Process for preparing pharmaceutical composition containing N-acyl-2,3-benzodiazepine deriratives

• Main Authors: F. ANDRASI, P. BERZSENYI, S. FARKAS
• Format: Patent
• Language: Chinese; English
• Published: 28.01.2004
• Edition: 7
• 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

本发明涉及含有新的通式(I)的N-酰基-2，3-苯并二氮杂∴衍生物，其立体异构体和酸加成盐的药物组合物的制备方法，通式(I)的化合物及含有该化合物的药物组合物对中枢神经系统具有重要的作用，特别是具有弛缓肌肉、抗惊厥和保护神经的作用，因此该化合物可用于治疗各种源于中枢神经系统的疾病，以下所示的通式(I)中的各取代基定义见说明书。∴ 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.