Hoffmann-la Roche Inc.

Siena Biotech S.p.a.

F. Hoffmann-la Roche Ag

Eoin Power

Thomas Johannes Woltering

Wolfgang Wostl

Wolfgang Guba

Robert Narquizian

Hans Hilpert

Harald Mauser

Mark Rogers-Evans

Alexander Mayweg

David Banner

Matteo Andreini

Massimiliano Travagli

Emanuele Gabellieri

Emmanuel Pinard

Roland Humm

Didier Rombach

Alexander V Mayweg

Michela Valacchi

Guido Marconi

The present invention relates to 1,4 Oxazines of formula I having BACE1 and/or BACE2 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 and type 2 diabetes.

1,4 oxazines as BACE1 and/or BACE2 inhibitors

This invention relates to compounds of the formula wherein A, B and Rto Rare as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.

2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds

The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides of formula I having BACE1 and/or BACE2 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 and type 2 diabetes.

2-amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides

The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 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 and type 2 diabetes.

3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines

The present invention relates to a compounds of formula I wherein R, R, R, R, R, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (&#x3b2;-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated &#x3b2;-amyloid levels or &#x3b2;-amyloid deposits, particularly Alzheimer's disease.

4,5-dihydro-oxazol-2-yl amine derivatives

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Siena, Italy

Eoin Power