Heterocyclic Compounds

Matches 651 - 700 out of 2,717	< 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 >

Document	Document Title
WO/1999/026661A1	A COVALENT CONJUGATE OF CLOZAPINE WITH A FATTY ACID AND ITS USE FOR TREATING SCHIZOPHRENIA The invention provides compositions that include conjugates of a fatty acid molecule, preferably $i(cis)-docosahexaenoic acid, and clozapine. The conjugates are useful in treating psychological disorders such as schizophrenia.
WO/1999/024024A2	TREATMENT OF T-HELPER CELL TYPE 2 MEDIATED IMMUNE DISEASES WITH RETINOID ANTAGONISTS Retinoids with retinoid receptor antagonistic activity called retinoid antagonists, pharmaceutically acceptable salts and pharmaceutically acceptable hydrolyzable esters thereof, have been found to be efficacious in the treatment of T-he...
WO/1999/024428A1	OXAZOLIDINONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS A compound of Formula (I) or a pharmaceutically acceptable salt thereof, which is antimicrobial agents, effective against various human and veterinary pathogens, including gram positive aerobic organisms, gram negative organisms, and ana...
WO/1999/021834A1	HETEROARYL DIAZACYCLOALKANES AS CHOLINERGIC LIGANDS AT NICOTINIC ACETYLCHOLINE RECEPTORS The present invention discloses compounds of formula (I) any of its enantiomers or any mixture thereof, isotopes thereof or a pharmaceutically acceptable salt thereof; wherein n is 1, 2 or 3; m is 0, 1 or 2; R represents hydrogen, alkyl,...
WO/1999/020599A1	PHARMACEUTICALLY ACTIVE COMPOUNDS AND METHODS OF USE The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the inv...
WO/1999/020281A1	NOVEL BENZODIAZEPINE DERIVATIVES AS ANTIARRHYTHMIC AGENTS This invention is concerned with novel compounds represented by structural formula (I) which are useful in the treatment of arrhythmia.
WO/1999/018967A1	ANALGESIC COMPOSITIONS Pharmaceutical formulations, particularly suitable for treating chronic and neuropathic pain comprise an opioid-potentiating amount of a CCK antagonist and an analgesic amount of an opioid in a pharmaceutically acceptable biphasic carrie...
WO1999011624B1	OXO-SUBSTITUTED COMPOUNDS, PROCESS OF MAKING, AND COMPOSITIONS AND METHODS FOR INHIBITING PARP ACTIVITY Compound, compositions containing compounds, methods of using compounds, and processes of making compounds, of formula (I) containing at least one ring nitrogen, or a pharmaceutically acceptable base or acid addition salt, hydrate, ester...
WO/1999/018951A1	INHIBITORS OF FARNESYL PROTEIN TRANSFERASE Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of formulas (I), (II), their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates th...
WO/1999/019306A2	2,3-BENZODIAZEPIN-2-ONE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF PROTEIN TYROSINE KINASES Disclosed herein are small molecule, non-peptidyl inhibitors of protein tyrosine kinases, and methods for their use. The instant inhibitors are based on a 1,4-benzodiazepin-2-one nucleus. A compound represented by structural formula (I),...
WO/1999/018085A2	PREPARATION OF ASYMMETRIC CYCLIC UREAS THROUGH A MONOACYLATED DIAMINE INTERMEDIATE The present invention concerns an improved process for the preparation of asymmetric cyclic ureas as well as intermediates in the preparation of asymmetric cyclic ureas of formula (VI): wherein: R?7¿ is selected from the following: C¿1...
WO/1999/017776A1	NOVEL CYCLOALKENYL SUBSTITUTED COMPOUNDS Novel pyridyl or pyrimidinyl substituted cycloalkenyl compounds and compositions for use in therapy.
WO/1999/016313A1	2-METHYL-THIENO-BENZODIAZEPINE FORMULATION The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation of olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates the...
WO/1999/011649A2	PARP INHIBITORS, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS OF USING SAME The present invention relates to PARP inhibitors, pharmaceutical compositions comprising the same, and methods of using the same to treat tissue damage resulting from cell damage or death due to necrosis or apoptosis, effect neuronal act...
WO/1999/012034A1	AMINE COMPOUNDS AND COMBINATORIAL LIBRARIES COMPRISING SAME The present invention provides monocyclic, bicyclic and oligomeric amine compounds with at least two sites of diversity. These compounds are formed from monocyclic scaffolds which can be cyclized to form bicyclic amine scaffolds. These c...
WO/1999/009990A1	PHARMACEUTICAL SUSPENSION COMPRISING NEVIRAPINE HEMIHYDRATE An aqueous pharmaceutical suspension consisting essentially of nevirapine hemihydrate having a particle size between about 1 and 150 microns in diameter.
WO/1999/009991A1	NOVEL AMIDE DERIVATIVES Disclosed are the novel compounds represented by structural Formula (I), wherein A is a lipophilic group comprising an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group a...
WO/1999/006409A1	TRICYCLIC VASOPRESSIN AGONISTS This invention relates to new compounds selected from those of general formula (I), or a pharmaceutically acceptable salt, ester or prodrug form thereof, wherein D, E, and G are N or CH, which serve as vasopressin agonists and are useful...
WO/1999/005147A1	THIAZOLOBENZOHETEROCYCLES, PREPARATION AND MEDICINES CONTAINING SAME The invention concerns compounds of formula (I) in which: R¿1? represents a sulphur or selenium atom; R¿2? represents a hydrogen atom or an alkyl radical; -R¿3?-R¿4?-R¿5?-R¿6?- represents a chain of formula -CH¿2?-CH¿2?-CH¿2?-CH...
WO/1999/005124A1	NOVEL HEXAHYDRO-1,4-DIAZEPINE DERIVATIVES OR SALTS THEREOF Hexahydro-1,4-diazepine derivatives represented by general formula (1); pharmaceutically acceptable salts thereof; and drugs containing the same as the active ingredient, such as activated blood coagulation factor X inhibitor, wherein A:...
WO/1998/054229A1	USE OF YLIDES OF PHOSPHORUS AS SLIGHTLY NUCEOPHILIC STRONG BASES The invention concerns the use of ylides of phosphorus of general formula (I') in which R'�1?, R'�2?, R'�3?, R'�4?, R'�5? represent different variable groups, as a slightly nucleophilic base. The invention also concerns novel y...
WO/1998/047882A1	4,1-BENZOXAZEPINES, THEIR ANALOGUES, AND THEIR USE AS SOMATOSTATIN AGONISTS The present invention provides a compound of formula (I), wherein ring A is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; ring B is an optionally substituted aromatic hydrocarbon ring or aromatic hete...
WO/1998/046591A1	SELECTIVE FACTOR Xa INHIBITORS Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful $i(in vitro) or $i(in vivo) for preventing or treating coagulation disorders.
WO/1998/046576A2	HALO-ALKOXYCARBONYL PRODRUGS Halo-alkoxycarbonyl derivatives of formula (I) are provided as prodrug moieties for pharmaceutical agents containing a basic or polar nitrogen containing fucntionality. The prodrugs are provided as pharmaceutical compositions as well as ...
WO/1998/042696A1	NOVEL 2-(IMINOMETHYL)AMINO-PHENYL DERIVATIVES, PREPARATION, APPLICATION AS MEDICINES AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME The invention concerns novel 2-(iminomethyl)amino-phenyl derivatives, their preparation, their application as medicines and pharmaceutical compositions containing them.
WO/1998/038175A1	NOVEL 1,4-DIAZACYCLOHEPTANE DERIVATIVES AND THEIR USE IN HAIR OXIDATION DYES 1,4-diazacycloheptane derivatives of general formula (I), in which R?1�, R?2�, R?3� and R?4� independently represent hydrogen, a C�1-4? alkyl or hydroxyalkyl group or a C�2-4? dihydroxyalkyl group; X and Y independently repre...
WO/1998/038177A1	HETEROCYCLIC COMPOUNDS AND THEIR USE FOR INHIBITING $g(b)-AMYLOID PEPTIDE Disclosed are compounds which inhibit $g(b)-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits...
WO/1998/029561A1	ENZYMATIC RESOLUTION OF BENZODIAZEPINE-ACETIC ACID ESTERS WITH A LIPASE The present invention involves enantiomerically pure benzodiazepine acetic acid esters and methods of preparing them by resolving a racemic mixture utilizing a lipase.
WO/1998/028268A2	CYCLOALKYL, LACTAM, LACTONE AND RELATED COMPOUNDS AS $g(b)-AMYLOID PEPTIDE RELEASE INHIBITORS Disclosed are compounds for Formula (I) wherein the substituents are as defined in the claims which inhibit $g(b)-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclose...
WO/1998/025911A1	1,5-BENZODIAZEPINE DERIVATIVES 1,5-Benzodiazepine derivatives represented by general formula (I), salts thereof, and medicines containing the same as the active ingredient: (wherein R�1? represents hydrogen, lower alkyl, lower alkoxy or halogeno; R�2? and R�3? m...
WO/1998/023565A2	AMINOGUANIDINES AND ALKOXYGUANIDINES AS PROTEASE INHIBITORS Aminoguanidine and alkoxyguanidine compounds, including compounds of formula $i((I)) wherein X is O or NR?9� and R?1�-R?4�, R?6�-R?9�, R?11�, R?12�, R?a�, R?b�, R?c�, Y, Z, n and m are set forth in the specification, ...
WO/1998/020008A1	1-(3-AMINOINDAZOL-5-YL)-3-PHENYLMETHYL-CYCLIC UREAS USEFUL AS HIV PROTEASE INHIBITORS The present invention relates to compounds of formulae (I) and (II), or pharmaceutically acceptable salt forms or prodrugs thereof, which are useful as inhibitors of HIV protease, and to pharmaceutical compositions and diagnostic kits co...
WO/1998/018769A1	SUSTAINED-RELEASE DERIVATIVES OF HYDROXYLATED ANALOGS OF SUBSTITUTED 1-[2[BIS(ARYL)METHOXY]ETHYL]-PIPERAZINES AND -HOMOPIPERAZINES AND THEIR USE AS NONCOMPETITIVE ANTAGONISTS OF DOPAMINE REUPTAKE The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions comprising the same, and a method of using suc...
WO/1998/018473A1	BENZODIAZEPINE HYDRAZIDE DERIVATIVES AS INHIBITORS OF HIV INTEGRASE Compounds having a benzodiazepine hydrazide core are described. These compounds are useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutical...
WO/1998/016499A1	OXIME DERIVATIVES, HYDRAZONE DERIVATIVES, AND USE THEREOF Compounds having bactericidal activities and represented by general formula (I) and salts and hydrates thereof wherein R?1� represents an optionally substituted aryl, an optionally substituted alkyl or the like; R?2� represents an op...
WO/1998/015278A1	METHOD FOR STIMULATING BONE FORMATION A method for stimulating bone formation by administering integrin binding compounds which cause the release of osteocalcin from osteoblasts is disclosed.
WO/1998/015535A1	1,4-BENZODIAZEPINONES AND THEIR USES AS CCK ANTAGONISTS Benzodiazepine derivatives of formula (I) wherein R?2� is alkyl or cycloalkyl-alkyl when R?4� is hydrogen, or R?2� is a variety of specified groups when R?4� is alkyl, halogen or dialkylamino, are useful as cholecystokinin antago...
WO/1998/015532A1	SOLID PHASE SYNTHESIS OF HETEROCYCLIC COMPOUNDS Here we report a study on a reaction sequence on solid phase, suitable for the generation of molecular diversity on small heterocycles. For each reaction, suitable conditions on solid phase were worked out and a variety of reactive agent...
WO/1998/014192A1	VITRONECTIN RECEPTOR ANTAGONISTS Compounds having a benzodiazepinyl core structure are disclosed which are vitronectin receptor antagonists useful in the treatment of osteoporosis, angiogenesis, tumor growth and metastasis, atherosclerosis, restenosis and inflammation.
WO/1998/008822A1	1,3-DIHETEROCYCLIC METALLOPROTEASE INHIBITORS The invention provides compounds of formula (I) as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as ...
WO/1998/008823A1	HETEROCYCLIC METALLOPROTEASE INHIBITORS The invention provides compounds of formula (I) as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as ...
WO/1998/008825A1	1,4-HETEROCYCLIC METALLOPROTEASE INHIBITORS The invention provides compounds of formula (I) as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as ...
WO/1998/008827A1	HETEROCYCLIC METALLOPROTEASE INHIBITORS The invention provides compounds of formula (I) as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful inh...
WO/1998/007702A1	DIAMIDE COMPOUNDS AND DRUGS CONTAINING THE SAME Diamide derivatives represented by general formula (1), wherein A represents optionally substituted phenyl, etc.; B represents -CH=CH-, -C$m(Z)C-, -(CH=CH)�2?-, -C$m(Z)C-CH=CH-, -CH=CH-C$m(Z)C-, phenylene, etc.; and W represents (a) or...
WO/1998/007711A1	TROPONYL PIPERAZINES AS SELECTIVE DOPAMINE D4 RECEPTOR LIGANDS Described herein are compounds of general formula (I), a stereoisomer, solvate, or pharmaceutically acceptable salt thereof, wherein: R�1? is H, halo, aryl or aryl substituted with one or two groups independently selected from halo, C�...
WO/1998/004247A1	CELL ADHESION INHIBITORS The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds...
WO/1998/004247A2	CELL ADHESION INHIBITORS The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds...
WO/1998/004913A1	MOLECULAR MODEL FOR VLA-4 INHIBITORS Pharmacophore models of VLA-4 inhibitors, methods of identifying novel inhibitors and novel inhibitors identified by these methods.
WO/1998/001132A1	APOPTOSIS INDUCING ADAMANTYL DERIVATIVES AND THEIR USAGE AS ANTI-CANCER AGENTS The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid...
WO/1998/001164A1	TRICYCLIC RADIOLABELED D4 RECEPTOR LIGANDS Herein described are radiolabeled compounds useful to image D4 receptors $i(in vivo), of formula (I), wherein X?1� is selected from NH, O and S; X?2� is selected from CH and N; Z is selected from iodide, cyano, nitro, tri(loweralkyl)...

Matches 651 - 700 out of 2,717	< 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 >