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US 2014/0112867 A1Published application
[1,3]oxazines
AssigneeHoffmann-La Roche Inc.
InventorsEdilio Borroni, Luca Gobbi, Hans Hilpert, Michael Honer, Dieter Muri, Robert Narquizian, Alessandra Polara
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Abstract
The present invention provides compounds 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. The invention further provides a radio-labelled derivative thereof.
Claims34
A compound of formula I,
- wherein
- R1 is aryl or heteroaryl, each substituted by 1-4 substituents individually selected from halogen-C2-6-alkenyl, halogen-C2-6-alkynyl, C1-6-alkoxy-C2-6-alkenyl, C1-6-alkoxy-C2-6-alkynyl, C2-6-alkenyl-C1-6-alkoxy and C2-6-alkynyl-C1-6-alkoxy;
- R2 is halogen;
- R3 is C1-6-alkyl;
- R4 is selected from the group consisting of
- i) hydrogen,
- ii) C1-6-alkyl, and
- iii) halogen;
- R5 is selected from the group consisting of
- i) hydrogen,
- ii) C1-6-alkyl, and
- iii) halogen;
- R6 is selected from the group consisting of
- i) hydrogen, and
- ii) C1-6-alkyl;
- R7 is selected from the group consisting of
- i) hydrogen, and
- ii) C1-6-alkyl;
- and when R1 is heteroaryl substituted by C2-6-alkynyl-C1-6-alkoxy, then R4 and R5 are both hydrogen or are both halogen;
- or pharmaceutically acceptable salts thereof.
17 more elements
(canceled)
Dependencies are inferred from the claim text.