Method for inhibiting acyl-CoA : cholesterol acyltransferase

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514415, 514824, 514866, A61K 3140, A61K 31405

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active

061274038

ABSTRACT:
Heterocyclic derivatives of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors.
To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.

REFERENCES:
patent: 3824230 (1974-07-01), Hester, Jr.
patent: 5143919 (1992-09-01), Meguro et al.
patent: 5254590 (1993-10-01), Malen et al.
patent: 5256782 (1993-10-01), Meguro et al.
De Vries et al., "Potential Antiatherosclerotic Agents. 5..sup.l An Acyl-CoA: Cholesterol O-Acyltransferase Inhibitor with Hypocholesterolemic Activity", J. Med. Chem., 29, pp. 1131-1133 (1986).

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