Relay Therapeutics, Inc.

D.e. Shaw Research, LLC

Eisai R&d Management Co., Ltd.

Eisai Company, Limited

André Lescarbeau

Alexander M Taylor

Fabrizio Giordanetto

Kelley C Shortsleeves

Mark Andrew Murcko

Elizabeth Helen Kelley

W Patrick Walters

Eric Therrien

Toshihiko Kaneko

Mark Spyvee

Seiichi Kobayashi

Kenzo Muramoto

Kouichi Kikuchi

Motohiro Soejima

Ieharu Hishinuma

Boris M Seletsky

Heather Davis

Yimin Jiang

Thomas H McLean

Wanjun Zheng

Norihito Ohi

Xiang-Yi Li

Fabian Gusovsky

Bruce Decosta

Hiromitsu Yokohama

Marc Pesant

Ye Yao

Yan (Janet) Zhao

Jane Daun

Lynda Tremblay

Lucian V DiPietro

Hakan Gunaydin

Sathesh P Bhat

Markus Kristofer Dahlgren

Paul Maragakis

Jack Benjamin Greisman

Levi Charles Thomas Pierce

Jing Wang

Osama Suleiman

Yong Tang

Alexandre Larivée

Yanyan Zhang

Lucian V Dipietro

Zoe Prentice

Alessandro Boezio

Thomas Kendall

Jethro Beamish-cook

Aaron Dumas

Elisabeth Isaak

Piera Trinchera

Oleksandr Zhurakovskyi

Gaodeng Lian

Hanmo Zhang

Thomas H Mclean

Markus Kristofer Dahlgeren

The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.

SHP2 phosphatase inhibitors and methods of use thereof

The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K-α enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K-α signaling with the compounds and compositions of the disclosure.

Substituted isoindolines as PI3K-alpha inhibitors

The disclosure is in part directed to crystalline forms of N-(4-(4-amino-5-(3-fluoro-4-((4-methylpyrimidin-2-yl)oxy)phenyl)-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl)phenyl)methacrylamide represented by the following structure: its salts, its cocrystals, and variants thereof.

FGFR inhibitors and methods of making and using the same

The disclosure is in part directed to crystalline forms of (R)-1′-(3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-3H-spiro[benzofuran-2,4′-piperidin]-3-amine, its salt, and variants thereof.

SHP2 phosphatase inhibitors and methods of making and using the same

The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the invention. The present invention further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds ad compositions of the invention.

The present disclosure relates to compounds of formula (I) and pharmaceutical compositions thereof and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure. 

Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors

The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.

The present invention provides compounds having formula (I): 

Deazapurines and uses thereof

As discussed above, there remains a need for the development of novel therapeutic agents useful for treating inflammatory or autoimmune and proliferative diseases. The present invention provides novel compounds of general formula (I), and pharmaceutical compositions thereof, as described generally and in classes and subclasses herein, as well as methods of making and using such compounds.

The present invention provides compounds having formula (I), wherein R, R, Rand n are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of inflammatory or autoimmune and proliferative disorders and as inhibitors of cell adhesion molecule expression and inflammatory cytokine signal transduction generally 

Growing community of inventors

Somerville, MA, United States of America

André Lescarbeau