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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...
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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...
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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.
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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,...
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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.
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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.
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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...
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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...
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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...
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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...
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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-...
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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...
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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...
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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...
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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,...
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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...
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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...
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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...
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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...
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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...
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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.
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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.
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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...
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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...
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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...
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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...
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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...
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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.
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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...
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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.
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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...
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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...
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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...
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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...
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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...
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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...
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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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