Substituted 8′-pyri(MI)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a]pyrimidin-6-one derivatives
AssigneesSanofi-Aventis, Mitsubishi Pharma Corporation
InventorsNathalie Chereze, Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
Life of this patent
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Abstract
The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X, Y, R1, R2, R3, R4, o, m, n, p and q are as defined herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.
Claims5
A method of inhibiting the activity of glycogen synthase kinase 3-beta (GSK3-β), which comprises administering to a patient in need of said inhibition a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof:
- wherein:
- X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom;
- Y represents a bond, a carbonyl group, a methylene group optionally substituted by one or two groups chosen from a C1-6 alkyl group, a hydroxyl group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group or an amino group;
- R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the rings being optionally substituted by a C1-4 alkyl group, a C1-4 alkoxy group or a halogen atom;
- R2 represents a benzene ring or a naphthalene ring;
- the rings being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a methylenedioxy group, 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, a cyano, an amino, a C1-5 monoalkylamino group or a C2-10 dialkylamino group;
- R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom;
- R4 represents a hydrogen atom, a C1-4 alkoxy carbonyl group, a C3-6 cycloalkyl carbonyl group, a benzoyl group, a C1-6 alkyl group, the groups being optionally substituted by 1 to 4 substituents selected from a halogen atom, a hydroxyl group or a C1-4 alkoxy group;
- o and m represent 1 to 2;
- n represents 0 to 3;
- p represents 0 to 2;
- and
- q represents 0 to 2.
Dependencies are inferred from the claim text.