Exelixis, Inc.

Symphony Evolution, Inc.

Rhett Ronald Klein

Wei Xu

John M Nuss

Erick Wang Co

Donna Tra Le

Moon Jung Kim

Amy Lew Tsuhako

Wei Cheng

Yong Wang

Joerg Bussenius

Jason Jevious Parks

Neel Kumar Anand

Tsze Tsang

Kenneth D Rice

Lynne Canne Bannen

Vasu Jammalamadaka

Ping Huang

Morrison B Mac

Charles M Blazey

Simona Costanzo

Richard George Khoury

Larisa Dubenko

Owen Joseph Bowles

Diva Sze-Ming Chan

Steven Charles Defina

Zhaoyang Wen

William Bajjalieh

Amy Lew

Baili Chen

Maurizio Franzini

Ken Rice

Lynn Canne Bannen

Moon Hwan Kim

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

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

Growing community of inventors

Chicago, IL, United States of America

Rhett Ronald Klein