Hoechst Aktiengesellschaft

Manfred Forsch

Hermann J Gerhards

Wolfgang Schaub

What are disclosed are 1,4-benzodiazepines, having a carbamoyloxyamino group, of the following formula I ##STR1## tautomers thereof of the following formula IA ##STR2## physiologically tolerated salts thereof, said compounds having an anxiolytic action without sedating, a process for the preparation of these new compounds, pharmaceutical agents which contain the active compounds, and methods for treating anxiety states with said compounds.

Carbamoyloxyamino-1,4-benzodiazepines and medicaments containing these

Heterocyclic, spiro-linked amidines of the formula I ##STR1## and their physiologically acceptable salts, in which (a) n is 1 or 2; (b) R.sup.1 and R.sup.2 are hydrogen or alkyl radicals which, together with the nitrogen atom, can form a 5-, 6- or 7-membered ring which can be substituted by C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.2 -alkoxy, hydroxyl or C.sub.1 -C.sub.4 -alkoxy-carbonyl groups and in which one of the carbon atoms can also be replaced by an oxygen, sulfur or nitrogen atom, it being possible for the nitrogen atom to be substituted by hydrogen, by the formyl group or by a phenyl radical, which can in turn be monosubstituted or polysubstituted by a C.sub.1 to C.sub.4 -alkyl group or an alkoxy, methylenedioxy, hydroxyl, halogen, nitro or amino group, or it being possible for the nitrogen atom to be substituted by a C.sub.1 -C.sub.4 -alkyl group, or in which R.sup.1 represents hydrogen and R.sup.2 represents a C.sub.5 -C.sub.8 -cycloalkyl radical which can be substituted by C.sub.1 -C.sub.4 -dialkylamino groups; (c) R.sup.3 is hydrogen or methyl and (d) R.sup. 4 denotes a phenyl radical which is optionally monosubstituted or polysubstituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, methylenedioxy, hydroxyl, halogen, cyano, nitro, trifluoromethyl, amino, C.sub.2 -C.sub.5 -acylamino or mono- or di-C.sub.1 -C.sub.4 -alkylamino groups, or a thiophene radical, their stereoisomers and optical isomers, processes for their preparation and antidepressive medicaments containing these compounds.

Growing community of inventors

Nauheim, Germany

Manfred Forsch