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7589090 |
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 compounds being of formula (I):
wherein R 1 , R 2 , R 3 and R 4 are as defined herein.
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7459452 |
Dihydroxypyrimidine carboxamide inhibitors of HIV integrase
4,5-Dihydroxypyrimidine-6-carboxamides of formula:
are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R 1 , R 2 , R 3 and R 4 are defined herein. These...
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7435734 |
N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula:
are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R 1 , R 2 , R 3 and R 4 are defined...
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7335657 |
Cytokine inhibitors
Disclosed are compounds of formula (I)
Where Ar 1 , X, Y, Q, W, R 3 , R 4 , R 5 , R 6 and R y are defined herein. The compounds of the invention inhibit production of cytokines involved in...
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7323465 |
Alkansulfonamides as endothelin antagonists
The invention relates to novel alkansulfonamides of structure (I), wherein R 1 is a lowel alzyl group and the other variables are as defined in the description, and their use as active ingredients...
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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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7301021 |
Substituted imidazole compounds
Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
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7285549 |
Sulfamides and their use as endothelin receptor antagonists
The invention relates to novel sulfamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for...
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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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7273856 |
Linear basic compounds having NK-2 antagonist activity and formulations thereof
Described herein are compounds of formula (I) useful as antagonists of tachykinins in general, and in particular of neurokinin A; and the pharmaceutical formulations comprising the compounds of...
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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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7166595 |
Compounds, methods and compositions
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
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7160892 |
Pyrimidone compounds and pharmaceutical compositions containing the same
The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A 1 , A 2A , and A 2B receptors), particularly, compounds represented by the general...
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7151101 |
Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention relates to compounds...
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7101873 |
Pyrimidinedione derivatives
Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and...
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7094781 |
Sulfamides and their use as endothelin receptor antagonists
The invention relates to novel sulfamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for...
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7091209 |
Dihydroxypyridmidine carboxylic acids as viral polymerase inhibitors
A class of 2-aryl-4,5-dihydroxy-6-carboxypyrimidines of formula (I): wherein Ar is an optionally substituted aryl or heterocyclicgroup; as well as compounds of formula (I) which are derivatized at...
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7091201 |
Arylalkane-sulfonamides having endothelin-antagonist activity
The invention relates to novel aryl-alkane-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including...
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7057038 |
Kinetic resolutions of chiral 2- and 3-substituted carboxylic acids
One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic...
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7037916 |
Pyrimidine derivatives as IL-8 receptor antagonists
Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I...
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7034019 |
Prodrugs of HIV replication inhibiting pyrimidines
The present invention concerns compounds of formula (A 1 )(A 2 )N—R 1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric...
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6939872 |
2-anilino-pyrimidine derivatives as cyclin dependent kinase inhibitors
Compounds of the formula (I): wherein R 1 , R 2 , R 3 , p, q, and X are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are...
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6852717 |
Compounds useful as anti-inflammatory agents
Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are...
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6833372 |
Non-peptide GnRH agents, Pharmaceutical compositions, and methods for their use
Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent...
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6833364 |
Substituted pyrazole derivatives
The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R 1 , R 2 , R 3 , A, X and Y are each as defined, and to processes...
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6821971 |
Fused pyrazolone compounds which inhibit the release of inflammatory cytokines
The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms...
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6806367 |
Process for producing carbonyl hydrazones
This invention relates to a method for producing compounds of the formula (I) or their salts: wherein each of R 1 and R 2 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or...
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6787539 |
2,4,5,-trisubstituted pyrimidine derivatives
The invention relates to compounds of the formula wherein R 1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O) 2 -lower alkyl, —N(R)—(CH 2 ) n —N(R)...
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6756380 |
5-phenyl-pyrimidine derivatives
Compounds of the general formula are described: wherein R 1 is hydrogen or halogen; R 2 is hydrogen, halogen, lower alkyl or lower alkoxy; R 3 is halogen, trifluoromethyl, lower alkoxy or...
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6750342 |
Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and...
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6743914 |
Kinetic resolutions of chiral 2-and 3-substituted carboxylic acids
One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic...
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6743798 |
Substituted pyrazole derivatives condensed with six-membered heterocyclic rings
The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R 1 , R 2 , R 3 and A are each as defined, and to processes for their preparation and...
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6720322 |
Butyne diol derivatives
The present invention relates to novel butyne diol derivatives of the general formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also...
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6720321 |
1,4-disubstituted benzo-fused cycloalkyl urea compounds
Disclosed are compounds of the formula (I) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds. wherein n, X, A, L, J, p, Q, Y...
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6677337 |
1,2-dihydropyrazol-3-ones which controls inflammatory cytokines
The present invention relates to compounds which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, or enantiomeric and diasteriomeric forms or...
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6635636 |
Substituted 6-benzyl-4-oxopyrimidines, process for their preparation and pharmaceutical compositions containing them
The invention concerns novel substituted 6-benzyl-4-oxopyrimidines and pharmaceutically acceptable salts thereof. These compounds inhibit reverse transcriptase encoded by human immunodeficiency...
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6613764 |
Aspartic protease inhibitors
The present invention provides a compound of formula (I) wherein a, b, c, d, and e, are R 7 , OR 7 , SR 7 , NR 7 R 8 , NHCOR 7 , CO 2 R 7 , CN, NO 2 , NH 2 , N 3 , or a halogen. R 7 and R 8 are H...
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6579982 |
Pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar 1 , Z, R 1 , R 2 and R 3 are as defined in the specification, and to...
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6573377 |
Pyrazole derivatives and salts thereof
This invention provides compounds having antitumor effect, namely a compound represented by the following formula (I) or (Ia) having various substituents in which G and G 1 are condensed tricyclic...
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6562967 |
Kinetic resolutions of chiral 2-and-3-substituted carboxylic acids
One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic...
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6559155 |
Pyrimidinone derivatives for the treatment of atherosclerosis
Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA 2 and thereof use in treating inter alia atherosclerosis, in which: R 1 is COOH or a salt thereof, COOR 10 , CONR 11 R 12 , CN or...
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6548512 |
Nitrogen containing heteroaromatics as factor Xa inhibitors
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and...
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6525050 |
(4-oxo-2-pyrimidinyl)thioalkyl compounds useful as AICARFT inhibitors
Compounds of the formula: (where R 1 , R 2 and R 3 are defined in the specification) are inhibitors of AICARFT. These compounds, as well as their pharmaceutically acceptable salts, solvents,...
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6498253 |
Acylated aminophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators
Compounds of the formula (I) and salts thereof in which W 1 , W 2 , R, n, R 1 , R 2 , R 4 , X, Y and Z are as defined in claim 1 and R 3 is an acyl radical, are suitable as herbicides and...
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6440965 |
Substituted pyrimidine derivatives, their preparation and their use in the treatment of neurodegenerative or neurological disorders of the central nervous system
The present invention relates to novel derivatives of a series of substituted pyrimidines, to pharmaceutical compositions which contain them, to methods for their preparation and to their use in...
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6410483 |
Phenylsulfonylureas, processes for their preparation, and their use as herbicides and plant growth regulators
Compounds of the formula (I) and salts thereof in which R 1 -R 9 , W and A are as defined in formula (I) of claim 1 are suitable as herbicides and plant growth regulators. They can be prepared...
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6410482 |
(Het) arylsulfonylureas having an amino function, their presentation and their use as herbicides and plant growth regulators
(Het)Arylsulfonylureas having an imino function, their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which A is a...
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6395897 |
Nitrile compounds useful as reversible inhibitors of &num 9 cathepsin 5
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are...
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6380387 |
4-Pyrimidinyl-n-acyl-l phenylalanines
Compounds of Formula I are disclosed, having activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4, and accordingly useful for treating diseases whose symptoms and or...
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6372741 |
Use of CSAID™ compounds as inhibitors of angiogenesis
The present invention is to the novel use of a cytokine inhibitor, which cytokine is inhibited by the inhibition of the kinase CSBP/p38/RK, for the treatment of chronic diseases which are caused by...
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