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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...
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...
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.
7547782 Met kinase inhibitors  
The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer.
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...
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...
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...
7491730 Compositions useful as inhibitors of GSK-3  
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...
7470689 4-benzimidazol-2-ylpyridazin-3-one derivatives  
Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R 1 and R 2 are detailed in the description, and the physiologically tolerated salts...
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...
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...
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)...
7427618 Ethynyl derivatives as factor Xa inhibitors  
Novel compounds of the formula (I), in which R 1 , R 2 , R 3 , X and Y have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the...
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...
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...
RE40245 Gyrase inhibitors and uses thereof  
The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase...
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...
7323464 Pyridine and pyrimidine derivatives  
Compounds of formula (1) are described in which R a and R b is each independently a hydrogen atom or a group R c , or R a and R b together form an oxo (═O) or thio (═S) group; X is a N atom...
7320975 2-(2-pyridyl)-5-phenyl-6-aminopyrimidine, method and intermediate products for the production and use thereof for combating noxious fungi  
The invention relates to 2-(2-pyridyl)-5-phenyl-6-aminopyrimidines of formula I, wherein the substitutes and the index have the following meaning: R 1 represents halogen, hydroxy, hyano, hxo,...
7312216 N-phenyl-2-pyrimidine-amine derivatives  
The invention relates to N-phenyl-2-pyrimidine-amine derivatives of formula I wherein the substituents are defined as indicated in the description, to processes for the preparation thereof, to...
7312215 Benzimidazole C-2 heterocycles as kinase inhibitors  
Benzimidazole derivatives having the general formula I are provided. These compounds are useful as tyrosine kinase inhibitors, especially for the treatment of cancer.
7282504 Kinase inhibitors  
The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising...
7279576 Anti-cancer medicaments  
Novel compounds and methods of using those compounds for the treatment of oncological conditions are provided. In a preferred embodiment, modulation of the activation states of abl or bcr-abl...
7279475 Fluorinated di-aryl urea compounds  
Disclosed are compounds of formula(I): wherein R 1 , R 2 , W and X of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are...
7276502 Thiazoles useful as inhibitors of protein kinases  
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
7262200 Indazolinone compositions useful as kinase inhibitors  
The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as...
7259162 Benzazole derivatives and their use as JNK modulators  
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...
7226919 Compositions useful as inhibitors of protein kinases  
The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of...
7220736 Pyrimidine compounds  
A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR 4 —, —S—, —O—, —CH═N—,...
7217712 4-Substituted-5-cyano-1H-pyrimidin-6-(thi)ones as GSK-3 inhibitors  
The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions...
7205297 Substituted 5-alkynyl pyrimidines having neurotrophic activity  
The present invention relates to a series of novel substituted 5-alkynyl pyrimidines, pharmaceutical compositions which contain them, methods for their preparation, and their use in therapy,...
7199120 Pyrazolo-pyridine derivatives as antiherpes agents  
The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their...
7189717 Medicinal compositions promoting bowel movement  
The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound...
7186714 Imidazo[1,2-α]pyridine derivatives for the prophylaxis and treatment of herpes viral infections  
The present invention provides compounds of formula (I) wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use...
7179806 Δ1-pyrrolines used as pesticides  
The invention relates to novel Δ 1 -pyrrolines of the formula (I) in which R 1 , R 2 , R 3 , m, and Q have the meanings given in the disclosure, to a plurality of processes for preparing these...
7173028 Pyrimidine derivatives  
The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0R a to R e are defined as in claim 1, which are suitable for the treatment of illnesses characterised by...
7169781 Imidazole derivatives and their use as pharmaceutical agents  
Compounds of the general formula (I) are presented which arevaluable therapeutics for the treatment of cancer and cancer related diseases.
7166599 Trisubstituted pyrimidines  
The present invention relates to trisubstituted pyrimidines of formula wherein R a to R e are defined as in claim 1, which are suitable for the treatment of illnesses in which β-amyloid...
7166597 Fused pyrazole derivatives being protein kinase inhibitors  
Compounds of Formula (I): salts or solvates or physiologically functional derivatives thereof, wherein Z is CH or N, and R 1 , R 2 , and R 4 are various substituent groups, are protein kinase...
7163940 Pyrazolopyridinyl pyrimidine therapeutic compounds  
The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their...