Hoffmann-La Roche Inc.

C4 Therapeutics, Inc.

Hoffmann-Le Roche Inc.

F. Hoffmann-La Roche Ag

Cosimo Dolente

Bernd Kuhn

Roger David Norcross

Thomas Johannes Woltering

Patrick Schnider

Wolfgang Guba

Ulrike Obst Sander

Bjoern Bartels

Wolfgang Haap

Jens-Uwe Peters

Mark Rogers-Evans

Bernhard Fasching

Valerie Runtz-Schmitt

Andreas Kuglstatter

Walter Vifian

Christian Schnider

Roger Wermuth

David Hewings

Georg Jaeschke

Juergen Wichmann

Daniel Hunziker

Antonio Ricci

Daniel Rueher

Annick Goergler

Sandra Steiner

Christopher G Nasveschuk

Yanke Liang

Martin Duplessis

Michael Reutlinger

Yvonne Alice Nagel

Christa Ulrike Obst-sander

Piergiorgio Francesco Tommaso Pettazzoni

Didier Rombach

Daniela Krummenacher

Lilli Anselm

Katrina L Jackson

Mark E Fitzgerald

Philipp Cueni

Hasane Ratni

David Stephen Hewings

Haap Wolfgang

Fionn Susannah O'hara

Matilde Piras

Nadine Grether

Claudio Zambaldo

Delphine Gaufreteau

Thomas Woltering

Christa Ulrike Obst-Sander

Guido Galley

Virginie Brom

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

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 spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.

Spiro-oxazolones

The invention provides a novel compound having the general formula (I) or a pharmaceutically acceptable salt thereof. The compound of formula (I) can be used as a medicament.

Methylquinazolinone derivatives

The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

BACE1 inhibitors

The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

Pyridyl-triazabicycles

The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

Spiro-thiazolones

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Allschwil, Switzerland

Cosimo Dolente