Exelixis, Inc.

Exelixis Patent Company LLC

Sergey Epshteyn

James William Leahy

Timothy Patrick Forsyth

Jeff Z Chen

Grace Mann

Tai Phat Huynh

Brian Hugh Ridgway

Xian Shi

Craig Stacy Takeuchi

Gary Lee Lewis

Joan C Sangalang

Mohamed Ibrahim

Larry Wayne Mann

Morrison B Mac

Byung Gyu Kim

Matthew Sangyup Lee

John M Nuss

Yong Wang

Lisa Esther Dalrymple

Charles K Marlowe

William Bajjalieh

Robin Tammie Noguchi

Kevin Luke Schnepp

Suleyman Bahceci

Matthew A Williams

Neel Kumar Anand

Elena S Koltun

Csaba J Peto

Tsze Tsang

Kenneth D Rice

Abigail R Kennedy

S David Brown

Patrick C Kearney

Atwood Kim Cheung

Arlyn Arcalas

Hongwang Du

Peiwen Zhou

Wai Ki Vicky Chan

Moon Jung Kim

Wei Xu

David J Matthews

Lynne Canne Bannen

Vasu Jammalamadaka

Joerg Bussenius

Naing N Aay

Charles M Blazey

Longcheng Wang

Peter Lamb

Adam Galan

Larisa Dubenko

Erick Wang Co

Jean-Claire Limun Manalo

Richard George Khoury

Chris Allen Buhr

Jason Jevious Parks

Sunghoon Ma

Amy Lew Tsuhako

Tae-Gon Baik

Wei Cheng

Zerom Tesfai

Michael Pack

Henry William Beecroft Johnson

Brian Kane

Baili Chen

Lisa E Meyr

John Woolfrey

Lisa Esther Dalrymple Meyr

Nicole Miller

The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.

Inhibitors of the hedgehog pathway

This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R, R, R, and n1 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof.

4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as JAK-2 modulators and methods of use

Inhibitors of hedgehog pathway

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 having Formula (I) or a pharmaceutically acceptable salt thereof, wherein X, Rand Rare defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. 

Pyrimidinones as Casein Kinase II (CK2) modulators

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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Fremont, CA, United States of America

Sergey Epshteyn