| abstract |
The invention relates to substituted allylamine derivatives and nontoxic salts thereof useful as a cholesterol-depressing agent and represented by general formula (I), [wherein A?1 and A2¿ each represents a methine group, N, O or S; Q?1 and Q2¿ may contain 1 to 2 hetero atoms and form a 5- or 6-membered aromatic ring together with A1 or A2; X and Y each represents O, S, a carbonyl group, -CHRa- (wherein Ra represents H or an alkyl group) or -NRb- (wherein Rb represents H or an alkyl group) or, when taken together, X and Y represent a vinylene group or an ethynylene group; R1 represents a 5- or 6-membered heterocyclic ring containing 1 to 4 hetero atoms; R2 represents an alkyl, allyl, propargyl or cyclopropyl group; R?3 and R4¿ each represents an alkyl group or, when taken together, R?3 and R4¿ represent a cycloalkane together with the adjacent carbon atom; R5 represents H, an alkyl or alkoxy group; and R?6 and R7¿ each represents H, halogen, -OH, -CN, an alkyl or alkoxy group, provided that when one of X and Y represents O, S or -NRb- (wherein Rb is the same as described above), the other represents a carbonyl group or -CHRa- (wherein Ra is the same as described above)], a process for their preparation, and their use for treatment of hypercholesteremia, hyperlipemia and arteriosclerosis. |