aminoacylderivate 4.9 - dihydro - 10 - pyrido (3.2) thieno (3.2 - (e) (1.4) diazepinonen and 4.9 dihydro - 10 - pyrido (3.2) thieno (3,4 - (e) (1.4) diazepinonen,their manufacture and pharmaceutical preparations containing them.

摘要

(A) N-Aminoacyl-pyrido (b)(1,4)-diazepine derivs. of formula (I) (including possible enantiomeric forms) and their salts with pharmaceutically innocuous acids are new: A = a gp. of formula (Ia) or (Ib); R1 = H or CH3; n = 0, 1 or 2; R2 = H or CH3, being H when n is 2; M = 5- or 6-membered cyclic amino residue (opt. contg. another hetero atom, e.g. O, S or N) when n is 1 or 2, or 1-methyl-piperidin-4-yl or 1-methyl-piperidin-3-yl when n is 0. (B) Also new and claimed are intermediates of formula (III) (see 'Preparation') when A is a residue of formula (Ia). (I) are prepd. by reaction of N-unsubstd. cpds. of formula (III) with acylchlorides of formula (IV) or with an activated deriv. of (iso)nipecotic acid and, when (IV) is used, reaction of the product with a cyclic amine selected from pyrolidine, thiazolidine, morpholine, piperidine, piperazine or 4-methy piperazine: where (X=Cl, Br or I).