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

US8389513B2 · kind B2 · utility

Assignees

• Hoffmann-La Roche Inc. · US
• SIENA BIOTECH S.P.A. · IT

Inventors

• David Banner · Basel, CH
• Wolfgang Guba · Memmingen, DE
• Hans Hilpert · Reinach, CH
• Harald Mauser · Riehen, CH
• Alexander V. Mayweg · Basel, CH
• Robert Narquizian · La Valette-du-Var, FR
• Emmanuel Pinard · Rixheim, FR
• Eoin Power · Siena, IT
• Mark Rogers-Evans · Bottmingen, CH
• Thomas Woltering · Freiburg (Elbe), DE
• Wolfgang Wostl · Weil am Rhein, DE

Key dates

• Filing date: Dec 3, 2010
• Grant date: Mar 5, 2013
• Expiry date: Jun 30, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides of formula Ihaving 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.