Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Greta Vastakaite

Hasane Ratni

Werner Neidhart

Roland Jakob-Roetne

Anja Limberg

Bjoern Bartels

Michael Reutlinger

Jérôme Charles Sarie

Roland Jakob-roetne

The present invention relates to a compound of formula I, 1-1 or 1-2 wherein Ris hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, or lower alkoxy substituted by halogen; Rmay be different if n=2 or 3 n is 1, 2 or 3 Ar is a six membered heteroaryl group, selected from wherein Ris hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; Ris hydrogen or halogen; or to a pharmaceutically active acid addition salt 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. 

Bicyclic heteroaryl derivatives

The present invention relates to a compound of formula (I), wherein Ris hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; R may be the same or different, if n=2 or 3; n is 1, 2 or 3; m is 1, 2 or 3; Ar is a five or six membered heteroaryl group, selected from (II), (III), (IV) or (V) wherein Ris hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; Ris hydrogen or halogen; -( ) m-is &#x2014;(CH)&#x2014; or to pharmaceutically active acid addition salts 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-in-farct dementia, dementia pugilistica or Down syndrome. 

Bridged piperidine derivatives

The present invention relates to a compound of formula (I), wherein Ris hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; and Rmay be different if n is 2 or 3; Ris hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, CN, lower alkoxy or lower alkoxy substituted by halogen; X is CH or N; m is 1, 2 or 3; -( )is &#x2014;(CH)&#x2014;; n is 1, 2 or 3; Ar is a five membered heteroaryl group, selected from formula (A), (B), (C), (D), (E) or (F), wherein Ris hydrogen, methyl or chloro; Ris hydrogen or methyl; Ris F, Cl, CHFor CF; or to pharmaceutically active acid addition salts 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. 

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Zurich, Switzerland

Greta Vastakaite