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PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL PREPARATION ACTING ON THE CENTRAL NERVOUS SYSTEM BASED ON 5-PHENYLBENZODIAZEPINE DERIVATIVES, AND METHOD FOR PREPARING 5-PHENYLBODODIA ZEPARIC THESE BEFORE USE THEREFORE
PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL PREPARATION ACTING ON THE CENTRAL NERVOUS SYSTEM BASED ON 5-PHENYLBENZODIAZEPINE DERIVATIVES, AND METHOD FOR PREPARING 5-PHENYLBODODIA ZEPARIC THESE BEFORE USE THEREFORE
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机译:基于5-苯并二氮杂卓衍生物的中枢神经系统药物制剂的制备方法及使用前制备5-苯乙二氮卓类的方法
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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.
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机译:1337737半咔唑取代的苯并二氮杂衍生物TAKEDA YAKUHIN KOGYO KK 1970年11月18日[1969年11月18日] 28601/72从C1C标题中除以C2C通式III的化合物,其中环A和/或B任选地被一个或多个卤素,硝基,三氟甲基,C 1-6烷基,环烷基或C 1-4烷氧基; R为氢或C 1-6烷基; X是氧或硫; R 1 SP>为烃基;通过在肼衍生物I与异氰酸酯或异硫氰酸酯R 1 SP> NCX反应,可以制备4位氮为N-氧化物基团。可以通过使水合肼与合适的2-氨基-,2-甲基巯基或2-硫酮取代的苯并二氮杂反应制备中间体肼化合物I。当口服或肠胃外给药时,化合物Ⅲ与常用赋形剂的药物组合物表现出肌肉松弛,抗惊厥,镇静和睡眠诱导活性。
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