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WO/2000/056707A1 |
The present invention relates to diaryl thioethers, including substituted diphenyl thioethers. Furthermore, the present invention relates to the use of the aforementioned compounds as ligands for cellular receptors, including adenosine a...
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WO/2000/056721A1 |
The present invention provides a process for the synthesis of a compound or an array of compounds of formula (I). Compounds of formula (I) generally represent the therapeutically important class of compounds namely diversely substituted ...
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WO/2000/055153A1 |
The invention concerns amide derivatives of Formula (Ia) wherein X is - NHCO- or -CONH-; m is 0-3; R?1¿ is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-2; R?2¿ is a gr...
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WO/2000/053613A1 |
Novel compounds that may be used as chemical vapor deposition precursors, thermochromic materials, conductive polymers, light-emitting diode precursors, and molecular charge-transfer salt precursors are provided. In addition, a novel com...
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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/2000/044730A1 |
Compounds having formula (1) are useful in treating disease conditions mediated by matrix metalloproteinases and TACE, such as tumor growth, osteoarthritis, rheumatoid arthritis and degenerative cartilage loss.
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WO/2000/042849A1 |
A ras-farnesyltransferase inhibitor complex formed of ras-farnesyltransferase inhibitor or a pharmaceutically acceptable salt thereof, of formula (I), wherein n is 0 or 1; R¿1? is selected from Cl, Br, phenyl, pyridyl or cyano; R¿2? is...
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WO/2000/042040A1 |
Compounds of formula (I) are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer ther...
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WO/2000/041992A1 |
A novel process for the production of tertiary amines by reductive alkylation of second amine using hydrosilane and a Lewis acid is disclosed. The novel process has application in the preparationof imidazole-containing benzodiazepines, i...
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WO/2000/038618A2 |
This invention relates to novel lactams having formula (I) to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the pr...
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WO/2000/039110A1 |
Homopiperazines of formula (I), wherein R?1¿ is hydrogen, C¿1-8?alkyl, C¿2-8?alkenyl or C¿2-8?alkynyl substituted or unsubstituted with a variety of groups as defined herein; A is a ring selected from phenyl and naphthyl; R?2¿ at ea...
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WO/2000/039105A1 |
Tetrahydronaphthylhomopiperazines of formula (I), wherein p is 4 and R?1¿ at each occurrence is independently selected from hydrogen, halo, hydroxy, C¿1-6?alkyl, C¿1-6?alkoxy, haloC¿1-6?alkyl, cyano, nitro and C¿2-6?alkenyl; q is 7 ...
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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/2000/031073A1 |
Compounds represented by general formula (1) or salts thereof which are useful as the active ingredient of drugs for preventing and/or treating irritable bowel syndrome, systemic functional disorder of digestive tract or diarrhea, wherei...
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WO/2000/028947A2 |
The invention concerns the use of a substance specifically binding with the peripheral benzodiazepin receptor (PBR) for making a composition for preventing or treating skin stress. The invention also concerns compositions containing said...
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WO/2000/024400A1 |
Methods are disclosed utilizing the R enantiomer of tofisopam. This compound is useful in the treatment or prevention of anxiety or anxiety disorders while substantially reducing adverse effects associated with racemic tofisopam.
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WO/2000/023487A1 |
A solid support template for solid phase synthesis of amino group containing compounds is provided that comprises amino-ketone core compounds of the general formula: A-L-NH(CR¿1?R¿2?)¿n?COR¿3? linked to appropriate insoluble substrat...
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WO/2000/023428A1 |
Compounds represented by formula (I) or salts thereof: (I) wherein ring B represents an optionally substituted cyclic hydrocarbon group; Z represents hydrogen or an optionally substituted cyclic group; R?1¿ represents hydrogen, an optio...
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WO/2000/018408A1 |
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...
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WO/2000/014063A1 |
The invention provides agents and compounds (see (I) and (II)) for use in the treatment or prophylaxis of disease conditions caused or exacerbated by mammalian papillomaviruses, such as human papillomaviruses, as well as methods for the ...
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WO/2000/014073A1 |
The invention concerns benzodiazepinone derivatives of formula (I) wherein: R¿1?, R¿2? [A¿1?] and [A¿2?] are as defined in the description, their preparation method and intermediates therefor, their use as medicines, in particular as...
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WO/2000/010942A1 |
Processes are provided for the Mitsunobu alkylation reaction of carbon-carbon bond formation between a solid support reagent and a reagent in solution. The resulting novel products can be prepared as a combinatorial library by high-throu...
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WO/2000/009480A1 |
Sulfonyl derivatives represented by the following general formula (I): Q?1¿-Q?2¿-T?1¿-Q?3¿-SO¿2?-Q?A¿ and drugs containing the same (wherein Q?1¿ is an optionally substituted, saturated or unsaturated, five- or six-membered cyclic...
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WO/2000/007980A1 |
The invention concerns amide derivatives of the Formula (I) wherein R?3¿ is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl...
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WO/2000/007995A1 |
This invention relates to novel lactams of Formula (I) or a pharmaceutically acceptable salts or prodrug thereof, having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhib...
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WO/2000/006620A2 |
Various olefins may be polymerized using a catalyst system containing selected $g(a)-diimine, urethane or urea ligands, some of them novel, complexed to nickel, palladium or other selected transition metals. The polymers are useful as mo...
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WO/2000/004892A2 |
This invention is the coadministration of ACAT and MMP inhibitors for the reduction of both the macrophage and smooth muscle cell component of atherosclerotic lesions, thus impairing the expansion of existing lesions and the development ...
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WO/2000/004020A1 |
Compounds that inhibit the peptidyl-prolyl isomerase (rotamase) enzyme activity of the FK-506 binding protein (FKBP) and compositions comprising these compounds are described. The FKBP-inhibiting compounds have a bicyclic [3.3.1], [4.3.1...
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WO/2000/002851A1 |
The present invention relates to compounds of formula (I), wherein A?1¿, A?2¿, R?1¿, R?2¿, R?3¿, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases,...
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WO/2000/001376A2 |
New therapies can be devised based upon a demonstration of the role of glutamate in the pathogenesis of demyelinating disorders. Inhibitors of the interaction of glutamate with the AMPA and/or kainate receptor complex are likely to be us...
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WO/2000/000479A1 |
The present invention relates to 1,3-benzodiazepin-2-ones and 1,3-benzoxazepin-2-ones of formula (I) or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of H...
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WO/2000/000202A1 |
The invention provides the use of a compound that inhibits the activity of Janus family kinase 3 (JAK-3), or pharmaceutically acceptable salt thereof; for the manufacture of a medicament for inhibiting c-jun activation in mammalian or av...
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WO/1999/067219A1 |
Compounds of formula (I), wherein $i(W) is a cyclic group of the type (2); (3); $i(Y) is represented by the formula (II); these compounds inhibit $g(b)-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treat...
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WO/1999/067221A1 |
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 that include a compound which inhibi...
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WO/1999/066934A1 |
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...
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WO/1999/067220A1 |
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...
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WO/1999/065870A2 |
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural an...
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WO/1999/064403A1 |
1,5-Benzodiazepine derivatives represented by general formula (1) and drugs containing the same, wherein R?1¿ represents lower alkyl; R?2¿ and R?3¿ are the same or different and each represents hydrogen or lower alkyl; R?4¿ represent...
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WO/1999/059977A1 |
The invention relates to new substituted 1,3-diaza-2-(thi)oxo-cycloalkanes of general formula (I), in which n is 1, 2 or 3, Q is oxygen or sulphur, R?1¿ is alkyl, alkoxy, alkylamino, dialkylamino, alkenyl, alkinyl, cycloalkyl or cycloal...
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WO/1999/055684A1 |
The subject invention involves processes for making 2-oxopiperazine and homologous compounds using a solid support resin by (a) removing the protecting group from a N-protected amino acid ester of the resin (if present), (b) reacting the...
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WO/1999/054321A1 |
The invention is directed to physiologically active compounds of general formula (I): wherein R?1¿ represents R?5¿-L?3¿-, R?5¿-L?4¿-R?6¿-, R?5¿-L?4¿-R?7¿-L?5¿-, R?5¿-L?4¿-Ar?1¿-L?3¿-, R?5¿-L?4¿-Ar?1¿-L?6¿-R?6¿- or R?5Â...
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WO/1999/050237A1 |
Sulfonamide derivatives represented by general formula (1) or salts thereof, wherein A represents nitrogen, -CH=, etc.; Z represents oxygen, etc.; Ar?1¿ represents aryl, etc.; Ar?2¿ represents alkyl, etc.; R?a¿ represents hydrogen, et...
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WO/1999/047508A1 |
Compounds of formula (I), pharmaceutically acceptable salts or $i(in vivo) hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally ...
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WO/1999/046248A1 |
The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1$g(b) converting enzyme ('ICE') inhibitors represented by formula (I), wherein Y is (a) or (b). This invention also rela...
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WO/1999/043662A1 |
The subject invention involves processes for making 2-oxopiperazine and homologous compounds using a solid support resin by (a) removing the protecting group from an N-protected amino acid ester of the resin (if present), (b) reacting th...
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WO/1999/040075A1 |
Compounds represented by general formula (I) or salts thereof and prodrugs of the same which have an inhibitory effect on activated blood coagulation factor X and thus are useful as anticoagulating agents. In formula (I), R?1¿ represent...
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WO/1999/038844A1 |
The present invention relates to a method for preparing an N-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound of formula (I) wherein R¿a? is (II); R¿aa? is hydrogen, optionally substituted aliphatic or optionally substituted...
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WO/1999/037625A1 |
Compounds are provided having formula (I), wherein R, R¿1?, R¿2?, R¿3? and R¿4? are defined in the specification, which have matrix metalloproteinase inhibiting activity.
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WO/1999/032461A1 |
Compounds of formula (I): wherein R is hydrogen, C¿1-10?alkyl, C¿3-8?cycloalkyl, C¿3-8?cycloalkylC¿1-6?alkyl, phenylC¿1-6?alkyl or phenyl; R?1¿ is C¿1-6?alkyl, C¿2-6?alkenyl, C¿1-6?alkoxy, halo, hydroxy, C¿1-6?alkanoyl, haloC¿...
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WO/1999/029324A1 |
Drugs containing as the active ingredient compounds represented by general formula (I and II) and being useful in preventing and treating diabetes and complication thereof, wherein R?1¿ represents hydrogen or C¿1-6? alkyl; R?2¿ and R?...
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