1,3-oxazines as BACE1 and/or BACE2 inhibitors

摘要

The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines 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.

主权项

1. A compound of formula I,wherein
R1 is halogen; R2 is C1-6-alkyl; R3 is selected from the group consisting of hydrogen and C1-6-alkyl; R4 is selected from the group consisting of halogen and halogen-C1-6-alkoxy; R5 is —C(═O)—R6; and R6 is selected from the group consisting of heteroaryl,
heteroaryl substituted by 1-4 substituents individually selected from cyano, halogen, halogen-C1-6-alkoxy, halogen-C1-6-alkyl, C1-6-alkoxy, C3-6-cycloalkyl, C3-6-cycloalkyl-C1-6-alkoxy, C3-6-cycloalkyl-C2-6-alkynyl, C2-6-alkynyl-C1-6-alkoxy and C1-6-alkyl,C3-6-cycloalkyl, andC3-6-cycloalkyl substituted by 1-4 substituents individually selected from cyano, and halogenor a pharmaceutically acceptable salt thereof.