method for the preparation of a pharmaceutical preparation with effects on the central nervous system on the basis of 5 - fenylbenzodiazepinederivaten,and method for preparation of 5 - fenylbenzodiazepinederivaten, suitable for use in this method.

摘要

1337737 Semicarbazido substituted benzodiazepine derivatives TAKEDA YAKUHIN KOGYO KK 18 Nov 1970 [18 Nov 1969] 28601/72 Divided out of 1337736 Heading C2C Compounds of the general Formula III wherein rings A and/or B are optionally substituted by one or more halogen, nitro, trifluoromethyl, C 1-6 alkyl, cycloalkyl or C 1-4 alkoxy; R is hydrogen or C 1-6 alkyl; X is oxygen or sulphur; RSP1/SP is a hydrocarbon residue; and the nitrogen at the 4 position is optionally that of an N-oxide group may be prepared by reacting a hydrazino derivative I with an isocyanic acid ester or isothiocyanic acid ester RSP1/SPNCX. The intermediate hydrazino compound I may be prepared by reaction of hydrazine hydrate with an appropriate 2-amino-, 2-methyl mercapto or 2-thione substituted benzodiazepine. Pharmaceutical compositions of the compounds III with the usual excipients show muscle relaxing, anticonvulsant, sedative and sleep inducing activity when administered orally or parenterally.