Process for preparing pharmaceutical composition containing N-acyl-2,3-benzodiazepine derivatives as active ingredient

• Main Authors: FERENC ANDRASI, SANDOR FARKAS, PAL BERZSENYI
• Format: Patent
• Language: English
• Published: 26.08.1998
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

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) R stands 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; R means hydrogen; or R is absent when a double bond exists between the N(3) and C(4) atoms; R means a C1-3 alkyl group; or R and R together stand for a methylene group and no double bond is present between the N(3) and C(4) atoms; R means hydrogen or a C1-4 aliphatic acyl group; R represents 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 R and R 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.