N-ACYL-2,3-BENZODIAZEPINE DERIVATIVES AND PROCESS FOR THEIR PREPARATION

摘要

The invention refers to new N-acyl-2,3-benzodiazepine derivatives with the general formula I, their stereoisomers and acid addition salts, pharmaceutical preparations containing these and the preparation procedure. In the general formula (I) R stands for C1-6-aliphatic acyl group, optionally substituted with methoxy, cyano, carboxylic, amino, C1-4-alkylamino, di(C1-4-alkyl)amino, pyrrolidine, phthalimide or phenyl group and one or more halogens; or R is benzolyl, cyclopropane carbonyl, C1-5 alkylcarbamoyl or phenylcarbamoyl group; or R is absent in the case there is a double bond between N(3) and C(4) atoms; R1 stands for hydrogen; or R1 is absent in case there is a double bond between N(3) and C(4) atoms; R2 denotes C1-3-alkyl group, or R1 and R2 together denote methylene group provided no double bond is between the atoms of N(3) and C(4); R3 denotes hydrogen or C1-4-aliphatic acyl group; R4 stands for hydrogen, C1-6-aliphatic acyl group, optionally substituted by methoxy, cyano, carboxylic, amino, C1-4-alkylamino, di(C1-4-alkyl)amino, pyrrolidine, phthalimide or phenyl group with one or more halogens; as well as benzoyl, palmitoyl, cyclopropane carbonyl, C1-5-alkylcarbamoyl or phenylcarbamoyl group. The dashed lines denote valence bonds which are optionally present, provided there is no double bond between the N(3) and C(4) atoms in case when R3 and R4 denote hydrogen. Compounds with the general formula (I) have significant effects on the central nervous system, particularly relaxing, anticonvulsive and neuroprotective effects. Due to these characteristics they can be used in the treatment of various diseases which originate from the central nervous system.