Abstract: Described are RORy modulators of the formula (I), and N-oxides thereof, and pharmaceutically acceptable salts thereof, and solvates and hydrates thereof, wherein R1, R2, R3, R4, R5, R6, Ra, x, y, L, G, Z, the bond denoted by “q”, the ring system denoted by “A” and the ring system denoted by “B” are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORy activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORy activity, for example, autoimmune and/or inflammatory disorders.
Abstract: The present application describes modulators of MIP-1? of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, T, W, R1, R4, R5, R5a and R5b are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using said modulators are disclosed.
Type:
Grant
Filed:
August 5, 2009
Date of Patent:
December 17, 2013
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Percy H. Carter, Cullen L. Cavallaro, George V. De Lucca
Abstract: Provided herein are novel and useful combretastatin A-4 prodrug salts that increase the solubility of combretastatin A-4, readily regenerate combretastatin A-4 in vivo under normal physiological conditions, and which produce physiologically tolerable products as a result of the regeneration of combretastatin A-4.
Type:
Grant
Filed:
March 1, 2006
Date of Patent:
February 9, 2010
Assignee:
Bristol-Myers Squibb Co.
Inventors:
John J. Venit, Mandar V. Dali, Manisha M. Dali, Yande Huang, Charles E. Dahlheim, Ravindra W. Tejwani
Abstract: Provided herein are novel and useful combretastatin A-4 prodrug salts that increase the solubility of combretastatin A-4, readily regenerate combretastatin A-4 in vivo under normal physiological conditions, and which produce physiologically tolerable products as a result of the regeneration of combretastatin A-4.
Type:
Grant
Filed:
March 1, 2006
Date of Patent:
February 9, 2010
Assignee:
Bristol-Myers Squibb Co.
Inventors:
John J. Venit, Mandar V. Dali, Manisha M. Dali, Yande Huang, Charles E. Dahlheim, Ravindra W. Tejwani
Abstract: Provided herein are novel and useful combretastatin A-4 prodrug salts that increase the solubility of combretastatin A-4, readily regenerate combretastatin A-4 in vivo under normal physiological conditions, and which produce physiologically tolerable products as a result of the regeneration of combretastatin A-4.
Type:
Grant
Filed:
March 1, 2006
Date of Patent:
April 28, 2009
Assignee:
Bristol-Myers Squibb Co.
Inventors:
John J. Venit, Mandar V. Dali, Manisha M. Dali, Yande Huang, Charles E. Dahlheim, Ravindra W. Tejwani
Abstract: A method for preparing a compound having the formula: including the steps of: (a) cyclizing a compound of formula II: to form a compound of formula I: (b) deprotecting the nitrogen atom of the compound of formula I by amination or hydrogenation to form compound III.
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: 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: 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, processes for preparing and intermediates thereof.
Type:
Grant
Filed:
October 10, 2006
Date of Patent:
March 4, 2008
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Robert J. Cherney, Percy H. Carter, John V. Duncia, Daniel S. Gardner, Joseph B. Santella
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 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 invention provides imidazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.
Type:
Grant
Filed:
September 1, 2004
Date of Patent:
January 8, 2008
Assignee:
Bristol-Myers Squibb Co.
Inventors:
David S. Weinstein, Khehyong Ngu, Jeffrey A. Robl
Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
Abstract: Isolated nucleic acid and amino acid sequences for phenylalanine aminomutase enzyme and methods for purifying this enzyme are provided. Methods for altering biosynthesis of compounds in plant cell cultures are also provided. In particular, methods for altering production of taxanes and taxane-related compounds are provided.
Type:
Grant
Filed:
February 10, 2003
Date of Patent:
September 25, 2007
Assignee:
Bristol Myers Squibb Co.
Inventors:
Christopher L. Steele, Yijun Chen, Brian A. Dougherty, Sandra Hofstead, Kin S. Lam, Wenying Li, Zizhuo Xing
Abstract: The present invention relates to KCNQ proteins defining potassium channels. In particular, the invention concerns the human KCNQ2, human KCNQ3, murine KCNQ2, and rat KCNQ2 proteins reported herein. KCNQ2 and KCNQ3 proteins are nervous system-selective and may be involved in neurotransmission and neuroprotection. The KCNQ2 and KCNQ3 of the present invention can be used to assay for modulators of the proteins, which would be useful in treatment of such disorders as ataxia, myokymia, seizures, Alzheimer's disease, Parkinson's disease, age-associated memory loss, learning deficiencies, motor neuron diseases, epilepsy, stroke, and the like.
Type:
Grant
Filed:
April 24, 2002
Date of Patent:
August 28, 2007
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Michael A. Blanar, Wen-Pin Yang, Paul C. Levesque, Michael G. Neubauer, Wayne A. Little