| 摘要 |
Disclosed is a pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or an alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or an alkyl group, a sulphur atom, a methylene group; R1 represents a 2, 4 or 5-pyrimidine ring or a 4-pyridine ring; R2 represents a heterocyclic group, R3 represents a hydrogen atom, an alkyl group or a halogen atom; R4 represents a hydrogen atom or an alkyl group; R5 represents a hydrogen atom, an alkyl group; R7 represents a hydrogen atom or an alkyl group; and n represents 0 to 3 and m represents 1 in the form of a free base or of an addition salt with an acid exemplified by [1,5]Naphthyridine-2-carboxylic acid [Z-(1-methyl-6-oxo-1,6-dihydro- [4,4']bipyrimidinyl-2-yl)-ethyl]-amide, 6-Chloro-pyridine-2-carboxylic acid [Z-(1-methyl-6-oxo-1,6-dihydro- [4,4']bipyrimidinyl-2-yl)-ethyl]-amide and 2-Methoxy-N-[2-( 1-methyl-6-oxo-1 ,6-dihydro-[4,4']bipyrimidinyl-2-yl)-ethyl]-amide in treating Alzheimer's disease, Parkinson's disease, tauopathies, vascular dementia; acute stroke, traumatic injuries; cerebrovascular accidents, brain cord trauma, spinal cord trauma; peripheral neuropathies; retinopathies or glaucoma, noninsulin dependent diabetes; obesity; manic depressive illness; schizophrenia; cancers; parenchymal renal diseases or muscle atrophy and malaria. Also disclosed is a process to make said derivative by coupling a pyrimidone amine with a carboxylic acid derivative in basic conditions.
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