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US 9,067,926 B2Granted
Fluoromethyl-5,6-dihydro-4H-[1,3]OXAZINES
AssigneesHoffmann-La Roche Inc., Siena Biotech S.P.A.
InventorsHans Hilpert, Roland Humm, Thomas Woltering
Life of this patent
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Abstract
Provided herein is a compound of formula I: as wells as a pharmaceutical composition, a process of making and a method of using a compound of formula I. The compounds of formula I are BACE1 inhibitors useful for the treatement of, for example, Alzheimer's Disease.
Claims39
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 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,
- iii) heteroaryl, and
- iv) heteroaryl substituted by 1-4 substituents individually selected from 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;
- R2 is selected from the group consisting of
- i) hydrogen,
- ii) C1-6-alkyl, and
- iii) halogen;
- R3 is selected from the group consisting of
- i) C1-6-alkyl, and
- ii) halogen-C1-6-alkyl,
- R4 is halogen-C1-6-alkyl;
- or pharmaceutically acceptable salts thereof.
12 more elements
A process for preparing a compound of formula I, which process comprises reacting a compound of formula XΓ with a compound of formula XII:
Dependencies are inferred from the claim text.