Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

C4 Therapeutics, Inc.

Sandra Steiner

Bernd Kuhn

Roger David Norcross

Georg Jaeschke

Antonio Ricci

Daniel Rueher

Yvonne Alice Nagel

Martin Duplessis

Yanke Liang

Kiel Lazarski

Annick Goergler

Hasane Ratni

Werner Neidhart

Roland Jakob-Roetne

Anja Limberg

Cosimo Dolente

Bjoern Bartels

Michael Reutlinger

Angélique Patiny-Adam

David Hewings

Christa Ulrike Obst-sander

Emmanuel Pinard

Henner Knust

Katrin Groebke Zbinden

Wolfgang Guba

Ulrike Obst Sander

Giuseppe Cecere

Andreas Koblet

Valerie Runtz-Schmitt

Maria-Clemencia Hernandez

Christian Schnider

Andres Miguel Olivares Morales

Buelent Kocer

Lea Aurelie Bouche

Andreas Michael Tosstorff

Stefanie Katharina Mesch

Roland Jakob-roetne

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 invention relates to novel compounds having the general formula Ib wherein R, R, R, R, Rand Z are as described herein, composition including the compounds and methods of using the compounds.

Compounds

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 invention provides novel compounds having the general formula (I) or (II) wherein R, R, R, R, W, Y and Z are as described herein, compositions including the compounds and methods of using the compounds.

Isoxazolyl ether derivatives as GABA&#x3b1;5 PAM

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 a compound of formula I wherein  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.

Fused pyrimidine derivatives

The present invention relates to compounds of formula I,   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.

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Basel, Switzerland

Sandra Steiner