Hoffmann-la Roche Inc.

C4 Therapeutics, Inc.

F. Hoffmann-la Roche Ag

Daniel Rueher

Georg Jaeschke

Antonio Ricci

Eric Vieira

Lothar Lindemann

Heinz Stadler

Wolfgang Guba

Barbara Biemans

Synese Jolidon

Fionn O'Hara

Martin Duplessis

Bernd Kuhn

Yanke Liang

Luke Green

Kiel Lazarski

Annick Goergler

Sandra Steiner

Yvonne Alice Nagel

Christopher G Nasveschuk

Jean-Marc Plancher

Ryan E Michael

Alexander W Hird

Jae Young Ahn

Rainer Eugen Martin

Cosimo Dolente

David Hewings

Christa Ulrike Obst-sander

Ulrike Obst Sander

Buelent Kocer

Fionn O`hara

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 application relates to (106) specific heterocyclic compounds comprising a thiazole ring, an indazol and a 6,7-dihydro-5H-pyrrolo[1,2-c]imidazole system, to pharmaceutical compositions containing them and their medical use. The compounds are described as selective allosteric inhibitors of T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S containing EGFR mutants and thus useful for the treatment of cancer, in particular non-small cell lung cancer.

EGFR inhibitors for the treatment of cancer

The application relates to a compound of formula (I) containing a thiazole ring, an indazol ring and a 6,7-dihydro-5H-pyrrolo[1,2-c]imidazole ring system, to pharmaceutical compositions containing it and its medical use. The compounds are described as selective allosteric inhibitors of T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S containing EGFR mutants and thus useful for the treatment of cancer, in particular non-small cell lung cancer.

EGFR inhibitor for the treatment of cancer

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

The present invention relates to compounds that may be used in the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression or diabetes type 2.

Ethynyl derivatives

The present invention relates to positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) that may be used for the treatment of conditions such as Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.

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

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

The present invention relates to compounds that may be used for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2. Compounds of formula I are representative, where substituents are defined herein: or a pharmaceutically acceptable salt or acid addition salt, a racemic mixture, or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.

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Raedersdorf, France

Daniel Rueher