Exelixis, Inc.

Kevin Luke Schnepp

John M Nuss

James William Leahy

Mohamed Ibrahim

Xian Shi

Larry Wayne Mann

Sergey Epshteyn

Joan C Sangalang

Matthew A Williams

Timothy Patrick Forsyth

Jeff Z Chen

Grace Mann

Tai Phat Huynh

Atwood Kim Cheung

Craig Stacy Takeuchi

Brian Hugh Ridgway

Lisa Esther Dalrymple

Gary Lee Lewis

Robin Tammie Noguchi

Wei Xu

Neel Kumar Anand

Tsze Tsang

Csaba J Peto

David J Matthews

Kenneth D Rice

Lynne Canne Bannen

Vasu Jammalamadaka

Abigail R Kennedy

Morrison B Mac

Longcheng Wang

S David Brown

Peter Lamb

Larisa Dubenko

Erick Wang Co

Richard George Khoury

Jason Jevious Parks

Chris Allen Buhr

Sunghoon Ma

Tae-Gon Baik

Wei Cheng

Zerom Tesfai

Baili Chen

Nicole Miller

Lisa Esther Dalrymple Meyr

Chris A Buhr

Tsze H Tsang

Larry W Mann

Thimothy Patrick Forsyth

Mohamed Abdulkader Ibrahim

Lary Wayne Mann

Joan Cruz Sangalang

Matthew Alan Williams

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 NRR, or O&#x2014;R, wherein X is H, halo, C-Calkyl, NO, mono-, di-, or tri-halo substituted methyl, NRR,. C(O)O&#x2014;C-Calkyl, or N(R)&#x2014;C(O)&#x2014;C-Calkyl; Y is H, halo, OH, C-Calkyl, C-Calkyl-NR,R, NRR,, C-Calkoxy, &#x2014;N(R)&#x2014;(CH)NRR, &#x2014;C(O)O&#x2014;C-Calkyl, &#x2014;O&#x2014;(CH)&#x2014;NRR, &#x2014;C(O)&#x2014;C-Calkyl, &#x2014;C-C-alkyl-R, &#x2014;O&#x2014;R, &#x2014;C(O)&#x2014;R, &#x2014;O&#x2014;(CH)&#x2014;R, &#x2014;C(O)&#x2014;NRR, &#x2014;C(O)&#x2014;N(R)-aryl, &#x2014;C(O)&#x2014;N(R)(CH)&#x2014;NRR, &#x2014;C(O)&#x2014;N(R)&#x2014;(CH)-aryl &#x2014;C(O)&#x2014;N(R)&#x2014;(CH)-heterocyclyl; or X and Y together with the atoms to which they are attached form a 4-7 membered heterocyclyl or heteroaryl group containing one or two heteroatoms independently selected from O, N, and S. Z is H, NRR, &#x2014;S&#x2014;R, or &#x2014;O&#x2014;R 

Pyrimidine derivatives as kinase modulators and method of use

The present 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 kinases, particularly Tie-2. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.

Tie-2 modulators and methods of use

A compound according to Formula IV: or a pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof, wherein R, R, R, R, Rand X are as defined in the specification.

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.

Protein kinase modulators and methods of use

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Elk Grove, CA, United States of America

Kevin Luke Schnepp