Sankyo Company, Limited

Kyoto Pharmaceutical Industries, Ltd.

Shoji Kamiya

Hiroshi Matsui

Hiroaki Shirahase

Shohei Nakamura

Katsuo Wada

A heterocyclic derivative of the formula (I)wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.

Indolyl or indolinyl derivatives and medicinal use thereof as ACAT or lipid peroxidation inhibitors

Method of producing heterocyclic derivatives

Heterocyclic derivatives, method of production thereof and pharmaceutical use thereof

A heterocyclic derivative of the formula (I)

Heterocyclic derivatives and pharmaceutical use thereof

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.

Method for inhibiting acyl-CoA : cholesterol acyltransferase

Indolyl or indolinyl derivatives and medicinal use thereof as ACAT or

Heterocyclic derivatives, method of production thereof and

An imidazole derivative of the formula (I) ##STR1## wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof is described. A method for producing the compound or its salt, and its pharmaceutical use, particularly as an agent for the prophylaxis and treatment of the diseases induced by thromboxane A.sub.2 or histamine are described. Also, compounds of the formula (II) and (IV) ##STR2## wherein each symbol is as defined in the specification are described. The imidazole derivative and its parmacologically acceptable salt are useful as agents for the prophylaxis and treatment of the diseases induced by thromboxane A.sub.2 or histamine, and the intermediate compounds (II) and (IV) are novel compounds.

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Kyoto, Japan

Shoji Kamiya