Use of substituted 2-(diaza-bicyclo-alkyl)-pyrimidone derivatives for the treatment of neurodegenerative diseases
AssigneesSanofi-Aventis, Mitsubishi Pharma Corporation
InventorsAlistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Abstract
The invention relates to therapeutic uses of a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): Wherein R1, R2, R3, R4 and n are as defined herein. Specifically, the compounds of formula (I) are used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer's disease. The invention relates also to intermediates for the preparation of compound of formula (I).
Claims8
A method for the treatment of a disease selected from the group consisting of Alzheimer's disease, taupathies, non-insulin dependent diabetes, which comprises administering to a patient in need of said treatment a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof:
- wherein:
- n represents 1 or 2;
- R1 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom;
- R2 represents a hydrogen atom, a C1-6 alkyl group optionally substituted by 1 to 4 substituents selected from a halogen atom, a hydroxyl group, a C1-4 alkoxy group;
- a C1-2 perhalogenated alkyl group, a benzyl group, a phenethyl group, a benzyloxycarbonyl group, a C1-4 alkoxy carbonyl group, a benzene ring, a naphthalene ring, a quinoline ring, a phthalazine ring, a 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a benzenesulfonyl group, a benzoyl group, a pyridazine ring, a furan ring and an imidazole ring;
- each of the benzyl group, the phenethyl group, the benzyloxycarbonyl group, the benzenesulfonyl group, the benzoyl group and the benzene, naplithalene, quinoline, phthalazine, 5,6,7,8-tetrehydronaphthalene, pyridine, indole, pyrrole and thiophene rings being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a benzene ring, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, a C1-4 alkoxy group, a nitro group, a cyano group, an amino group, a C1-6 monoalkylamino group and a C2-10 dialkylamino group;
- R3 represents a 2, 4 or 5-pyrimidine ring or a 2,3 or 4-pyridine ring, the rings being optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom;
- and
- R4 represents a C1-4 alkyl group optionally substituted by a hydroxyl group, a C1-4 alkoxy group or a halogen atom.
Dependencies are inferred from the claim text.