Substituted amine derivatives having anti-hyperlipemia activity

C - Chemistry – Metallurgy – 07 – D

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C07D 333/20 (2006.01) A61K 31/33 (2006.01) C07D 213/30 (2006.01) C07D 233/61 (2006.01) C07D 263/32 (2006.01) C07D 277/24 (2006.01) C07D 333/16 (2006.01) C07D 333/18 (2006.01) C07D 333/24 (2006.01) C07D 333/32 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2038633

Abstract of the Disclosure Substituted amine derivatives represented by the general formula Image [I] 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, -CHRa-, -Rb= or -NRc- (Ra, Rb and Rc 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 -NRc-]; R is a heterocyclic ring of 5-6 members; R1 is H, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group, a lower alkynyl group or a cycloalkyl group; R2, R3, R4, R5 R6 and R7 are each H, a halogen or a lower alkyl group or two of them denote a single bond; R8 and R9 are each F, CF3 or a lower alkyl group or are a cycloalkane in combination thereof, and R10 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.

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