SUBSTITUTED ARYLAMIDDIAZEPINOPYRIMIDONE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES CAUSED BY GSK3β ANOMATIC ACTIVITY

摘要

A pyrimidone derivative represented by the formula (I), or a salt thereof, a solvate or a hydrate thereof, wherein Y is two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-6 alkyl group, and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C1-6 alkyl group, a sulfur atom, a methylene group optionally substituted by one or two groups selected from C1-4 alkyl group, hydroxyl group, C1-6 alkoxy group, Sperhaloalkyl group or amino group; R1 is a 2-, 3- or 4-pyridine ring or a 2-, 4- or 5-pyrimidine ring, and the ring is optionally substituted by a C1-6 alkyl group, C1-6 alkoxy group or halogen atom; R2 represents a hydrogen atom, C1-6 alkyl group or a halogen atom; R3 is a benzene ring or a naphthalene ring, and the rings are optionally substituted; R4 represents a hydrogen atom, a C1-6 alkyl group, a cycloalkyl group, a cycloalkyl-C1-6 alkyl group, a COO (C-alkyl) group, these groups being optionally substituted; R5 represents a hydrogen atom or a C1-6 alkyl group; and n is 0-3; and their therapeutic use for the treatment of neurodegenerative diseases caused by the abnormal activity of GSK3β.