Exelixis, Inc.

Baili Chen

John M Nuss

Neel Kumar Anand

Tsze Tsang

Kenneth D Rice

Erick Wang Co

Larisa Dubenko

Moon Jung Kim

Wei Xu

Yong Wang

Timothy Patrick Forsyth

Csaba J Peto

James William Leahy

Lynne Canne Bannen

David J Matthews

Vasu Jammalamadaka

Joerg Bussenius

Larry Wayne Mann

Morrison B Mac

Abigail R Kennedy

Ping Huang

Jeff Z Chen

Charles M Blazey

Grace Mann

Longcheng Wang

Simona Costanzo

Tai Phat Huynh

Peter Lamb

Craig Stacy Takeuchi

Richard George Khoury

Owen Joseph Bowles

Jason Jevious Parks

Chris Allen Buhr

Amy Lew Tsuhako

Lisa Esther Dalrymple

Sunghoon Ma

Sergey Epshteyn

Donna Tra Le

Diva Sze-Ming Chan

Steven Charles Defina

Xian Shi

Mohamed Ibrahim

Tae-Gon Baik

Rhett Ronald Klein

Kevin Luke Schnepp

Zerom Tesfai

Nicole Miller

Maurizio Franzini

Tsze H Tsang

Thimothy Patrick Forsyth

Mohamed Abdulkader Ibrahim

Lary Wayne Mann

The present invention relates to compounds of the Formula (I) and (II) wherein R, R, R-R, m, n, X-X, and Qare defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention. 

Kinase modulators and methods of use

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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Palo Alto, CA, United States of America

Baili Chen