Abstract: A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I): where X is S, O or N; Z is —T—COOR1 or —T—COR1; and T, R, R1, Ra, Rb, Rc, Rd, Z, A and B are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
Type:
Grant
Filed:
January 12, 2006
Date of Patent:
August 12, 2008
Assignee:
Bristol-Myers Squibb Company
Inventors:
Bingwei V. Yang, Lidia M. Doweyko, Arthur M. Doweyko
Abstract: The present invention relates to compounds having the formula, and pharmaceutically-acceptable salts, prodrugs, solvates, isomers, and/or hydrates thereof, wherein Q is an optionally-substituted pyridyl, ring; R2 is alkyl or an amino group as defined herein; and Z is optionally-substituted C(?O)NR6, wherein R6 is lower alkyl or cyclopropyl. The compounds are surprisingly advantageous in preparing pharmaceutical compositions for treating p38 kinase related conditions and/or in methods of treating conditions associated with the activity of p38 kinase in a patient.
Type:
Grant
Filed:
May 3, 2004
Date of Patent:
July 8, 2008
Assignee:
Bristol-Myers Squibb Company
Inventors:
Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Rulin Zhao, Bang-Chi Chen, Stephen T. Wrobleski
Abstract: Fused heterocylic compounds of the following Formula wherein R1, R2, R5, Z, J1 and J2 are described herein, and analogs thereof are provided which are useful in treating leukocyte activation-associated disorders.
Type:
Grant
Filed:
November 6, 2003
Date of Patent:
June 10, 2008
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Joseph Barbosa, William J. Pitts, Junqing Guo
Abstract: Pyrrolizine compounds having the formula (I), or pharmaceutically-acceptable salts thereof, are effective in treating inflammatory or immune diseases, where A is a four- to seven-membered saturated ring, K is O or S, and R1, R2, R3 n, and M are defined in the specification.
Type:
Grant
Filed:
August 18, 2005
Date of Patent:
May 20, 2008
Assignees:
Bristol-Myers Squibb Company, Cerep SA
Inventors:
T. G. Murali Dhar, Dharmpal S. Dodd, Dominique Potin, Michele Launay
Abstract: The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory- and immune-associated diseases, and have the structure including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein X is selected from N, O, and S; Y is N or CR6; Z is a ring; and where R, Ra, Rb, Rc, Rd, R1, R2, R3, R4, and R5 are as defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising such compounds.
Type:
Grant
Filed:
January 12, 2006
Date of Patent:
April 22, 2008
Assignee:
Bristol-Myers Squibb Co.
Inventors:
James Sheppeck, T. G. Murali Dhar, Lidia Doweyko, John Gilmore, David Weinstein, Hai-Yun Xiao, Bingwei V. Yang, Arthur M. Doweyko
Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) its stereoisomers thereof, or a solvate thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR1R2 or CH2NR1R2 and where R, R?, Ra, Rb, Rc, Rd, Z, A and B are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
Abstract: The invention relates to a class of novel non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein Z, R, R4, R5, Ra, Rb, Rc, and Rd, are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
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: 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: A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) its stereoisomers thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof, where Z is S, O or NH; and R, R1, R2 Ra, Rb, Rc, Rd, Z, A and B are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein B, J, K, Z, R, Ra, Rb, Rc, Rd, Rq, Rw, m and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
Type:
Grant
Filed:
January 13, 2005
Date of Patent:
August 7, 2007
Assignee:
Bristol-Myers Squibb Company
Inventors:
David S. Weinstein, John L. Gilmore, James Sheppeck, Bingwei Vera Yang, Soong-Hoon Kim, Wayne Vaccaro
Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where R1–R9, X, Y and Z are defined herein.
Type:
Grant
Filed:
June 10, 2004
Date of Patent:
June 26, 2007
Assignee:
Bristol-Myers Squibb Company
Inventors:
Sara Sabine Hadida-Ruah, Xiaohui He, Johnny Yasuo Nagasawa
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: The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5?-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.
Type:
Grant
Filed:
June 19, 2003
Date of Patent:
April 17, 2007
Assignee:
Bristol-Myers Squibb Company
Inventors:
Henry H. Gu, T. G. Murali Dhar, Edwin J. Iwanowicz
Abstract: The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K and L are independently, O or S; Q is —C(?O)— or optionally substituted C1-6alkylene; Ar is optionally-substituted aryl or heteroaryl; J1, J2, J3 and Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; R1 is N or C(R9); and R2, and R3, are as defined in the specification.
Type:
Grant
Filed:
October 1, 2004
Date of Patent:
April 3, 2007
Assignees:
Bristol-Myers Squibb Company, Cerep SA
Inventors:
T. G. Murali Dhar, Edwin Iwanowicz, Michele Launay, Dominique Potin, Magali Jeannine Blandine Maillet, Eric Nicolai
Abstract: A class of substituted spiro-hydantoin compounds (II) having the formula: its pharmaceutically acceptable salts, enantiomers, solvates, or prodrugs thereof, wherein R16 is a substituted pyridinyl group, as defined herein, is provided. Pharmaceutical compositions and methods of treating anti-inflammatory and/or immune diseases with the pyridyl-substituted spiro-hydantoin compounds are also objectives of this invention.
Type:
Grant
Filed:
December 13, 2005
Date of Patent:
March 6, 2007
Assignee:
Bristol-Myers Squibb Company
Inventors:
T. G. Murali Dhar, Michele Launay, Dominique Potin, Scott Hunter Watterson, Zili Xiao
Abstract: Compounds having the formula, enantiomers, diastereomers, solvates and salts thereof, where R1, R2, R3, R4, A, X, and J are described herein, are inhibitors of calcium channel function, and are useful in treating calcium channel-dependent disorders, including hypertension.
Type:
Grant
Filed:
July 22, 2004
Date of Patent:
January 23, 2007
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Natesan Murugesan, Gregory S. Bisacchi, William R. Ewing, Guixue Yu, Zhengxiang Gu, Todd Friends, Minsheng Zhang
Abstract: The present invention relates to substituted dihydropyrimidine inhibitors of calcium channel function having formula I where A, a, J, R1, R2 R3, R4, and R5, are defined herein; pharmaceutical compositions comprising said compounds; and methods of treating calcium channel-dependent disorders, including hypertension.
Type:
Grant
Filed:
July 23, 2004
Date of Patent:
January 2, 2007
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Natesan Murugesan, Gergory S. Bisacchi, William R. Ewing, Zhengxiang Gu
Abstract: Acyl guanidine compounds of the following Formula wherein R1, R2, R3, R4 and L are described herein, and pharmaceutical compositions thereof, are useful in treating leukocyte activation-associated disorders.