Constellation Pharmaceuticals, Inc.

Genentech, Inc.

Relay Therapeutics, Inc.

D.e. Shaw Research, LLC

Genetech, Inc.

Alexander M Taylor

Brian K Albrecht

Christopher G Nasveschuk

Alexandre Cote

Steven R Magnuson

Fabrizio Giordanetto

F Anthony Romero

Michael Charles Hewitt

Victor S Gehling

Terry Crawford

Vickie Hsiao-Wei Tsui

W Patrick Walters

Yves LeBlanc

Jean-Christophe P Harmange

Mark Andrew Murcko

André Lescarbeau

Eric Therrien

Martin Duplessis

Richard Pastor

Rishi G Vaswani

Daniel J Burdick

Elizabeth Helen Kelley

Kelley C Shortsleeves

Jack Benjamin Greisman

Andrew Charles Good

Jeremy M Murray

Sarah Bronner

James Richard Kiefer, Jr

Yong Tang

James E Audia

Alexandre Côté

Paul Maragakis

Yves Leblanc

Steven F Bellon

Shumei Wang

Thomas H McLean

Les A Dakin

Sathesh P Bhat

Markus Kristofer Dahlgren

Jun Liang

Kevin X Chen

Lucian V DiPietro

Hakan Gunaydin

Kwong Wah Lai

James Richard Jr Kiefer

Levi Charles Thomas Pierce

Anthony F Romero

Bing-Yan Zhu

Fei Wang

Jing Wang

Birong Zhang

Steven Elliot Kauder

Patrick Cyr

Jiangpeng Liao

Heike Schoenherr

Demetri T Moustakas

Brandi M Hudson

Alessandro Boezio

Mary M Mader

Yanyan Zhang

Jackson G Egen

Marc Adler

Bakary-Barry Touré

Christopher G Nasveschuck

Gaodeng Lian

Dina A Sharon

Ravi Kurukulasuriya

Pelin Ayaz

Thomas H Mclean

Markus Kristofer Dahlgeren

Kevin Chen

Jean-Christophe Harmange

Michael C Hewitt

The present disclosure relates to novel compounds of formula I-1, and pharmaceutical compositions thereof, and methods for inhibiting the activity of FGFR 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 FGFR signaling with the compounds and compositions of the disclosure.

FGFR inhibitors and methods of use thereof

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 SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.

Pyrazolo[3,4-b]pyrazine SHP2 phosphatase inhibitors and methods of use thereof

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

Cellular biological activities are tightly controlled by intracellular signaling processes initiated by extracellular signals. Protein tyrosine phosphatases, which remove phosphate groups from tyrosine phosphorylated signaling molecules, play equally important tyrosine roles as protein kinases in signal transduction. SHP-2, a cytoplasmic SH2 domain containing protein tyrosine phosphatase, is involved in the signaling pathways of a variety of growth factors and cytokines. Recent studies have clearly demonstrated that this phosphatase plays an important role in transducing signal relay from the cell surface to the nucleus, and is a critical intracellular regulator in mediating cell proliferation and differentiation.

Pyrazolo[3,4-b]pyrazine derivatives as SHP2 phosphatase inhibitors

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 invention relates to novel compounds having the general formula: 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 suppressing tumor cell growth, ameliorating the pathogenesis of systemic lupus erythematosus, and the treatment of various other disorders, including Noonan syndrome, diabetes, neutropenia, neuroblastoma, melanoma, juvenile leukemia, juvenile myelomonocytic leukemia, chronic myelomonocytic leukemia, acute myeloid leukemia, and other cancers associated with SHP2 deregulation with the compounds and compositions of the invention, alone or in combination with other treatments. Other cancers associated with SHP2 deregulation include HER2-positive breast cancer, triple-negative breast cancer, ductal carcinoma of the breast, invasive ductal carcinoma of the breast, non-small cell lung cancer, esophageal cancer, gastric cancer, squamous-cell carcinoma of the head and neck (SCCHN), and colon cancer.

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 relates to methods for treating PCAF mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R, R-R, X, and each Rhave any of the values defined in the specification. Also included are novel compounds of formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

Therapeutic compounds and uses thereof

The present invention relates to compounds of formula (I): and salts thereof, wherein: R-Rhave any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of BRG1, BRM and/or PB1. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various BRG1-mediated disorders, BRM-mediated disorders and/or PB1-mediated disorders.

Provided herein are compounds of formula I: and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.

The present invention relates to compounds useful as inhibitors of one or more histone demethylses, such as KDM2b. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

The present invention relates to compounds of formula (I): and to salts thereof, wherein R, R, R, and Rhave any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.

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Cambridge, MA, United States of America

Alexander M Taylor