The present invention relates to 1-phenylalkyl-3-phenylurea derivatives and 1-phenylalkyl-3-phenylthiourea derivatives which are potent in reducing a lipid level in blood and, therefore, useful as therapeutical medicines for hyperlipemia and atherosclerosis.
Heretofore, it has been considered that hyperlipemia caused by metabolic disorder of lipids results in arteriosclerosis and is one of the major dangerous factors causing ischemic heart disease or cerebral embolism.
Recently, it was revealed that an enzyme, acyl-CoA: cholesterol acyltransferase (ACAT) acts an important role at lipid metabolism, especially cholesterol metabolism It is expected that compounds having an inhibitory activity of the enzyme, ACAT, actually inhibit the absorption of cholesterol at intestine, reduce the level of cholesterol in blood, and inhibit the deposition of cholesterol on arterial wall. Therefore, compounds having an inhibitory activity of ACAT, are useful as therapeutical medicines for atherosclerosis as well as hyperlipemia.
As examples for such compounds having an inhibitory activity of ACAT, 1-phenylalkyl-3-phenylurea derivatives are disclosed in Japanese Patent Application Laid-Open (KOKAI) No.316761/88, No.93569/89, No.6455/90, No. 6456/90, No. 6457/90, No. 258756/90, and 275848/90.
The compound according to the present invention is novel and has a high inhibitory activity of ACAT and a high cholesterol reducing action in blood.
USPTO Backgrounds
USPTO Backgrounds