Abstract: Novel 1-substituted benzodiazepine derivatives and salt thereof having the formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a halogen atom, a nitro group, a cyano group, a lower alkoxy group or a trifluoromethyl group; R.sub.2 is a pyridyl group or a group of the formula ##STR2## wherein R.sub.5 and R.sub.6 represent individually a hydrogen atom, a halogen atom, a lower alkyl group or a trifluoromethyl group); R.sub.3 is a hydrogen atom or a lower alkyl group; R.sub.4 is a lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl group; m is 1 or 2; and n is an integer of 1 to 4, and a process for preparation thereof and pharmaceutical use of the same.The benzodiazepine derivatives are effective as tranquillizers, muscle-relaxants and hypnotics.

Abstract: 1,4-Benzodiazepine derivatives of the formula, ##STR1## wherein R.sub.1 is hydrogen, a lower alkyl, a haloalkyl, a cycloalkylalkyl, an alkoxyalkyl, an acyloxyalkyl, an alkylthioalkyl, an alkylaminoalkyl, a dialkylaminoalkyl, a hydroxyalkyl, carbamoyl, or an N-alkylcarbamoyl; R.sub.2 is hydrogen or a lower alkyl; X is hydrogen, a halogen, nitro, or trifluoromethyl; A is a group of the formula, ##STR2## (wherein Y and Z each represent hydrogen, a halogen, a lower alkyl, or nitro) and a salt thereof, are prepared by reacting a 1,4-benzodiazepin-2-one compound of the formula, ##STR3## wherein R.sub.1, R.sub.2, X, Y and Z are the same as defined above, with diborane in an inert solvent.

Abstract: Novel 1-substituted benzodiazepine derivatives and salt thereof having the formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a halogen atom, a nitro group, a cyano group, a lower alkoxy group or a trifluoromethyl group; R.sub.2 is a pyridyl group or a group of the formula ##STR2## wherein R.sub.5 and R.sub.6 represent individually a hydrogen atom, a halogen atom, a lower alkyl group or a trifluoromethyl group); R.sub.3 is a hydrogen atom or a lower alkyl group; R.sub.4 is a lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl group; m is 1 or 2; and n is an integer of 1 to 4, and a process for preparation thereof and pharmaceutical use of the same.

Abstract: Benzodiazepine derivatives of the formula, ##SPC1##Wherein R.sub.1 is a C.sub.2-4 alkenyl group, R.sub.2 is a halogen atom and R.sub.3 is a hydrogen or halogen atom, which are useful as minor tranquilizer and anticonvulsant. These compounds are prepared by reacting a compound of the formula, ##SPC2##Wherein R.sub.1, R.sub.2, and R.sub.3 are as defined above, with a compound of the formula, ##EQU1## wherein X is an oxygen or sulfur atom.