THEOPHYLLIN DERIVATIVES, AND PROCESS FOR THEIR PREPARATION

摘要

Antitussive compounds of the formula I IMAGE (I) or physiologically acceptable acid addition salts thereof are disclosed, where A stands for straight or branched chain C1-5 alkylene or IMAGE R1 stands for straight or branched chain C1-10 alkyl, halogenoalkyl, hydroxyalkyl, C5-6 cycloalkyl, vinyl, 2-ethoxyethyl, carbonylalkyl or aminoalkyl of the formula IMAGE wherein R stands for hydrogen or methyl, n is 0 to 3, R2 stands for hydrogen or straight or branched chain alkyl, R3 stands for hydrogen or straight or branched chain alkyl or, R2 and R3 together with the nitrogen atom may form a 5-6 membered ring, which ring can optionally contain an oxygen or a second nitrogen atom, the latter, optionally substituted by methyl or, R1 can stand for a phenyl group of the formula R4R5C6H3 wherein R4 and R5 represent independently hydrogen, chlorine, hydroxy, methoxy, ethoxy, methyl or amino or, R1 may further stand for hydroxy, in this case the compound of the formula I may exist according to the conditions in the form of tautomers of the formula Ia IMAGE (Ia) or IMAGE (Ib) and R1 may further stand for benzyl, 2,2-diphenylethyl or theophyllin-7-yl-methyl.