Abstract: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
Abstract: The invention is directed to the family of aggrecan degrading metallo proteases (ADMPs) that exhibit the ability to cleave the aggrecan core protein between amino acid residues Glu373-Ala374. The invention encompasses the nucleic acids encoding such enzymes, processes for production of recombinant ADMPs, compositions containing such enzymes, and the use of these enzymes in various assays and for the development of novel inhibitors for use as therapies for diseases involving aggrecanase-mediated degradation of cartilage or other aggrecanase-associated diseases.
Type:
Grant
Filed:
August 9, 2000
Date of Patent:
May 23, 2006
Assignee:
Bristol-Myers Squibb Pharma Comp.
Inventors:
Elizabeth C. Arner, Timothy C. Burn, Robert A. Copeland, Carl P. Decicco, Ruiqin Liu, Ronald Magolda, Michael Pratta, Kimberly A. Solomon, Micky D. Tortorella, James M. Trzaskos, Fude Yang
Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.
Abstract: The present invention relates to pyrazolotriazines according to formula (I) and stereoisomers, isomers and salts thereof wherein R1-R5 are selected from certain alkyl, aryl and heteroaryl species as defined in the specification wherein all of the compounds are useful as CRF antagonists and are thus useful in the treatment of neurological disorders as well as a multitude of other CRF associated diseases or conditions.
Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.
Type:
Grant
Filed:
October 26, 2002
Date of Patent:
March 28, 2006
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Thomas D. Harris, John A. Barrett, Alan P. Carpenter, Jr., Milind Rajopadhye
Abstract: The present invention relates to 1,3-benzodiazepin-2-ones and 1,3-benzoxazepin-2-ones of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P—M—M4I 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:
October 21, 2004
Date of Patent:
February 28, 2006
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Donald J. P. Pinto, Michael J. Orwat, Patrick Y. S. Lam
Abstract: The present application describes 6–5, 6—6, or 6–7 heterobicycles of Formula I or pharmaceutically acceptable salt forms thereof: wherein ring P is a 6-membered heteroaromatic and ring M is a 5-, 6-, or 7-membered non-aromatic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
Abstract: Low density microspheres, methods for preparing same, and use of same as contrast agents are described. The microspheres have a void having a volume that comprises at least about 75% of the total volume of the microspheres, and which contains a gas or the vapor of a volatile liquid selected from the group consisting of aliphatic hydrocarbons, chlorofluorocarbons, tetraalkyl silanes and perfluorocarbons.
Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4-P-M-M4 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:
October 21, 2004
Date of Patent:
February 7, 2006
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: Antibodies directed against an antigenic determinant of high molecular weight kininogen domain 5, particularly a determinant located in the region formed by light chain amino acids Gly(440) to Lys(502), inhibit angiogenesis.
Type:
Grant
Filed:
November 10, 2000
Date of Patent:
February 7, 2006
Assignees:
Temple University-of the Commonwealth System of Higher Education, Bristol-Myers Squibb Pharma Company
Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??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:
May 20, 2004
Date of Patent:
January 24, 2006
Assignee:
Bristol-Myers-Squibb Pharma Company
Inventors:
Donald J. P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Jennifer X. Qiao, Patrick Y. S. Lam, Stephanie L. Koch
Abstract: Thus the present invention describes novel compounds comprising 1-10 targeting moieties; a chelator (Ch); and 0-1 linking groups (Ln) between the targeting moiety and chelator; wherein the targeting moiety is a matrix metalloproteinase inhibitor; and wherein the chelator is capable of conjugating to a cytotoxic radioisotope. The present invention also provides novel compositions of the compounds of the invention, kits and their uses in treatment of diseases associated with MMPs.
Type:
Grant
Filed:
February 14, 2001
Date of Patent:
January 24, 2006
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Carl P. Decicco, David J. Nelson, John A. Barrett, Alan P. Carpenter Jr., Jingwu Duan, Milind Rajopadhye
Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
Type:
Grant
Filed:
August 7, 2003
Date of Patent:
January 10, 2006
Assignee:
Bristol-Myers Squibb Pharma, Company
Inventors:
John V. Duncia, Joseph B. Santella, Dean A. Wacker, Wenqing Yao, Changsheng Zheng
Abstract: The present application describes novel cyclic ?-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-? inhibitors.
Type:
Grant
Filed:
February 13, 2004
Date of Patent:
January 10, 2006
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Zhonghui Lu, Thomas P. Maduskuie, Jr., Matthew E. Voss, Chu-Biao Xue, Jingwu Duan, Gregory Ott, Lihua Chen, Carl Decicco
Abstract: Thus the present invention describes diagnostic agents comprising a diagnostic metal and a compound, wherein the compound comprises: 1-10 targeting moieties; a chelator; and 0-1 linking groups between the targeting moiety and chelator; wherein the targeting moiety is a matrix metalloproteinase inhibitor; and wherein the chelator is capable of conjugating to the diagnostic metal. The present invention also provides novel compositions of the compounds of the invention, kits, and their uses in diagnosis of diseases associated with MMPs.
Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
Abstract: Detectably labeled macrophage scavenger receptor antagonists useful for the diagnosis and monitoring of various cardiovascular diseases including but not limited to atherosclerosis, vulnerable plaque, coronary artery disease, renal disease, thrombosis, transient ischemia due to clotting, stroke, myocardial infarction, organ transplant, organ failure and hypercholesterolemia.
Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
Abstract: The present invention relates to tricyclic 2-pyridone compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
Type:
Grant
Filed:
June 10, 2003
Date of Patent:
November 29, 2005
Assignee:
Bristol-Myers Squibb Pharma
Inventors:
James D. Rodgers, Haisheng Wang, Mona Patel, Argyrios Arvanitis, Anthony J. Cocuzza