(5)-Methyl-isoxazole-(3)-carboxylate salts - hypolipaemics antilipolytics, prepd. by reacting substd. theophylline derivs. with (5)-methyl-isoxazole-(3)-carboxylic acid

摘要

New 5-metyl-isoxazole-3-carboxylates are salts of formula (I). In this formula R1 and R2 are H; 1-4C alkyl; hydroxyalkyl; alkoxyalkyl; or cycloalkyl. (I) have lipolysis-inhibiting and triglyceride-lowering activity. They can be used therapeutically for the treatment of hyperlipidaemias. Dosage as 1-10 mg one or more times per day. Details of biological tests showing the effects of (I; R1=Me, R2=CH2CH2OH) on lipid metabolism in rats are given in the specification. Thus, serum triglycerides are significantly lowered by doeses up to 5 mg/kg. The effect on serum cholesterol is only short-term: 300 mg/kg p.o. only lowers serum cholesterol for 3 hrs. after administration. Blood sugar levels are significantly lowered by does of 200 and 300 mg/kg.