SUGAR-SUBSTITUTED 2-AZETIDINONE USEFUL AS TREATING AGENT FOR HYPOCHOLESTEROLEMIA

摘要

PROBLEM TO BE SOLVED: To provide a sugar-substituted 2-azetidinone useful as an agent for hypocholesterolemia for the treatment and prevention of atherosclerosis. SOLUTION: The objective compound is expressed by formula I [R26 is H or OG1; G and G1 are each H or the like; Ar1 is an aryl or the like; Ar2 is an aryl or the like; Q is a bond or the like; and R1 is (CH2)q ((q) is 2-6) or the like], e.g. 1-O-[4-[trans-(3R,4S)-1-(4-fluorophenyl)-2-oxo-3-[3-[(S)-hydroxy-4- iodophenyl]propyl]]-4-4-azetidinyl]phenyl]-β-D-glucuronic acid. The compound of formula I can be produced e.g. by reacting an azetinone of formula II (R26A is H or OH) with a sugar derivative of formula III (R30 is H or CNHCCl3). The daily administration dose of the compound of formula I for hypocholesterolemia is preferably 0.001-30 mg/kg body weight, especially 0.001-1 mg/kg body weight.