Abstract: 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 variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
Type:
Grant
Filed:
April 16, 2010
Date of Patent:
December 11, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jennifer X. Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
Type:
Grant
Filed:
October 5, 2010
Date of Patent:
October 16, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
Bruce A. Ellsworth, William R. Ewing, Elizabeth Jurica
Abstract: 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 responsive to modulation of P2Y1 receptor activity.
Type:
Grant
Filed:
November 17, 2009
Date of Patent:
September 25, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
James C. Sutton, Zulan Pi, Rejean Ruel, Alexandre L'Heureux, Carl Thibeault, Patrick Y. S. Lam
Abstract: The present invention provides novel benzamide derivatives of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, W, Y, Z, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
Abstract: 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 responsive to modulation of P2Y1 receptor activity.
Type:
Grant
Filed:
April 17, 2008
Date of Patent:
November 8, 2011
Assignee:
Bristol-Myers Squibb Company
Inventors:
Timothy F. Herpin, George C. Morton, Robert P. Rehfuss, R. Michael Lawrence, Michael A. Poss, Jacques Y. Roberge, Timur Gungor
Abstract: 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, R8, and R9 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.
Abstract: 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, B, C, W, Y, Z1, Z2, Z3, Z4, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
Type:
Grant
Filed:
December 17, 2007
Date of Patent:
October 18, 2011
Assignee:
Bristol-Myers Squibb Company
Inventors:
Nicholas Ronald Wurtz, Eldon Scott Priestley, Daniel L. Cheney, Xiaojun Zhang, Brandon Parkhurst, Vladimir Ladziata
Abstract: 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, X3, X4, R6, and R15 are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
Abstract: 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, R3, W, D and R2 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
Abstract: 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 herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
Type:
Grant
Filed:
October 5, 2009
Date of Patent:
November 30, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Donald J. P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith
Abstract: 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 defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
Type:
Grant
Filed:
June 26, 2006
Date of Patent:
October 19, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Hannguang J. Chao, R. Michael Lawrence, Rejean Ruel, James C. Sutton
Abstract: 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 variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
Type:
Grant
Filed:
June 26, 2006
Date of Patent:
June 1, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jennifer Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
Abstract: 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 defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
Abstract: 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, X4, R4, R5, R13, R14, R15 and R16 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
Type:
Grant
Filed:
May 9, 2006
Date of Patent:
May 4, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Mimi L. Quan, Cailan Wang, Jinglan Zhou, Jon J. Hangeland, Dietmar A. Seiffert, Robert M. Knabb
Abstract: 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 defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
Type:
Grant
Filed:
June 26, 2006
Date of Patent:
April 20, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
James C. Sutton, Jennifer X. Qiao, Carl Thibeault, Rejean Ruel
Abstract: 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 diseases responsive to modulation of P2Y1 receptor activity.
Type:
Grant
Filed:
May 8, 2008
Date of Patent:
March 9, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Hannguang J. Chao, Huji Tuerdi, Timothy F. Herpin, Jacques Y. Roberge, Yalei Liu, Michael R. Lawrence, Robert P. Rehfuss, Charles G. Clark, Jennifer X. Qiao, Timur Gungor, Patrick Y. S. Lam, Tammy C. Wang, Rejean Ruel, Alexandre L'Heureux, Carl Thibeault, Gilles Bouthillier, Dora M. Schnur
Abstract: 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 responsive to modulation of P2Y1 receptor activity.
Type:
Grant
Filed:
January 17, 2006
Date of Patent:
January 12, 2010
Assignee:
Bristol-Myers Squibb COmpany
Inventors:
James C. Sutton, Zulan Pi, Rejean Ruel, Alexandre L'Heureux, Carl Thibault, Patrick Y. S. Lam
Abstract: 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. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
Type:
Grant
Filed:
November 7, 2008
Date of Patent:
January 12, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
Abstract: 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 herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
Type:
Grant
Filed:
December 13, 2006
Date of Patent:
December 1, 2009
Assignee:
Bristol-Myers Squibb Company
Inventors:
Donald J. P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith, II
Abstract: 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 of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
Type:
Grant
Filed:
January 9, 2006
Date of Patent:
November 24, 2009
Assignee:
Bristol-Myers Squibb Company
Inventors:
Xiaojun Zhang, Eldon Scott Priestley, Alexandra A. Nirschl, Yan Zou