Exelixis, Inc.

Mei Pharma, Inc.

S David Brown

Wei Xu

David J Matthews

John M Nuss

Morrison B Mac

Patrick C Kearney

Moon Jung Kim

Elena S Koltun

Lynne Canne Bannen

Vasu Jammalamadaka

Amy Lew Tsuhako

Yong Wang

James William Leahy

Naing N Aay

Shumeye Mamo

Michael P Prisbylla

Erick Wang Co

Brian Hugh Ridgway

Sergey Epshteyn

Donna Tra Le

Xian Shi

Gary Lee Lewis

Mohamed Ibrahim

Charles K Marlowe

William Bajjalieh

Hongwang Du

Peiwen Zhou

Robin Tammie Noguchi

Michael Pack

Wai Ki Vicky Chan

Zerom Tesfai

Brian Kane

Lynne Canne-Bannen

Rickard George Khoury

Matthew A Williams

Timothy Patrick Forsyth

Larry Wayne Mann

Jeff Z Chen

Ping Huang

Grace Mann

Atwood Kim Cheung

Tai Phat Huynh

Adam Galan

Richard George Khoury

Jason Jevious Parks

Cristiana A Zaharia

Lisa Esther Dalrymple

Joan C Sangalang

Byung Gyu Kim

Wei Cheng

Arlyn Arcalas

Matthew Sangyup Lee

Adam Antoni Galan

Kevin Luke Schnepp

Henry William Beecroft Johnson

Maurizio Franzini

John Woolfrey

Lisa E Meyr

Moon Hwan Kim

Patrick Kearney

Steven James Richards

Provided herein are (alpha-substituted aralkylamino or heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.

(Alpha-substituted aralkylamino and heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, pharmaceutical compositions thereof, and their use in treating proliferative diseases

Provided herein are (alpha-substituted aralkylamino or heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases. 

The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.

Phosphatidylinositol 3-kinase inhibitors and methods of their use

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

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

Compounds of formula (I), useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R, R, Q, X and Rare as defined above. Pharmaceutical compositions and methods of treating diseases and conditions, such as cancer, are also disclosed. 

Pyridopyrimidinone inhibitors of PIM-1 and/or PIM-3

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

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

Human ADAM-10 inhibitors

Growing community of inventors

San Carlos, CA, United States of America

S David Brown