Exelixis, Inc.

Symphony Evolution, Inc.

Amy Lew Tsuhako

Moon Jung Kim

Wei Xu

John M Nuss

Erick Wang Co

Donna Tra Le

Joerg Bussenius

Rhett Ronald Klein

Neel Kumar Anand

Elena S Koltun

Tsze Tsang

Kenneth D Rice

Vasu Jammalamadaka

Morrison B Mac

Ping Huang

Charles M Blazey

Patrick C Kearney

S David Brown

Hongwang Du

Peiwen Zhou

Wai Ki Vicky Chan

Yong Wang

Csaba J Peto

Naing N Aay

Shumeye Mamo

Michael P Prisbylla

Jean-Claire Limun Manalo

Larisa Dubenko

Jason Jevious Parks

Owen Joseph Bowles

Cristiana A Zaharia

Jeffry Kimo Curtis

Steven Charles Defina

Wei Cheng

Arlyn Arcalas

Michael Pack

Brian Kane

Lynne Canne-Bannen

Rickard George Khoury

Lynne Canne Bannen

Abigail R Kennedy

Simona Costanzo

Richard George Khoury

Angie Inyoung Kim

Chris Allen Buhr

Sunghoon Ma

Diva Sze-Ming Chan

Sergey Epshteyn

Mohamed Ibrahim

Zhaoyang Wen

Anagha Abhijit Joshi

Eileen E Jackson-Ugueto

Baili Chen

Jason R Harris

Stephanie Ng

Maurizio Franzini

Ken Rice

Lynn Canne Bannen

Moon Hwan Kim

Patrick Kearney

Tsze H Tsang

Mohamed Abdulkader Ibrahim

Adam Antoni Galan

Steven James Richards

The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.

Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture

A compound having Formula I: or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Formula I are inhibitors of Casein kinase II (CK2) pathways. 

Pyrimidinones as casein kinase II (CK2) modulators

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

6-phenylpyrimidinones as PIM modulators

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 relates to compounds of the Formula (I) and (II) wherein R, R, R-R, m, n, X-X, and Qare defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention. 

Kinase modulators and methods of use

The invention provides compounds of formula (I) and methods for inhibition of kinases, more specifically p70S6 kinases, and more preferably p70S6, Akt-1 and Akt-2 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. 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. 

[1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases

The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.

Human adam-10 inhibitors

Compounds of formula III: wherein R, R, X, Y, Q, Rand Rare as defined in the specification, pharmaceutically acceptable salts thereof, and methods of use thereof.

P70S6 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. More specifically, the invention provides oxindole derivatives which inhibit, regulate and/or modulate kinase receptor, particularly VEGF receptor 2 (Flk-1/KDR), FGFR1, and PDGFR (alpha and beta), signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.

Substituted 3-(diarylmethylene)indolin-2-ones and methods of their use

Human ADAM-10 inhibitors

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Milpitas, CA, United States of America

Amy Lew Tsuhako