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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...
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...
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...
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...
7482356 Bicyclic pyrazolone cytokine inhibitors  
The present invention relates to 6,7-dihydro-5H-pyrazolo[1,2α]pyrazol-1-ones which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or...
7479495 N-heterocyclic inhibitors of TNF-α expression  
N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of...
7473695 4-imidazolin-2-one compounds  
The present invention relates to a compound of the formula [I]: wherein G 1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: ...
7473691 Pyrazole compounds useful as protein kinase inhibitors  
This invention describes novel protein kinase inhibitors of formula VII: wherein G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or...
7470700 Dipeptidyl peptidase inhibitors  
Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV inhibitors comprising Formula I: wherein the substituents are as described herein.
7470685 Pyrimidine compounds  
This invention features pyrimidine compounds of formula (I): R 1 is in which one of R a and R b is H or alkyl, and the other is aryl or heteroaryl optionally substituted with R d and R...
7470783 Photocleavable protecting groups and methods for their use  
Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally...
7470701 Substituted 2,5-heterocyclic derivatives  
The present invention relates to new substituted five-membered compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with...
7465736 Azole methylidene cyanide derivatives and their use as protein kinase modulators  
An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of...
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...
7462625 Gonadotropin-releasing hormone receptor antagonists and methods relating thereto  
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ...
7462619 Pyridazine, pyrimidine and pyrazine ethyne compounds  
In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring...
7459460 Trisubstituted heteroaromatic compounds as calcium sensing receptor modulators  
Trisubstituted heteroaromatic compounds having the structure are provided, wherein X is C or N; A and B are each independently CH or N, with the proviso that A and B cannot both be CH; R...
7459455 Pyrimidine compounds  
Pyrimidine derivatives, which are useful as TIE-2 and/or VEGFR-2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as...
7456190 Compositions useful as protein kinase inhibitors  
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...
7456191 N-Aryl-sulfoximine-substituted pyrimidines as CDK-and/or VEGF inhibitors, their production and use as pharmaceutical agents  
This invention relates to pyrimidine derivatives of general formula (I) in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of...
7449474 Tri-substituted ureas as cytokine inhibitors  
The present invention relates to 1,1,3-tri-substituted ureas which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian...
7449471 5-phenylpyrimidines, their preparation, compositions comprising them and their use  
5-Phenylpyrimidines of the formula I in which the substituents and the index are as defined below: R 1 ,R 2 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl,...
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...
7446109 Carbonylamino-derivatives as novel inhibitors of histone deacetylase  
This invention comprises the novel compounds of formula (I) wherein n, m, t, R 1 , R 2 , R 3 , R 4 , R 5 , L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic...
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 ...
7442705 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...
7442701 Amino-heterocycles as VR-1 antagonists for treating pain  
The present invention provides a compound of formula (I): wherein V represents NR 5 , O, S, SO or S(O) 2 ; W and X each independently represent CH or N; Y represents N, CH or C—Ar 2 , with the...
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...
7439268 Compositions containing prodrugs of florfenicol and methods of use  
The present invention provides compositions and methods for administering florfenicol to mammals. The compositions contain a prodrug of florfenicol in a pharmaceutically acceptable carrier. In one...
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)...
7429599 Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK  
This invention generally relates to methods for treating or preventing a condition responsive to JNK inhibition, such as a metabolic condition, comprising administering to a patient in need thereof...
7427627 N-(4-(4-methylthiazol-5-yl) pyrimidin-2-yl)-N-phenylamines as antiproliferative compounds  
The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases...
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...
7423148 Small molecule PI 3-kinase inhibitors and methods of their use  
Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a...
7419984 Pyrimidines and uses thereof  
The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor-cells.
7417048 Aryl-substituted derivatives of cycloalkyl and branched chain alkyl carboxylic acids useful as antinociceptive drugs for peripheral targets  
Novel peripheral antinociceptive compounds are disclosed having a pharmacophore unit that target small-diameter nerve fibers that transmit signals of pain and discomfort from the soma and viscera....
7407965 Phosphonate analogs for treating metabolic diseases  
The invention is related to phosphorus substituted compounds with activity for treating metabolic diseases and/or disorders, e.g., diabetes and hypercholesterolemia, compositions containing such...
7405221 Substituted pyrimidines  
Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases...
7396836 Pyrimidine compound and medicinal composition thereof  
A compound having excellent adenosine receptor (A 1 , A 2A , A 2B receptor) antagonistic action, of the following formula, a salt thereof or a solvate of them: wherein, R 1 and R 2 , same or...
RE40332 Fungicidal trifluoromethylalkylamino-triazolopyrimidines  
The novel compounds of formula I: wherein (R 1 , R 2 , Hal and L 1 through L 5 are defined in the specification) show selective fungicidal activity. The new compounds may be processed with...
7371759 HMG-CoA reductase inhibitors and method  
Compounds are provided having the following structure which are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example,...
7368455 6,7-Dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines  
The present invention relates to 2-(4-fluorophenyl)-3-(2-phenoxy-pyrimidin-4-yl)-6,7-dihydro- 5H-pyrazolo-[1,2-a]pyrazol-1-one, including all enantiomeric and diasteriomeric forms and...
7361665 Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases  
The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein R 1 , R 2 , A, G, and W are as described in the specification. These...
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...
7358258 Prodrugs of an ERK protein kinase inhibitor  
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...
7351733 Tetrahydrocarbazole derivatives and their pharmaceutical use  
The present invention relates to novel compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.
7351711 Tricyclic indanyls as integrin inhibitors  
The present invention is directed to substituted indanyl compounds of Formula (I): Useful for treating integrin-mediated disorders such as, but not limited to unstable angina, thromboemboic...