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7615562 |
2-aminopyrimidine derivatives and their medical use
A compound of formula I or a pharmaceutically acceptable salt, ester or prodrug thereof wherein the variables have the meanings as defined in the specification. Further disclosed are a method of...
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7615553 |
Inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein n, R 1 , R 2 , R 3 , R 4 , Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their...
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7612080 |
GTPase inhibitors and use thereof for controlling platelet hyperactivity
The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such...
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7605166 |
Methods and compositions for treating rheumatoid arthritis
This application relates to methods and compositions for treating rheumatoid arthritis by administering a combination therapy comprising methotrexate and an antibody to alpha-4 integrin or an...
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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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7598260 |
CDK-inhibitory pyrimidines, their production and use as pharmaceutical agents
This invention relates to pyrimidine derivatives of general formula I
in which R 1 , R 2 , X, A and B have the meanings that are contained in the description, as inhibitors of the...
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7595323 |
N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof
The present invention relates to an N-phenyl-2-pyrimidine-amine derivative showing a superior effect on lung cancer, gastric cancer, colon cancer, pancreatic cancer, hepatoma, prostatic cancer,...
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7592349 |
Diarylamine-containing compounds and compositions, and their use as modulators of c-kit receptors
Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity...
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7585870 |
HIV replication inhibiting pyrimidines and triazines
This invention concerns HIV replication inhibitors of formula (I), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms...
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7582648 |
Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms...
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7582646 |
Pyrimidine derivatives for treatment of hyperproliferative disorders
Pyrimidine derivatives of formula (I)
in which J and Y represent aromatic or heteroaromatic rings; R 2 , G, G′, and G″ represent substituent groups and R 2a represents H or halogen; L...
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7582645 |
Pyrimidine derivatives for treatment of hyperproliferative disorders
Pyrimidine derivatives of formula (I) in which J and Y represent aromatic or heteroaromatic rings; R 2 , G, G′, and G″ represent substituent groups and R 2a represents H or halogen; L...
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7579466 |
Pyrimidinyl sulfonamide compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds, which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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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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7579344 |
Pyrimidine derivatives possessing cell-cycle inhibitors activity
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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7576093 |
Method of treatment of bone-related disorders or conditions
The present invention relates to a new use of a compound of the formula (I)
wherein R 1 is NH 2 , piperazin-1-yl, 4-methylpiperazin-1-yl,4-methyl-1,4-diazepan-1-yl or 4-ethylpiperazin-1-yl; R 2...
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7566724 |
Glycine derivative and use thereof
The compounds of the disclosure, for example, the compound represented by the formula:
has excellent therapeutic and prophylactic effects against inflammatory bowel disease. Further, they are...
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7563894 |
Diarylamine-containing compounds and compositions, and their use as modulators of c-kit receptors
Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity...
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7560551 |
Aurora kinase modulators and method of use
The present invention relates to chemical compounds having a general formula I
wherein A 1 , A 2 , C 1 , C 2 , D, L 1 , L 2 , Z and R 1-8 are defined herein, and synthetic intermediates, which...
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7560483 |
Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require...
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7560464 |
Polycyclic pyrimidines as potassium ion channel modulators
The present invention provides a genus of polycyclic pyrimidines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and...
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7550473 |
Pyrimidine derivatives useful as inhibitors of PKC-theta
Disclosed are novel compounds of formula (I):
wherein 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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7547691 |
[4-(Benzo[B]thiophen-2-yl) Pyrimidin-2-yl]-amine derivatives as IKK-beta inhibitors for the treatment of cancer and inflammatory diseases
The present invention provides compounds of Formula I: useful in the treatment of cancer and inflammatory diseases.
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7538117 |
Crystalline and amorphous pyrimidine compounds and processes for preparing pyrimidine compounds
Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-
one having a diffraction peak at a diffraction angle (2θ±0.2°) of 9.7° and/or 21.9° in a powder X-ray diffraction are...
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7538116 |
Treatment of sexual disorders
The present invention relates to a method of treatment of sexual dysfunction e.g. female sexual disfunction by administering to a person in need of treatment an effective amount of gepirone as...
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7531548 |
HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines
HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a 1 =a 2 -a 3 =a 4 - is...
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7531547 |
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 methods comprising administering to a subject in need thereof an effective amount of a...
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7528143 |
Bi-aryl meta-pyrimidine inhibitors of kinases
The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak...
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7524874 |
Vanilloid receptor ligands and their use in treatments
Compounds having the general structure
and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster...
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7524855 |
Selected benzofuran derivatives
The invention relates to new benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including...
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7524854 |
Benzofuran derivatives and their use in the treatment of microbial infections
The invention relates to new benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including...
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7524849 |
5-arylpyrimidines as anticancer agents
This invention relates to certain 5-arylpyrimidine compounds or a pharmaceutically acceptable salt thereof, and compositions containing said compounds or a pharmaceutically acceptable salt thereof,...
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7521453 |
Pyrimidine derivatives as modulators of insulin-like growth factor-1 receptor (IGF-I)
The invention provides compounds of formula
in which R 1 , R 2 , R 3 and R 4 have the meanings defined in the specification; processes for the preparation; pharmaceutical compositions...
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7517890 |
GTPase inhibitors and methods of use
The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such...
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7514446 |
Pyrimidine 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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7514445 |
Heteroaryl amines as glycogen synthase kinase 3β inhibitors (GSK3 inhibitors)
This invention concerns a compound of formula
a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a...
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7514428 |
Pesticidal 1-aryl-3-amidoxime-pyrazole derivatives
1-Arylpyrazole-3-substituted-amidoxime derivatives of formula (Ia) or (Ib):
or salts thereof, wherein the various symbols are as defined in the description, and pesticidal compositions thereof,...
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7511052 |
Pyrimidinyl amide compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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7507737 |
Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4receptor
Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H 4 receptor activity, including...
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7504410 |
Chk-, Pdk- and Akt-inhibitory pyrimidines, their production and use as pharmaceutical agents
This invention relates to pyrimidine derivatives of general formula (I) as inhibitors of kinases, their production as well as their use as medications for treating various diseases.
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7501430 |
RAF inhibitors and their uses
The present invention provides imidazooxazole and imidazothiazole compounds and their synthesis. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as...
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7501424 |
N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof
The present invention relates to a novel N-phenyl-2-pyrimidine-amine derivative represented by the above formula (1) and its salt showing a superior effect on cancer in warm-blooded animals, such...
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7501417 |
Aminocarbonyl-derivatives as novel inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein n, R 1 , R 2 , R 3 , R 4 , L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity;...
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7501415 |
Selective inhibitors of ERK protein kinase and uses thereof
Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a...
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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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7491731 |
Crystal structure of liganded cFMS kinase domain
A crystal structure of the cfms kinase domain, co-crystal structure with a bound small molecule, as well as methods of using the same in the discovery of cfms inhibitors and in the treatment 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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7488734 |
Methods of treating hormone-related conditions using thio-oxindole derivatives
The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which...
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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,...
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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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