| 摘要 |
Disclosed are substituted 2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one and 2-pyrimidin-4-yl-pyrimido[2,1-a]isoquinolin-4-one derivatives as represented by the general formula (I), wherein: R1 is a pyridin-4-yl or pyrimidin-4-yl moiety; R2 and R3 are hydrogen; R4 is hydrogen or a halogen atom; R7, R8, R9, R10 independently are selected from hydrogen, halogen, alkoxy, nitro, hydroxyl or amino; in form of a free base or of an addition salt with an acid, or a solvate thereof, or a hydrate thereof. Of particular importance are the compounds 2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one, 10-bromo-2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one, 10-methoxy-2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one, 8-nitro-2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one, 8-amino-2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one, 10-hydroxy-2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one, 10-methoxy-2-pyrimidin-4-yl-pyrimido[2,1-a]isoquinolin-4-one, 2-pyridin-4-yl-6,7-dihydro-pyrimido[2,1-a]isoquinolin-4-one and 9,10-dimethoxy-2-pyridin-4-yl-6,7-dihydro-pyrimido[2,1-a]isoquinolin-4-one. Further disclosed are GSK3b and tau protein kinase 1 inhibitor medicaments which comprises a compound as defined above for the treatment of neurodegenerative diseases (such as Alzheimer's disease, Parkinson's disease, tauopathies, vascular dementia; acute stroke, traumatic injuries etc.); non-insulin dependent diabetes; obesity; manic depressive illness; schizophrenia; alopecia; cancer; malaria; bone diseases etc.
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