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WO/2000/044706A1 |
A process which comprises converting a $g(a)-amino acid ester into the corresponding imine to thereby protect the amino group of the ester, reacting the imine with a halomethyllithium to form an N-protected $g(a)-amino halomethyl ketone,...
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WO/2000/044709A2 |
Compound of the formula (B) are useful in treating disease conditions mediated by TNF-$g(a), such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage l...
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WO/2000/044701A1 |
Norbornadienyl derivatives represented by general formula (1) (wherein R?1¿ and R?2¿ are the same or different and each is either an aromatic group containing a heteroatom or a phenyl group having one to three substituents selected fro...
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WO/2000/044714A1 |
The invention relates to novel S-nitrosothiols derived from penicillamine or glutathione of general formula (I), wherein A and B are phenyl groups or together represent a -CH¿2?-Q-CH¿2?- radical forming a six-membered ring in which Q r...
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WO/2000/044713A1 |
The invention concerns compounds of formula (I) which are useful in treating disease conditions mediated by TNF-$g(a), such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease an...
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WO1999064033A9 |
This invention relates to novel multibinding compounds that bind to the enzyme phosphodiesterase V (PDE V) and modulate its activity. The compounds of this invention comprise 2-10 PDE V modulator (particularly inhibitor) ligands covalent...
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WO1999066944A9 |
Disclosed are novel multi-binding compounds (agents) which bind cellular receptors. The compounds of this invention comprise a plurality of ligands each of which can bind to such cellular receptors thereby modulating the biological proce...
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WO1999063994A9 |
Disclosed are multibinding compounds which inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate limiting enzyme in cholesterol biosynthesis. The multibinding compounds of this invention containing from 2 ...
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WO2000003743A9 |
The present invention relates to compositions and methods for inhibiting fungal growth. In particular, the present invention relates to methods for use as anti-fungal agents of inhibitors, and compositions thereof, of fungal prenyltransf...
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WO/2000/043360A1 |
High-quality N-protected S-phenylcysteine compounds represented by general formula (1) are easily, simply and efficiently isolated in high yield by salting out the compounds as salts thereof with bases in the presence of water. In said f...
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WO/2000/041998A1 |
Propargylether derivatives of formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R¿1? is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R¿2? and R¿3? are each independently hydrogen or...
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WO1999064048A9 |
Disclosed are multibinding compounds which inhibit the enzyme HIV reverse transcriptase, an enzyme which catalyzes the conversion of viral RNA to single stranded DNA. The multibinding compounds of this invention containing from 2 to 10 l...
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WO/2000/041505A2 |
The invention features a compound having the formula (I) below. The invention also relates to a pharmaceutical composition including (a) a compound of formula (I) and (b) a pharmaceutically-acceptable carrier. The invention further relat...
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WO/2000/041990A1 |
The invention relates to novel compounds of formula (I), wherein R stands for phenyl, phenyl which has been substituted by C¿1-4?alkyl, C¿1-4?alkoxy or halogen, naphthyl or an aromatic ring with heteroatoms; X means O, S, SO oder SO¿2...
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WO2000001687A9 |
Novel benzothiepines, derivatives, and analogs thereof; methods of preparing such compounds; pharmaceutical compositions containing such compounds; and methods of using these compounds and compositions in the preparation of a medicament,...
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WO/2000/040210A2 |
This invention relates to a topical composition for treating amino acid based substrates comprising a protected thiol compound having the formula R—(S—Pr)¿m? where R is a functional group, S is sulfur, and Pr is a heterocyclic prote...
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WO/2000/040552A1 |
The present application relates to novel aminomalonamides of formula (1) and pharmaceutical composition thereof which are useful for inhibiting matrix metallo-proteinases.
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WO/2000/040239A1 |
This invention relates to substituted benzanilides which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, bu...
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WO/2000/040593A2 |
Method and reagent composition for covalent attachment of target molecules, such as nucleic acids, onto the surface of a substrate. The reagent composition includes groups capable of covalently binding to the target molecule. Optionally,...
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WO1999064035A9 |
Disclosed are multibinding compounds which are beta 2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system...
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WO/2000/039088A1 |
Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof. The compounds act to antagonize the action of the glucagon peptide hormone.
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WO/2000/039070A1 |
This invention relates to compounds, pharmaceutical compositions, and methods of using compounds of formula (I); A is O or S; R is C¿1?-C¿10? straight or branched chain alkyl, C¿2?-C¿10? straight or branched chain alkenyl, C¿2?-C¿1...
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WO/2000/039078A1 |
The present invention relates to methods for production of sulfurized diphenyloxides wherein a diphenyloxide is reacted with elemental sulfur in the presence of solid acid catalyst. The solid acid catalyst can be a zeolite or a catalytic...
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WO/2000/039081A2 |
The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing...
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WO/2000/039077A2 |
New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R¿1? is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R¿2? and R¿3? are the same o...
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WO/2000/039079A1 |
The invention concerns a method for preparing aromatic diphenyl thioethers. More particularly the invention concerns the preparation of 4-chloro-4'-thiomethyldiphenylether. The inventive method for preparing an aromatic diphenyl thioethe...
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WO/2000/037438A1 |
The present invention relates to novel thio-aminotetralin compounds of formula (I) wherein Z, X, R¿1?, R¿2?, R¿3?, R¿4?, R¿5?, and R¿6? are defined herein. The compounds are useful in pain management.
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WO/2000/037429A2 |
The present invention relates to small molecules according to formula (I) which are potent inhibitors of a $g(a)¿4?$g(b)¿1? mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing $g(a)¿4?$g(b)¿1? ad...
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WO/2000/037440A1 |
Optionally fluorine-substituted alkyl or alkenyl poly(ethylene oxides) the compounds of general formula (1) in which R is an alkyl group with 10-20 carbon atoms, an alkenyl group with 10-20 carbon atoms or a fluoroalkyl or fluoroalkenyl ...
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WO/2000/037439A1 |
A method for the preparation of aromatic hydroxythiols including oxidizing an aromatic aminothiol to form an aminodisulfide compound; forming a bis-diazonium salt of the aminodisulfide compound; and reacting the bis-diazonium salt with w...
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WO/2000/037430A2 |
Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. T...
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WO1999064034A9 |
The present invention is directed to multibinding compounds which are beta 2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis, and the like. They are...
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WO/2000/035442A1 |
The invention relates to novel hydroxy diphenylurea sulfonamides, compositions and intermediates thereof. The hydroxy diphenylurea sulfonamides are useful in the treatment of disease states mediated by the chemokine, Interleukin-8.
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WO/2000/035866A2 |
A method for the preparation of hydroxythiol compounds by reacting a hydroxyl-protected halide compound having the structure: X-R-OPg with magnesium in a Grignard-suitable solvent to form a hydroxyl-protected magnesium halide compound, w...
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WO/2000/034226A1 |
The application discloses synthetic derivatives of original polyamines in which a carbon atom to the original polyamine comprises an amide group inhibits the e cellular uptake of a natural polyamine by specifically binding a cellular tra...
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WO/2000/034236A1 |
The present invention provides lipidized conjugates comprising an amino group-containing biologically active substance and a lipophilic group capable of penetrating a biological membrane. Under neutral or mildly acidic conditions, includ...
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WO/2000/032567A1 |
Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R?1¿-R?4¿ are as defined in the specification....
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WO/2000/032568A2 |
(57) Abstract The invention relates to $g(a)-sulfin- and $g(a)-sulfonamino acid amides of general formula (I), including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R¿8? is C¿1?-C¿6?alk...
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WO/2000/031030A1 |
The present invention relates to compounds of general formula (I) wherein X¿1? and X¿2? are different from each other and have the meanings reported in the following description. Y is a simple bond, C¿1?-C¿12? linear or branched alky...
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WO/2000/031009A1 |
The invention concerns functional trifluorovinyl monomers and their copolymerisation with fluorinated olefins and the use of said trifluorovinyl monomers for forming fluorinated elastomers. The invention also concerns the copolymers resu...
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WO/2000/029394A1 |
Disclosed is a method for the production of isoxazols of formula (I), wherein the substituents have the following meanings: R?1¿ hydrogen, C¿1?-C¿6?-alkyl, R?2¿ hydrogen, C¿1?-C¿6?-alkyl, R?3¿, R?4¿, R?5¿ hydrogen, C¿1?-C¿6?-a...
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WO/2000/027809A1 |
The invention concerns a method for preparing methionine aminoamide. The invention also concerns the preparation of methionine without co-production of salts, from an aqueous solution containing essentially methionine aminonitrile by pro...
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WO/2000/027812A1 |
The invention relates to novel phenyl-substituted cyclic enaminones of formula (I), wherein Ar, X, Z, Y, K, n and m have the meanings cited in the description, to various methods and intermediate products, to the production thereof, and ...
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WO/2000/027810A1 |
The present invention provides valuable intermediates which can be used in the synthesis of a compound having polyene chain structure, processes for preparing the same, and a process for preparing $g(b)-carotene by using said intermediat...
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WO/2000/027803A1 |
The invention relates to compounds of formula (I) which have inhibitory effects on farnesyl transferase. Some of these compounds present in vitro inhibition of farnesyl transferase at concentrations < 1 $g(m)M. The compounds provided for...
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WO/2000/027378A2 |
Subject of the present invention are pharmaceutical compositions containing nonpeptidic cystine derivatives of general formula (I) wherein R¿1? and R¿3? may be the same or different and are selected from hydrogen, an aromatic or non-ar...
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WO/2000/026184A1 |
The invention relates to bisphenyl thiocompounds of formula (I), wherein X¿1? to X¿5? independently represent H, Cl, F, OH, SH, R, -OR and -SR, wherein R is an organic radical with 1 to 18 C atoms, which can be an alkyl or alkenyl radi...
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WO1999064038A9 |
Novel multibinding compounds are disclosed. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of binding to an nAChR receptor, thereby modulating the biological processes/f...
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WO1999063988A9 |
Disclosed are multibinding compounds which inhibit nitric oxide synthases (NOSs), enzymes which form nitric oxide and L-citrulline from L-arginine. The multibinding compounds of this invention contain from 2 to 10 ligands covalently atta...
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WO1999064031A9 |
The present invention is directed to multibinding compounds which are beta 2-adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis, and the like. They are...
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