Abstract: Novel benzisoxazole compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, ar(C.sub.1 -C.sub.3)alkoxy or halogen or, when taken together, they form C.sub.1 -C.sub.2 alkylenedioxy, Alk is C.sub.1 -C.sub.4 alkylene and A is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each C.sub.1 -C.sub.4 alkyl or, when taken together with the adjacent nitrogen atom, they represent a 5-6 membered nitrogen-containing heterocyclic ring which may contain any additional hetero atom and R.sub.5 is C.sub.1 -C.sub.4 alkyl or aryl), and non-toxic salts thereof, which possess various pharmaceutical activities.

Abstract: 1-Polyhaloalkyl-2(1H)-quinazoline derivatives of the formula, ##STR1## wherein R is polyhaloalkyl having C.sub.2 -C.sub.4 alkyl; and R.sub.1, R.sub.2 and R.sub.3 are individually hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, trifluoromethyl or halogen, have excellent anti-inflammatory and analgesic activities with very low toxicity. These quinazolinone derivatives can be prepared, for example, by reacting a trihalogenoacetamidobenzophenone derivative with ammonia.

Abstract: Imidazo- and pyrimido[2,1-b]quinazolines of the formula, ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, trifluoromethyl, nitro, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or R.sub.1 and R.sub.2 may together represent methylenedioxy; R.sub.3 is hydrogen, C.sub.1-4 alkyl, phenyl or substituted phenyl of the formula, ##STR2## (wherein R is halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy); R.sub.4 is hydrogen, C.sub.1-4 alkyl or aralkyl; and A is C.sub.2-3 alkylene wich may be optionally substituted by one or two C.sub.1-2 alkyl radicals, and pharmaceutically acceptable acid addition salts thereof, are prepared by reacting a compound of the formula, ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined above; and X is oxygen or sulfur, with a halogenating agent at a temperature of about 30.degree. C. to about 180.degree. C. In the above imidaxo- and pyrimido[2,1-b]quinazolines, those having C.sub.1-4 alkyl, or ##STR4## as R.sub.

Abstract: Viral infections caused by viruses which belong to, e.g. Pox, Herpes, Adeno, Myxo, Paramyxo groups are controlled by administering an effective amount of quinazoline derivatives of the formula ##STR1## wherein R.sub.1 is cyclo, C.sub.3 -C.sub.8 alkyl, cyclo C.sub.3 -C.sub.8 alkyl C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 -C.sub.4 alkyl, C.sub.2-C.sub.5 alkenyloxy C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylthio C.sub.1 -C.sub.4 alkyl, polyhalo C.sub.1- C.sub.4 alkyl, a group of the formula ##STR2## (wherein m is an integer of 1 to 3; and R.sub.4 and R.sub.5 are individually C.sub.1 -C.sub.4 alkyl, and may form together with the adjacent nitrogen atom an unsubstituted or C.sub.1 -C.sub.4 alkyl substituted 3 to 6 membered saturated heterocyclic ring, which may contain another nitrogen or oxygen atom) or a group of the formula --C.sub.n H.sub.2n --R.sub.6 (wherein n is 0 or an integer of 1 to 3; and R.sub.

Abstract: Novel benzisoxazole compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, ar(C.sub.1 14 C.sub.3) alkoxy or halogen or, when taken together, they form C.sub.1 -C.sub.2 alkylenedioxy, Alk is C.sub.1 -C.sub.4 alkylene and A is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each C.sub.1 -C.sub.4 alkyl or, when taken together with the adjacent nitrogen atom, they represent a 5-6 membered nitrogen-containing heterocyclic ring which may contain any additional hetero atom and R.sub.5 is C.sub.1 -C.sub.4 alkyl or aryl), and non-toxic salts thereof, which possess various pharmaceutical activities.

Abstract: Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or halogen and R.sup.3 is hydrogen or methyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are each as defined above or their non-toxic salts, or by condensation of the corresponding compounds of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are each defined above, and X is a conventional interchangeable group such as halogen or sulfonyloxy with methylamine or dimethylamine.

Abstract: Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein Ar.sup.1 represents a phenyl group having one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and trifluoromethyl, of which at least one is present at the o- or m-position, Ar.sup.2 represents an unsubstituted phenyl group or a phenyl group substituted with one or more substituents selected from the group consisting of halogen and C.sub.1 -C.sub.4 alkyl, R represents hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl and R' represents C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein Ar.sup.1, Ar.sup.2, R and R' are each as defined above or by condensation of the corresponding compounds of the formula: ##STR3## wherein Ar.sup.1 and Ar.sup.

Abstract: 3,4-Dihydro-2(1H)-quinazolinone derivatives of the formula, ##STR1## wherein R.sub.1 and R.sub.2 signify individually a hydrogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, a trifluoromethyl group, a lower alkylthio group, a lower alkylsulfonyl group or a halogen atom; R.sub.3 signifies a phenyl group, a halophenyl group, a lower alkylphenyl group, a lower alkoxyphenyl group, a trifluoromethylphenyl group, a lower cycloalkyl group, a lower cycloalkenyl group, a pyridyl group, a pyrrolyl group, a furyl group, a thienyl group or a naphthyl group; R.sub.

Abstract: 1,4-Substituted-2(1H)-quinazolinone derivatives are prepared by contactng a 2-aminophenyl ketone derivative with an alkaline agent such as alkali metal, alkali metal hydride, alkali metal amide, etc., reacting the thus obtained metal salt of 2-aminophenyl ketone derivative with a reactive ester of alcohols, reacting the thus obtained 2-(N-mono-substituted amino)-phenyl ketone derivative with a lower alkyl haloformate or a benzyl haloformate, and reacting the thus obtained carbamate derivative with ammonia. The 1,4-substituted-2(1H)-quinazolinone derivatives have excellent pharmacological properties, particularly as anti-inflammatory and analgesic effects.

Abstract: Novel N-substituted heterocyclic derivatives represented by the formula, ##STR1## wherein R is hydrogen or lower alkanoyl; R.sub.1 is hydrogen, lower alkyl, lower alkoxy, halogen, nitro, trifluoromethyl, amino or N-lower alkanoylamino; R.sub.2 is hydrogen, halogen, amino or N-lower alkanoylamino; W is oxygen, sulfur, sulfinyl or sulfonyl; and Y is ##STR2## (wherein R.sub.3 is hydrogen, lower alkyl or lower alkanoyl; and R.sub.4 is hydrogen, halogen or lower alkyl), and pharmaceutically acceptable salts thereof, which have excellent anti-inflammatory, analgesic, sedative, anti-convulsive or anti-hypertensive activities.

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 compounds of the formula: ##STR1## wherein R is a hydrogen or fluorine atom, W is an oxygen atom or an ethylenedioxy or ethylenedithio group and Z is a certain secondary amino group, which are useful as central nervous system depressants, can be prepared by the reaction of a compound of the formula: ##STR2## wherein X is a halogen atom and R and W are each as defined above with a secondary amine of the formula: H--Z wherein Z is as defined above, in case of W being ethylenedioxy or ethylenedithio, optionally followed by hydrolysis and can be reduced to give a compound of the formula: ##STR3## wherein R and Z are each as defined above, which are useful as antipsychotic and/or analgesic agents.

Abstract: 2(1H)-Quinazolinone derivatives, which are useful as anti-inflammatory agents, are prepared by heating or hydrolyzing an acylurea derivative. The acylurea derivative can be prepared by either reacting an indole derivative with an oxidizing agent or reacting an imidazolidine derivative with water, an alkanol or ammonia.

Abstract: Acylhydrazone compounds having excellent pyschotropic activity which are represented by the formula: ##STR1## wherein Z is selected from the groups having the formulas: ##STR2## wherein n is an integer of from 0 to 2 and R.sup.1 -R.sup.12 are as defined hereinbelow.

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: 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: 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 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.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 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.