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US 2019/0337936 A1Published application
Bace1 inhibitors
AssigneeHoffmann-La Roche Inc.
InventorsBjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
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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.
Claims27
A compound of formula I,
- A is a heteoayl group,
- A is a heteroaryl group,
- B is a heteroaryl group,
- R1 is selected from the group consisting of
- i) C1-6-alkyl and
- ii) halogen-C1-6-alkyl;
- R2 is selected from the group consisting of
- i) C1-6-alkyl, and
- ii) halogen-C1-6-alkyl;
- or R1 and R2 form together with the C-atom they are attached to, a C3-6-cycloalkyl-, wherein the C3-6-cycloalkyl- is optionally substituted by one or more substituents selected from the group consisting of halogen and hydroxyl;
- R3 is selected from the group consisting of
- i) hydrogen,
- ii) C3-6-cycloalkyl,
- iii) halogen-C1-6-alkyl, and
- iv) C1-6-alkyl;
- R4 is selected from the group consisting of
- i) hydrogen, and
- ii) C1-6-alkyl;
- R5 is selected from the group consisting of
- i) C1-6-alkyl, and
- ii) halogen-C1-6-alkyl;
- R6 is halogen;
- R7 is selected from the group consisting of
- i) amino,
- ii) cyano,
- iii) hydrogen,
- iv) OH,
- v) halogen,
- vi) C1-6-alkyl,
- vii) C1-6-alkyl-C3-6-cycloalkyl,
- viii) halogen-C1-6-alkyl,
- ix) C1-6-alkoxy-C1-6-alkyl,
- x) C2-6-alkynyl,
- xi) C2-6-alkynyl-C1-6-alkyl,
- xii) C2-6-alkynyl-C1-6-alkoxy
- xiii) C1-6-alkoxy, and
- xiv) halogen-C1-6-alkoxy;
- or pharmaceutically acceptable salts thereof.
35 more elements
The invention as hereinbefore described.
Dependencies are inferred from the claim text.