Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
AssigneesF. Hoffmann-La Roche AG, Siena Biotech S.P.A.
InventorsHans Hilpert, Roland Humm, 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.
Claims40
A compound of formula I,
- wherein
- R 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.
4-28. (canceled)
A process for preparing a compound of formula, which process comprises reacting a compound of formula XI′ with a compound of formula XII to a compound of formula I.
A pharmaceutical composition comprising:
- a compound of formula I and a pharmaceutically acceptable carrier and/or a pharmaceutically acceptable auxiliary substance.
A method for the therapeutic and/or prophylactic treatment of Alzheimer's disease or amyotrophic lateral sclerosis (ALS), arterial thrombosis, autoimmune/inflammatory diseases, cancer such as breast cancer, cardiovascular diseases such as myocardial infarction and stroke, dermatomyositis, Down's Syndrome, gastrointestinal diseases, Glioblastoma multiforme, Graves Disease, Huntington's Disease, inclusion body myositis (IBM), inflammatory reactions, Kaposi Sarcoma, Kostmann Disease, lupus erythematosus, macrophagic myofasciitis, juvenile idiopathic arthritis, granulomatous arthritis, malignant melanoma, multiple mieloma, rheumatoid arthritis, Sjogren syndrome, Spinocerebellar Ataxia 1, Spinocerebellar Ataxia 7, Whipple's Disease or Wilson's Disease, said method comprising:
- administering a compound of formula I to a human being or animal.
Dependencies are inferred from the claim text.