Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's disease.
Type:
Grant
Filed:
April 9, 2008
Date of Patent:
January 1, 2013
Assignee:
Bristol-Myers Squibb Company
Inventors:
Anne Marinier, Marco Dodier, Stephan Roy, Kurt Zimmermann, Xiaopeng Sang, Mark D. Wittman, David R. Langley, Ramkumar Rajamani
Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making them useful as anticancer agents.
Abstract: The present invention provides for tricyclic compounds having the formula (I), wherein R1, R2, R5, R6, R7, and R8 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
Type:
Grant
Filed:
April 23, 2010
Date of Patent:
September 18, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
William J. Pitts, James Kempson, Junqing Guo, Jagabandhu Das, Charles M. Langevine, Steven H. Spergel, Scott Hunter Watterson
Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
Type:
Grant
Filed:
January 28, 2011
Date of Patent:
September 11, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
Mark D. Wittman, Kurt Zimmermann, Xiaopeng Sang
Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit protein kinase activity thereby making them useful as anticancer agents.
Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
Type:
Grant
Filed:
September 2, 2010
Date of Patent:
June 19, 2012
Assignee:
Bristol-Meyers Squibb Company
Inventors:
Ashok V. Purandare, James W. Grebinski, Amy Hart, Jennifer Inghrim, Gretchen Schroeder, Honghe Wan
Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anti-cancer agents and for the treatment of Alzheimer's Disease.
Abstract: The invention relates to 2,4-dibromoropyrrolo[1,2-f][1,2,4]triazine, which is an intermediate useful in preparing 2,4-disubstituted pyrrolotriazine compounds, and a process for preparing the intermediate.
Abstract: The invention provides compounds of formula II: and pharmaceutically acceptable salts thereof. The formula II thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
Type:
Grant
Filed:
December 19, 2007
Date of Patent:
April 3, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
Anne Marinier, Claude A. Quesnelle, Marco Dodier, Stephan Roy, Patrice Gill, Mark D. Wittman, David R. Langley
Abstract: The invention relates to 4-chloro-2-iodopyrrolo[1,2-f][1,2,4]triazine, which is an intermediate useful in preparing 2,4-disubstituted pyrrolotriazine compounds, and a process for preparing said intermediate.
Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making them useful as anticancer agents.
Abstract: Crystalline form, Form N-1, of [(1R),2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester (Compound I) is provided. Also provided are a pharmaceutical composition and an oral dosage form comprising the Form N-1 of Compound I as well as a method of using the Form N-1 of Compound I in the treatment of cancer and other proliferative diseases.
Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
Type:
Grant
Filed:
March 26, 2009
Date of Patent:
February 1, 2011
Assignee:
Bristol-Myers Squibb Company
Inventors:
Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
Abstract: Macrolactams are made by feeding aromatic amino acids as replacement starter units to a mutant strain of the geldanamycin-producing microorganism Streptomyces hygroscopicus var. geldanus NRRL 3602, wherein the gene cluster encoding enzymes for the biosynthesis of the natural starter unit 3-amino-5-hydroxybenzoic acid has been deleted.
Type:
Grant
Filed:
January 23, 2008
Date of Patent:
December 21, 2010
Assignee:
Kosan Biosciences, Inc.
Inventors:
Gary W. Ashley, Hugo Menzella, Janice Lau Wee, John R. Carney
Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents.
Type:
Grant
Filed:
January 4, 2008
Date of Patent:
December 14, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Marco Dodier, Claude A. Quesnelle, Anne Marinier
Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
Type:
Grant
Filed:
September 24, 2008
Date of Patent:
December 7, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
Type:
Grant
Filed:
March 6, 2009
Date of Patent:
October 26, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Rajeev S. Bhide, Zhen-Wei Cai, Ligang Qian, Stephanie Barbosa, Louis Lombardo, Jeffrey Robl
Abstract: The invention relates to an improved process for preparing [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester of the formula: Compound I has been shown to be useful for the treatment of certain types of cancer.
Type:
Grant
Filed:
April 20, 2007
Date of Patent:
March 2, 2010
Assignee:
Britsol-Myers Squibb Company
Inventors:
Gerard A. Crispino, Mourad Hamedi, Thomas L. LaPorte, John E. Thornton, Jaan A. Pesti, Zhongmin Xu, Paul C. Lobben, David K. Leahy, Jale Muslehiddinoglu, Chiajen Lai, Lori Ann Spangler, Robert P. Discordia, Francis S. Gibson
Abstract: The invention relates to 2,4-dichloropyrrolo[1,2-f][1,2,4]triazines, which are intermediates useful in preparing at least one 2,4-disubstituted pyrrolotriazine compound, and at least one method for making such intermediates.
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:
January 23, 2007
Date of Patent:
November 10, 2009
Assignee:
Bristol-Myers Squibb Company
Inventors:
Percy H. Carter, Cullen L. Cavallaro, George V. De Lucca