| 摘要 |
The invention relates to new N-acyl-2,3-benzodiazepine derivatives of general formula I, their stereoisomers and acid addition salts, and pharmaceutical compositions containing them and a process for their preparation, having the general formula I <IMAGE> R indicates an aliphatic C1-6 acyl group optionally substituted by a methoxy, cyano, carboxyl, amine, alkylamine, C1-4, di(alkyl C1-4) amine, pyrrolidine, phthalimide or phenyl group or by one or more halogens, or R is a benzoyl, cyclopropane carbamoyl, alkyl carbamoyl, C1-5 or phenylcarbamoyl group, or R is absent when there is a double bond between the N(3) and C(4) atoms, R1 indicates hydrogen, or R1 is absent when there is a double bond between the N(3) and C(4) atoms, R2 indicates a C1-3 alkyl group or R1 and R2 indicate a methylene group and there is no double bond present between the N(3) and C(4) atoms, R3 indicates hydrogen or C1-4 aliphatic acyl group, R4 indicates hydrogen, an aliphatic C1-6 acyl group optionally substituted by a methoxy, cyano, carboxy, amine, C1-4 alkylamine, di(C1-4 alkyl) amine, pyrrolidine, phthalimide or phenyl group, or by one or more halogens, and a benzoyl, palmitoyl, cyclopropane carbonyl, C1-5 alkyl carbamoyl or phenyl carbamoyl group, and the dotted lines represent bonds of valencies which may optionally be present, provided that there is no double bond between the N(3) and C(4) atoms when both R3 and R4 are hydrogen. Compounds of general formula I have useful effects on the central nervous system, particularly a muscle relaxing, anticonvulsant and neuro-protective effect. Thus they can be useful for the treatment of various diseases originating in the central nervous system.
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