B3-2300) are compounds of Formula I where X2, Z1, , G11, R2, G20, G21, m, t q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2(X2) are identical to those in Table Bl except for Ri which equals CO2Et.

Table B4 : Compounds (B4-1)- (B4-2300) are compounds of Formula I where X2, Z', G°, (G11, R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H Z2 (X2) q-H or Z2 are identical to those in Table B1 except for R'which equals CO2n-Pr.

Table B5 : Compounds (B5-1)- (B5-2300) are compounds of Formula I where X2, Z', Gio G", R2, G20, G21, m, t, q and Z2(X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for R'which equals CO2t-Bu.

Table B6 : Compounds (B6-1)- (B6-2300) are compounds of Formula I where X2, Zl, G10, G", R2, G20, G21, m, t q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for R'which equals CO2cyclopropyl.

Table B7 : Compounds (B7-1)- (B7-2300) are compounds of Formula I where X2, Z', G10 G11, R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for RI which equals C02Bn.

Table B8 : Compounds (B8-1)- (B8-2300) are compounds of Formula I where X2, Z1, Gio, G", R2, G20 G2l m, t, q and Z2(X2)-[(C=G20)-G21]-H, Z2(X2) q-H or Z2 (X2) are identical to those in Table B1 except for RI which equals CO2CH2CH2Ph.

Table B9 : Compounds (B9-1)- (B9-2300) are compounds of Formula I where X2, Z1, G10, G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2(X2) are identical to those in Table Bl except for RI which equals CO2CH2CF3.

Table B10 : Compounds (B10-1)-(B10-2300) are compounds of Formula I where X2, Z1, G10, G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2 (X2) q-H or Z2 (X2) are identical to those in Table Bl except for RI which equals CO2CH20Me.

Table B11 : Compounds (B11-1)-(B11-2300) are compounds of Formula I where X2, , G10, G11, R2, G20, G21, m, t, q and Z2(X2)-[(C=G20)-G21]-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for R1 which equals CO2allyl.

Table B12 : Compounds (B12-1)-(B12-2300) are compounds of Formula I where X2, Zi, G10, G", R2, G20 G21, m, t, q and Z2 (X2)-[(C=G20)-G20]-H, Z2(X2) q-H or Z2 are identical to those in Table Bl except for R1 which equals C02Ph.

Table B13 : Compounds (B13-1)-(B13-2300) are compounds of Formula I where X2, Z1, G10 G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for R1 which equals CO2-2 (OMe) Ph.

Table B14 : Compounds (B14-1)-(B14-2300) are compounds of Formula I where X2, Z1, G10 G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2) q-H or Z2 (X2) are identical to those in Table B1 except for R1 which equals C02-3- (OMe) Ph.

Table B15 : Compounds (B15-1)-(B15-2300) are compounds of Formula I where X2, ZI, G'O, G", R2, G20 G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2) q-H or Z2 (X2) are identical to those in Table B1 except for RI which equals C02-4- (OMe)-Ph.

Table B16 : Compounds (B16-1)-(B16-2300) are compounds of Formula I where X2, Z1, G10 G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2) q-H or Z2 (X2) are identical to those in Table B1 except for R1 which equals CO2-2 (Me) Ph.

Table B17 : Compounds (B17-1)-(B17-2300) are compounds of Formula I where X2, Z1, G10 G", R2, G20, G21, m t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for RI which equals CO2-3 (Me) Ph.

Table B18 : Compounds (B18-1)-(B18-2300) are compounds of Formula I where X2, Z1 G10, G11, R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2) q-H or Z2 (X2) are identical to those in Table B1 except for RI which equals CO2-4 (Me) Ph.

Table B19 : Compounds (B19-lj-(B19-2300) are compounds of Formula I where X2, Z1 G10 G11, R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2(X2) are identical to those in Table Bl except for R1 which equals CO2-4 (NO4) Ph.

Table B20 : Compounds (B20-1)- (B20-2300) are compounds of Formula I where X2, Z', G10 G", R2 G20, G21, m t, q and Z2(X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 are identical to those in Table B1 except for RI which equals CO2SiMe3.

Table B21 : Compounds (B21-1)- (B21-2300) are compounds of Formula I where X2, Zl, G10 G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2) q-H or Z2 (X2) are identical to those in Table B1 except for R'which equals C (=O) N (H) Me.

Table B22 : Compounds (B22-1)- (B22-2300) are compounds of Formula I where X2, Z1, Gio G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for RI which equals C (=O) NMe2.

Table B23 : Compounds (B23-1)- (B23-2300) are compounds of Formula I where X2, Z1, G10 G11, R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H,Z2(X2) q-H or Z2 (X2) are identical to those in Table B1 except for R'which equals C (=O) NBn2.

Table B24 : Compounds (B24-1)- (B24-2300) are compounds of Formula I where X2, Z1, Gio Gii, R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for R'which equals C (=O) N (Me) Bn.

Table B25 : Compounds (B25-1)- (B25-2300) are compounds of Formula I where X2, Z1, Gi, G11, R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2 (X2) q-H or Z2 (X2) are identical to those in Table B1 except for R'which equals C (=O) N (Me) Ph.

Table B26 : Compounds (B26-1)- (B26-2300) are compounds of Formula I where X2, Zi, Gio G11, R2, G20, G21, m, t q and Z2 (X2)-[(c=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table Bl except for Ri which equals C (=O) N (H) Ph.

Table B27 : Compounds (B27-1)- (B27-2300) are compounds of Formula I where X2, , G10, G11, R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2(X2) are identical to those in Table B1 except for R1 which equals C (=O) N (H) NMe2.

Table B28 : Compounds (B28-1)- (B28-2300) are compounds of Formula I where X2, Z1, Gio G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for R'which equals CO2n-octyl.

Table B29 : Compounds (B29-1)- (B29-2300) are compounds of Formula I where X2, Zi, G10 G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for RI which equals C (=O) N (H)/t-Bu.

Table B30 : Compounds (B30-1)- (B30-2300) are compounds of Formula I where X2, Z1, GIO, Gll R2 G20 G21, m t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2(X2) are identical to those in Table B1 except for R3 which equals C (=O) N (H) N (H) CO2Et.

Table B31 : Compounds (B31-1)- (B31-2300) are compounds of Formula I where X2, Z1 GIO, G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for RI which equals C (=O) N (H) N (H) CO2t-Bu.

Table B32 : Compounds (B32-1)- (B32-2300) are compounds of Formula I where X2, Z1 GIO, Gll R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2) q-H or Z2 (X2) are identical to those in Table B1 except for RI which equals C (=O) N (H) N=CHMe.

Table B33 : Compounds (B33-1)- (B33-2300) are compounds of Formula I where X2, Z1, G10 G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]=H, Z2 (X2) q-H or Z2 are identical to those in Table B1 except for R1 which equals C (=O) N (H) N=CMe2.

Table B34 : Compounds (B34-1)- (B34-2300) are compounds of Formula I where X2, Z1 G10, G11, R2, G20, G21, m, t q and Z2(X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for Ri which equals C (=O) N (H) N=CHPh.

Table B35 : Compounds (B35-1)-(B35-2300) are compounds of Formula I where X2, Z, G10 G11, R2, G20, G21, m, t q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for R'which equals C (=O) SPh.

Table B36 : Compounds (B36-1)- (B36-2300) are compounds of Formula I where X2, Z1 G10, G", R', G, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for R'which equals C (=O) SEt.

Table B37 : Compounds (B37-1)- (B37-2300) are compounds of Formula I where X2, Z1 GIO, G11, R2, G21, G21, m, t q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for R'which equals C (=O) Sn-Bu.

Table B38 : Compounds (B38-1)- (B38-2300) are compounds of Formula I where X2, Z1, G10 G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2 (X2) q-H or Z2 (X2) are identical to those in Table B1 except for R1 which equals C (=O) N (H) OMe.

Table B39 : Compounds (B39-1)- (B39-2300) are compounds of Formula I where X2, Z1, G'O, G", R2 G20, G21, m t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-h or Z2 (X2) are identical to those in Table B1 except for R1 which equals C (=O) N (H) OBn.

Table B40 : Compounds (B40-1)- (B40-2300) are compounds of Formula I where X2, Z1, Gio, G", R2, G20, G21, m, t, q and Z2 (X2)-[(C=G20)-G21]-H, Z2(X2)q-H or Z2 (X2) are identical to those in Table B1 except for RI which equals C (=O) N (H) NH2.

Table B41 : Compounds (B41-1)- (B41-2300) are compounds of Formula I where X2, Z1, G10, G11, R2, G20, G21, m, t q and Z2 (X2)-[(C=G20)-G21]-H,Z2(X2)q-H or Z2 (X2) are identical to those in Table Bl except for R1 which equals C (=O) N (H) OH.

Table C describes additional examples of compounds of Formula I which can be made using the procedures described hereinbefore, where R2 is hydrogen, m = 1, q = 0, t = 0 or 1 and the pharmaceutical (a veterinary drug) which defines the pharmaceutical moiety of these examples is Z' (Xl) m-H. The following groups, Z' (Xl) m- H,X1,G10,G11,R1,G20,G21, t and Z2 are defined within Table C.

Table C Cmpd Z1(X1)m-H X1 G10 G11 R1 G20 G21 # C-1 albendazole N O O CO2H O O 1 methyl C-2 clioquinol O O O CO2H O O 1 C(CH3)3 C-3 febantel N O O CO2H O O 1 Ph C-4 fenbendazole N O O Co2H O O 1 4Me(Ph) C-5 guaifenesin O 0 O CO2H--0 C1 C-6 mibolerone O O O CO2H--0 {N (Et) 3}+Cl C-7 omeprazole N O O CH2H - - 0 {N (Me) 2Ph} +Cl- C-8 oxazepam O O O CO2Me O O 1 methyl C-9 piroxicam N O O CO2Me O O 1 C(CH3)3 C-10 primidone N O O CO2Me O O 1 Ph C-11 procainamide N O O CO2Me O O 1 4Me(Ph) C-12 thiabendazole N O O CO2Me--0 C1 C-13 warfarin O O O CO2Me--0 {N (Et) 3} +Cl- C-14 albendazole N O O C02Me--0 {N (Me) 2Ph} +Cl# C-15 clioquinol O O O CO2Et O O 1 methyl C-16 febantel N O O CO2Et--0 C1 C-17 fenbendazole N O S CO2n-Pr O O 1 methyl C-18 guaifenesin O O S CO2n-Pr--0 C1 C-19 mibolerone O O O CO2n-Bu O O 1 methyl C-20 omeprazole N O O CO2n-Bu O O 1 C(CH3)3 C-21 oxazepam O O O CO2n-Bu O O 1 Ph C-22 Piroxicam N O S CO2n-Bu O O 1 4Me(Ph) C-23 primidone N O S CO2n-Bu O O 1 CF3CH2 C-24procainamideN 0 0C02n-Bu--0C1 C-25 thiabendazole N O O C02n-Bu--0 {N (Et) 3} +Cl- C-26 warfarin O O O CO2n-Bu - - 0 {N (Me) 2PH}+Cl# <BR> <BR> C-27 albendazole N O O CO2n-Bu - - 0 O#C(CH3)3 C-28 clioquinol O O O CO2-Bn O O 1 methyl C-29 febantel N O O CO2-Bn O O 1 C(CH3)3 C-30 fenbendazole N O O CO2-Bn O O 1 Ph C-31 guaifenesin O O S CO2-Bn O O 1 4Me(Ph) C-32 mibolerone O O S CO2-Bn O O 1 CF3CH2 C-33 omeprazole N O O CO2-Bn--0 C1 C-34 oxazepam O O O CO2-Bn--0 {N (Et) 3}+Cl- C-35 piroxicam N 0 O C02-Bn--0 {N (Me) 2Ph}+Cl- <BR> <BR> C-36 primidone N O O CO2-Bn O O 0 O#C(CH3)3<BR> <BR> <BR> <BR> C-37 procainamide N O O COSMe O O 1 methyl C-38 thiabendazole N O S COSMe O O 1 C(CH3)3 C-39 warfarin O O O COSMe--0 C1 C-40 albendazole N O 0 COSMe O O 0 {N (Et) 3} +Cl C-41 clioquinol O O S COSEt O O 1 methyl C-42 febantel N 0 O COSEt--0 Cl C-43 fenbendazole N O O COSn-Bu O O 1 methyl C-44 guaifenesin O O S COSn-Bu--0 C1 C-45 mibolerone O O O COSBn O O 1 methyl C-46 omeprazole N 0 O COSBn--0 Cl C-47 oxazepam O O O CONHMe O O 1 methyl C-48 piroxicam N O O CONHMe O O 1 C(CH3)3 <BR> <BR> C-49 primidone N O O CONHEt O O 1 methyl<BR> <BR> <BR> <BR> <BR> <BR> C-50 procainamide N O O CONHn-Pr O O 1 methyl C-51 thiabendazole N O O CONHn-Bu O O 1 methyl C-52 warfarin O O O CONHn-Bu O O 1 C(CH3)3 C-53 albendazole N O O CONHn-Bu O O 1 Ph C-54 clioquinol O O O CONHn-Bu O O 1 4Me(Ph) C-55 febantel N O O CoNHn-Bu O O 1 CF3CH2 C-56 fenbendazole N O 0 CONHn-Bu--0 Cl C-57 guaifenesin O O O CONHn-Bu O O 0 {N (Et) 3} +Cl C-58 mibolerone O O O CONH-Bn O O 1 methyl C-59 omeprazole N O O CONH-Bn O O 1 C(CH3)3 C-60 oxazepam O 0 O CONH-Bn--0 {N (Et) 3} +Cl- C-61 piroxicam N O O CONNNH2 O O 1 methyl C-62 primidone N O O CONHNHMe O O 1 methyl C-63 procainamide N O O CONHNHEt O O 1 methyl C-64 thiabendazole N O O CONHNHPr O O 1 methyl C-65 warfarin O O O CONHNHt-Bu O O 1 C(CH3)3 <BR> <BR> C-66 albendazole N O O CONHNHCO2Me O O 1 C (CH3) 3 C-67 cliquinol O O O CONHNHCO2Et O O 1 C(CH3)3 C-68 febantel N O O CONHNHCO2t-Bu O O 1 C(CH3)3 <BR> <BR> C-69 fenbendazole N O O CONHNHCO2Bn O O 1 C (CH3) 3<BR> <BR> <BR> <BR> <BR> C-70 guaifenesin O O O CONHN=CHMe O O 1 methyl C-71 mibolerone O O 0 CONHN=CHMe--0 {N (Et) 3} +Cl.

C-72 omperazole N O O CONHN=CHPh O O 1 methyl C-73 oxazepam O O O CONHN=CHPh O O 1 C(CH3)3 C-74 disopyramide N O O CO2H O O 1 methyl C-75 disopyramide N O O CO2H O O 1 C(CH3)3 C-76 disopyramide N O O CO2H O O 1 Ph C-77 disopyramide N O O CO2H O O 1 4Me(Ph) C-78 disopyramide N O O CO2H--0 Cl C-79 disopyramide N O O CO2H - - 0 {N (Et) 3}+Cl.

C-80 disopyramide N O O CO2H--0 {N (Me) 2Ph} +Cl- C-81 disopyramide N O O CO2Me O O 1 methyl C-82 disopyramide N O O CO2Me O O 1 C(CH3)3 <BR> <BR> C-83 disopyramide N O O CO2Me O O 1 Ph<BR> <BR> <BR> <BR> <BR> C-84 disopyramide N O O CO2Me O O 1 4Me (Ph)<BR> <BR> <BR> <BR> <BR> C-85 disopyramide N O O CO2Me--0 C1 C-86 aminocaproic acid N O O CO2Me--0 {N (Et) 3} +Cl C-87 aminocaproic acid N O O CO2Me--0 {N (Me) 2Ph} +Cl.

C-88 aminocaproic acid N O O CO2Et 0 0 1 methyl <BR> <BR> C-89 aminocaproic acid N O O CO2Et--0 C1<BR> <BR> <BR> <BR> <BR> C-90 aminophylline N O S CO2n-Pr O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-91 aminophylline N O S C02n-Pr--0 Cl<BR> <BR> <BR> <BR> <BR> <BR> C-92 aminophylline N O O CO2n-Bu O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-93 aminophylline N O O CO2n-Bu O O 1 C (CH3) 3 C-94 aminophylline N O O CO2n-Bu O O 1 Ph C-95 aminophylline N O S CO2n-Bu 0 0 1 4Me(Ph) C-96 aminophylline N O S CO2n-Bu 0 0 1 CF3Ch2 C-97 aminophylline N O O CO2n-Bu--0 Cl C-98 aminophylline N O O CO2n-Bu - - 0 {N (Et) 3} +Cl.

C-99 aminophylline N O O CO2n-Bu--0 {N (Me) 2Ph} +Cl- C-100 aminophylline N O O CO2n-Bu--0 O-C (CH3) 3<BR> <BR> <BR> <BR> <BR> C-101 amprolium N O O CO2-Bn O O 1 methyl C-102 amprolium N O O CO2-Bn O O 1 C(CH3)3 C-103 amprolium N O O CO2-Bn O O 1 Ph C-104amproliumN 0 SCOz-Bn0014Me (Ph) C-105 amprolium N O S CO2-Bn O O 1 CF3CH2<BR> <BR> <BR> <BR> <BR> C-106 atipamezole N O O C02-Bn--0 Cl C-107 atipamezole N O 0 COz-Bn--0 {N (Et) 3} +Cl C-108 atipamezole N O O CO2-BN - - 0 {N (Me) 2PH}+Cl C-109 atipamezole N O O CO2-Bn--0 OC (CH3) 3<BR> <BR> <BR> <BR> <BR> C-110 atipamezole N O O COSMe O O 1 methyl C-111 atipamezole N O S COSMe O O 1 C(CH3)3 C-112 atipamezole N O O COSMe--0 Cl C-113 atipamezole N O O COSMe--0 {N (Et) 3} +Cl C-114 benazepril N O S COSEt O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-115 benazepril N O 0 COSEt--0 Cl<BR> <BR> <BR> <BR> <BR> C-116 benazepril N O O COSn-Bu O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-117 benazepril N O S COSn-Bu--0 Cl<BR> <BR> <BR> <BR> C-118 benazepril N O O COSBn O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-119 benazepril N O O COSBn--0 Cl<BR> <BR> <BR> <BR> <BR> C-120 benazepril N O O CONHMe O O 1 methyl C-121 benazepril N O O CoNHMe O O 1 C(CH3)3 C-122 benazepril N O O CONHEt O O 1 methyl<BR> <BR> <BR> <BR> C-123 cisapride N O O CONHn-Pr O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-124 detomidine N O O CONHn-Bu O O 1 methyl C-125 enalapril O O O CONHn-Bu O O 1 C(CH3)3 C-126 enalapril O O O CONHn-Bu O O 1 Ph C-127 enalapril O O O CONHn-Bu O O 1 4Me(Ph) C-128 enalapril O O O CONHn-Bu O O 1 CF3CH2 C-129 enalapril O O O CONHn-Bu - - O Cl C-130 enalapril O O O CONHn-Bu--0 {N (Et) 3} +Cl C-131 enalapril N O O CONH-Bn O O 1 methyl C-132 enalapril N O O CONH-Bn O O 1 C(CH3)3 C-133 enalapril N O O CONH-Bn--0 {N (Et) 3} +Cl# C-134 enalapril N O O CONNH2 O O 1 methyl C-135 enalapril N O O CONHNHMe O O 1 methyl C-136 enalapril N O O CONHNHEt O O 1 methyl C-137 enalapril N O O CONHNHPr O O 1 methyl C-138 enalapril N O O CONHNHt-Bu O O 1 C(CH3)3 C-139 enalapril N O O CONHNHCO2Me O O 1 C(CH3)3 C-140 enalapril N O O CONHNHCO2Et O O 1 C(CH3)3 C-141 enalapril N O O CONHNHCO2t-Bu O O 1 C(CH3)30 C-142 enalapril N O O CONHNHCO2bN O O 1 C(CH3)3 C-143 enalapril N O O CONHN=CHMe O O 1 methyl C-144 enalapril N O O CONHN=CHMe--0 {N (Et) 3} +Cl- C-145 enalapril N O O CONHN=CHPh O O 1 methyl C-146 enalapril N O O CONHN=CHPh O O 1 C(CH3)3 C-147 enalapril N O O CO2H O O 1 methyl C-148 enalapril N O O CO2H O O 1 C(CH3)3 C-149 enalapril N O O CO2H O O 1 Ph C-150 enalapril N O O CO2H O O 1 4Me(Ph) C-151 enalapril N O O CO2H--0 C1 C-152 enalapril N O O C02H--0 {N (Et) 3} +Cl C-153 enalapril N O O CO2H--0 {N (Me) 2Ph} +Cl- C-154 enalapril N O O CO2Me O O 1 methyl C-155 enalapril N O O CO2Me O O 1 C(CH3)3 <BR> <BR> C-156 enalapril N O O CO2Me O O 1 Ph<BR> <BR> <BR> <BR> <BR> C-157 fluconazole N O O CO2H O O 1 methyl C-158 fluconazole N O O CO2H O O 1 C(CH3)3 C-159 fluconazole N O O CO2Me O O 1 Ph C-160 fluconazole N O O CO2Me O O 1 4ME(Ph) C-161 fluconazole N O O Co2Me - - 0 Cl C-162 fluconazole N O O CO2Me - 0 {N (Et) 3}+Gl# C-163 fluconazole N O O CO2Me - - 0 {N (Me) 2PH}+Cl# C-164 fluconazole N O O CO2Me O O 1 methyl C-165 fluconazole N O O CO2Me O O 1 C(CH3)3 C-166 fluconazole N O O CO2Et O O 1 Ph C-167 fluconazole N O O CO2n-Pr O O 1 4Me(Ph) C-168 fluconazole N O O CO2n-Bu - - 0 Cl C-169 fluconazole N O O CO2-Bn - - 0 {N (Et) 3} +Cl C-172 fluconazole N O O COSMe - - 0 {N (Me) 2Ph} +Cl- C-171 fluconazole N O O COSEt O O 1 methyl C-172 fluconazole N O O COSn-Bu O O 1 C(CH3)3 C-173 fluconazole N O O CONHMe O O 1 Ph C-174 fluconazole N O O CONHEt O O 1 4Me(Ph) C-175 fluconazole N O O CONHn-Bu--0 C1 C-176 fluconazole N O O CONH-Bn - - 0 {N (Et) 3} +Cl C-177 fluconazole N O O CONNH2--0 {N (Me) 2Ph} +Cl <BR> <BR> C-178 fluconazole N O O CONHNHMe O O 1 methyl<BR> <BR> <BR> <BR> C-179 fluconazole N O O CONHNHEt O O 1 C (CH3) 3<BR> <BR> <BR> <BR> <BR> C-180 fluconazole N O O CONHNHPr O O 1 Ph C-181 fluconazole N O O CONHNHt-Bu 0 0 1 4Me(Ph) C-182 fluconazole N O O CONHNHCO2Me - - 0 Cl C-183 fluconazole N O O CONHNHCO2Et - - 0 {N (Et) 3} +Cl- C-184 fluconazole N O O CONHNHCO2t-Bu--0 {N (Me) 2Ph}+CL# C-185 fluconazole N O O CONHNHCO2Bn O O 1 methyl C-186 fluconazole N O 0 CONHN=CHMe 0 O 1 C (CH3) 3 C-187 fluconazole N O O CONHN=CHMe O O 1 4Me(Ph) C-188 fluconazole N O O CONHN=CHPh--0 C1 C-189 fluconazole N O O CONHN=CHPh - - 0 {N (Et) 3}+Cl# C-190 hetacillin N O O CO2Me O O 1 4Me(Ph) C-191 imidacloprid N O O CO2Me--0 C1 C-192 imidacloprid N O O CO2Me - - 0 {N (Et) 3} +Cl# C-193 imidacloprid N O O CO2Me - - 0 {N (Me) 2Ph} +Cl# C-194 imidacloprid N O O CO2Et O O 1 methyl C-195 imidacloprid N O O CO2Et - - 0 Cl <BR> <BR> C-196 imidacloprid N O S CO2n-Pr O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-197 imidacloprid N O S CO2n-Pr--0 C1 C-198imidaclopridN00C02n-Bu001methyl C-199 imidacloprid N O O CO2n-Bu O O 1 C(CH3)3 C-200imidaclopridN 0 0C02n-Bu0 0 1Ph C-201 imidacloprid N O S CO2n-Bu O O 1 4Me(Ph) C-202 imidacloprid N O S CO2n-Bu O O 1 CF3CH2 C-203imidaclopridN00C02n-Bu--0Cl C-204imidaclopridN00C02n-Bu--0 {N (Et) 3} +Cl C-205imidaclopridN00C02n-Bu--0 {N (Me) 2Ph} +Cl- C-206imidaclopridN00C02n-Bu--0OC (CHs) 3 C-207 imidacloprid N O O CO2-Bn O O 1 methyl C-208 imidacloprid N O O CO2-Bn O O 1 C(CH3)3 C-209 imidacloprid N O O CO2-Bn O O 1 Ph C-210 imidacloprid N O S CO2-Bn O O 1 4Me(Ph) C-211 imidacloprid N O S CO2-Bn O O 1 CF3CH2 C-212 imidacloprid N 0 O C02-Bn--0 Cl C-213 imidacloprid N 0 O C02-Bn--0 {N (Et) 3} +Cl C-214 imidacloprid N O O CO2-Bn--0 {N (Me) 2Ph} +Cl- <BR> <BR> C-215 imidacloprid N O O CO2-Bn--0 OC (CH3) 3 C-216 imidacloprid N O O COSMe O O 1 methyl <BR> <BR> C-217 imidacloprid N O S COSMe O O 1 C (CH3) 3<BR> <BR> <BR> <BR> <BR> C-218 imidacloprid N O 0 COSMe--0 Cl C-219 imidacloprid N O O COSMe--0 {N (Et) 3} +Cl- <BR> <BR> C-220 imidacloprid N O S COSEt O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-221 imidacloprid N O O COSEt--0 Cl C-222 imidacloprid N O O COSn-Bu O O 1 methyl C-223 imidacloprid N 0 S COSn-Bu--0 Cl C-224 imidacloprid N O O COSBn O O 1 methyl C-225 imidacloprid N 0 O COSBn--0 Cl C-226 imidacloprid N O O CONHMe O O 1 methyl C-227 imidacloprid N O O CONHMe O O 1 C(CH3)3 C-228 imidacloprid N O O CONHEt O O 1 methyl <BR> <BR> C-229 imidacloprid N O O CONHn-Pr O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-230 imidacloprid N O O CONHn-Bu O O 1 methyl C-231 imidacloprid N O O CONHn-Bu O O 1 C(CH3)3 <BR> <BR> C-232 imidacloprid N O O CONHn-Bu O O 1 Ph<BR> <BR> <BR> <BR> <BR> C-233 imidacloprid N O O CONHn-Bu O O 1 4Me (Ph) C-234 imidacloprid N O O CONHn-Bu O O 1 CF3CH2 C-235 imidacloprid N 0 O CONHn-Bu--0 Cl C-236 imidacloprid N 0 O CONHn-Bu--0 {N (Et) 3} +Cl- C-237 imidacloprid N O O CONH-Bn O O 1 methyl C-238 imidacloprid N O O CONH-Bn O O 1 C(CH3)3 C-239 imidacloprid N O O CONH-Bn--0 {N (Et) 3} +Cl C-240 imidacloprid N O O CONNH2 O O 1 methyl C-241 ketamine N O O CONHNHMe O O 1 methyl C-242 ketamine N O O CONHNHEt O O 1 methyl C-243 ketamine N O O CONHNHPr O O 1 methyl C-244 ketamine N O O CONHNHt-Bu O O 1 C(CH3)3 C-245 ketamine N O O CONHNHCO2Me O O 1 C(CH3)3 <BR> <BR> C-246 ketamine N O O CONHNHC02Et O O 1 C (CH3) 3<BR> <BR> <BR> <BR> <BR> C-247 ketamine N O O CONHNHCO2t-Bu O O 1 C (CH3) 3 C-248 ketamine N O O CONHNHCO2Bn O O 1 C(CH3)3 C-249 ketamine N O O CONHN=CHMe O O 1 methyl C-250 ketamine N O O CONHN=CHMe - - 0 {N(Et)3}+Cl- C-251 ketamine N O O CONHN=CHPh O O 1 methyl C-252 ketamine N O O CONHN=CHPh O O 1 C(CH3)3 C-253 lidocaine N O O CO2H O O 1 methyl C-254 licomycin N O O CO2H O O 1 C(CH3)3 C-255 lomustine N O O CO2H O O 1 Ph C-256 lomustine N O O CO2H O O 1 4Me(Ph) C-257 lomustine N O O CO2H--0 C1 C-258 lomustine N O 0 CO2H--0 {N (Et) 3} +Cl- C-259 lomustine N O O CO2H - - 0 {N (Me) 2Ph} +Cl- C-260 lomustine N O O CO2Me O O 1 methyl C-261 lomustine N O O CO2Me O O 1 C(CH3)3 C-262 lomustine N O O CO2Me O O 1 Ph C-263 lomustine N O O CO2Me O O 1 4Me(Ph) C-264lomustineN 0 0C02Me--0Cl C-265lomustineN 0 0C02Me--0 {N (Et) 3} +Cl- C-266lomustineN00C02Me--0 {N (Me) 2Ph} +Cl- C-267 lomustine N O O CO2Et O O 1 methyl C-268 lomustine N O O C02Et--0 Cl C-269 lomustine N O S CO2n-Pr O O 1 methyl C-270lomustineN 0 SC02n-Pr--0Cl C-271 lomustine N O O CO2n-Bu O O 1 methyl C-272 lomustine N O O CO2n-Bu O O 1 C(CH3)3 C-273 mechlorethamine N O 0 C02n-Bu 0 O 1 Ph C-274 mechlorethamine N O S CO2n-Bu O O 1 4Me(Ph) C-275 mechlorethamine N O S CO2n-Bu O O 1 CF3CH2 C-276 mechlorethamine N O O CO2n-Bu--0 C1 C-277 mechlorethamine N O O CO2n-Bu--0 {N (Et) 3} +Cl- C-278 mechlorethamine N O O CO2n-Bu--0 {N (Me) 2Ph} +Cl- C-279 mechlorethamine N O O CO2n-Bu - - 0 O-C(CH3)3 C-280 meclofenamic acid N O O CO2-Bn O O 1 methyl C-281 mercaptopurine N O O CO2-Bn O O 1 C(CH3)3 C-282 methotrexate N O O CO2-Bn O O 1 Ph C-283 mexiletine N O S CO2-Bn O O 1 4Me(Ph) C-284 mexiletine N O S CO2-Bn O O 1 CF3CH2 C-285 mexiletine N O O CO2-Bn - - 0 Cl C-286mexiletineN00C02-Bn--0 {N (Et) 3} +Cl C-287 mexiletine N 0 O CO2-Bn--0 {N (Me) 2Ph} +Cl- C-288 mexiletine N O O CO2-Bn - - 0 OC(CH3)3 C-289 mexiletine N O O COSMe O O 1 methyl C-290 mexiletine N O S COSMe O O 1 C(CH3)3 C-291 mexiletine N O 0 COSMe--0 Cl C-292 mexiletine N O O COSMe - - 0 {N (Et) 3} +Cl C-293 mexiletine N O S COSEt O O 1 methyl C-294 mexiletine N O O COSEt - - 0 Cl C-295 mexiletine N 0 O COSn-Bu O 0 1 methyl C-296mexiletineN 0 SCOSn-Bu--0Cl C-297 mexiletine N O O COSBn O O 1 methyl <BR> <BR> C-298 mexiletine N 0 O COSBn--0 Cl<BR> <BR> <BR> <BR> C-299 mexiletine N O O CONHMe O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-300 mexiletine N O O CONHMe O O 1 C (CH3) 3<BR> <BR> <BR> <BR> C-301 mexiletine N O O CONHEt O O 1 methyl C-302 mexiletine N O O CONHn-Pr O O 1 methyl<BR> <BR> <BR> <BR> C-303 mexiletine N O O CONHn-Bu O O 1 methyl C-304 mexiletine N O O CONHn-Bu O O 1 C(CH3)3 C-305 mexiletine N O O CONHn-Bu O O 1 Ph C-306 mexiletine N O O CONHn-Bu O O 1 4Me(Ph) <BR> <BR> C-307 mexiletine N O O CONHn-Bu O O 1 CF3CH2<BR> <BR> <BR> <BR> C-308 mexiletine N O O CONHn-Bu--0 Cl C-309 mexiletine N O O CONHn-Bu - - 0 {N (Et) 3}+Cl- C-310 ormetoprim N O O CONH-Bn O O 1 methyl C-311 prostaglandin E1 O O O CONH-Bn O O 1 C(CH3)3 C-312 quinacrine N O O CONH-Bn - - 0 {N (Et) 3}+Cl- C-313 quinacrine N O O CONNH2 O O 1 methyl <BR> <BR> C-314 quinacrine N O O CONHNHMe O O 1 methyl<BR> <BR> <BR> C-315 quinacrine N O O CONHNHEt O O 1 methyl<BR> <BR> <BR> <BR> C-316 quinacrine N O O CONHNHPr O O 1 methyl C-317 quinacrine N O O CONHNHt-Bu O O 1 C(CH3)3 C-318 quinacrine N O O CONHNHCO2Me O O 1 C(CH3)3 C-319 quinacrine N O O CONHNHCO2Et O O 1 C(CH3)3 C-320 quinacrine N O O CONHNHCO2t-Bu O O 1 C(CH3)3 C-321 quinacrine N O O CONHNHCO2Bn O O 1 C(CH3)3 C-322 quinacrine N O O CONHN=CHMe O O 1 methyl C-323 quinacrine N O O CONHN=CHMe - - 0 {N (Et) 3} +Cl- <BR> <BR> C-324 quinacrine N O O CONHN=CHPh O O 1 methyl<BR> <BR> <BR> <BR> C-325 quinacrine N O O CONHN=CHPh O O 1 C (CH3) 3<BR> <BR> <BR> <BR> C-326 quinidine N O O CO2H O O 1 methyl C-327 quinidine N O O CO2H O O 1 C(CH3)3 <BR> <BR> C-328 quinidine N O O CO2H O O 1 Ph<BR> <BR> <BR> C-329 quinidine N O O CO2H O O 1 4Me (Ph)<BR> <BR> <BR> <BR> C-330 quinidine N O O COzH--0 Cl C-331 quinidine N O O CO2H--0 {N (Et) 3} +Cl- C-332 quinidine N O O C02H 0 O 0 {N (Me) 2Ph} +Cl- C-333 quinidine N O O CO2Me - - 1 methyl C-334 quinidine N O O CO2Me O O 1 C(CH3)3 C-335 quinidine N O O CO2Me O O 1 Ph <BR> <BR> C-336 quinidine N O O CO2Me O O 1 4Me (Ph)<BR> <BR> <BR> <BR> C-337 quinidine N O O CO2Me--0 Cl C-338 quinidine N O O CO2Me--0 {N (Et) 3} +Cl- C-339 quinidine N O O CO2Me--0 {N (Me) 2Ph}+Cl- <BR> <BR> C-340 quinidine N O O CO2Et O O 1 methyl<BR> <BR> <BR> <BR> C-341 quinidine N'O O CO2Et O O 0 Cl C-342 quinidine N O S CO2n-Pr O O 1 methyl C-343 quinidine N O S CO2n-Pr--0 C1 C-344 quinidine N O O CO2n-Bu O O 1 methyl C-345 sulfachlor- N O O CO2n-Bu O O 1 C(CH3)3 pyridazine C-346 sulfadiazine N O O CO2n-Bu O O 1 Ph C-347 sulfamethoxazole N O S CO2n-Bu O O 1 4Me(Ph) C-348 theophylline N O S CO2n-Bu O O 1 CF3CH2 C-349 theophylline N O O CO2n-Bu--0 C1 C-350 theophylline N O O CO2n-Bu--0 {N (Et) 3} +Cl- C-351 theophylline N O O CO2n-Bu--0 {N (Me) 2Ph}+Cl- <BR> <BR> C-352 theophylline N O O CO2n-Bu--0 OC (CH3) 3 C-353 theophylline N O O CO2-Bn O O 1 methyl C-354 theophylline N O O CO2-Bn O O 1 C(CH3)3 C-355 theophylline N O O CO2-Bn O O 1 Ph C-356 theophylline N O S CO2-Bn O O 1 4Me(Ph) C-357 theophylline N O S CO2-Bn O O 1 CF3CH2 C-358 theophylline N O O COz-Bn--0 Cl C-359 theophylline N O O CO2-Bn--0 {N (Et) 3} +Cl C-360 theophylline N O O CO2-Bn - - 0 {N (Me) 2Ph}+Cl- <BR> <BR> C-361 theophylline N O O CO2-Bn O O 0 OC (CH3) 3<BR> <BR> <BR> <BR> <BR> C-362 theophylline N O O COSMe O O 1 methyl C-363 theophylline N O S COSMe O O 1 C(CH303 C-364 theophylline N O O COSMe--0 Cl C-365 theophylline N O O COSMe--0 {N (Et) 3} +Cl- C-366 theophylline N O S COSEt O O 1 methyl <BR> <BR> C-367 theophylline N O O COSEt--0 Cl<BR> <BR> <BR> <BR> <BR> C-368 theophylline N O O COSn-Bu O O 1 methyl C-369 theophylline N O S COSn-Bu--0 Cl <BR> <BR> C-370 theophylline N O O COSBn O O 1 methyl<BR> <BR> <BR> <BR> C-371 theophylline N O O COSBn--0 Cl<BR> <BR> <BR> <BR> <BR> C-372 theophylline N O O CONHMe O O 1 methyl C-373 theophylline N O O CONHMe O O 1 C(CH3)3 <BR> <BR> C-374 theophylline N O O CONHEt O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-375 theophylline N O O CONHn-Pr O O 1 methyl<BR> <BR> <BR> <BR> C-376 theophylline N O O CONHn-Bu O O 1 methyl C-377 tiletamine N O O CONHn-Bu O O 1 C(CH3)3 <BR> <BR> C-378 tiletamine N O O CONHn-Bu O O 1 Ph<BR> <BR> <BR> <BR> <BR> C-379 tiletamine N O O CONHn-Bu O O 1 4Me (Ph) C-380 tiletamine N O O CONHn-Bu O O 1 CF3CH2 C-381 tiletamine N O O CONHn-Bu--0 Cl C-382 tiletamine N O O CONHn-Bu--0 {N (Et) 3} +Cl <BR> <BR> C-383 tiletamine N O O CONH-Bn O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-384 tiletamine N O O CONH-Bn O O 1 C (CH3) 3 C-385 tiletamine N O O CONH-Bn - - 0 {N (Et) 3} +Cl C-386 tiletamine N O O CONNH2 O O 1 methyl <BR> <BR> C-387 tiletamine N O O CONHNHMe O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-388 tiletamine N O O CONHNHEt O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-389 tiletamine N O O CONHNHPr O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-390 tiletamine N O O CONHNHt-Bu O O 1 C (CH3) 3 C-391 tiletamine N O O CONHNHCO2Me O O 1 C(CH3)3 C-392 tiletamine N O O CONHNHCO2Et O O 1 C(CH3)3 C-393 tiletamine N O O CONHNHCO2t-Bu O O 1 C(CH3)3 <BR> <BR> C-394 tiletamine N O O CONHNHCO2Bn O O 1 C (CH3) 3<BR> <BR> <BR> <BR> <BR> C-395 tiletamine N O O CONHN=CHMe O O 1 methyl C-396 tiletamine N O O CONHN=CHMe - - 0 {N (Et) 3} +Cl- <BR> <BR> C-397 tiletamine N O O CONHN=CHPh O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-398 tiletamine N O O CONHN=CHPh O O 1 C (CH3) 3<BR> <BR> <BR> <BR> <BR> C-399 tocainide N O O C02H O O 1 methyl C-400 tocainide N O O CO2H O O 1 C(CH3)3 C-401 tocainide N O O CO2H O O 1 Ph <BR> <BR> C-402tocainideN00COzH0014MeTh)<BR> <BR> <BR> <BR> <BR> C-403 tocainide N O O CO2H--0 C1 C-404 tocainide N O O CO2H--0 {N (Et) 3} +Cl C-405 tocainide N O O C02H--0 {N (Me) 2Ph} +Cl- C-406tocainideN 0 0C02Me001methyl C-407 tocainide N O O CO2Me O O 1 C(CH3)3 C-408 tocainide N O O CO2Me O O 1 Ph C-409 tocainide N O O CO2Me O O 1 4Me(Ph) C-410tocainideN 0 0C02Me--0C1 C-411 tocainide N O O CO2Me--0 {N (Et) 3}+Cl- C-412tocainideN00C02Me--0 {N (Me) 2Ph} +Cl- C-413 tocainide N O O CO2Et O O 1 methyl <BR> <BR> C-414 tocainide N O O CO2Et--0 C1<BR> <BR> <BR> <BR> <BR> C-415 tocainide N O S CO2n-Pr O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-416 tocainide N O S CO2n-Pr--0 C1<BR> <BR> <BR> <BR> <BR> C-417 tocainide N O O CO2n-Bu O O 1 methyl C-418 tocainide N O O CO2n-Bu O O 1 C(CH3)3 C-419 tocainide N O O CO2n-Bu O O 1 Ph C-420 tocainide N O S CO2n-Bu O O 1 4Me(Ph) C-421 tocainide N O S CO2n-Bu O O 1 CF3CH2 C-422tocainideN 0 0C02n-Bu--0C1 C-423tocainideN00C02n-Bu--0 {N (Et) 3} +Cl- C-424 tocainide N O O CO2n-Bu--0 {N (Me) 2Ph}+Cl- C-425 tocainide N O O CO2n-Bu - - 0 OC(CH3)3 C-426 vincristine N O O CO2-Bn O O 1 methyl C-427 xylazine N O O CO2-Bn O O 1 C(CH3)3 C-428 xylazine N O O CO2-Bn O O 1 Ph C-429 xylazine N O S CO2-Bn O O 1 4ME(Ph) C-430 xylazine N O S CO2-Bn O O 1 CF3CH2 C-431 xylazine N O O CO2-Bn - - 0 Cl C-432 xylazine N O O CO2-Bn--0 {N (Et) 3}+Cl- C-433 xylazine N O O CO2-Bn--0 {N (Me) 2Ph}+Cl- C-434 xylazine N O O CO2-Bn - - 0 OC(CH3)3 C-435 xylazine N O O COSMe O O 1 methyl C-436 xylazine N O S COSMe O O 1 C(CH3)3 C-437 xylazine N O O COSMe--0 C1 C-438 xylazine N O O COSMe - - 0 {N (Et) 3} +Cl- C-439 xylazine N O S COSEt O O 1 methyl C-440xylazineN 0 0COSEt--0C1 C-441 xylazine N O O COSn-Bu O O 1 methyl C-442 xylazine N O S COSn-Bu--0 C1 C-443 xylazine N O O COSBn O O 1 methyl C-444 xylazine N O O COSBn--0 C1<BR> <BR> <BR> <BR> <BR> <BR> C-445 xylazine N O O CONHMe O O 1 methyl C-446 xylazine N O O CONHMe O O 1 C(CH3)3 C-447 xylazine N O O CONHEt O O 1 methyl C-448 xylazine N O O CONHn-Pr O O 1 methyl<BR> <BR> <BR> <BR> <BR> C-449 xylazine N O O CONHn-Bu O O 1 methyl C-450 xylazine N O O CONHn-Bu O O 1 C(CH3)3 C-451 xylazine N O O CONHn-Bu O O 1 Ph C-452 xylazine N O O CONHn-Bu O O 1 4Me(Ph) C-453 xylazine N O O CONHn-Bu O O 1 CF3CH2<BR> <BR> <BR> <BR> <BR> C-454 xylazine N O O CONHn-Bu--0 C1 C-455 xylazine N 0 O CONHn-Bu--0 {N (Et) 3} +Cl- C-456 xylazine N O O CONH-Bn O O 1 methyl

C-457 xylazine N O O CONH-Bn O O 1 C (CH3) 3 C-458 xylazine N O O CONH-Bn--0 {N (Et) 3}+Cl- C-459 xylazine N O 0 CONNH2 O O 1 methyl C-460 xylazine N O O CONHNHMe O O 1 methyl C-461 xylazine N O O CONHNHEt O O 1 methyl C-462 xylazine N O 0 CONHNHPr O O 1 methyl C-463 xylazine N O 0 CONHNHt-Bu O O 1 C (CH3) 3 C-464 xylazine N O O CONHNHCO2Me O O 1 C (CH3) 3 C-465 xylazine N00 CONHNHC02Et 0 0 1 C (CH3) 3 C-466 xylazine N00 CONHNHC02t-Bu 0 0 1 C (CH3) 3 C-467 xylazine N O 0 CONHNHCO2Bn O O 1 C (CH3) 3 C-468 xylazine N O O CONHN=CHMe O O 1 methyl C-469 xylazine N 0 O CONHN=CHMe--0 {N (Et) 3} +Cl- C-470 xylazine N O O CONHN=CHPh O O 1 methyl C-471 xylazine N O 0 CONHN=CHPh O O 1 C (CH3) 3 Table D describes additional examples of compounds of Formula I which can be made using the procedures described hereinbefore, where R2 is hydrogen, m = 0, q = 1, t = 0 or 1 and the pharmaceutical (a veterinary drug) which defines the pharmaceutical moiety of these examples is Z2 (X2)-[(C=G20)-G21]-H, Z2(X2) q-H or Z2 (X2).). The following groups, Z1, G'°, G", R1, G20, G21, t, X2 and Z2(X2)-[(C=G20)- G21]-H, Z2 (X2) q-H or Z2 (X2) are defined within Table D.

Table D Cmpd# Zi G10 G11 R1 G20 G21 t x2 Z2 (X2) q-[(C=G20)- G2'] t-H or when t = 0, Z2 (X2) q or Z2(X2)q-H D-1 methyl O 0 CO2H - - 0 N albendazole D-2 methyl O O C02H--0 O clioquinol D-3 n-propyl O O CO2H - - 0 N febantel D-4 n-propyl O O CO2H--0 N fenbendazole D-5 C (CH3) 3 O O CO2H - - 0 O guaifenesin D-6 C (CH3) 3 O O CO2H-0 O mibolerone D-7 Ph O O CO2H - - 0 N omeprazole D-8 Ph O O CO2Me - - 0 O oxazepam D-9 4Cl (Ph) O O C02Me--0 N piroxicam D-10 4Cl (Ph) O O C02Me--0 N primidone D-11 methyl O O C02Me--0 N procainamide D-12 methyl O O C02Me--0 N thiabendazole D-13 n-propyl O O C02Me--0 0 warfarin D-14 n-propyl O O CO2Me - - 0 N albendazole D-15 Ph O O CO2Et - - 0 O clioquinol <BR> <BR> D-16 Ph O O CO2Et--0 N febantel D-17 methyl O S CO2n-Pr - - 0 N fenbendazole D-18 n-propyl O S CO2n-Pr - - 0 O guaifenesin D-19 C(CH3)3 O O CO2n-Bu - - 0 O mibolerone <BR> <BR> D-20 Ph O O CO2n-Bu--0 N omeprazole D-21 PhO O O CO2n-Bu - - 0 O oxazepam D-22 PhNH O S CO2n-Bu - - 0 N prioxicam D-23 4Cl (Ph) O S CO2n-Bu 0 N primidone D-24 4Cl (Ph) O O O CO2n-Bu - - 0 N procainamide D-25 4Cl (Ph) NH O O COzn-Bu--0 N thiabendazole <BR> <BR> D-26 pyrid-2-yl O O C02n-Bu--0 O warfarin<BR> <BR> <BR> <BR> <BR> D-27 pyrid-4-yl 0 O COzn-Bu--0 N albendazole<BR> <BR> <BR> <BR> <BR> D-28 methyl O O C02-Bn--0 O clioquinol D-29 n-propyl O O CO2-Bn - - 0 N febantel D-30 C(CH3)3 O O CO2-Bn - - 0 N fenbendazole D-31 Ph O S CO2-Bn - - 0 O guaifenesin D-32 PhO O S CO2-Bn - - 0 O mibolerone D-33 PhNH O O CO2-Bn - - 0 N omeprazole D-34 4Cl (Ph) O O CO2-Bn - - 0 O oxazepam D-35 4Cl (Ph) O O O CO2-Bn - - 0 N prioxicam D-36 4Cl (Ph) NH O O CO2-Bn - - 0 N primidone <BR> <BR> D-37 pyrid-2-yl O O COSMe--0 N procainamide<BR> <BR> <BR> <BR> <BR> D-38 pyrid-4-yl 0 S COSMe--0 N thiabendazole<BR> <BR> <BR> <BR> <BR> D-39 methyl O O COSMe--0 O warfarin<BR> <BR> <BR> <BR> <BR> D-40 n-propyl O O COSMe--0 N albendazole D-41 C(CH3)3 O S COSEt - - 0 O clioquinol <BR> <BR> D-42 Ph O O COSEt--0 N febantel D-43 PhO O O COSn-Bu - - 0 N fenbendazole <BR> <BR> <BR> D-44 Ph-NH 0 S COSn-Bu--0 O guaifenesin D-45 4Cl (Ph) O O COSBn--0 O mibolerone D-46 4Cl (Ph) O O O COSBn - - 0 N omeprazole D-47 4Cl (Ph) NH 0 O CONHMe--0 O oxazepam D-48 pyrid-2-yl O O CONHMe - - 0 N piroxicam D-49 pyrid-4-yl O O CONHEt - - 0 N primidone <BR> <BR> D-50 methyl 0 O CONHn-Pr--0 N procainamide<BR> <BR> <BR> <BR> <BR> D-51 n-propyl O O CONHn-Bu--0 N thiabendazole<BR> <BR> <BR> <BR> D-52 C (CHs) 3 O O CONHn-Bu--0 O warfarin D-53 Ph O O CONHn-Bu - - 0 N albendazole D-54 PhO O O CONHn-Bu - - 0 O clioquinol D-55 Ph-NH O O CONHn-Bu - - 0 N febantel D-56 4Cl (Ph) 0 O CONHn-Bu--0 N fenbendazole D-57 4Cl (Ph) O O O CONHn-Bu--0 O guaifenesin D-58 4Cl (Ph) NH O O CONH-Bn - - 0 O mibolerone <BR> <BR> D-59 pyrid-2-yl 0 O CONH-Bn--0 N omeprazole<BR> <BR> <BR> <BR> <BR> D-60 pyrid-4-yl O O CONH-Bn--0 O oxazepam<BR> <BR> <BR> <BR> <BR> D-61 methyl O O CONNH2--0 N piroxicam<BR> <BR> <BR> <BR> <BR> D-62 n-propyl O O CONHNHMe--0 N primidone D-63 C(CH3)3 O O CONHNHEt - - 0 N procainamide <BR> <BR> D-64 Ph 0 O CONHNHPr--0 N thiabendazole D-65 PhO O O CONHNHt-Bu - - 0 O warfarin D-66Ph-NH00CONHNHC02Me-0Nalbendazole D-67 4Cl (Ph) O O CONHNHCO2Et - - 0 O clioquinol D-68 4Cl (Ph) O O O CONHNHCO2t-Bu - - 0 N febantel D-69 4Cl (Ph) NH O O CONHNHCO2Bn - - 0 N fenbendazole <BR> <BR> D-70 pyrid-2-yl O O CONHN=CHMe--0 O guaifenesin<BR> <BR> <BR> <BR> <BR> D-71 pyrid-4-yl O O CONHN=CHMe--0 O mibolerone D-72 methyl O O CONHN=CHPh - - 0 N omeprazole <BR> <BR> D-73 n-propyl O O CONHN=CHPh--0 O oxazepam D-74 methyl O O CO2H O O 1 C captopril D-75 ethyl O O CO2H O O 1 C captopril <BR> <BR> D-76n-propyi00C02H001Ccaptopril D-77 C(CH3)3 O O CO2H O O 1 C captopril D-78 MeO O O CO2H O O 1 C captopril <BR> <BR> D-79EtO00C02H001Ccaptopril D-80n-PrO00C02H001Ccaptopril D-81 MeNH O O CO2Me O O 1 C captopril <BR> <BR> D-82 EtNH 0 O CO2Me O 0 1 C captopril<BR> <BR> <BR> <BR> <BR> D-83 n-PrNH 0 O CO2Me O 0 1 C captopril<BR> <BR> <BR> <BR> D-84n-PrO00C02Me001Ccaptopril<BR> <BR> <BR> <BR> D-85PhO00C02Me001Ccaptopril D-86 Ph-NH O O CO2Me O O 1 C captopril D-87 4Cl (Ph) O O CO2Me O O 1 C captopril D-88 4Cl (Ph) O O O CO2Et O O 1 C captopril D-89 4Cl (Ph) NH O O CO2Et O O 1 C captopril D-90 MeO O S CO2n-Pr O O 1 C captopril <BR> <BR> D-91EtO0SC02n-Pr001Ccaptopril<BR> <BR> <BR> <BR> D-92n-PrO00C02n-Bu001Ccaptopril D-93 MeNH O O CO2n-Bu O O 1 C captopril <BR> <BR> D-94EtNH0QC02n-Bu001Ccaptopril<BR> <BR> <BR> <BR> D-95 n-PrNH 0 S C02n-Bu O 0 1 C captopril D-96 n-PrO O S CO2n-Bu O O 1 C captopril <BR> <BR> D-97PhO00C02n-Bu001Ccaptopril D-98 Ph-NH O O CO2n-Bu O O 1 C captopril D-99 4Cl (Ph) 0 O C02n-Bu O 0 1 C captopril D-100 4Cl (Ph) O O O CO2n-Bu O O 1 C captopril D-101 MeO O O CO2-Bn O O 1 C cephapirin D-102 EtO O O CO2-Bn O O 1 C cephapirin D-103 n-PrO O O CO2-Bn O O 1 C cephapirin D-104 MeNH O S C02-Bn O 0 1 C cephapirin D-105 EtNH O S CO2-Bn O O 1 C cephapirin D-106 n-PrNH O O CO2-Bn O O 1 C cephapirin D-108PhO00C02-Bn001Ccephapirin D-109 Ph-NH O O CO2-Bn O O 1 C cephairin D-110 4Cl (Ph) O O COSMe O O 1 C cephapirin D-111 4Cl (Ph) O O S COSMe O O 1 C cephapirin D-112 4Cl (Ph) NH O O COSme O O 1 C cephapirin D-113 MeO O O COSMe O O 1 C cephapirin D-114 EtO O S COSEt O O 1 C cephapirin <BR> <BR> D-115n-PrO00COSEt001Ccephapirin D-116 MeNH O O COSn-Bu O O 1 C cephapirin D-117 EtNH O S COSn-Bu O O 1 C cephapirin <BR> <BR> D-118 n-PrNH O O COSBn O O 1 C cephapirin D-119 n-PrO O O COSBn O O 1 C cephapirin D-120 PhO O O CONHMe O O 1 C cephapirin <BR> <BR> D-121 PhNH O O CONHMe O O 1 C cephapirin D-122 4Cl (Ph) O O CONHEt O O 1 C cephapirin D-123 4Cl (Ph) O O O CONHn-Pr O O 1 C cephapirin D-124 4Cl (Ph) NH O O CONHn-Bu O O 1 C cephapirin D-125 MeO O O CONHn-Bu O O 1 C cephapirin D-126 EtO O O CONHn-Bu O O 1 C cephapirin D-127 n-PrO O O CONHn-Bu O O 1 C cephapirin <BR> <BR> D-128 MeNH O O CONHn-Bu O O 1 C cephapirin<BR> <BR> <BR> <BR> <BR> D-129 EtNH O O CONHn-Bu O O 1 C cephapirin<BR> <BR> <BR> <BR> <BR> D-130 n-PrNH O O CONHn-Bu O 0 1 C cephapirin D-131 n-PrO O O CONH-Bn O O 1 C cephapirin D-132 PhO O O CONH-Bn O O 1 C cephapirin <BR> <BR> D-133 Ph-NH O O CONH-Bn O O 1 C cephapirin D-134 4Cl (Ph) O O CONNH2 O O 1 C cephapirin D-135 4Cl (Ph) O O O CONHNHMe O O 1 C cephapirin D-136 4Cl (Ph) NH O O CONHNHEt 0 O 1 C cephapirin D-137 MeO O O CONHNHPr O O 1 C cephapirin D-138 EtO O O CONHNHt-Bu O O 1 C cephapirin D-139 n-PrO O O CONHNHCO2Me O O 1 C cephapirin <BR> <BR> D-140 MeNH O O CONHNHCOzEt 0 O 1 C cephapirin<BR> <BR> <BR> <BR> <BR> D-141 EtNH O O CONHNHCO2t-Bu O O 1 C cephapirin<BR> <BR> <BR> <BR> D-142 n-PrNH O 0 CONHNHCOzBn 0 O 1 C cephapirin<BR> <BR> <BR> <BR> <BR> D-143n-PrO00CONHN=CHMe001Ccephapirin D-144 PhO O O CONHN=CHMe O O 1 C cephapirin <BR> <BR> D-145 Ph-NH O O CONHN=CHPh O O 1 C cephapirin D-146 4Cl (Ph) NH O O CONHN=CHPh O 0 1 C cephapirin <BR> <BR> D-147 methyl O O C02H--0 N cephapirin D-148 ethyl O O CO2H - - 0 N cephapirin <BR> <BR> D-149 n-propyl O O CO2H--0 N cephapirin<BR> <BR> <BR> <BR> <BR> D-150 C (CH3) 3 O 0 CO2H--0 N cephapirin D-151 MeO O O CO2H - - 0 N cephapirin D-152 EtO O O CO2H - - 0 N cephapirin D-153 n-PrO O O CO2H - - 0 N cephapirin D-154 MeNH O O CO2Me - - 0 N cephapirin D-155 EtNH O O CO2Me - - 0 N cephapirin D-156 n-PrNH O O CO2Me - - 0 N cephapirin D-157 n-PrO O O CO2Me - - 0 N cephapirin D-158 PhO O O CO2Me - - 0 N cephapirin <BR> <BR> D-159 PhNH O O C02Me--0 N cephapirin D-160 4Cl (Ph) O O CO2Me - - 0 N cephapirin D-161 4Cl (Ph) O O O CO2Et - - 0 N cephapirin D-162 4Cl (Ph) NH O O CO2Et - - 0 N cephapirin <BR> <BR> D-1G3 Ph-NH O S CO2n-Pr--0 N cephapirin D-164 4Cl (Ph) O S CO2n-Pr 0 N cephapirin D-165 4Cl (Ph) O O O CO2n-Bu - - 0 N cephapirin D-166 4Cl (Ph) NH O O CO2n-Bu - - 0 N cephapirin <BR> <BR> D-167 pyrid-2-yl O O CO2n-Bu--0 N cephapirin D-168 pyrid-4-yl O S CO2n-Bu - - 0 N cephapirin D-169 MeO O S CO2n-Bu - - 0 N cephapirin D-170 EtO O O CO2n-Bu - - 0 N cephapirin D-171 n-PrO O O CO2n-Bu - 0 N cephapirin D-172 PhO O O CO2n-Bu - - 0 N cephapirin D-173 MeO O O CO2n-Bu O O 1 C ketoprofen D-174 EtO O O CO2n-Bn O O 1 C ketoprofen D-175 n-PrO O O CO2-Bn O O 1 C ketoprofen D-176 (CH3) 3CO O O CO2-Bn O O 1 C ketoprofen D-177 MeNH O S CO2-Bn O O 1 C ketoprofen D-178 EtNH O S CO2-Bn O O 1 C ketoprofen <BR> <BR> D-179 n-PrNH O O CO2-Bn O O 1 C ketoprofen D-180 (CH3) 3CNH O O CO2-Bn O O 1 C ketoprofen D-181 PhO O O CO2-Bn O O 1 C ketoprofen <BR> <BR> D-182 PhNH O O CO2-Bn O O 1 C ketoprofen D-183 4Cl (Ph) O O COSMe O O 1 C ketoprofen D-184 4Cl (Ph) O O S COSMe O O 1 C ketoprofen D-185 4Cl (Ph) NH O O COSMe O O 1 C ketoprofen D-186 MeO O O COSMe O O 1 C ketoprofen <BR> <BR> D-187EtO0SCOSEt001Cketoprofen D-188 n-PrO O O COSEt O O 1 C ketoprofen D-189 (CH3) 3CO O O COSn-Bu O O 1 C ketoprofen <BR> <BR> D-190 MeNH O S COSn-Bu O O 1 C ketoprofen<BR> <BR> <BR> <BR> <BR> D-191 EtNH O O COSBn O O 1 C ketoprofen<BR> <BR> <BR> <BR> <BR> D-192 n-PrNH O O COSBn O O 1 C ketoprofen D-193 (CH3) 3CNH O O CONHMe O O 1 C ketoprofen D-194 PhO O O CONHMe O O 1 C ketoprofen <BR> <BR> D-195 Ph-NH O O CONHEt 0 O 1 C ketoprofen D-196 4Cl (Ph) O O CONHn-Pr O O 1 C ketoprofen D-197 4Cl (Ph) O O O CONHn-Bu O O 1 C ketoprofen D-198 4Cl (Ph) NH O O CONHn-Bu O O 1 C ketoprofen D-199 MeO O O CONHn-Bu O O 1 C ketoprofen D-200 EtO O O CONHn-Bu O O 1 C ketoprofen D-201 n-PrO O O CONHn-Bu O O 1 C ketoprofen D-202 (CH3) 3CO O O CONHn-Bu O O 1 C ketoprofen <BR> <BR> D-203 MeNH O 0 CONHn-Bu 0 O 1 C ketoprofen<BR> <BR> <BR> <BR> <BR> D-204 EtNH O O CONH-Bn O O 1 C ketoprofen<BR> <BR> <BR> <BR> <BR> D-205 n-PrNH O O CONH-Bn O O 1 C ketoprofen D-206 (CH3) 3CNH O O CONH-Bn O O 1 C ketoprofen <BR> <BR> D-207PhO00CONNH2001Cketoprofen D-208 Ph-NH O O CONHNHMe O O 1 C ketoprofen D-209 4Cl (Ph) O O CONHNHEt O O 1 C ketoprofen D-210 4Cl (Ph) O O O CONHNHPr O O 1 C ketoprofen D-211 4CH30 (Ph) O O O CONHNHt-Bu O O 1 C ketoprofen D-212 4NO2 (Ph) O O O CONHNHCO2Me O O 1 C ketoprofen D-213 4Cl (Ph) NH O O CONHNHC02Et O O 1 C ketoprofen D-214 4MeO (Ph) NH O O CONHNHCO2t-Bu O O 1 C ketoprofen <BR> <BR> D-215MeO00CONHNHC02Bn001Cketoprofen D-216 EtO O O CONHN=CHMe O O 1 C ketoprofen <BR> <BR> D-217n-PrO00CONHN=CHMe001Cketoprofen D-218 (CH3) 3CO O O CONHN=CHPh O O 1 C ketoprofen <BR> <BR> D-219 MeNH O O CONHN=CHPh O O 1 C ketoprofen D-220 EtNH O O CO2H O O 1 C ketoprofen <BR> <BR> D-221 n-PrNH O O CO2H O O 1 C ketoprofen D-222 (CH3) 3CNH O O CO2H O O 1 C ketoprofen D-223 PhO O O CO2H O O 1 C ketoprofen D-224 PhNH O O CO2H O O 1 C ketoprofen D-225 4Cl (Ph) O O CO2H O O 1 C ketoprofen D-226 4Cl (Ph) O O O CO2H O O 1 C ketoprofen D-227 4CH3O (Ph) O O O CO2Me O O 1 C ketoprofen D-2284N02 (Ph) O O O CO2Me O O 1 C ketoprofen D-229 4Cl (Ph) NH O O CO2Me O O 1 C ketoprofen D-230 4MeO (Ph) NH O O CO2Me O O 1 C ketoprofen D-231 PhNH O O CO2Me O O 1 C ketoprofen D-234 4Cl (Ph) NH O O CO2Et O O 1 C ketoprofen D-235 4MeO (Ph) NH O O CO2Et O O 1 C ketoprofen D-236 PhO O S CO2n-Pr O O 1 C ketoprofen D-237 PhNH O S CO2n-Pr O O 1 C ketoprofen D-238 methyl O O CO2n-Bu O O 1 C ketoprofen<BR> <BR> <BR> <BR> <BR> <BR> D-239 ethyl O O CO2n-Bu O O 1 C ketoprofen D-240 n-propyl O O CO2n-Bu O O 1 C ketoprofen D-241 C(CH3)3 O S CO2n-Bu O O 1 C ketoprofen D-242 MeO O S CO2n-Bu O O 1 C ketoprofen D-243EtO00C02n-Bu001Cketoprofen D-244 n-PrO O O CO2n-Bu O O 1 C ketoprofen D-245 MeNH O O CO2n-Bu O O 1 C ketoprofen D-246 EtNH O O CO2n-Bu O O 1 C ketoprofen D-247 n-PrNH O O CO2-Bn O O 1 C valproic acid D-248 n-PrO O O CO2-Bn O O 1 C valproic acid D-249 PhO O O CO2-Bn O O 1 C valproic acid D-250 Ph-NH O S CO2-Bn O O 1 C valproic acid D-251 4Cl (Ph) O S CO2-Bn O O 1 C valproic acid D-252 4Cl (Ph) O O O CO2-Bn O O 1 C valproic acid D-253 4CH30 (Ph) O O O CO2-Bn O O 1 C valproic acid D-254 4NO2 (Ph) O O O CO2-Bn O O 1 C valproic acid D-255 4Cl (Ph) NH O O CO2-Bn O O 1 C valproic acid D-256 4F (Ph) NH O O COSMe O O 1 C valproic acid D-257 4MeO (Ph) NH O S COSMe O 0 1 C valproic acid D-258 pyrid-2-yl O O COSMe O O 1 C valproic acid<BR> <BR> <BR> <BR> <BR> D-259 pyrid-4-yl O O COSMe O O 1 C valproic acid D-260MeO0SCOSEt001Cvalproicacid D-261 EtO O O COSEt O O 1 C valproic acid D-262 n-PrO O O COSn-Bu O O 1 C valproic acid D-263 PhO O S COSn-BU O O 1 C valproic acid D-264 MeNH O O COSBn O O 1 C valproic acid<BR> <BR> <BR> <BR> <BR> D-265 PhNH O O COSBn O O 1 C valproic acid D-266 MeO O O CONHMe O O 1 C valproic acid D-267 EtO O O CONHMe O O 1 C valproic acid D-268 n-PrO O O CONHEt O O 1 C valproic acid D-269 (CH3) 3CO O O CONHn-Pr O O 1 C valproic acid D-270 MeNH O O CONHn-Bu O O 1 C valproic acid D-271 EtNH O O CONHn-Bu O O 1 C valproic acid D-272 n-PrNH O O CONHn-Bu O O 1 C valproic acid D-273 (CH3) 3CNH O O CONHn-Bu O O 1 C valproic acid D-274 PhO O O CONHn-Bu O O 1 C valproic acid D-275 PhNH O O CONHn-Bu O O 1 C valproic acid D-276 4Cl (Ph) O O CONHn-Bu O O 1 C valproic acid D-277 4Cl (Ph) O O O CONH-Bu O O 1 C valproic acid D-278 4Cl (Ph) NH00CONH-Bn001 Cvalproicacid D-279 MeO O O CONH-Bn O O 1 C valproic acid D-280 EtO O O CONNH2 O O 1 C valproic acid <BR> <BR> D-281n-PrO00CONHNHMe001 Cvalproicacid D-282 (CH3) 3CO00CONHNHEt001 Cvalproicacid D-283 MeNH O O CONHNHPr O O 1 C valproic acid D-284 EtNH O O CONHNHt-Bu O O 1 C valproic acid D-285 n-PrNH O O CONHNHCO2Me O O 1 C valproic acid D-286 (CH3) 3CNH O O CONHNHCO2Et O O 1 C valproic acid D-287 PhO O O CONHNHCO2t-Bu O O 1 C valproic acid <BR> <BR> D-288 PhNH O O CONHNHCO2Bn O O 1 C valproic acid D-289 4Cl (Ph) O O CONHN=CHMe O O 1 C valproic acid D-290 4Cl (Ph) O O O CONHN=CHMe O O 1 C valproic acid D-291 4Cl (Ph) NH O O CONHN-CHPh O O 1 C valproic acid D-292 MeO O O CONHN=CHPh O O 1 C valproic acid D-293 EtO O O CO2H O O 1 C valproic acid D-294 n-PrO O O CO2H O O 1 C valproic acid D-295 (CH3) 3CO00C02H001 Cvalproicacid D-296MeNH00C02H001 Cvalproicacid D-297 EtNH O O CO2H O O 1 C valproic acid D-298 n-PrNH O O CO2H O O 1 C valproic acid D-299 (CH3) 3CNH00COzH001 Cvalproicacid D-300PhO00C02Me001 Cvalproicacid<BR> <BR> <BR> <BR> D-301PhNH00C02Me001 Cvalproicacid D-302 4Cl (Ph) 00C02Me001 Cvalproicacid D-303 4Cl (Ph) O O O CO2Me O O 1 C valproic acid D-304 4CH3O (Ph) O O O CO2Me O O 1 C valproic acid D-305 4NO2 (Ph) O O O CO2Me O O 1 C valproic acid D-306 4Cl (Ph) NH00C02Me001 Cvalproicacid D-307 4F (Ph) NH00C02Et001 Cvalproicacid D-308 4Me0 (Ph) NH O O CO2Et O O 1 C valproic acid D-309 MeO O S CO2n-Pr O O 1 C valproic acid D-310 EtO O S CO2n-Pr O O 1 C valproic acid D-311 n-PrO O O CO2n-Bu O O 1 C valproic acid D-312 (CH3) 3CO O O CO2n-Bu O O 1 C valproic acid D-313 MeNH O O CO2n-Bu O O 1 C valproic acid D-314 EtNH O S CO2n-Bu O O 1 C valproic acid D-315 n-PrNH O S CO2n-Bu O O 1 C valproic acid D-316 (CH3) 3CNH00C02n-Bu001 Cvalproicacid D-317 PhO O O CO2n-Bu O O 1 C valproic acid D-318 PhNH O O CO2n-Bu O O 1 C valproic acid D-319 4Cl (Ph) 00C02n-Bu001 Cvalproicacid D-320 methyl O O CO2-Bn - - 0 N acepromazine D-321 ethyl O O CO2-Bn - - 0 N aminopropazine D-322 n-propyl O O CO2-Bn - - 0 N amiodarone D-323 C(CH3)3 O S CO2-Bn - - 0 N amitriptyline D-324 MeO O S CO2-Bn - - 0 N atropine D-325 EtO O O CO2-Bn - - 0 N atropine D-326 n-PrO O O CO2-Bn - - 0 O atropine D-327 MeNH O 0 C02-Bn--0 O atropine D-328EtNH00C02-Bn--0 Nazaperone D-329 n-PrNH O O COSMe - 0 N buspirone D-330 n-PrO O S COSMe - 0 N chlorpheniramine D-331 PhO O O COSMe - - 0 N clemastine D-332 Ph-NH O 0 COSMe--0 N cloinipramine D-333 4Cl (Ph) O S COSEt--0 N cyproheptadine D-334 4Cl (Ph) O O O COSEt-0 N diethylcarbamazine D-335 4CH30 (Ph) O O O COSn-Bu - - 0 N diltiazem D-336 4NO2 (Ph) O O S COSn-Bu--0 N diphenhydramine D-337 4Cl (Ph) NH O O COSBn - - 0 N diphenoxylate D-338 4F (Ph) NH O 0 COSBn--0 N doxapram D-339 4MeO (Ph) NH O 0 CONHMe--0 N doxepin D-340 pyrid-2-yl O O CONHMe--0 N doxylamine D-341 pyrid-4-yl O O CONHEt - - 0 N droperidol D-342 MeO O O CONHn-Pr - - 0 N fentanyl D-343 EtO O O CONHn-Bu - - 0 N fentanyl D-344 n-PrO O O CONHn-Bu - - 0 N fluconazole D-345 PhO O O CONHn-Bu - - 0 N fluconazole <BR> <BR> <BR> D-346 MeNH O O CONHn-Bu--0 N fluconazole<BR> <BR> <BR> <BR> <BR> D-347 Ph-NH O 0 CONHn-Bu--0 N fluconazole D-348 EtNH O O CONHn-Bu - - 0 N fluconazole D-349 n-PrNH O O CONHn-Bu--0 N fluconazole D-350 (CH3) sCNH O O CONH-Bn--0 N fluconazole D-351 PhO O O CONH-Bn - - 0 N fluconazole D-352 Ph-NH O O CONH-Bn--0 N fluconazole D-353 4Cl (Ph) O O CONNH2 - - 0 N fluconazole <BR> <BR> D-354 methyl O O CONHNHMe--0 N fluconazole<BR> <BR> <BR> <BR> <BR> D-355 ethyl O O CONHNHEt--0 N fluconazole<BR> <BR> <BR> <BR> <BR> D-356 n-propyl O O CONHNHPr--0 N fluconazole<BR> <BR> <BR> <BR> D-357 C (CH3) 3 O O CONHNHt-Bu 0 N fluconazole D-358 MeO O O CONHNHCO2Me - - 0 N fluconazole D-359 EtO O O CONHNHCO2Et - - 0 N fluconazole D-360 n-PrO O O CONHNHCO2t-Bu - - 0 N fluconazole <BR> <BR> <BR> D-361 MeNH O O CONHNHCO2Bn--0 N fluconazole<BR> <BR> <BR> <BR> <BR> D-362 EtNH O O CONHN=CHMe--0 N fluconazole<BR> <BR> <BR> <BR> <BR> D-363 n-PrNH O 0 CONHN=CHMe--0 N fluconazole D-364 (CH3) 3CNH O O CONHN=CHPh - - 0 N fluconazole D-365 PhO O O CONHN=CHPh - - 0 N fluconazole D-366 methyl O O CO2H--0 N fluconazole D-367 ethyl O O CO2H - - 0 N fluconazole D-368 n-propyl O O CO2H - - 0 N fluconazole D-369 C (CH3) 3 O O CO2H 0 N fluconazole D-370 MeO O O CO2H - - 0 N fluconazole D-371 EtO O O CO2H - - 0 N fluconazole D-372 n-PrO O O CO2H - - 0 N fluconazole <BR> <BR> D-373 MeNH O O CO2Me--0 N fluconazole<BR> <BR> <BR> <BR> <BR> D-374 EtNH O O C02Me--0 N fluconazole D-375 n-PrNH O O CO2Me - - 0 N fluconazole D-376 n-PrO O O CO2Me - - 0 N fluconazole D-377 PhO O O CO2Me - - 0 N fluconazole D-378 Ph-NH O O CO2Me--0 N fluconazole D-379 4Cl (Ph) O O CO2Me - - 0 N fluconazole D-380 4Cl (Ph) O O O CO2Et - - 0 N fluconazole D-381 4Cl (Ph) NH O O CO2Et 0 N fluconazole D-382 MeO O S CO2n-Pr - - 0 N fluconazole D-383 EtO O S CO2n-Pr - - 0 N fluconazole D-384 n-PrO O O CO2n-Bu - - 0 N fluconazole <BR> <BR> D-385 MeNH O O CO2n-Bu--0 N fluconazole<BR> <BR> <BR> <BR> <BR> D-386 EtNH O O CO2n-Bu--0 N fluconazole<BR> <BR> <BR> <BR> <BR> D-387 n-PrNH O S CO2n-Bu--0 N fluconazole D-388 n-PrO O S CO2n-Bu - - 0 O fluconazole D-389 PhO O O CO2n-Bu - - 0 O fluconazole <BR> <BR> D-390 PhNH O O CO2n-Bu--0 O fluconazole D-391 4Cl (Ph) O O CO2n-Bu - - 0 O fluconazole D-392 4Cl (Ph) O O O CO2n-Bu - - 0 O fluconazole D-393 MeO O O CO2-Bn - - 0 O fluconazole D-394 EtO O O CO2-Bn - - 0 O fluconazole D-395 n-PrO O O CO2-Bn - - 0 O fluconazole D-396 (CH3)3CO O S CO2-Bn - - 0 O fluconazole D-397 MeNH O S C02-Bn--0 O fluconazole<BR> <BR> <BR> <BR> <BR> D-398 EtNH O O CO2-Bn--0 O fluconazole<BR> <BR> <BR> <BR> D-399 n-PrNH 0 O C02-Bn--0 O fluconazole D-400 (CH3) 3CNH O O CO2-Bn--0 O fluconazole D-401 PhO O O CO2-Bn - - 0 O fluconazole <BR> <BR> D-402 Ph-NH O O COSMe--0 O fluconazole D-403 4Cl (Ph) O S COSMe - - 0 O fluconazole D-404 methyl 0 O COSMe--0 O fluconazole<BR> <BR> <BR> <BR> <BR> D-405 ethyl O O COSMe--0 O fluconazole<BR> <BR> <BR> <BR> D-406 n-propyl O S COSEt-0 O fluconazole<BR> <BR> <BR> <BR> <BR> D-407 C (CH3) 3 O O COSEt-0 O fluconazole D-408 MeO O O COSn-Bu - - 0 O fluconazole <BR> <BR> D-409 EtO O S COSn-Bu-0 O fluconazole D-410 n-PrO O O COSBn - 0 O fluconazole D-411 MeNH O O COSBn - 0 O fluconazole <BR> <BR> D-412 EtNH O O CONHMe-0 O fluconazole<BR> <BR> <BR> <BR> <BR> D-413 n-PrNH 0 O CONHMe-0 O fluconazole D-414 n-PrO O O CONHEt - 0 O fluconazole D-415 PhO O O CONHn-Pr - 0 N hydrocodone <BR> <BR> D-416 Ph-NH O O CONHn-Bu-0 O hydrocodone D-417 methyl O O CONHn-Bu - - 0 N hydroxyzine D-418 ethyl O O CONHn-Bu - - 0 N itraconazole D-419 n-propyl O O CONHn-Bu--0 N levamisole D-420 C(CH3)3 O O CONHn-Bu - - 0 N meclizine D-421 MeO O O CONHn-Bu - - 0 N meclizine D-422 EtO O O CONHn-Bu - - 0 N meclizine D-423 n-PrO O O CONH-Bn - - 0 N meclizine D-424 MeNH O O CONH-Bn - - 0 N meclizine D-425 EtNH O O CONH-Bn - - 0 N meclizine <BR> <BR> D-426 n-PrNH O O CONNH2--0 N meclizine D-427 n-PrO O O CONHNHMe - - 0 N meclizine D-428 PhO O O CONHNHEt - - 0 N meclizine <BR> <BR> D-429 Ph-NH O O CONHNHPr--0 N meclizine D-430 4Cl (Ph) O O CONHNHt-Bu - - 0 N meclizine D-431 4Cl (Ph) 0 O O CONHNHCO2Me--0 N meclizine D-432 4Cl (Ph) NH O O CONHNHCO2Et--0 N meclizine D-433 MeO O O CONHNHCO2t-Bu - - 0 N meclizine D-434 EtO O O CONHNHCO2Bn - - 0 N meclizine D-435 n-PrO O O CONHN=CHMe - - 0 N meclizine <BR> <BR> D-436 MeNH O O CONHN=CHMe--0 N meclizine<BR> <BR> <BR> <BR> <BR> D-437 EtNH O O CONHN=CHPh--0 N meclizine<BR> <BR> <BR> <BR> <BR> D-438 n-PrNH O O CONHN=CHPh--0 N meclizine D-439 methyl O O CO2H - - 0 N meperidine D-440 ethyl O O CO2H - - 0 N meperidine D-441 n-propyl O O CO2H - - 0 N meperidine <BR> <BR> D-442 C (CH3) 3 O O CO2H 0 N meperidine D-443 MeO O O CO2H - - 0 N meperidine D-444 EtO O O CO2H - - 0 N meperidine D-445 n-PrO O O CO2H - - 0 N meperidine D-446 MeNH O O CO2Me - - 0 N meperidine D-447 EtNH O O CO2Me - - 0 N meperidine D-448 n-PrNH O O CO2Me - - 0 N meperidine D-449 n-PrO O O CO2Me - - 0 N meperidine D-450 PhO O O CO2Me - - 0 N meperidine <BR> <BR> D-451 Ph-NH O O CO2Me--0 N meperidine D-452 4Cl (Ph) O O CO2Me - - 0 N meperidine D-453 4Cl (Ph) O O O CO2Et - - 0 O meperidine D-454 4Cl (Ph) NH O O CO2Et - - 0 O meperidine D-455 methyl O O CO2n-Pr - - 0 O meperidine <BR> <BR> D-456 ethyl O O CO2n-Pr--0 O meperidine<BR> <BR> <BR> <BR> D-457 n-propyl O O C02n-Bu--0 N meperidine D-458 C(CH3)3 O O CO2n-Bu - - 0 N meperidine D-459 MeO O O CO2n-Bu - - 0 N meperidine D-460 EtO O S CO2n-Bu - - 0 N meperidine D-461 n-PrO O S CO2n-Bu - - 0 N meperidine <BR> <BR> D-462 MeNH O O CO2n-Bu--0 N meperidine D-463 EtNH O O CO2n-Bu - - 0 N meperidine D-464 n-PrNH O O CO2n-Bu - - 0 N meperidine D-465 n-PrO O O CO2n-Bu - - 0 N meperidine D-466 PhO O O CO2-Bn - - 0 N meperidine D-467 Ph-NH O O CO2-Bn - - 0 N meperidine D-468 4Cl (Ph) O O CO2-Bn - - 0 N meperidine D-469 4Cl (Ph) O O S CO2-Bn - - 0 N meperidine D-470 4MeO (Ph) O O S CO2-Bn - - 0 N meperidine D-471 4NO2 (Ph) O O O C02-Bn--0 N meperidine D-472 4Cl (Ph) NH O O CO2-Bn - - 0 N meperidine D-473 4F (Ph) NH O O C02-Bn--0 N meperidine D-474 4MeO (Ph) NH O O CO2-Bn - - 0 N meperidine D-475 pyrid-2-yl O O COSMe--0 N meperidine<BR> <BR> <BR> <BR> <BR> D-476 pyrid-4-yl O S COSMe--0 N meperidine<BR> <BR> <BR> <BR> D-477 methyl O O COSMe--0 N meperidine<BR> <BR> <BR> <BR> <BR> D-478 ethyl O O COSMe--0 N meperidine<BR> <BR> <BR> <BR> <BR> D-479 methyl O S COSEt--0 N meperidine<BR> <BR> <BR> <BR> <BR> D-480 ethyl O O COSEt--0 N meperidine<BR> <BR> <BR> <BR> <BR> D-481 n-propyl O O COSn-Bu--0 N meperidine D-482 C(CH3)3 O S COSn-Bu - - 0 N meperidine D-483 MeO O O COSBn - - 0 N meperidine D-484 EtO O O COSBn - - 0 N meperidine D-485 n-PrO O O CONHMe - - 0 N meperidine <BR> <BR> D-486 MeNH O O CONHMe--0 N meperidine D-487 ETNH O O CONHEt - - 0 N meperidine D-488 n-PrNH O O CONHn-Pr - - 0 N meperidine D-489 n-PrO O O CONHn-Bu - - 0 N meperidine D-490 PhO O O CONHn-Bu - - 0 N meperidine D-491 Ph-NH O O CONHn-Bu - - 0 N meperidine D-492 4Cl (Ph) O O CONHn-Bu - 0 N meperidine D-493 4Cl (Ph) O O O CONHn-B - - 0 N meperidine D-494 4CH30 (Ph) O O O CONHn-Bu - - 0 N meperidine D-495 4NO2 (Ph) 0 O O CONHn-Bu--0 N meperidine D-496 4C1 (Ph) NH O O CONH-Bn - - 0 N methenamine D-497 4F (Ph) NH O O CONH-Bn - - 0 N methenamine D-498 4MeO (Ph) NH O O CONH-Bn - - 0 N methenamine <BR> <BR> D-499 pyrid-2-yl O O CONNH2--0 N methenamine<BR> <BR> <BR> <BR> <BR> D-500 pyrid-4-yl O O CONHNHMe--0 N methenamine<BR> <BR> <BR> <BR> <BR> <BR> D-501 methyl O O CONHNHEt--0 N methenamine D-502 ethyl O O CONHNHPr - - 0 N methenamine <BR> <BR> D-503 n-propyl O O CONHNHt-Bu--0 N methenamine<BR> <BR> <BR> <BR> <BR> <BR> D-504 C (CH3) 3 O O CONHNHCO2Me--0 N methenamine D-505 MeO O O CONHNHCO2Et - - 0 N methenamine D-506 EtO O O CONHNHCO2T-Bu - - 0 N methenamine D-507 n-PrO O O CONHNHCO2Bn - - 0 N methenamine D-508 MeNH O O CONHN=CHMe - - 0 N methenamine D-509 EtNH O O CONHN=CHMe - - 0 N methenamine D-510 n-PrNH O O CONHN=CHPh - - 0 N methenamine D-511 n-PrO O O CONHN=CHPh - - 0 N methenamine D-512 PhO O O CO2H - - 0 N methenamine <BR> <BR> <BR> D-513 Ph-NH O O CO2H--0 N morantel D-514 4Cl (Ph) O O CO2H - - 0 N morantel D-515 4Cl (Ph) O O O CO2H - - 0 N morantel D-516 4CH30 (Ph) O O O CO2H - - 0 N morantel D-517 4NO2 (Ph) O O O CO2H - - 0 N morantel D-518 4Cl (Ph) NH O O CO2H 0 N morantel D-519 4F (Ph) NH O O CO2Me 0 N morantel D-520 4MeO (Ph) NH O O CO2Me - - 0 N morantel <BR> <BR> D-521 pyrid-2-yl O O C02Me--0 N morantel<BR> <BR> <BR> <BR> <BR> <BR> D-522 pyrid-4-yl O O CO2Me--0 N morantel<BR> <BR> <BR> <BR> <BR> D-523 methyl O O CO2Me--0 N morantel<BR> <BR> <BR> <BR> <BR> D-524 ethyl O O CO2Me--0 N morantel D-525 n-propyl O O CO2Me - - 0 N morantel <BR> <BR> D-526 C (CH3) 3 O O CO2Et 0 N morantel D-527 MeO O O CO2Et - - 0 N morantel D-528 EtO O O CO2n-Pr - - 0 N morantel D-529 n-PrO O O CO2n-Pr - - 0 N morantel <BR> <BR> D-530 MeNH O O CO2n-Bu--0 N morantel<BR> <BR> <BR> <BR> <BR> D-531 EtNH O O CO2n-Bu--0 N morantel<BR> <BR> <BR> <BR> <BR> D-532 n-PrNH O O CO2n-Bu--0 N morantel D-533 n-PrO O O CO2n-BU - 0 N morantel D-534 PhO O O CO2n-Bu - - 0 N morantel <BR> <BR> <BR> D-535 Ph-NH O S CO2n-Bu--0 N naltrexone D-536 4Cl (Ph) O S C02n-Bu--0 N naltrexone D-537 4Cl (Ph) O O S CO2n-Bu - - 0 N naltrexone<BR> <BR> <BR> <BR> D-538 4CH30 (Ph) O O O CO2n-Bu - - 0 N naltrexone<BR> <BR> <BR> <BR> D-539 4NO2 (Ph) O O O CO2-Bn - - 0 N naltrexone<BR> D-540 4Cl (Ph) NH O O CO2-Bn 0 N naltrexone<BR> <BR> <BR> <BR> <BR> <BR> <BR> <BR> D-541 4F (Ph) NH O O CO2-Bn - - 0 N naltrexone<BR> <BR> <BR> <BR> D-542 4MeO (Ph) NH 0 O COz-Bn--0 N naltrexone<BR> <BR> <BR> <BR> <BR> D-543 pyrid-2-yl O O C02-Bn--0 N naltrexone<BR> <BR> <BR> <BR> D-544 pyrid-4-yl O O CO2-Bn - - 0 N naltrexone<BR> <BR> <BR> <BR> <BR> D-545 methyl O O CO2-Bn - - 0 N oxybutynin<BR> <BR> <BR> <BR> D-546 ethyl O O CO2-Bn - - 0 N oxybutynin<BR> <BR> <BR> <BR> <BR> D-547 n-propyl O O CO2-Bn - - 0 N oxybutynin<BR> <BR> <BR> <BR> D-548 C(CH2)8 O O COSMe - - 0 N oxybutynin<BR> <BR> <BR> <BR> <BR> D-549 MeO O O COSMe - - 0 N oxybutynin<BR> <BR> <BR> <BR> D-550 EtO O O COSMe - - 0 N oxybutynin<BR> <BR> <BR> <BR> D-551 n-PrO O O COSMe - - 0 N oxybutynin<BR> <BR> <BR> <BR> <BR> D-552 MeNH O O COSEt - - 0 N oxybutynin<BR> <BR> <BR> <BR> D-553 EtNH 0 O COSEt--0 N pentazocine<BR> <BR> <BR> <BR> D-554 n-PrNH 0 0 COSn-Bu-0N pentazocine<BR> <BR> <BR> <BR> <BR> D-555 n-PrO O O COSn-Bu - - 0 N pentazocine<BR> <BR> <BR> <BR> D-556 PhO O O COSBn - - 0 N pentazocine<BR> <BR> <BR> <BR> <BR> D-557 Ph-NH O O COSBn - - 0 N pentazocine<BR> <BR> <BR> <BR> D-558 4Cl(Ph) O O CONHMe - - 0 N pentazocine<BR> <BR> <BR> <BR> <BR> D-559 4Cl (Ph) 0 O O CONHMe--0 N pentazocine<BR> <BR> <BR> <BR> D-560 4MeO(Ph)O O O CONHET - - 0 N pentazocine<BR> <BR> <BR> <BR> D-561 methyl O O CONHn-Pr - - 0 N pentazocine<BR> <BR> <BR> <BR> <BR> D-562 ethyl O O CONHn-Bu--0 N pentazocine<BR> <BR> <BR> <BR> D-563 n-propyl 0 0 CONHn-Bu-0N pentazocine<BR> <BR> <BR> <BR> D-564 C(CH3)3 O O CONHn-Bu - - 0 N pentazocine<BR> <BR> <BR> D-565 MeO O O CONHn-Bu - - 0 N pentazocine<BR> <BR> D-566 EtO O O CONHn-Bu - - 0 N pentazocine<BR> <BR> <BR> <BR> D-567 n-PrO O O CONHn-Bu - - 0 N pentazocine<BR> <BR> <BR> <BR> <BR> <BR> D-568 MeNH O O CONHn-Bu - - 0 N pentazocine<BR> <BR> <BR> D-569 EtNH O O CONH-Bn - - 0 N pentazocine<BR> <BR> <BR> <BR> D570 n-PrNH O O CONH-Bn - - 0 N pentazocine<BR> <BR> <BR> <BR> <BR> D-571 n-PrO O O CONH-Bn - - 0 N pentazocine<BR> <BR> <BR> <BR> D-572 PhO O O CONN2 - - 0 N pentazocine<BR> <BR> <BR> <BR> <BR> D-573 PH-NH O O CONHNHMe - - 0 N pentazocine<BR> <BR> <BR> <BR> D-574 4Cl(Ph) O O CONHNHEt - - 0 N pentazocine<BR> <BR> <BR> <BR> <BR> D-575 4Cl (Ph) O O 0 CONHNHPr--0 N pentazocine<BR> <BR> <BR> <BR> D-576 4CH30 (Ph) O O O CONHNHt-Bu - - 0 N pentazocine<BR> <BR> <BR> <BR> D-577 4NO2(Ph)O O S CONHNHCO2Me - - 0 N pentazocine<BR> <BR> <BR> <BR> <BR> D-578 4Cl(Ph)NH O S CONHNHCO2Et - - 0 N pentazocine<BR> <BR> <BR> <BR> D-579 4F(Ph)NH O S CONHNHCO2t-Bu - - 0 N pentazocine<BR> <BR> <BR> <BR> <BR> D-580 4MeO (Ph) NH O O CONHNHCO2Bn - - 0 N pentazocine<BR> <BR> <BR> <BR> D-581 pyrid-2-yl O 0CONHN=CHMe--0 N pentazocine<BR> <BR> <BR> <BR> D-582 pyrid-4-yl O O CONHN=CHMe - - 0 N pentazocine<BR> <BR> <BR> <BR> <BR> D-583 methyl O O CO2H - - 0 N pentazocine<BR> <BR> <BR> <BR> D-584 ethyl O O CO2H - - 0 N promazine<BR> <BR> <BR> <BR> D-585 n-propyl O O CO2H - - 0 N pyrantel<BR> <BR> <BR> <BR> <BR> D-586 C (CH3) 3 O O CO2H 0 N selegiline<BR> <BR> <BR> <BR> D-587 MeO O O CO2H - - 0 N tiamulin<BR> D-588 EtO O O CHO2H - - 0 N verapamil D-589 n-PrO O O CO2H - 0 N verpamil <BR> <BR> D-590MeNH00C02Me-0 Nverapamil D-591 EtNH O O CO2Me - - 0 N verapamil D-592 n-PrNH O O CO2Me - - 0 N verapamil D-593 n-PrO O O CO2Me - - 0 N verapamil D-594 PhO O O CO2Me - - 0 N verapamil <BR> <BR> D-595 Ph-NH O O CO2Me--0 N verapamil D-596 4Cl (Ph) O O CO2ME - - 0 N verapamil D-597 4Cl (Ph) O 0 0 CO2Et 0 N verapamil D-598 4CH30 (Ph) O O O CO2Et - - 0 N verapamil D-599 4NO2 (Ph) O O O CO2nPr - - 0 N verapamil D-600 4Cl (Ph) NH O O CO2n-Pr 0 N verapamil D-601 4F (Ph) NH O O CO2n-Bu 0 N verapamil D-602 4MeO (Ph) NH O O CO2n-Bu 0 N verapamil <BR> <BR> D-603 pyrid-2-yl O O CO2n-Bu--0 N verapamil D-604 pyrid-4-yl O O CO2n-Bu - - 0 N verapamil D-605 4NO2 (Ph) O O O CO2n-Bu - - 0 N verapamil D-606 4Cl (Ph) NH O O CO2n-Bu - - 0 N verapamil D-610 pyrid-4-yl 0 O C02-Bn--0 N verapamil D-611 methyl O O CO2-Bn--0 N verapamil D-612 ethyl 0 O C02-Bn--0 N verapamil D-613 n-propyl O O CO2-Bn - - 0 N verapamil D-614 C(CH3)3 O O CO2-Bn - - 0 N verapamil D-615 MeO O S CO2-Bn - - 0 N verapamil D-616 EtO O S CO2-Bn - - 0 N verapamil D-617 n-PrO O S CO2-Bn - - 0 N verapamil <BR> <BR> D-618 MeNH O O CO2-Bn--0 N verapamil<BR> <BR> <BR> <BR> <BR> <BR> D-619 EtNH 0 O COSMe--0 N verapamil<BR> <BR> <BR> <BR> <BR> D-620 n-PrNH 0 O COSMe--0 N verapamil D-621 n-PrO O O COSMe - - 0 N verapamil D-622 PhO O O COSMe - - 0 N verapamil <BR> <BR> D-623 Ph-NH 0 O COSEt--0 N verapamil D-624 4Cl (Ph) 0 O COSEt--0 N verapamil D-625 4Cl (Ph) O O O COSn-Bu - - 0 N verapamil D-626 4CH30 (Ph) O 0 O COSn-Bu--0 N verapamil D627 4NO2 (Ph) O O O COSBn - - 0 N verapamil D-628 4Cl (Ph) NH O 0 COSBn--0 N verapamil D-629 4F (Ph) NH O O CONHMe - - 0 N verapamil D-630 4MeO (Ph) NH 0 O CONHMe--0 N verapamil D-631 pyrid-2-yl O O CONHEt - - 0 N verapamil D-632 pyrid-4-yl 0 O CONHn-Pr-0 N verapamil

Escherichia coli 8739 and Staphylococcus aureus 6538 Minimum Inhibitory Concentration (MIC) Test Methods and Results Several compounds of this invention were tested for biological activity in vitro against Escherichia coli 8739 and Staphylococcus aureus 6538 described below. The following test procedures were employed.

MIC Determination : The lowest concentration of test compound required to inhibit Escherichia coli 8739 and Staphylococcus aureus 6538 was determined by a high resolution minimum inhibitory concentration (HRMIC) test. Varying amounts of the test compounds were added to minimal salts glucose medium (Maniatis, T., Fritsch, E. F., Sambrook, J. 1982 Molecular Cloning, page 68) supplemented with 0. 1% yeast extract (M9GY) in a 96-well microtiter plate. Ten-fold serial dilutions were performed on a Biomek 2000 Workstation to obtain a range of closely spaced concentrations of test compound as shown in Figure 1. A cell suspension of inoculum, adjusted to provide 106 CFU/mL in each well, was added to the microtiter plate. Microtiter plates were incubated at 30 °C for 24 h and then were checked for the presence or absence of microbial growth in each well. The concentration of compound in the first microtiter well demonstrating no growth was the minimum inhibitory concentration (MIC) for the test compound.

Figure 1 Concentration (ppm active ingredient) of a test compound in a HRMIC test using a 10, 000 ppm active ingredient stock solution of the test compound. Test com pound 1 Test com ound 2 1 2 3 4 5 6 7 8 9 10 11 12 A 1000 100 10 1 0. 1 0 1000 100 10 1 0. 1 0 B 800 80 8 0. 8 0. 08 0 800 80 8 0. 8 0. 08 0 C 700 70 7 0. 7 0. 07 0 700 70 7 0. 7 0. 07 0 D 600 60 6 0. 6 0 06 0 600 60 6 0. 6 0. 06 0 E 500 50 5 0. 5 0. 05 0 500 50 5 0. 5 0. 05 0 F 400 40 4 0. 4 0. 04 0 400 40 4 0. 4 0. 04 0 G 300 30 3 0. 3 0. 03 0 300 30 3 0. 3 0. 03 0 H2002020. 2002002020. 200 Table 11 : MIC (ppm AI*) of Kathon CG Biocide, Norfloxacin and compound 8-1 vs S. aureus 6538 and E. coli 8739 : Compound S. aureus 6538 E. coli 8739 Gram-positive Gram-negative Kathon CG Biocide 0. 4 0. 75 Norfloxacin 0. 9 0. 2 8-1 0. 06 2. 5 Table 12 : MIC (ppm AI*) of compounds 8-2, 8-3 and 8-4 vs S. aureus 6538 and E. coli 8739 : Compound S. aureus 6538 E. coli 8739 Gram-positive Gram-negative 8-2 0. 45 3 8-3 4. 5 40 8-4 0.7 >1000