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7629341 Human ADAM-10 inhibitors  
The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its...
7625895 Diphenyl-dihydro-imidazopyridinones  
and the pharmaceutically acceptable salts and esters thereof, X, R 1 , R 2 , Y 1 and Y 2 are described herein inhibit the interaction of MDM2 protein with a p53-like peptide and hence have anti...
7618961 Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1  
The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the...
7618960 Morpholine type cinnamide compound  
The present invention relates to a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein R 1 , R 2 , R 3 , and R 4 are the same or different and each...
7615550 Substituted piperazines,(1,4) diazepines, and 2,5-diazabicyclo (2.2.1)iieptanes as histamine H1 and/or H3 antagonists or histamine H3 reverse antagonists  
The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the...
7605159 Cathepsin cysteine protease inhibitors and their use  
The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F,...
7601714 Pyrimidine derivatives useful as inhibitors of PKC-theta  
Disclosed are novel compounds of formula (I): wherein X, Y, R 1 , R 2 and R 3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of...
7595314 Benzoyl-piperazine derivatives  
A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia,...
7592450 Piperazinyl-, piperidinyl- and morpholinyl-derivatives as inhibitors of histone deacetylase  
This invention comprises the novel compounds of formula (I) wherein t, R 1 , R 2 , L, Q, X, Y, Z and (a) have defined meanings, having histone deacetylase inhibiting enzymatic activity; their...
7589090 Diaminopyrimidines as P2X3 and P2X2/3 modulators  
Compounds and methods for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist, the compounds being of formula (I): wherein R 1 , R 2 , R 3 and R 4 are as defined herein.
7585858 N-sulfonylcarboximidamide apoptosis promoters  
Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
7579349 4-(pyrazol-3-ylamino) pyrimidine derivatives for use in the treatment of cancer  
A compound of Formula (I); wherein the substituents are as defined in the text for use in modulating insulin-like growth factor 1 receptor activity in a warm blooded animal such as man.
7572921 Substituted benzylimidazoles useful for the treatment of inflammatory diseases  
The invention comprises a class of derivatives of substituted benzylimidazoles of the formula (I) and methods for making the same. These compounds are useful for the treatment of inflammatory...
7572793 3-Substituted-4-pyrimidone derivatives  
A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R 1 represents...
7550462 Piperazinediones as oxytocin receptor antagonists  
Compounds of formula (I) wherein R 1 is 2-indanyl, R 2 is 1-methylpropyl, R 3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R 4 represents methyl and R 5 ...
7547702 4-amino-quinazolines  
Quinazolines of the formula (I) in which R, R 1 , R 2 , R 3 , R 4 and Y have the meaning indicated in Patent claim 1 , and their salts or solvates as glycoprotein 1 bIX antagonists.
7544683 Cyclohexyl derivatives  
The present invention relates to compounds of formula I wherein R 1 and R 2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...
7541359 N-heteroarylpiperazinyl ureas as modulators of fatty acid amide hydrolase  
Certain N-heteroarylpiperazinyl urea compounds of Formula (I), as defined in the specification, are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical...
7531536 Pyrazole compounds useful as protein kinase inhibitors  
This invention describes novel pyrazole compounds of formula IIIa: wherein R 1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl,...
7531532 Pyridine derivative and pyrimidine derivative  
A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor...
7528135 Pyridine derivatives as H3 antagonists  
The present invention relates to compounds of formula I wherein R 1 , R 2 and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to...
7524845 Azaindazole compounds and methods of use  
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in...
7507733 11b-HSD1 inhibitors for the treatment of diabetes  
Compounds of the formula (I): as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 5 have the significance given in claim 1 can be used in the form of...
7504396 Substituted heterocyclic compounds and methods of use  
The present invention relates to pyrimidine or pyridine carboxamides or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell...
7501407 Pyrimidine A2B selective antagonist compounds, their synthesis and use  
The subject invention provides compounds having the structure: wherein R 1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5...
7494994 Phenylpyridylpiperazine compounds  
A compound selected from those of formula (I): wherein: X represents a C(O) or SO 2 group, R 1 represents an aryl group or a group NR 3 R 4 wherein R 3 and R 4 are as defined in the...
7491732 Compositions and methods for inhibition of the JAK pathway  
The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of...
7488727 Thiazole compounds useful as inhibitors of protein kinase  
The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3,...
7485638 Pyrimidine compounds  
Compounds of the formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described...
7470686 Method of inhibiting the expression and/or the activity of JNK  
The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said...
7465728 Derivatives of 4-(imidazol-5-yl)-2-(4-sulfoanilino)pyrimidine with CDK inhibitory activity  
Compounds of the formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described...
7459452 Dihydroxypyrimidine carboxamide inhibitors of HIV integrase  
4,5-Dihydroxypyrimidine-6-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R 1 , R 2 , R 3 and R 4 are defined herein. These...
7456175 Piperazinyl-pyridine derivatives  
The present invention relates to compounds of formula I wherein R 1 , R 2 , X, Y, Z and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as...
7449456 Diaminopyrimidinecarboxamide derivative  
A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is...
7449462 Triazole derivatives which inhibit vasopressin antagonistic activity  
Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: Het represents 2-pyridinyl or 2-pyrimidinyl; R 1 represents H, C 1-3 alkyl or a...
7442699 Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto  
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R 1 ...
7442698 Substituted heterocyclic compounds and methods of use  
The present invention relates to pyrimidine or pyridine carbamate compounds having the general Formula I: and pharmaceutically acceptable salts or derivatives thereof. Also included are methods...
7442697 4-imidazolyl substituted pyrimidine derivatives with CDK inhibitory activity  
Compounds of the formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described...
7435734 N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase  
N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R 1 , R 2 , R 3 and R 4 are defined...
7432255 1H-indol-5-yl-piperazin-1-yl-methanone derivatives  
The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein in formula I is: wherein R 1 to R 4 are as defined in the description and claims....
7432260 Pyrimidine compounds  
The present invention relates to substituted pyrimidines of formula I, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs)...
7427612 Benzoyl-piperazine derivatives  
A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia,...
7427626 2-Anilino-4-(imidazol-5-yl)-pyrimidine derivatives and their use as cdk (cdk2) inhibitors  
Compounds of the formula (I), and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Also described are processes for their preparation and their use as...
7414047 Piperazinyl and diazapanyl benzamides and benzthioamides  
Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
7384943 Substituted chroman derivatives  
The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives having the formula (I) wherein X is N; Y is NR 2 CH 2 , CH 2 NR 2 , NR 2 CO, CONR...
7378108 Percutaneous absorption preparation of compound having angiotensin II antagonistic activity  
The present invention provides a percutaneous absorption preparation which comprises a compound having angiotensin II antagonistic activity and which allows the compound to permeate through the...
7365069 Pyrimidone derivatives  
The present invention relates to novel pyrimidones of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their...
7351708 Pyrrolo [2,3-b] pyridine derivatives  
The present invention relates to compounds of formula I wherein R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...
7351700 Aminomethylpyrimidines as allosteric enhancers of the GABAB receptors  
The present invention relates to compounds of formula wherein X is —S— or —NH—; R 3 /R 4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7...
7348323 Pyrrolo [2,3-c] pyridine derivatives  
The present invention relates to compounds of formula I wherein R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...