Novel 2,9-disubstituted-4h-pyrido[1,2-a]pyrimidin-4-ones

Details Novel 2,9-disubstituted-4h-pyrido[1,2-a]pyrimidin-4-ones Novel 2,9-disubstituted-4h-pyrido[1,2-a]pyrimidin-4-ones

C - Chemistry, Metallurgy

07

D

167/218, 260/245

C07D 413/14 (2006.01) A61K 31/505 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2040086

Novel 2,9-disubstituted-4H-pyrido[1,2-a]pyrimidin-4-ones having the formula Image the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein Alk represents C1-4alkanediyl, D is a bicyclic heterocycle of formula Image wherein R1 represents C1-4alkyl, hydroxyC1-4alkyl, carboxaldehyde, carboxyl, C1-10alkylcarbonyloxyC1-4alkyl; each R2 represents hydrogen or C1-4alkyl; R3 represents C1-4alkyl, hydroxyC1-4alkyl or methyl substituted with phenyl, 5-methyl-2-furanyl or 3-pyridinyl; and R4 represents C1-3alkyl, phenyl, 5-methyl-2-furanyl or 3-pyridinyl. are potent antagonists of dopamine and are therapeutically useful in treating patients suffering from acute psychoses. Processes of preparing said compounds and compositions thereof.

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