Pyridobenzoxazepine derivatives

摘要

Novel 5-substituted-6-oxo-5,6-dihydropyrido-[2,3-b][1,4] benzoxazepines of the general formula (wherein R1 represents a hydrogen or halogen atom or an amino, acylamino, acyl or C1- 5 alkyl or alkoxy group and R2 represents a hydrogen atom, or R1 and R2 together complete a fused-on benzene ring, and R represents a straight or branched alkenyl or haloalkenyl group, or a straight or branched alkyl group optionally substituted by at least one halogen atom, by a C1- 5 alkoxy group, by an aryl group optionally carrying one or more halogen or C1- 5 alkyl or alkoxy substituents, or by a basic group -NR3R4 wherein R3 and R4 represent C1- 5 alkyl groups or jointly form with N a heterocyclic ring which may contain a further heteroatom and/or may be substituted by C1- 5 alkyl groups) are prepared by reacting alkali metal derivatives of the corresponding 5-unsubstituted compounds with compounds RX (wherein X is the residue of a reactive ester). When R1 in the product is to represent NH2, this group is preferably protected (e.g. by acylation) during the reaction. Compounds containing a basic substituent may subsequently be converted to acid addition salts.ALSO:Pharmaceutical compositions having antipyretic, anticonvulsive, analgesic and sedative activity comprise, in association with a pharmaceutical carrier or excipient, at least one compound of the general formula: (wherein R1 represents a hydrogen or halogen atom or an amino, acylamino, acyl or C1-5 alkyl or alkoxy group and R2 represents a hydrogen atom, or R1 and R2 together complete a fused-on benzene ring, and R represents a straight or branched alkenyl or haloalkenyl group, or a straight or branched alkyl group optionally substituted by at least one halogen atom, by a C1-5 alkoxy group, by an aryl group optionally carrying one or more halogen or C1-5 alkyl or alkoxy substituents, or by a basic group -NR3R4 wherein R3 and R4 represent C1-5 alkyl groups or jointly form with N a heaterocyclic ring which may contain a further heteroatom and/or may be substituted by C1-5 alkyl groups) or a non-toxic acid addition salt thereof if it contains a basic group. The preparations are preferably in unit dosage forms suitable for oral, rectal or parenteral administration. They may contain other compatible active ingredients such as sedatives (e.g. phenobaribtone or its sodium salt, or codeine salts), N-(2-amino-3,5-dibromobenzyl)-N-methylcyclohexylammonium chloride, or ascorbic acid.