Hoffmann-la Roche Inc.

C4 Therapeutics, Inc.

Syntex (u.s.a.) Inc.

F. Hoffmann-la Roche Ag

Annick Goergler

Roger David Norcross

Guido Galley

Georg Jaeschke

Antonio Ricci

Daniel Rueher

Fabian Dey

Christopher G Nasveschuk

Bernd Kuhn

Katrin Groebke Zbinden

Yanke Liang

Martin Duplessis

Kiel Lazarski

Eric Andre Kusznir

Philipp Schmid

Sandra Steiner

Ryan E Michael

Yvonne Alice Nagel

Alexander W Hird

Jae Young Ahn

Sabine Kolczewski

Stephan Roever

Philippe Pflieger

Cosimo Dolente

Henri Stalder

Thierry Godel

David Hewings

Christa Ulrike Obst-sander

Hasane Ratni

Werner Neidhart

Roland Jakob-Roetne

Michael Patrick Dillon

Jens-Uwe Peters

Ulrike Obst Sander

Torsten Hoffmann

Anja Limberg

Eric Argirios Kitas

Rosa Maria Rodriguez Sarmiento

Bjoern Bartels

Michael Reutlinger

Giuseppe Cecere

Christian Schnider

Daniela Krummenacher

Helmut Jacobsen

Moreno Attilio Wichert

Buelent Kocer

Adrian Britschgi

Dawn Muszynski Barsy

Hai-Ying Cai

Reinhard Heck

Alina Tirla

Stefan Berchtold

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 provides selected glutarimides which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

Glutarimides for medical treatment

The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

Dihydrobenzimidazolones for medical treatment

The present invention provides compounds and intermediates. The present invention also provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation. The present invention also provides compounds that may be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.

Spirocyclic compounds

The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation. The present invention also provides compounds that may be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.

The present invention provides dihydroquinolinone compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

Dihydroquinolinones for medical treatment

The present invention relates to a compound of formula I, HetAr is a five or six membered heteroaryl group, selected from wherein Ris hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen, and may be the same or different, if two Roccur; Ris lower alkyl or a mono- or polydeutered derivative thereof, lower alkyl substituted by halogen or lower alkoxy, lower alkenyl unsubstituted or substituted by halogen, cycloalkyl or CH-cycloalkyl unsubstituted or substituted by halogen, heterocycloalkyl or CH-heterocycloalkyl unsubstituted or substituted by lower alkyl; Ris halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or S(O)-lower alkyl; n is 1, 2 or 3; if n is &#x3e;1, then Rmay be the same or different; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome. 

Phenoxytriazoles

The present invention relates to compounds TAAR receptor antagonists of formula I wherein X, R, L, Ar and Rare as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I. 

6-amino-5,6,7,8-tetrahydronaphthalen-2-yl or 3-aminochroman-7-yl derivatives

The present invention relates to compounds of formula wherein Rand Rare as described herein. Compounds of the invention are useful in the treatment and/or prophylaxis of diseases associated with TAAR modulation.

Morpholine compounds and uses thereof

Growing community of inventors

Colmar, France

Annick Goergler