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WO/2000/001669A2 |
The present invention relates to 2-nitro-5-(phenylthio)-anilines which are obtained by reacting 5-chlorine-2-nitroanilines with thiophenols and ammonia in a solvent.
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WO/2000/001383A1 |
RGD mimetics which combine a nitroaryl moiety with an arylether/$g(a)-aminoacid/guanidine framework exhibit activity as antagonists toward various integrins and as inhibitors of angiogenesis.
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WO/2000/000465A1 |
The invention provides hydrazine derivatives of formula (I) wherein R?1¿ is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R?2¿ is an acyl group derived from an $g(a)-, $g(b)-, $g(...
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WO/2000/000468A1 |
Thyroid hormone analogues are disclosed. Methods of using such analogues and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.
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WO/2000/000470A1 |
Compounds represented by general formula (I) and salts thereof, wherein each symbol is as defined in the specification. Because of inhibiting the N type calcium channel, the compounds of general formula (I) are useful as preventives and/...
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WO/2000/000469A2 |
Novel alkyl ketone compounds having potent cytotoxic activity are described as antitumor agents and are particularly effective against leukemia and breast tumor cells. The compounds of the invention have formula (I), wherein R¿1?-R¿4?,...
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WO/1999/067206A1 |
Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular...
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WO/1999/067201A1 |
Compounds of formula (I) wherein: R is methyl substituted by one to three groups selected from alkyl, aryl, alkenyl, and alkynyl; n is 0 or 1; R?1¿ is arylmethyl or heterocyclylmethyl; R?2¿ is alkyl, alkenyl, cycloalkyl or cycloalkenyl...
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WO/1999/067208A1 |
Derivatives of hydroxyphenylsulfanylbenzoic and hydroxyphenylsulfanylarylacetic acids of formula (I), wherein X is H, halogen or NO¿2? group, a is 0 or 1, and m is 2 to 4 if Z is either 4-acetyl-3-hydroxy-2-propylphenoxy of formula (II)...
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WO/1999/065878A1 |
A process for preparing intermediates and benzoquinolin-3-one pharmaceuticals, such pharmaceuticals are effective in treating conditions consequent on 5$g(a)-reductase.
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WO/1999/065922A2 |
A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by five formulas (I), (II), (III), (IV), (V). Each of the R groups is defined in the disclosure.
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WO/1999/064042A1 |
Disclosed are novel multi-binding compounds (agents) which bind alpha-1A adrenergic receptors. The compounds of this invention comprise a plurality of ligands each of which can bind to such receptors thereby modulating the biological pro...
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WO/1999/063996A1 |
Disclosed are multibinding compounds which are agonists, partial agonists, inverse agonists or antagonists of the 5HT¿2? receptors, which are involved in neurological disorders. The multibinding compounds of this invention containing fr...
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WO/1999/064051A1 |
Novel multibinding compounds are disclosed. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of inhibiting bacterial Type II DNA topoisomerase, thereby modulating the biol...
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WO/1999/064052A1 |
This invention relates to novel multibinding compounds that bind to leukotriene receptors and inhibit their activity. In particular, cysteinal leukotriene receptor antagonists and, most particularly leukotriene D¿4? receptor antagonist ...
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WO/1999/063944A2 |
Disclosed are novel multi-binding compounds (agents) which bind estrogen receptors. The compounds of this invention comprise a plurality of ligands each of which can bind to such receptors thereby modulating the biological processes/func...
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WO/1999/064442A1 |
Fluorinated oligopeptides, especially those having 4,4-difluoro-2-amino butyric acid at the C terminus, may be effective inhibitors of hepatitis C virus NS3 protease. Examples of hexapeptides of the invention, optimised for binding in th...
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WO/1999/063940A2 |
Disclosed are multibinding compounds which inhibit H?+¿/K?+¿-ATPase, an enzyme which is involved in the control of acid secretion in the stomach. The multibinding compounds of this invention containing from 2 to 10 ligands covalently a...
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WO/1999/064393A1 |
The invention relates to novel antiestrogens of general formula (I), wherein the substituents which have the meanings cited in the description. The novel compounds concern a) pure antiestrogens or b) antiestrogens having a partial estrog...
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WO/1999/064394A1 |
Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein a and b are 0-2, provided that the sum is 0-3; Q is (i) or (-N=); X is -O-, -S-, -SO-, -SO¿2?-, -CH(OR?8¿)-, -C(O)-, -C(R?23¿)¿2?-, optionally substitute...
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WO/1999/064037A1 |
Novel multi-binding compounds are disclosed that modulate enzymatic processes. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of binding to an enzyme, enzyme substrate o...
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WO/1999/063993A1 |
Disclosed are multibinding compounds which are agonists, partial agonists, inverse agonists or antagonists of the D¿1? receptors, preferably, agonists of the D¿1? receptors, which are involved in neurological disorders. The multibindin...
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WO/1999/063999A1 |
This invention relates to novel multibinding compounds (agents) that are H1-histamine receptor antagonists and pharmaceutical compositions comprising such compounds. Accordingly, the multibinding compounds and pharmaceutical compositions...
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WO/1999/064385A1 |
The present invention relates to a method for condensing at least one carbonyl compound on an electroattractor radical on a carbocyclic aromatic thioether or ether, characterised in that the electroattractor radical present on said carbo...
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WO/1999/063930A2 |
This invention relates to novel multibinding compounds that bind to angiotensin (AT) receptors and modulate their activity. The compounds of this invention comprise 2-10 AT receptor ligands covalently connected by a linker or linkers, wh...
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WO/1999/064053A1 |
The present invention is directed to multibinding compounds which are $g(b)3-adrenergic receptor agonists and are therefore useful in the treatment and prevention of metabolic disorders such as obesity, diabetes, and the like.
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WO/1999/064032A1 |
Disclosed are methods for synthesizing large collections of diverse multimeric compounds as well as iterative processes for evaluating key molecular constraints imparting multibinding properties to multimeric compounds. Also disclosed ar...
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WO/1999/062870A1 |
A novel compound 3-{4-[2-(4-$i(tert)-Butoxycarbonylaminophenyl)ethoxy]phenyl}
-(S)-2-ethoxy propanoic acid having formula (I) and pharmaceutically acceptable salts, solvates, and crystalline forms thereof, a process and intermediates for...
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WO/1999/062872A1 |
A novel 3-aryl-2-hydroxypropionic acid derivative, having formula (I) and pharmaceutically acceptable salts, solvates, and crystalline forms thereof, a process and intermediate for its manufacture, pharmaceutical preparations containing ...
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WO/1999/062871A1 |
Novel 3-aryl proprionic acid derivatives and analogs, having general formula (I) and stereo- and optical isomers and racemates thereof as well as pharmaceutically acceptable salts, solvates and crystalline forms thereof, process for thei...
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WO/1999/062874A1 |
A process for producing highly pure trifluoro methylthiomethyl benzene derivatives, which are useful as intermediates in synthesizing drugs and pesticides, at a high yield by using readily available materials without resort to flon. This...
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WO/1999/062520A1 |
Certain six-membered aromatic and heteroaromatic-dioxo-butyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV...
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WO/1999/062890A1 |
The present invention relates to compounds of formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X?1¿, R?1¿, R?2¿ and R?3¿ are as defined herein. The invention also relates to pharmaceutical ...
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WO/1999/062506A1 |
The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable $i(in vivo) cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (...
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WO/1999/062875A1 |
The present invention relates to novel amidino compounds of formula (I), or a salt, solvate, or physiologically functional derivative thereof; wherein R?1¿ is selected from C¿1-4? alkyl, C¿3-4? cycloalkyl, C¿1-4? hydroxyalkyl, and CÂ...
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WO/1999/062962A1 |
The present invention is directed to new, energy-efficient photoinitiators in the form of $g(a)-amino enol ether compounds. The present invention is also directed to a method of generating reactive species which includes exposing one or ...
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WO/1999/062505A2 |
The invention is directed to a method of treating a neurodegenerative disorder in a subject in need thereof which comprises administering to the subject an amount of a compound effective to inhibit the interaction of amyloid-beta with al...
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WO/1999/061413A1 |
Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula: (T)¿x?A-B-D-E...
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WO/1999/061414A1 |
Compounds represented by general formula (1) which are useful as remedies and preventives for diseases caused by acceleration in the sodium/proton exchange system, wherein R¿1?, R¿2?, R¿3?, R¿4? and R¿5? represent each hydrogen, alk...
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WO/1999/061416A1 |
The invention concerns substituted dithio-bis-nitrobenzenes (dithio-bis-nitrobenzylamines, dithio-bis-nitrobenzamides or dithio-bis-nitrophenacyls) and their uses as alternative substrates for NAD(P)H-dependent disulphide-reductase enzym...
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WO/1999/060047A1 |
A process for easily preparing a polysulfide polymer which contains in the main chain repeating polysulfide units exceeding disulfide in the number of constituent sulfur atoms to therefore function as the vulcanizing agent for rubbers ha...
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WO/1999/059527A2 |
The invention relates to oxidizing agents for coloration of keratin fibers, especially hair, based on a combination of developer-coupler substances, characterized in that they contain at least one 2,5-diamino-1-phenylbenzene derivative o...
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WO/1999/059941A1 |
The invention concerns a method for orthometalation of a carbocyclic aromatic derivative bearing at least an electron donor group, characterised in that it consists in reacting said carbocyclic aromatic derivative with an efficient amoun...
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WO/1999/058495A1 |
The invention concerns compounds of formula (I): R-A-R' wherein: A is as defined in the description; R represents a group (V), wherein R'¿a? and R''¿a? are as defined in the description, or R forms with A a cyclic structure as defined ...
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WO/1999/058122A1 |
The present invention relates to novel fatty acid analogues of the general formula (I): CH¿3?-[CH¿2?]¿$i(m)?-[x¿$i(i)?-CH¿2?]¿$i(n)?-COOR, as defined in the specification, which can be used for the treatment and/or prevention of di...
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WO/1999/058121A1 |
The present invention relates to novel fatty acid analogous of the general forumla I: CH¿3?-[CH¿2?]¿m?-[x¿i?-CH¿2?]¿n?-COOR, as defined in the specification, which can be used for the treatment and/or prevention of obesity, fatty l...
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WO/1999/058123A2 |
The present invention relates to novel fatty acid analogues of the general formula (I): CH¿3? -[CH¿2?]¿$i(m)? - [x¿$i(i)? - CH¿2?]¿$i(n)? - COOR, wherein $i(n) is an integer from 1 to 12, and wherein $i(m) is an integer from 0 to 2...
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WO/1999/058120A1 |
There is disclosed a use of non-$g(b)-oxidizable fatty acid analogues of the general formula (I): Alkyl-X-CH¿2?COOR, wherein alkyl represents a saturated or unsaturated hydrocarbon group of from 8-22 carbon atoms, X represents O, S, SO,...
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WO/1999/058509A1 |
The invention relates to a method for producing isoxazolene of the formula (I), where the substituents have the following meanings: R?1¿ is hydrogen, C¿1?-C¿6? alkyl, R?2¿ is C¿1?-C¿6? alkyl, R?3¿, R?4¿, R?5¿ are hydrogen, C¿1?...
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WO/1999/058496A1 |
The invention concerns compounds of formula (I): R-A-R' wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R?1¿, R?2¿, R?3¿, v and R?4¿ are as defined in the description; R' repr...
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