Constellation Pharmaceuticals, Inc.

C4 Therapeutics, Inc.

Genentech, Inc.

Hoffmann-la Roche Inc.

Boehringer Ingelheim International Gmbh

Genetech, Inc.

F. Hoffmann-la Roche Ag

Martin Duplessis

Christopher G Nasveschuk

Brian K Albrecht

Yanke Liang

James E Audia

Georg Jaeschke

Jean-Christophe P Harmange

Antonio Ricci

Daniel Rueher

Victor S Gehling

Kiel Lazarski

Rishi G Vaswani

Alexander M Taylor

Alexandre Cote

Les A Dakin

Bernd Kuhn

Andrew John Phillips

Steven R Magnuson

Minsheng He

James A Henderson

Annick Goergler

Andrew Cook

Terry Crawford

Sandra Steiner

Chi-Li Chen

Yves LeBlanc

Yvonne Alice Nagel

Andrew Charles Good

F Anthony Romero

Clint A James

Ryan E Michael

Patrick Deroy

Alexander W Hird

Jae Young Ahn

Louis Morency

Christiane Yoakim

Claudio F Sturino

Richard Pastor

Daniel J Burdick

Yong Tang

Jean-Eric Lacoste

Martin Tremblay

Joannie Minville

Sébastien Morin

Juergen Wichmann

Pierre Louis Beaulieu

Ulrike Obst Sander

Bruno Simoneau

Cosimo Dolente

Teddy Halmos

Vickie Hsiao-Wei Tsui

Shumei Wang

Anne-Marie Faucher

James Gillard

Lee Fader

Carl Thibeault

Paul John Edwards

Alexandre Côté

Sylvie Goulet

Sebastien Morin

Alexandre Gagnon

Mathieu Parisien

Eric Malenfant

Oliver Hucke

Katrina L Jackson

Mark E Fitzgerald

David Hewings

Anthony F Romero

Marc Adler

Buelent Kocer

Piergiorgio Francesco Tommaso Pettazzoni

Simon Suprenant

Christopher Lemke

Daniel Hunziker

Daniela Krummenacher

Andrew S Cook

The invention provides compounds that degrade the epidermal growth factor receptor (EGFR) including mutant forms via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The compounds are useful for the treatment of various cancers.

Isoindolinone and indazole compounds for the degradation of EGFR

The present invention provides compounds or their pharmaceutically acceptable salts and their pharmaceutical compositions that can be administered to a host such as a human in need thereof for the treatment of a disorder, such as cancer, mediated by mutant BRAF. The compounds efficiently degrade Class I, II and III mutant BRAF proteins.

Therapeutics for the degradation of mutant BRAF

This invention provides Degronimers that have E3 Ubiquitin Ligase targeting moieties (Degrons) that can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation. The invention also provides Degrons that can be used to treat disorders mediated by cereblon or an Ikaros family protein, and methods of use and compositions thereof as well as methods for their preparation.

N/O-linked degrons and degronimers for protein degradation

The present invention provides compounds which are selective allosteric inhibitors of T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.

Isoindolinone derivatives as selective allosteric inhibitors of Egfr mutant cancers

This invention provides amine-linked C-glutarimide Degronimers for therapeutic applications as described further herein, and methods of use and compositions thereof as well as methods for their preparation, wherein the C-glutarimide Degronimers have the formula:

Substituted piperidine Degronimers for Target Protein degradation

The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.

2-benzopyrazinyl-n-heteroaryl-2-phenyl-acetamide compounds

N/O-linked Degrons and Degronimers for protein degradation

The present invention provides substituted isoindole compounds which are selective allosteric EGFR inhibitors, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances, generally of Formula: or a pharmaceutically acceptable salt thereof.

Substituted isoindole allosteric EGFR inhibitors

Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with LSD1. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with LSD1.

LSD1 inhibitors and uses thereof

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.

Growing community of inventors

Somerville, MA, United States of America

Martin Duplessis