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US 11,447,478 B2Granted
BACE1 inhibitors
AssigneeHoffmann-La Roche Inc.
InventorsHans Hilpert, Roland Humm, Thorsten Muser, Christian Schnider, Roger Wermuth, Thomas Woltering
Life of this patent
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Abstract
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.
Claims24
A compound of formula I,
- wherein
- R1 is selected from the group consisting of
- i) aryl,
- ii) aryl substituted by 1-4 substituents individually selected from amino, cyano, cyano-C1-6-alkyl, halogen, halogen-C1-6-alkoxy, halogen-C1-4-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, C2-6-alkynyl-C1-6-alkoxy, C2-6-alkynyl and C1-6-alkyl,
- iii) heteroaryl, and
- iv) heteroaryl substituted by 1-4 substituents individually selected from amino, cyano, cyano-C1-4-alkyl, halogen, halogen-C1-6-alkoxy, halogen-C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, C2-6-alkynyl-C1-4-alkoxy, C2-6-alkynyl and C1-4-alkyl;
- R2 is selected from the group consisting of
- i) hydrogen,
- ii) C1-4-alkyl, and
- iii) halogen;
- R3 is selected from the group consisting of
- i) C1-6-alkyl, and
- ii) halogen-C1-6-alkyl,
- R4 is selected from the group consisting of
- i) halogen, and
- ii) hydrogen,
- R5 is halogen-C1-4-alkyl;
- or a pharmaceutically acceptable salt thereof.
15 more elements
The compound of formula I, of formula Ia-1
- wherein
- R1 is selected from the group consisting of
- i) aryl,
- ii) aryl substituted by 1-2 substituents individually selected from amino, cyano, cyano-C1-6-alkyl, halogen, halogen-C1-6-alkoxy, halogen-C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, C2-6-alkynyl-C1-6-alkoxy, C2-6-alkynyl and C1-4-alkyl,
- iii) heteroaryl, and
- iv) heteroaryl substituted by 1-2 substituents individually selected from amino, cyano, cyano-C1-6-alkyl, halogen, halogen-C1-6-alkoxy, halogen-C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, C2-6-alkynyl-C1-6-alkoxy, C2-6-alkynyl and C1-6-alkyl;
- and
- R3 is selected from the group consisting of
- i) C1-6-alkyl, and
- ii) halogen-C1-6-alkyl,
- R4 is selected from the group consisting of
- i) halogen, and
- ii) hydrogen,
- or a pharmaceutically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.