Thieno-pyrido-azepine and thieno-naphthyridine derivs. - useful as anorectics, antiphlogistics and hypoglycaemics

摘要

Thienopyridines of formula (I) and their physiologically acceptable salts with inorganic or organic acids are new:- In (I) R1 is H, lower alkyl opt. substd. by aryl, lower carbalkoxy or organic acyl. R2 = lower alkyl or aryl. R3 and R4 = H or lower alkyl. A= 5-membered, satd. or unsatd. ring contg. as atom, n and m = 0-4 provided m + n = 3 or 4. Pref. cpds., have alkyl gps. of 1-5C; aryl of 6-10C; carbalkoxy of 2-6C and acyl of 1-5C opt. substd. by aryl. (I) are prepd. by reacting an amino-R2CO- substd. thiophene derivs. with an oxo-heterocycle. (I) are anorectics, antiphlogistics and hypoglycaemics useful in treating obesity, psychotic conditions and ulcers. A typical cpd., ethyl 5,6,8,9-tetrahydro-10-methyl- H-thieno 2',3':5,6 pyrido 2,3-d azepine-7-carboxylate (Ia) has acute oral LD50 in mice 200 mg/kg and ED50 for suppressing food consumption in rats of 7.8 mg/kg orally.