Abstract: A process for preparing a .beta.-lactam derivative having a hydrogen atom on the nitrogen atom of the .beta.-lactam ring, which comprises reacting a .beta.-lactam derivative having a mono- or diarylmethyl group on the nitrogen atom of the .beta.-lactam ring with an acid or ceric ammonium nitrate to cleave the bond between the nitrogen atom and the mono- or diarylmethyl group; and novel .beta.-lactam derivatives useful as intermediates for the synthesis of pharmaceutical agents.

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: 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: A 1-alkyl-1,2,4,5-tetrahydro-3H-1,4-benzodiazepine derivative is produced by contacting a 1-aminoethyl-indole derivative with a suitable oxidizing agent and then reducing the resulting 1-acyl-2,3-dihydro-1H-1,4-benzodiazepine derivative. The starting 1-aminoethyl-indole derivative is prepared by subjecting a 3-phenyl-indole derivative to cyanomethylation (or carbamoylemethylation) and then reducing the resulting 1-cyanomethyl- (or 1-carbamoylmethyl)-indole derivative. The 1-acyl-1,2,4,5-tetrahydro-3H-1,4-benzodiazepine derivative is useful as a tranquillizer, muscle-relaxant, etc.

Abstract: 1-Substituted-1,2-dihydrothieno[2,3-d]-pyrimidin-2-ones of the formula, ##STR1## wherein R is lower alkyl or cyclopropylmethyl, R.sub.1 is halogen, lower alkyl or nitro, R.sub.2 is hydrogen or lower alkyl and R.sub.3 is hydrogen or halogen, are obtained by treating a trihaloacetamidothiophene derivative with ammonia. These compounds have excellent pharmacological activities such as uricosuric activity.

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.

Abstract: Novel thienopyrimidine derivatives which have excellent pharmacological uricosuric activity are prepared by reacting a thiophene derivative with cyanic acid or a salt thereof, urea or a reactive ester of carbamic acid. If desired, alkylated, halogenated or nitrated thienopyrimidine derivatives are produced by reacting thienopyrimidine derivatives with an alkylating, halogenating or nitrating agent, respectively.