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8101622 Pyridopyrimidinone inhibitors of PI3Kα and mTOR  
The invention is directed to Compounds of Formula I: optionally as a single stereoisomer or mixture of stereoisomers thereof, and additionally optionally as a pharmaceutically acceptable salt...
8076345 2-cyanophenyl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine compounds, compositions and uses thereof  
Fused heterocyclic compounds are provided according to formula 1: where R1, R2, R3, and m are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the...
8058282 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy  
Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
8058283 7H-pyrido[3,4-D]pyrimidin-8-ones, their manufacture and use as protein kinase inhibitors  
Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds,...
8044062 Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha  
The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
8030318 Fused bicyclic inhibitors of HCV  
Substituted fused bicyclic pyrimidine compounds having an amide-substituted pyridylamine group at C-4 of the pyrimidine ring are useful in the treatment of conditions associated with HCV.
8030317 MAPK/ERK kinase inhibitors  
Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture...
8022077 Pyrido[2,3-d]pyrimidines useful as HCV inhibitors, and methods for the preparation thereof  
The present invention relates to the use of pyrido[2,3-d]pyrimidines of formula (I) wherein L, R1, R2 and R3 have specific meaning. The present invention also relates to the use of the compounds of...
8008310 Derivatives of pyrido[2,3-d]pyrimidine, the preparation thereof, and the therapeutic application of the same  
Derivatives of pyrido[2,3-d]pyrimidine are provided having formula (I) with Ar1, Ar2 and R1 as defined herein, which are useful for treating cell proliferative conditions, and to the preparation...
7923450 Modulators for amyloid beta  
The invention relates to compounds of formula wherein R1, R2, R3, R4, X and Y are as defined herein and to pharmaceutically active acid addition salts thereof. The compounds can be used for the...
7910595 Anti-viral compounds  
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-...
7879866 Inhibition of the activity of the capsaicin receptor in the treatment of obesity or obesity-related diseases and disorders  
The present invention provides a method of treating diseases or disorders benefiting from inactivating or down regulating the activity of the capsaicin receptor in a mammal by inhibiting the...
7868018 Compounds and compositions as protein kinase inhibitors  
The invention provides compounds of Formula I: wherein R1-R6 are described in the Summary of the Invention; the pharmaceutical compositions comprising such compounds and methods of using such...
7851468 Substituted pyrazolo[3,4-d]pyrimidines  
The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that...
7846927 N,N′-diphenylurea derivatives suitable as kinase inhibitors  
Compounds of the formula (I), in which R1, R3 and X have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia,...
7842698 Pyridine methylene azolidinones and use thereof phosphoinositide inhibitors  
The present invention relates to pyridine methylene azolidinone compounds of Formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular...
7750016 Hydroxyalkyl substituted pyrido-7-pyrimidin-7-ones  
Compounds of the Formula: where X1, Ar1, R1, and R2 are as defined herein, and compositions comprising the same. Also provided are methods for using compounds of Formula I in treating p38 mediated...
7745451 Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds and compositions thereof useful in the treatment of conditions associated with neurological and inflammatory disorders and dysfunctions  
Fused heterocyclic compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4′, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for t...
7696213 4-methylpyridopyrimidinone compounds  
The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha...
7687502 Substituted quinazoline or pyridopyrimidine derivative  
The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is...
7678801 Compounds  
Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use use in therapy as CSBP/RK/p38 kinase inhibitors.
7662828 Substituted 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine-2-yl compounds and 5,6,7,8-tetrahydroquinazoline-2-yl compounds  
Substituted 5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-2-yl and 5,6,7,8-tetrahydro-quinazolin-2-yl compounds, corresponding to formula I processes for the production thereof, pharmaceutical...
7662827 Pyrazole derivatives having tyrosine kinase inhibitory activity  
Compounds of the formula (I), in which R, X, R1, R2, R3 and R4 have the meanings indicated in Claim (1), are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be...
7648986 Substituted thieno[3,2-D]pyrimidines as Rho kinase inhibitors  
Disclosed are compounds and derivatives thereof their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating...
7645764 Kinase inhibitors and methods for using the same  
Compounds of formula I: wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds, pharmaceutical compositions, methods of using the compounds for...
7622470 Treatment of T-cell lymphoma using 10-propargyl-10-deazaaminopterin  
T cell lymphoma is treated by administering to a patient suffering from T cell lymphoma a therapeutically effective amount of 10-propargyl-10-deazaaminopterin. Remission is observed in human...
7618975 4-arylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof  
Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of...
7601713 Kinase inhibitors and their uses  
The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein...
7582643 Heterocyclic compounds useful in treating diseases and conditions  
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such...
7572801 Pyridopyrimidinone derivatives which are HM74A agonists  
The invention is concerned with novel pyridopyrimidinone derivatives of formula (I): wherein R1 to R8, X, Y, m and n are as defined in the description and in the claims. The compounds of the...
7547695 Pyridopyrimidinones  
The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and X′ have the designations cited in patent claim 1. Said compounds are inhibitors of tyrosine k...
7544682 Pyrido-pyrimidine derivatives, preparation thereof, and therapeutic use thereof  
The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I) and acid addition salts, hydrates and solvates thereof, as...
7531545 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives useful as inhibitors of β-secretase (BACE)  
The present invention is directed to novel 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease...
7524852 Bicyclic pyrimidine derivatives  
[wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m+n is 4 or less; R1 represents —NR4R5 (wherein R4 and R5 may be the same or different and each r...
7504406 Derivatives of pyrido[2,3-d]pyrimidine, the preparation thereof, and the therapeutic application of the same  
The invention relates to derivatives of pyrido[2,3-d]pyrimidine, to the preparation thereof, and to the therapeutic application of the same.
7456168 2-(pyridin-2-ylamino)-pyrido[2,3, d]pyrimidin-7-ones  
The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent...
7442710 Substituted phenyl methanones  
The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R″ andR1, R2,R3, R4,R5, and R6 are as defined in the specification and to pha...
7361662 Pyridopyrimidinone compounds, method for production thereof and medicaments comprising the same  
A compound of formula (I): wherein: R1, R2, R3, R4 are defined in the description, its enantiomers, diastereoisomers, tautomers and also addition salts thereof with a pharmaceutically acceptable...
7348331 Hydroxyalkyl substituted pyrido-7-pyrimidin-7-ones  
Compounds of the Formula: where X1, Ar1, R1, and R2 are as defined herein, and compositions comprising the same. Also provided are methods for using compounds of Formula I in treating p38 mediated...
7329664 Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues  
Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and...
7323472 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds  
The present invention is directed to the novel use of a CSBP/p38 inhibitor for the treatment, including prophylaxis of inflammation enhanced cough in a mammal in need thereof.
7279484 Heterocyclic compounds  
The inventive subject matter relates to compounds, pharmaceutical compositions, and kits containing a heterocyclic compound represented by the formula (I) wherein R is an alkyl group optionally...
7235551 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases  
Novel substituted pyrimidol[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
7232824 Quinazoline derivatives as medicaments  
Quinazoline derivatives have the formula: or the pharmaceutically acceptable salts thereof;wherein each of Z5, Z6, Z7 and Z8 is N or CH and wherein one or two Z5, Z6, Z7 and Z8 are N and wherein...
7208489 2-(pyridin-2-ylamino)-pyrido [2,3-d]pyrimidin-7-ones  
The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent...
7202249 Antagonists of chemokine receptors  
Compounds are provided which are antagonists of chemokine receptor activity. The compounds thereof have the structure including enantiomers, diastereomers, tautomers, pharmaceutically acceptable...
7189731 Substituted 7-azaquinazoline compounds useful as p38 kinase inhibitors  
Compounds having the formula (I) or (II), are useful as p38 kinase inhibitors, wherein R is an optionally substituted alkyl, cycloalkyl, or aryl; R6 is hydrogen or lower alkyl; R7 is hydrogen or a...
7189732 Pyrido[2,3-d]pyrimidine dichloro-phenyl derivatives  
The invention describes compounds of the general formula I a process for their manufacture, compositions containing them and their manufacture as well as the use of these compounds as...
7163941 Pyrido[2,3-d]pyrimidin-7-carboxylic acid derivatives, their manufacture and use as pharmaceutical agents  
The invention describes compounds of the general formula I a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as...
7157466 Quinazoline ditosylate salt compounds  
Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorde4rs characterized by aberrant erbB family PTK activity.
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