5H-2,3-BENZODIAZEPINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

• Main Authors: ZOLYOMI, GABOR, ANDRASI, FERENC, LANG, ZSUZSANNA, ELEKES, ISTVAN, LANG, TIBOR, KOROESI, JENO, BOTKA, PETER, BERZSENYI, PAL, GOLDSCHMIDT, KATALIN, HAMORI, TAMAS
• Format: Patent
• Language: English; French
• Published: 11.12.1990
• Edition: 5
• 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 new 5H-2,3-benzodiazepine derivatives and a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same. According to the invention the new 5H-2,3-benzodiazepines corresponding to the general formula (I), (I) wherein R and R1 each represent hydrogen, chlorine, C1-4 alkyl or C1-4 alkoxy, R2 stands for hydrogen or C1-4 alkyl, R3 and R4 each denote C1-4 alkyl, or combined they denote methylene, and pharmaceutically acceptable acid addition salts thereof are prepared by reducing a compound of the general formula (II), (II) wherein R, R1, R2, R3 and R4 have the above-defined meanings, in an organic solvent, and, if desired, converting the thus-obtained compound of the general formula (I) into a pharmaceutically acceptable acid addition salt, or liberating a free base of the general formula (I) from its salt and converting it into another acid addition salt. The new 5H-2,3-benzodiazepine derivatives of the invention possess valuable central nervous effect and in particular exert antiaggressive, anxiolytic, narcosis potentiating and soporific properties. The pharmaceutical compositions according to the invention containing as active ingredient at least one compound of the general formula (I) or a pharmaceutically acceptable acid addition salt thereof can be used to advantage in the therapy.