Exelixis, Inc.

Symphony Evolution, Inc.

Donna Tra Le

Wei Xu

John M Nuss

Erick Wang Co

Moon Jung Kim

Amy Lew Tsuhako

Vasu Jammalamadaka

Rhett Ronald Klein

Shumeye Mamo

Morrison B Mac

Lynne Canne Bannen

Zhaoyang Wen

Wei Cheng

Amy Lew

Yong Wang

Joerg Bussenius

Michael P Prisbylla

S David Brown

Richard George Khoury

Jason Jevious Parks

Lynne Canne-Bannen

Rickard George Khoury

Neel Kumar Anand

Tsze Tsang

Kenneth D Rice

Ping Huang

Charles M Blazey

Simona Costanzo

Larisa Dubenko

Owen Joseph Bowles

Diva Sze-Ming Chan

Steven Charles Defina

William Bajjalieh

Baili Chen

Lynn Canne Bannen

Moon Hwan Kim

Maurizio Franzini

Ken Rice

Erick W Co

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. Even more specifically, the invention provides compounds for modulating c-Kit kinase activity and methods of treating diseases mediated by c-Kit activity utilizing the compounds and pharmaceutical compositions thereof.

C-kit modulators and methods of use

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, with selectivity versus MMP-1. 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.

Human ADAM-10 inhibitors

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

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San Jose, CA, United States of America

Donna Tra Le