Patent number: 8211929
Abstract: The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR1R1a, or O—R1, wherein X is H, halo, C1-C6 alkyl, NO2, mono-, di-, or tri-halo substituted methyl, NR13R,14.
Type:
Grant
Filed:
December 28, 2005
Date of Patent:
July 3, 2012
Assignee:
Exelixis, Inc.
Inventors:
Jeff Chen, Lisa Esther Dalrymple Meyr, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Mohamed Abdulkader Ibrahim, James W. Leahy, Gary Lee Lewis, Grace Mann, Larry W. Mann, Robin Tammie Noguchi, Brian Hugh Ridgway, Joan Cruz Sangalang, Kevin Luke Schnepp, Xian Shi, Craig Stacy Takeuchi, Matthew Alan Williams, John Nuss, Atwood K. Cheung
Patent number: 7704995
Abstract: This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.
Type:
Grant
Filed:
May 2, 2003
Date of Patent:
April 27, 2010
Assignee:
Exelixis, Inc.
Inventors:
Chris A. Buhr, Tae-Gon Baik, Sunghoon Ma, Zerom Tesfai, Longcheng Wang, Erick Wang Co, Sergey Epshteyn, Abigail R Kennedy, Baili Chen, Larisa Dubenko, Neel Kumar Anand, Tsze H. Tsang, John M. Nuss, Csaba J Peto, Kenneth D. Rice, Mohamed Abdulkader Ibrahim, Kevin Luke Schnepp, Xian Shi, James William Leahy, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Grace Mann, Larry Wayne Mann, Craig Stacy Takeuchi, Peter Lamb, David J. Matthews, Nicole Miller
Publication number: 20080249079
Abstract: The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR1R1a, or O—R1, wherein X is H, halo, C1-C6 alkyl, NO2, mono-, di-, or tri-halo substituted methyl, NR13R,14.
Type:
Application
Filed:
December 28, 2005
Publication date:
October 9, 2008
Applicant:
EXELIXIS, INC.
Inventors:
Jeff Chen, Lisa Esther Dalrymple Meyr, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Mohamed Abdulkader Ibrahim, James W. Leahy, Gary Lee Lewis, Grace Mann, Larry W. Mann, Robin Tammie Noguchi, Brian Hugh Ridgway, Joan Cruz Sangalang, Kevin Luke Schnepp, Xian Shi, Craig Stacy Takeuchi, Matthew Alan Williams, John Nuss, Atwood K. Cheung