GB996490A - Dibenzazepine derivatives - Google Patents

Abstract

The invention comprises compounds of the general formula <FORM:0996490/C2/1> (wherein X1 and X2 each represent a hydrogen atom or jointly represent an additional bond, Z represents an alkylene radical having a straight or branched chain of 2-6 carbon atoms, R1 represents an alkyl or alkenyl radical of at most 5 carbon atoms or a phenylalkyl or phenyl radical, and R2, R3, R4 and R5 each independently represent a hydrogen atom or an alkyl or alkenyl radical of at most 5 carbon atoms, and wherein alkyl radicals R3 and R4 may be bound to each other direct or through an oxygen atom or an alkylimino group) and their acid addition salts and quaternary ammonium compounds, and the preparation thereof by reacting a halide or ester or the benzoyl derivative of an N-carboxylic acid of the general formula <FORM:0996490/C2/2> with a diamine of the general formula <FORM:0996490/C2/3> are reacting a haloalkylamide of the general formula <FORM:0996490/C2/4> (wherein Hal represents chlorine or bromine) with an amino compound R3NHR4, and in either case, if desired, converting the product into a salt by treatment with an inorganic or organic acid or (where R3 and R4 are not hydrogen) into a quaternary ammonium compound by treatment with a reactive ester of an aliphatic or araliphatic alcohol. Haloalkylamides IV (Hal=Cl) are prepared by reacting a halide or ester of an acid II with an aminoalkanol and treating the resulting hydroxyalkylamide with thinylchloride. Halides of acids II are prepared by reacting the corresponding 5-unsubstituted compounds with phosgene. Pharmaceutical preparations comprise compounds I or their acid addition or quaternary ammonium salts and pharmaceutical carriers. They have local anaesthetic, anticonvulsive, antiallergic, antiemetic and sedative activity and potentiate the action of other pharmaceuticals, e.g. anaesthetics, whilst those containing the quaternary ammonium salts have garglion-blocking activity.