Exelixis, Inc.

Exelixis Patent Company LLC

Wyeth

Brian Hugh Ridgway

James William Leahy

Timothy Patrick Forsyth

Jeff Z Chen

Grace Mann

Tai Phat Huynh

Sergey Epshteyn

Craig Stacy Takeuchi

Gary Lee Lewis

Joan C Sangalang

Xian Shi

Matthew Sangyup Lee

Morrison B Mac

Byung Gyu Kim

Yong Wang

Larry Wayne Mann

Mohamed Ibrahim

Charles K Marlowe

William Bajjalieh

Robin Tammie Noguchi

Suleyman Bahceci

Amedeo A Failli

Matthew A Williams

John M Nuss

Patrick C Kearney

S David Brown

Atwood Kim Cheung

William Jay Moore

Adam Galan

Lisa Esther Dalrymple

Hongwang Du

Peiwen Zhou

Kevin Luke Schnepp

Henry William Beecroft Johnson

Wei Xu

Mark Anthony Ashwell

Elena S Koltun

Lynne Canne Bannen

Naing N Aay

Vasu Jammalamadaka

Madelene M Antane

William Ronald Solvibile

Richard George Khoury

Jason Jevious Parks

Albert John Molinari

Wei Cheng

Arlyn Arcalas

Molly Hoke

Wai Ki Vicky Chan

Michael Pack

Brian Kane

Lisa E Meyr

John Woolfrey

Lisa Esther Dalrymple Meyr

Amy Tsai-Ting Lee

Mark Antony Ashwell

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

This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention.

JAK-2 modulators and methods of use

Synthetic methods are provided for production of compounds of the formula: where R, R, R, R, R, R, R, R, R, R, R, R, Rand Rare as defined in the specification.

Processes for preparing 6-alkyl-5-arylsulfonyl-dihydrophenanthridines

This invention provides a compound of formulae (I) or (II) having the structureor a pharmaceutically acceptable salt thereof which are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflammatory bowel disease, arthritis, type II diabetes, and autoimmune diseases such as multiple sclerosis and rheumatiod arthritis.

Substituted dihydrophenanthridinesulfonamides

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Belmont, CA, United States of America

Brian Hugh Ridgway