Antilipolytic medicaments contg. thiophene derivs - with a thioalkanoic acid, thioalkanol or thioalkanal-acetal gp.

摘要

Antilipolytic medicaments contain thiophene derivs. of formula (I):- (where one of R1-R4 is Rx, 0, 1 or 2 of R1-R4 are Ry, and the rest are H; Rx is -S-CHR5-COOH, -S-CHR5-CH2OH or -S-CHR5-CH(OAlk)2, where R5 is H or 1-6C alkyl and alk is 1-4C alkyl; Ry is 1-6C alkyl, 1-6C alkylthio or CHO), or enantiomers and/or salts thereof, opt. in combination with conventional additives and carriers. The medicaments inhibit the prodn. of free fatty acids (FFA) due to lipolysis in the fatty tissue, and are thus useful for the treatment of arteriosclerosis (by suppressing the conversion of FFA into triglycerides in the liver) and diabetes mellitus (since FFA interfere with glucose utilisation). Unlike known natilipolytics, they are not subject to tachyphylaxia (loss of activity on repeated administration) or the rebound phenomenon (increase in FFA levels after initial lowering), and they have no effect on the heart frequency.