Substituted amine derivatives having anti-hyperlipemia activity.

摘要

Substituted amine derivatives represented by the general formula <CHEM> wherein Q is -C-D-E-F-G-M- or -N-H-I-J-K-L- [C, D, E, F, G, H, I, J, K and L are each O, S, a carbonyl group, -CHR<a>-, -R<b>= or -NR<c>- (R<a>, R<b> and R<c> are each H or a lower alkyl group), M and N are each an aromatic ring of 5-6 members optionally having a halogen, OH, LN, a lower alkyl group or a lower alkoxy group, provided that L is not O, S, or -NR<c>-]; R is a heterocyclic ring of 5-6 members; R<1> is H, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group, a lower alkynyl group or a cycloalkyl group; R<2>, R<3>, R<4>, R<5> R<6> and R<7> are each H, a halogen or a lower alkyl group or two of them denote a single bond; R<8> and R<9> are each F, CF3 or a lower alkyl group or are a cycloalkane in combination thereof; and R<1><0> is H, F, CF3 an acetoxy group, a lower alkyl group or a lower alkoxy group. These compounds inhibit biosynthesis of cholesterol in mammals by inhibiting their squalene epoxidase, and thereby lower their blood cholesterol values. Therefore, these compounds are expected to be effective as an agent for treatment and prophylaxis of diseases caused by excess of cholesterol, for example, obesity, hyperlipemia and arteriosclerosis and heart and encephalic diseases accompanying them.