Exelixis, Inc.

University of Michigan

Mohamed Ibrahim

James William Leahy

John M Nuss

Sergey Epshteyn

Xian Shi

Gary Lee Lewis

Robin Tammie Noguchi

Kevin Luke Schnepp

Timothy Patrick Forsyth

Larry Wayne Mann

Jeff Z Chen

Grace Mann

Patrick C Kearney

Tai Phat Huynh

Brian Hugh Ridgway

Joan C Sangalang

Matthew A Williams

Neel Kumar Anand

Elena S Koltun

Csaba J Peto

Tsze Tsang

Kenneth D Rice

Abigail R Kennedy

Atwood Kim Cheung

S David Brown

Craig Stacy Takeuchi

Lisa Esther Dalrymple

Arlyn Arcalas

Hongwang Du

Peiwen Zhou

Wai Ki Vicky Chan

Henry William Beecroft Johnson

Moon Jung Kim

Wei Xu

Jolanta Grembecka

Tomasz Cierpicki

Duxin Sun

Lynne Canne Bannen

David J Matthews

Kevin Lloyd Greenman

Vasu Jammalamadaka

Joerg Bussenius

Naing N Aay

Dmitry Borkin

Morrison B Mac

Charles M Blazey

Longcheng Wang

Peter Lamb

Richard George Khoury

Jean-Claire Limun Manalo

Larisa Dubenko

Erick Wang Co

Adam Galan

Chris Allen Buhr

Jason Jevious Parks

Amy Lew Tsuhako

Sunghoon Ma

Xiaoqin Li

Wei Cheng

Byung Gyu Kim

Tae-Gon Baik

Jay L Hess

Matthew Sangyup Lee

Zerom Tesfai

Joon Won Jeong

Michael Pack

Brian Kane

Baili Chen

Nicole Miller

Artem Plekhov

Lisa E Meyr

John Woolfrey

Lisa Esther Dalrymple Meyr

The present disclosure relates generally to thienopyrimidine and thienopyridine compounds and methods of use thereof. In particular embodiments, the present disclosure provides compositions comprising thienopyrimidine and thienopyridine compounds of Formula 3: and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins.

Compositions comprising thienopyrimidine and thienopyridine compounds and methods of use thereof

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

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

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 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.

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

Growing community of inventors

Mountain View, CA, United States of America

Mohamed Ibrahim