173087-59-7Relevant articles and documents
N-Acyl-2,3-benzodiazepine derivatives, pharmaceutical compositions containing them and process for preparing same
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, (2008/06/13)
The invention relates to novel N-acyl-2,3-benzodiezapine derivatives of the general formula (I), their stereoisomers and acid-addition salts, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) Rstands for a C1 6 aliphatic acyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C1 4 alkylamino, di(C1 4 alkyl)amino, pyrrolidino, phthalimido or phenyl group, or by one or more halogen(s); or R is a benzoyl, cyclopropanecarbonyl, C1 5 alkylcarbamoyl or phenylcarbamoyl group; or R is absent when a double bond exists between the N(3) and C(4) atoms; R1means hydrogen; or R1 is absent when a double bond exists between the N(3) and C(4) atoms; R2means a C1 3 alkyl group; or R1 and R2together stand for a methylene group and no double bond is present between the N(3) and C(4) atoms; R3means hydrogen or a C1 4 aliphatic acyl group; R4represents hydrogen; a C1 6 aliphatic acyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C1 4 alkylamino, di(C1 4 alkyl)amino, pyrrolidino, phthalimido or phenyl group or by one or more halogen(s); as well as a benzoyl, palmitoyl, cyclopropanecarbonyl, C1 5 alkylcarbamoyl or phenylcarbamoyl group; and the dotted lines represent valence bonds optionally being present, with the proviso that no double bond exists between the N(3) and C(4) atoms when both R3 and R4 stand for hydrogen. The compounds of the general formula (I) possess valuable central nervous system effects, particularly muscle-relaxant, anticonvulsive and neuroprotective action. Thus, they may be useful for the treatment of various diseases of central nervous system origin.
