Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Hasane Ratni

Georg Jaeschke

Anja Limberg

Rosa Maria Rodriguez Sarmiento

Rosa Maria Rodriguez-Sarmiento

Michael Reutlinger

Sandra Steiner

Christian Schnider

Weichun Chen

Annick Goergler

Beat Frei

Jérôme Charles Sarie

Greta Vastakaite

Guocai Zhang

Christian Kramer

Jennifer Louise Carter

Christian Jenny

Stefan Berchtold

Virginie Brom

Bjoern Bartels

Werner Neidhart

Roland Jakob-roetne

Guido Galley

Karlheinz Baumann

Emmanuel Pinard

Delphine Gaufreteau

Claudio Zambaldo

Matilde Piras

Fionn Susannah O'hara

The invention provides 7-phenoxy-N-(3-azabicyclo[3.2.1]octan-8-yl)-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazol-2-amine derivatives and related compounds of the general formula (I) wherein R, Ar, n and m are as described herein, compositions including the compounds, processes of manufacturing the compounds and the compounds for use in methods of medical treatment. The present compounds are as gamma-secretase modulators for the treatment of diseases associated with the deposition of β-amyloid in the brain, such as Alzheimer's disease, cerebral amyloid angiopathy, cochlear synaptopathy, hearing loss, hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome. The present description discloses the preparation of exemplary compounds as well as pharmacological data thereof (e.g. pages 54 to 74; examples 1 to 64; table). An exemplary compound is e.g. (R)-7-(3,5-difluorophenoxy)-N-((1R,5S,8s)-3-(6-methoxypyridazin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazol-2-amine (example 1).

7-phenoxy-N-(3-azabicyclo[3.2.1]octan-8-yl-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazol-2-amine derivatives and related compounds as gamma- secretase modulators for the treatment of alzheimer's disease

The invention provides new bicyclic heteroaryl compounds having the general formula (I) wherein R, Ar, n and m are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

Bicyclic heteroaryl derivatives

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Basel, Switzerland

Hasane Ratni