Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
Type:
Grant
Filed:
September 17, 2002
Date of Patent:
November 22, 2005
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Donald J. P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y. S. Lam, Stephanie L. Koch
Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
August 8, 2001
Date of Patent:
June 14, 2005
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
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:
April 26, 2002
Date of Patent:
February 22, 2005
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 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 20, 2002
Date of Patent:
February 22, 2005
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Chu-Biao Xue, Carl P. Decicco, Xiaohua He
Abstract: The present application describes novel 1,1-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, S, S(O), and S(O)2 and the other variables are defined in the present specification, which are useful as metalloprotease and as TNF-&agr; inhibitors.
Abstract: This invention relates generally to a novel class of fused heterocyclic compounds of the Formula (I) or Formula (II):
or pharmaceutically acceptable salt forms thereof, 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.
Type:
Grant
Filed:
April 8, 2002
Date of Patent:
September 14, 2004
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Irina C. Jacobson, Mimi L. Quan, Ruth R. Wexler
Abstract: The present application describes to novel bicyclic hydroxamates derivatives of formula I:
or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, B1, B2, R1, and C are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), aggrecanase, or a combination thereof.
Abstract: A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below from appropriate pyrrolidinones is described.
These compounds are useful as intermediates for MMP and TACE inhibitors.
Type:
Grant
Filed:
March 14, 2003
Date of Patent:
August 3, 2004
Assignee:
Bristol-Myers Squibb Company
Inventors:
Nicholas A. Magnus, Pasquale N. Confalone, Scott A. Savage, Matthew Yates, Robert E. Waltermir, David J. Meloni, Silvio Campagna
Abstract: The present application describes 1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-ones of the following formula or pharmaceutically acceptable salt forms thereof:
wherein ring Rb is 3-amido or 4-methoxy, Ra can be cyano, trifluoromethyl, or amido, and R can be a substituted phenyl, a substituted imidazolyl, or a substituted pyridine. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
Type:
Grant
Filed:
April 17, 2002
Date of Patent:
June 15, 2004
Assignee:
Bristol-Myers Squibb Pharms Company
Inventors:
Donald Joseph Philip Pinto, Robert Anthony Galemmo, Jr., Michael James Orwat, Mimi Lifen Quan
Abstract: The present invention relates to the process for the preparation of the compound of Formula I:
from its corresponding 3-cyano-4-fluorophenyl-pyrazole and intermediates useful therein.
Type:
Grant
Filed:
May 7, 2003
Date of Patent:
June 8, 2004
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Hui-Yin Li, Luigi Anzalone, Fuqiang Jin, David J. Meloni, Jung-Hui Sun, Lucius T. Rossano, Christopher A. Teleha, Jiacheng Zhou, Thomas E. Smyser
Abstract: The present application describes novel cyclic &bgr;-amino acid derivatives 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 and/or as TNF-&agr; inhibitors.
Type:
Grant
Filed:
March 16, 2001
Date of Patent:
June 1, 2004
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Jingwu Duan, Gregory Ott, Lihua Chen, Carl Decicco, Zhonghui Lu, Thomas P. Maduskuie, Jr., Chu-Biao Xue
Abstract: The present application describes novel spiro-cyclic &bgr;-amino acid derivatives of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms a 3-11 membered spiro-carbocycle or spiro-heterocycleon ring B, and the other variables are defined in the present specification, which are useful as as matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), and/or aggrecanase inhibitors.
Type:
Grant
Filed:
March 12, 2002
Date of Patent:
April 13, 2004
Assignee:
Bristol-Myers Squibb Pharma
Inventors:
Gregory R. Ott, Xiao Tao Chen, Jingwu Duan, Matthew E. Voss
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.
Abstract: The present application describes monocyclic or bicyclic carbocycles and heterocycles and derivatives thereof of Formula I:
or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
October 29, 2001
Date of Patent:
March 23, 2004
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Irina C. Jacobson, Ruth R. Wexler, Shuaige Wang, Joanne M. Smallheer
Abstract: The present application describes 1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-ones of Formula I or pharmaceutically acceptable salt forms thereof:
wherein ring R is 3-amido or 4-methoxy, R1 is trifluoromethyl or amido, and R2 is aminomethyl, N-methylaminomethyl, and N,N-dimethylaminomethyl. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
Abstract: The present application describes novel amides and derivatives thereof of formula I:
or pharmaceutically acceptable salt forms thereof, wherein these compounds are useful as inhibitors of matrix metalloproteinases, TNF-&agr;, and aggrecanase.
Type:
Grant
Filed:
February 12, 2002
Date of Patent:
February 10, 2004
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Jingwu Duan, Carl P. DeCicco, David J. Nelson, Chu-Biao Xue
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.
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: The present invention relates to the process for the preparation of the compound of Formula I:
from its corresponding 3-cyano-4-fluorophenyl-pyrazole and intermediates useful therein.
Type:
Grant
Filed:
September 21, 2001
Date of Patent:
December 23, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Hui-Yin Li, Luigi Anzalone, Fuqiang Jin, David J. Meloni, Jung-Hui Sun, Christopher A. Teleha, Jia C. Zhou, Thomas E. Smyser
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.