Exelixis, Inc.

Robin Tammie Noguchi

James William Leahy

Gary Lee Lewis

Mohamed Ibrahim

John M Nuss

Brian Hugh Ridgway

Sergey Epshteyn

Xian Shi

Matthew A Williams

Timothy Patrick Forsyth

Larry Wayne Mann

Jeff Z Chen

Grace Mann

Patrick C Kearney

Atwood Kim Cheung

Tai Phat Huynh

S David Brown

Joan C Sangalang

Kevin Luke Schnepp

Henry William Beecroft Johnson

Wei Xu

Elena S Koltun

Lynne Canne Bannen

Vasu Jammalamadaka

Naing N Aay

Morrison B Mac

Adam Galan

Richard George Khoury

Craig Stacy Takeuchi

Jason Jevious Parks

Lisa Esther Dalrymple

Wei Cheng

Byung Gyu Kim

Peiwen Zhou

Matthew Sangyup Lee

Arlyn Arcalas

Hongwang Du

Joon Won Jeong

Michael Pack

Wai Ki Vicky Chan

Brian Kane

Lisa E Meyr

John Woolfrey

Lisa Esther Dalrymple Meyr

This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.

Acetanilide sphingosine-1-phosphate receptor antagonists

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

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

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San Bruno, CA, United States of America

Robin Tammie Noguchi