Abstract: The present application describes novel lactams and derivatives thereof of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring B is a 4-8 membered cyclic amide comprising 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
Type:
Grant
Filed:
July 10, 2001
Date of Patent:
September 16, 2003
Assignee:
Bristol-Myers Squibb Pharme Company
Inventors:
Thomas P Maduskuie, Jingwu Duan, Stephen E Mercer
Abstract: The present application describes novel lactams and derivatives thereof of formula I:
or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
Type:
Grant
Filed:
March 12, 2002
Date of Patent:
August 26, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jingwu Duan, Carl P. Decicco, Zelda R. Wasserman, Thomas P. Maduskuie, Jr.
Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
Type:
Grant
Filed:
December 4, 2001
Date of Patent:
August 5, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Patrick Y. S. Lam, Charles G. Clark, John M. Fevig, Robert A. Galemmo, Qi Han, Irina C. Jacobson, Renhau Li, Donald J. P. Pinto, Ruth R. Wexler
Abstract: The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I:
or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
Type:
Grant
Filed:
May 16, 2002
Date of Patent:
August 5, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Robert A. Galemmo, Jr., Celia Dominguez, John M. Fevig, Qi Han, Patrick Y. Lam, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
Abstract: The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
June 22, 2001
Date of Patent:
July 29, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Donald J. P. Pinto, Mimi L. Quan, Francis J. Woerner
Abstract: This invention relates generally to heteroaryl-phenyl substituted compounds that are inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
Abstract: The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula I:
or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
November 17, 2000
Date of Patent:
May 27, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
James Russell Pruitt, John Matthew Fevig, Mimi Lifen Quan, Donald Joseph Phillip Pinto
Abstract: The present application describes inhibitors of factor Xa of formula I:
or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3 may be N or C and J, Ja, and Jb combine to form a substituted carbocycle or heterocycle.
Type:
Grant
Filed:
January 29, 2001
Date of Patent:
April 22, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Qi Han, Celia Dominguez, Eugene C. Amparo, Jeongsook M. Park, Mimi L. Quan, Karen A. Rossi
Abstract: 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 D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
January 27, 2000
Date of Patent:
April 15, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Donald Joseph Phillip Pinto, James Russell Pruitt, Joseph Cacciola, John Matthew Fevig, Qi Han, Michael James Orwat, Mimi Lifen Quan, Karen Anita Rossi
Abstract: The present application describes nitrogen containing heteroaromatics with ortho-substituted P1's and derivatives thereof of formula I:
or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D is substituted ortho to G on E and may be CH2NH2, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
April 12, 2001
Date of Patent:
April 15, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Robert A. Galemmo, Jr., Lori L. Bostrom, Donald J. P. Pinto, Karen A. Rossi
Abstract: The present invention provides of method of preparing phenyl-substituted azoles. This method uses an efficient ligand-accelerated Ullmann coupling reaction of anilines with azoles. The coupling products are useful for preparing factor Xa inhibitors.
Type:
Grant
Filed:
July 25, 2001
Date of Patent:
April 1, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Jiacheng Zhou, Pasquale N. Confalone, Hui-Yin Li, Philip Ma, Lynette M. Oh, Lucius T. Rossano, Charles G. Clark, Chris Teleha
Abstract: The present application describes N-(amidinophenyl)cyclourea analogs of formula I:
which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
May 5, 1999
Date of Patent:
February 18, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Thomas Peter Maduskuie, Jr., Robert Anthony Galemmo, Jr., Celia Dominguez, Mimi Lifen Quan, Karen Anita Rossi, Petrus Fredericus Wilhelmus Stouten, Jung-Hui Sun, Brian Lloyd Wells
Abstract: The present application describes heteroaryl-phenyl heterobicycles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
June 22, 2001
Date of Patent:
January 14, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Donald J. P. Pinto, Mimi L. Quan, Francis J. Woerner, Renhua Li
Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
Type:
Grant
Filed:
January 2, 2002
Date of Patent:
December 31, 2002
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Patrick Y. S. Lam, Charles G. Clark, Renhau Li, Donald J. P. Pinto
Abstract: The present application describes novel &bgr;-amino acid derivatives of formula I:
or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, Ua, Xa, Ya, Za, R1, R2, R3, R4, and R4a are defined in the present specification, which are useful as metalloprotease and/or as TNF-&agr; inhibitors.
Type:
Grant
Filed:
March 16, 2001
Date of Patent:
December 17, 2002
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Jingwu Duan, Bryan W. King, Carl Decicco, Thomas P. Maduskuie, Jr., Matthew E. Voss
Abstract: The present application describes novel lactams and derivatives thereof of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring B is a 4-8 membered lactam containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as inhibitors of matrix metalloproteinases, TNF-&agr;, and aggrecanase.
Abstract: A novel process for making 1,3,5-trisubstituted pyrazoles of the type shown below from appropriate phenyl hydrazines is described.
These compounds are useful as factor Xa inhibitors.
Type:
Grant
Filed:
December 3, 2001
Date of Patent:
October 15, 2002
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Jiacheng Zhou, Lynette May Oh, Pasquale N. Confalone, Hui-Yin Li, Philip Ma
Abstract: The present application describes novel lactams and derivatives thereof of formula I:
or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic sulfonamide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
Type:
Grant
Filed:
February 10, 1999
Date of Patent:
September 24, 2002
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Jingwu Duan, Lihua Chen, Robert J. Cherney, Carl P. Decicco, Matthew E. Voss
Abstract: The present application describes disubstituted pyrazolines and triazolines of formulae I and II:
or pharmaceutically acceptable salt forms thereof, wherein one of M1 and M2 maybe N and D may be a variety of N-containing groups, which are useful as inhibitors of factor Xa.
Abstract: This invention relates generally to nitrogen containing heterobicycles of formulas A and B:
which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.