Abstract: The present application describes imidazo-heterobicycles of formulas I and III:
or pharmaceutically acceptable salt or prodrug forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
Type:
Grant
Filed:
July 3, 2001
Date of Patent:
January 6, 2004
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Patrick Y. Lam, Charles G. Clark, Qi Han, Thomas E. Richardson
Abstract: Compounds having the formula (I),
are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, IXa, Xa, and/or XIa, wherein ring B is phenyl or pyridyl, W is preferably C(═O)NR4R5, L is a linker group, X2 comprises nitrogen or carbon, Z is an optionally-substituted monocyclic or bicyclic ring system, and R1, R2, R3, R4, R5 and R6 are as defined in the specification.
Type:
Grant
Filed:
November 7, 2001
Date of Patent:
November 4, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Gregory S. Bisacchi, James C. Sutton, William A. Slusarchyk, Uwe D. Treuner, Guohua Zhao, Daniel L. Cheney, Yan Shi, Shung C. Wu
Abstract: The present application describes novel 1,2-disubsituted cyclic derivatives of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-8 membered non-aromatic ring consisting of: carbon atoms, 0-1 carbonyl groups, 0-1 double bonds, and from 0-2 ring heteroatoms selected from O, N, NR2, and S(O)p and the other variables are defined in the present specification, which are useful as metalloprotease and as TNF-&agr; inhibitors.
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 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 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 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: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
Abstract: This invention relates to novel isoxazolines and isoxazoles of formula (I):
or a pharmaceutically acceptable salt or prodrug form thereof. The invention relates to novel isoxazolines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
Type:
Grant
Filed:
July 13, 2001
Date of Patent:
November 5, 2002
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Joanne M. Smallheer, Shuaige Wang, Prabhakar Kondaji Jadhav
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: This invention relates to novel isoxazolines of formula (I):
or a pharmaceutically acceptable salt form thereof. This invention also relates to novel isoxazolines of formula (I) which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
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: The present application de gibes novel cyclic hydroxamic acids of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.
Type:
Grant
Filed:
June 17, 1999
Date of Patent:
August 6, 2002
Inventors:
Chu-Biao Xue, Carl P. Decicco, Xiaohua He
Abstract: The present application describes 6-membered aromatics of formula I:
or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(═NH)NH2, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
February 15, 2000
Date of Patent:
July 30, 2002
Assignee:
Bristol - Myers Squibb Pharma Company
Inventors:
James Russell Pruitt, Donald Joseph Phillip Pinto, Mimi Lifen Ouan, Ruth Richmond Wexler
Abstract: The present application describes nitrogen containing heterobicyclics and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
July 2, 2002
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
John M. Fevig, Joseph Cacciola, Charles G. Clark, Qi Han, Patrick Yuk Sun Lam, Donald J.P. Pinto, James R. Pruitt, Mimi L. Quan, Karen A. Rossi
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 1, 2000
Date of Patent:
June 11, 2002
Inventors:
Jingwu Duan, Carl P. Decicco, Zelda R. Wasserman, Thomas P. Maduskuie, Jr.
Abstract: The present application describes aryl sulfonyls of formula I:
or pharmaceutically acceptable salt or prodrug forms thereof, wherein D, E, and M are defined below, are effective factor Xa inhibitors.