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Attorney: Sun; Jing G.


Number of patents: 85
Last date: November 29, 2011

1      
NumberTitleIssue Date
8067420Substituted pyrazinone melanin concentrating hormone receptor-1 antagonists and methods
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1
11/29/2011
8053450Amino-benzazoles as P2Yreceptor inhibitors with pyridine ring and heterocyclic components
The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases respo...
11/08/2011
80442422-(aryloxy) acetamide factor VIIa inhibitors useful as anticoagulants
The present invention relates generally to novel 2-(aryloxy)acetamides of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables W, Y, Z, R7
10/25/2011
8039506Bicyclic lactam factor VIIa inhibitors useful as anticoagulants
The present invention provides novel bicyclic lactams derivatives, and analogues thereof, of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, ...
10/18/2011
8012984Substituted pyrazinone melanin concentrating hormone receptor-1 antagonists and methods
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1
09/06/2011
7989433Substituted thieno[3,2-D]pyrimidines as melanin concentrating hormone receptor-1 antagonists
The present invention provides compounds having the following Formula IA and IB, which are useful as MCHR1 antagonists, and includes prodrugs and pharmaceutically acceptable salts thereof: ...
08/02/2011
7973159Non-basic melanin concentrating hormone receptor-1 antagonists
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compo...
07/05/2011
7960569Indole antagonists of P2Yreceptor useful in the treatment of thrombotic conditions
The present invention provides indole compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables ring A, X1, X2, X
06/14/2011
7956049Melanin concentrating hormone receptor-1 antagonists
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1a, R1b, R1c, Q, A, ...
06/07/2011
7842708Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor XIa inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined her...
11/30/2010
7816382Linear urea mimics antagonists of P2Yreceptor useful in the treatment of thrombotic condition
The present invention provides novel urea mimics and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, W, and R6 are as d...
10/19/2010
7728008N-linked heterocyclic antagonists of P2Yreceptor useful in the treatment of thrombotic conditions
The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variab...
06/01/2010
7714002Carbocycle and heterocycle antagonists of P2Yreceptor useful in the treatment of thrombotic conditions
The present invention provides novel urea mimics and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, W, and R6 are as d...
05/11/2010
7709646Tetrahydroquinoline derivatives useful as serine protease inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables A, B, L1, L2, X1, X2, X3
05/04/2010
7700620C-linked cyclic antagonists of P2Yreceptor useful in the treatment of thrombotic conditions
The present invention provides novel C-linked cyclic compounds and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as ...
04/20/2010
7674828Urea antagonists of P2Yreceptor useful in the treatment of thrombotic conditions
The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating disease...
03/09/2010
7645799Substituted biaryl compounds as factor XIa inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein....
01/12/2010
7645778Heteroaryl compounds as P2Yreceptor inhibitors
The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases r...
01/12/2010
7626039Arylpropionamide, arylacrylamide, ayrlpropynamide, or arylmethylurea analogs as factor XIa inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined her...
12/01/2009
7622585Phenylglycinamide derivatives useful as anticoagulants
The present invention relates generally to phenylglycinamide derivatives that inhibit serine proteases. In particular it0 is directed to novel phenylglycinamide derivatives, and analogues thereof, which are useful as selective inhibitors of serine protease enzymes o...
11/24/2009
7595317Barbituric acid derivatives as inhibitors of TNF-α converting enzyme (TACE) and/or matrix metalloproteinases
The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R
09/29/2009
7592331Macrocyclic factor VIIa inhibitors useful as anticoagulants
The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, L, M, W, Z, R1
09/22/2009
7579472Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones
A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.
08/25/2009
7576098Heterocyclic compounds as inhibitors of factor VIIa
The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable salt, solvate, or prodrug form thereof, which are useful as selective i...
08/18/2009
7550499Urea antagonists of P2Yreceptor useful in the treatment of thrombotic conditions
The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of ...
06/23/2009
7482372Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5
01/27/2009
7470712Amino-benzazoles as P2Yreceptor inhibitors
The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases respo...
12/30/2008
7459564Substituted biaryl compounds as factor XIa inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein....
12/02/2008
7456195Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants
The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, ...
11/25/2008
7453002Five-membered heterocycles useful as serine protease inhibitors
The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V):
11/18/2008
7435821Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones
A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors. ...
10/14/2008
7429604Six-membered heterocycles useful as serine protease inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, X1, X2, X3, X4
09/30/2008
7417063Bicyclic heterocycles useful as serine protease inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, L1, L2, X1, X2,...
08/26/2008
7388021Urea antagonists of P2Yreceptor useful in the treatment of thrombotic conditions
The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating disease...
06/17/2008
7388096Crystalline forms of a factor Xa inhibitor
The instant invention provides crystalline forms of 1-(3-chlorophenyl)-7-oxo-6-[4-(2-oxo-1 (2H)pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide and its solvates thereof; processes for the production of such crystalline forms; pharmaceuti...
06/17/2008
7381732Pyrazolobenzamides and derivatives as factor Xa inhibitors
The present application describes pyrazolobenzamides and derivatives thereof of Formula I: P4-P-M-M4I or pharmaceutically acceptable salt forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-...
06/03/2008
7371864Crystalline forms of a factor Xa inhibitor
The instant invention provides crystalline forms of 3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one and its solvates thereof; processes for the production of such crystalline form...
05/13/2008
73122141, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors
The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa. ...
12/25/2007
7312218Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or hetero...
12/25/2007
7304157Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones
A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inh...
12/04/2007
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