Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Christian Schnider

Thomas Johannes Woltering

Wolfgang Guba

Bjoern Bartels

Roger Wermuth

Jens-Uwe Peters

Wolfgang Haap

Ulrike Obst Sander

Andreas Kuglstatter

Mark Rogers-Evans

Cosimo Dolente

Roland Humm

Angélique Patiny-Adam

Hasane Ratni

Hans Hilpert

Georg Jaeschke

Werner Neidhart

Roland Jakob-Roetne

Guido Galley

Luca Claudio Gobbi

Anja Limberg

Rosa Maria Rodriguez Sarmiento

Annick Goergler

Michael Reutlinger

Giuseppe Cecere

Valerie Runtz-Schmitt

Sandra Steiner

Maria-Clemencia Hernandez

Daniela Krummenacher

Thorsten Muser

Andrés Miguel Olivares Morales

Lea Aurelie Bouche

Stefan Berchtold

Stefanie Katharina Mesch

Andreas Michael Tosstorff

Roland Jakob-roetne

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 invention provides novel heterocyclic compounds having the general formula (I) or (II), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.

Benzodiazepine derivatives as GABA a GAMMA1 PAM

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 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 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.

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. 

5-aryl-1-imino-1-oxo-[1,2,4]thiadiazines

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Basel, Switzerland

Christian Schnider