Exelixis, Inc.

Exelixis Patent Company LLC

Joan C Sangalang

James William Leahy

Brian Hugh Ridgway

Sergey Epshteyn

Xian Shi

Gary Lee Lewis

Timothy Patrick Forsyth

Jeff Z Chen

Grace Mann

Tai Phat Huynh

Craig Stacy Takeuchi

John M Nuss

Morrison B Mac

Yong Wang

Larry Wayne Mann

Mohamed Ibrahim

Charles K Marlowe

Byung Gyu Kim

William Bajjalieh

Matthew Sangyup Lee

Kevin Luke Schnepp

Suleyman Bahceci

Matthew A Williams

Atwood Kim Cheung

Lisa Esther Dalrymple

Robin Tammie Noguchi

Wei Xu

Lynne Canne Bannen

Vasu Jammalamadaka

S David Brown

Richard George Khoury

Jason Jevious Parks

Wei Cheng

Lisa Esther Dalrymple Meyr

Brain Hugh Ridgway

Larry W Mann

Craig Takeuchi

Tai Huynh

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

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

The present invention relates to compounds of the Formula I, wherein L, X, Y, Z, R, R, Rand Rare defined herein. The invention also provides methods of using the compounds for inhibition of kinases, more specifically ALK kinases. 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; (Formula I). 

Anaplastic lymphoma kinase 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.

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Mountain View, CA, United States of America

Joan C Sangalang