Patents Represented by Attorney Jing S. Belfield
  • Patent number: 7015217
    Abstract: The present application describes novel cyclic sulfone derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof. In formula I, A is selected from —COR5, —CO2H, —CO2R6, —C(O)NHOH, —C(O)NHOR5, —C(O)NHOR6, —NHRa, —N(OH)COR5, —N(OH)CHO, —SH, —CH2SH, —S(O)(?NH)Ra, —S(?NH)2Ra, —SC(O)Ra, —PO(OH)2, and —PO(OH)NHRa; B is a thiomorpholine ring; X is absent or is CR3R4; and Ua, Xa, Ya, Za, R1, R2, Rb, and q are defined in the present specification.
    Type: Grant
    Filed: October 7, 2002
    Date of Patent: March 21, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jingwu Duan, Chu-Biao Xue
  • Patent number: 6878710
    Abstract: This invention relates generally to a novel class of bicyclic heterocyclic compounds of the Formula (I): 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: May 22, 2002
    Date of Patent: April 12, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Irina C. Jacobson, Mimi L. Quan, Yun-Long Li, Ruth R. Wexler, Patrick Y. S. Lam
  • Patent number: 6835841
    Abstract: A novel process for the asymmetric synthesis of substituted cyclic &bgr;-amino-carboxylates of the type shown in the specification from appropriate &bgr;-enamino-ester starting materials is described. These compounds are useful as intermediates for MMP and TACE inhibitors.
    Type: Grant
    Filed: September 11, 2003
    Date of Patent: December 28, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joerg Deerberg, Douglas D. McLeod, Tai-Yuen Yue
  • Patent number: 6825215
    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.
    Type: Grant
    Filed: January 9, 2002
    Date of Patent: November 30, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Xiao-Tao Chen, Chu-Biao Xue
  • Patent number: 6825208
    Abstract: This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine protease enzymes, especially factor VIIa; pharmaceutical compositions containing the same; and methods of using the same as anticoagulant agents for modulation of the coagulation cascade.
    Type: Grant
    Filed: August 20, 2002
    Date of Patent: November 30, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Jinglan Zhou, Leslie Robinson, Nikolaus M. Gubernator, Eddine Saiah, Xu Bai, Xin Gu
  • Patent number: 6790845
    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
  • Patent number: 6770763
    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
  • Patent number: 6770647
    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.
    Type: Grant
    Filed: August 15, 2002
    Date of Patent: August 3, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: James E. Sheppeck, Jingwu Duan
  • Patent number: 6750225
    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
  • Patent number: 6747158
    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
  • Patent number: 6743807
    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
  • Patent number: 6740649
    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, NR1, and S(O)p, and 0-1 carbonyl groups and the other variables 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, pharmaceutical compositions containing the same, and methods of using the same.
    Type: Grant
    Filed: September 16, 2002
    Date of Patent: May 25, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory R. Ott, Xiao-Tao Chen, Jingwu Duan, Zhonghui Lu
  • Patent number: 6730689
    Abstract: The present application describes N-[4-(1H-imidazol-1-yl)-2-fluorophenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides and derivatives thereof of, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: May 4, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventor: Mimi L. Quan
  • Patent number: 6720329
    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
  • Patent number: 6716841
    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.
    Type: Grant
    Filed: July 26, 2002
    Date of Patent: April 6, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Irina C. Jacobson, Mimi L. Quan
  • Patent number: 6713467
    Abstract: Compounds of formula I and II, or pharmaceutically-acceptable salts thereof, are useful as inhibitors of Factor VIIa, Factor IXa, Factor Xa, Factor FXIa, tryptase, and urokinase, wherein ring B is phenyl or pyridyl, L is a linker, and R1-R27, W, Z1, and Z2 are as defined in the specification.
    Type: Grant
    Filed: November 7, 2001
    Date of Patent: March 30, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory S. Bisacchi, James C. Sutton, Shung C. Wu
  • Patent number: 6710058
    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
  • Patent number: 6706730
    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.
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: March 16, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Donald Joseph Philip Pinto
  • Patent number: 6689771
    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
  • Patent number: 6689770
    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.
    Type: Grant
    Filed: February 12, 2002
    Date of Patent: February 10, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Ruth R. Wexler, Irina C. Jacobson