EP1136482A1 — 2-Amino-3-(alkyl)-pyrimidone derivatives as GSK3beta inhibitors

USPTO Abstract

A pyrimidone derivative represented by formula (I) or a salt thereof: <CHEM> Wherein : R1 represents a hydrogen atom or a C1-6 alkyl group; R2 represents a C1-6 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula -(CH2)2-X-(CH2)2- or -(CH2)2 -X-(CH2)3- where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; and R4 represents a C1-6 alkyl group optionally substituted by a C6,10 aryl group which may be substituted. And 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 GSK3 beta such as Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal trauma, and peripheral neuropathies.