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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,...
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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...
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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...
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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.
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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.
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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,...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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 ...
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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...
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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...
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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)...
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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...
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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...
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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...
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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...
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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...
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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...
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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,...
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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...
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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.
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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—,...
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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...
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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,...
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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...
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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...
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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...
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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...
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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...
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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.
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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...
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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...
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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...
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