Abstract: Indolylacetic acid derivatives, which have excellent anti-inflammatory, antipyretic and analgesic activities, represented by the formula, ##STR1## wherein X.sub.1 and X.sub.2 are each methylene; A is an unsubstituted ethylenically unsaturated hydrocarbon chain having up to 5 carbon atoms; m is 0 or 1; n is 1 or 2; R.sub.3 is alkyl having up to 4 carbon atoms; cycloalkyl having 3 to 7 carbon atoms, unsubstituted or C.sub.1 -C.sub.4 alkyl-, nitro-, trifluoromethyl-, methylenedioxy-, ethylenedioxy- or halogen-substituted phenyl, or halogen-, C.sub.1 -C.sub.4 alkyl- or phenyl-substituted or benzene ring-condensed C.sub.3 -C.sub.7 cycloalkyl, or unsubstituted or halogen-, C.sub.1 -C.sub.4 alkyl- or phenyl-substituted or benzene ring-condensed C.sub.5 -C.sub.6 cycloalkenyl; and B is ##STR2## .

Abstract: 3,4-Dihydro-2(1H)-quinazolinone derivatives of the formula, ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkylthio or lower alkoxy, or, when taken together, R.sub.1 and R.sub.2 may form methylenedioxy; R.sub.3 is polyhalo-lower alkyl; R.sub.4 is phenyl, halophenyl, lower alkoxyphenyl, lower alkylphenyl or thienyl; and X is oxygen or sulfur, which are known to be very useful intermediates for the preparation of anti-inflammatory and analgesic agents, are obtained in a high yield by reacting a compound of the formula, ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and X are as defined above, with a compound of the formula,R.sub.4 --CHOwherein R.sub.4 is as defined above, with heating in the presence of a zinc halide as a catalyst.

Abstract: Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, aryl(C.sub.1 -C.sub.4)alkyl or (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl and n represents 1 or 2, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.

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: Butyrophenone compounds having excellent psychotropic activities represented by the formula: ##STR1## wherein R.sup.1 is a halogen atom, R.sup.2 is a lower alkyl group, and Z is a group of either one of the formulae: ##STR2## (wherein the dotted line indicates the optional presence of an additional single bond linkage, R.sup.3 is a hydrogen atom or a hydroxyl group but only when said additional single bond linkage is not present and R.sup.4 is a hydrogen atom or a phenyl or benzyl group optionally substituted with one or two substituents selected from the group consisting of halogen, lower alkyl, lower alkyoxy and trifluoromethyl on the benzene ring (except monohalophenyl)), ##STR3## (wherein the dotted line indicates the optional presence of an additional single bond linkage, R.sup.5 is a hydrogen atom or a lower alkyl group and R.sup.6 and R.sup.7 are each a hydrogen atom, a halogen atom or a lower alkyl group), ##STR4## (wherein R.sup.8 is a hydrogen atom or a lower alkyl group and R.sup.

Abstract: Ortho-acylated anilide derivatives represented by the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each C.sub.1 - .sub.3 alkyl, and n is 1 or 2, and salts thereof.

Abstract: An alalgetic composition which comprises, as an active ingredient, a therapeutically effective amount of a synergistic mixture of an indole-3-acetic acid derivative of the formula, ##STR1## wherein R is a halobenzoyl, piperonyloyl or cinnamoyl group and R.sub.1 is a 5-methoxy or 5,6-methylenedioxy group; and a narcotic or anti-narcotic analgesic selected from the group consisting of a compound of the formula, ##STR2## wherein R.sub.2 and R.sub.3 are each a C.sub.1 - C.sub.3 alkyl group and R.sub.4 is a 4-(4-fluorophenyl)-4-oxobutyl, cyclopropylmethyl or 3-methyl-2-butenyl group; a compound of the formula, ##STR3## wherein R.sub.5 is a hydrogen atom or a C.sub.1 - C.sub.3 alkyl group; a compound of the formula, ##STR4## and a compound of the formula, ##STR5## wherein R.sub.6 is a C.sub.1 - C.sub.3 alkyl group; and a pharmaceutically acceptable carrier or diluent and its preparation and a method of obtaining analgesia which comprises administering the same to a patient.

Abstract: An N-(.omega.-amino)alkylaniline derivative of the formula: ##STR1## and its pharmaceutically acceptable salts, which are useful as neuroleptic agents and can be prepared by reacting a compound of the formula: ##STR2## with a compound of the formula:H--A[wherein R is hydrogen, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.7 alkanoyl or aroyl, R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.7 alkyl or C.sub.1 -C.sub.7 alkoxy,A is ##STR3## (wherein R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.7 alkoxy or trifluoromethyl), ##STR4## (wherein R.sub.2 is as defined above and R.sub.3 is hydrogen, C.sub.1 -C.sub.7 alkyl or C.sub.1 -C.sub.7 alkanoyl), ##STR5## (wherein R.sub.2 is as defined above or ##STR6## (wherein R.sub.2 and R.sub.3 are each as defined above) and n is 2, 3 or 4].

Abstract: Novel olefinic aryl ketone compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, halogen, C.sub.1-4 alkyl, or C.sub.1-4 alkoxy, R.sup.2 is hydrogen or halogen, and X is a group of the formula: ##STR2## and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reaction of an acetylenic alcohol of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are each as defined above with formaldehyde and an piperidine compound of the formula: , or its non-toxic salt; reduction of the resultant acetylenic aryl alcohol; and oxidation of the resultant olefinic aryl alcohol.

Abstract: Novel olefinic aryl ketone compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, halogen, C.sub.1.sub.-4 alkyl, or C.sub.1.sub.-4 alkoxy, R.sup.2 is hydrogen or halogen, and R.sup.3 and R.sup.4 are each hydrogen, halogen, C.sub.1.sub.-4 alkyl or trifluoromethyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reaction of an acetylenic alcohol of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above, with formaldehyde and an amine of the formula: ##STR3## wherein R.sup.3 and R.sup.4 are each as defined above; reduction of the resultant acetylenic aryl alcohol; and oxidation of the resultant olefinic aryl alcohol.

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 phenoxyalkylamine derivative of the formula: ##STR1## and its pharmaceutically acceptable salts, which are useful as neuroleptic agents and a process for their preparation by reacting a compound of the formula: ##STR2## with a compound of the formula: ##STR3## wherein R.sub.1 and R.sub.2 are each hydrogen, halogen, C.sub.1 -C.sub.7 alkyl or C.sub.1 -C.sub.7 alkoxy, X is oxygen, sulfur, sulfinyl or NR (in which R is hydrogen or C.sub.1 -C.sub.7 alkyl), m and n are each an integer of 2, 3 or 4, and Y and Y' are each amino or halogen but they are different from each other.

Abstract: Novel butyrophenone derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydroxyl group or ##STR2## (wherein R.sub.6 and R.sub.7 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.2 represents an optionally substituted phenyl group or ##STR3## (wherein R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.4 represents a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group, R.sub.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group, R.sub.10 represents a hydrogen atom or an acyl group represented by R.sub.3 CO- (wherein R.sub.3 is a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group) and Z represents two hydrogen atoms or an oxygen atom, provided that when Z is an oxygen atom and R.sub.

Abstract: Phenoxypropylamine derivatives of the formula: ##STR1## (in which R.sub.2 is a halogen atom or a trifluoromethyl group) and R.sub.1 is a halogen atom or a C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 alkenyl group, and their pharmaceutically acceptable salts, which are useful as neuroleptic agents and can be prepared by reacting a compound of the formula: ##STR2## wherein X is a halogen atom and R.sub.1 is as defined above with a compound of the formula:H-Ywherein Y is as defined above.

Abstract: Triazoloquinazolines of the formula, ##STR1## wherein R.sub.1 is C.sub.1.sub.-4 alkyl or aryl; R.sub.2 and R.sub.3 are independently hydrogen, halogen, trifluoromethyl, nitro, C.sub.1.sub.-4 alkyl or C.sub.1.sub.-4 alkoxy, or R.sub.2 and R.sub.3 together may form methylenedioxy; and R.sub.4 is hydrogen, C.sub.1.sub.-4 alkyl, aralkyl, C.sub.1.sub.-4 haloalkyl, or C.sub.3.sub.-6 cycloalkyl; and pharmaceutically acceptable acid addition salts thereof are prepared by (a) reacting a 2-hydrazinoquinazoline derivative with a carboxylic acid or reactive derivative thereof, (b) cyclizing a 2-acylhydrazinoquinazoline derivative with heating or (c) reacting a triazolylbenzophenone derivative with ammonia. Said triazoloquinazolines and pharmaceutically acceptable acid addition salts thereof show excellent anti-inflammatory and analgesic activities.

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: Novel 4-amino-1-butanol derivatives having excellent depressant activity on central nervous system. A preferred compound of the disclosure is 4-[2-(2-alkoxyphenoxy)ethylamino]-1-(4-fluorophenyl)-1-butanol and its pharmaceutically acceptable salts.

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: Novel phenoxyethylamine derivatives of the formula: ##SPC1##Wherein R.sub.1 and R.sub.2 are each hydrogen, halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.4 and R.sub.5 are each hydrogen or C.sub.1 -C.sub.4 alkoxy and R is alkyl or aralkyl, and non-toxic pharmaceutically acceptable salts thereof, which are useful as central nervous system depressants and anti-hypertensive agents and can be prepared by reducing a compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.4, R.sub.5 and R are each as defined above and A is ##EQU1## (wherein R.sub.3 is as defined above) with a reducing agent.

Abstract: A 1,4-benzodiazepine derivative, or a pharmaceutically acceptable acid salt thereof, of the formula, ##SPC1##Wherein R.sub.1 is hydrogen, halogen, nitro or trifluoromethyl; R.sub.2 and R.sub.3 are independently hydrogen, halogen, lower alkyl or trifluoromethyl; R.sub.4 is lower alkyl, alkenyl, trihaloalkyl, alkoxyalkyl, alkenyloxyalkyl, alkoxyalkoxyalkyl, alkanoyloxyalkyl, cycloalkylalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl or a group of the formula ##EQU1## in which R.sub.6 and R.sub.7 are independently lower alkyl, and n is an integer of 1 to 4; and R.sub.5 is hydrogen or lower alkyl, is obtained by reacting a benzophenone derivative of the formula, ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above, with a 2-isocyanatoacetyl chloride derivative of the formula ##EQU2## wherein R.sub.5 is as defined above.