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: Fused quinazolinone derivatives of the formula, ##SPC1##Wherein R.sub.1 and R.sub.2 are individually hydrogen, C.sub.1.sub.-4 alkyl, C.sub.1.sub.-4 alkoxy, nitro, C.sub.1.sub.-4 alkylsulfonyl or halogen; R.sub.3 is pyridyl, thienyl or a group of the formula ##SPC2##Wherein R.sub. 4 is hydrogen or halogen; R is hydrogen, C.sub.1.sub.-4 alkyl, C.sub.2.sub.-5 alkenyl, aralkyl, (C.sub.3.sub.-6 cycloalkyl)C.sub.1.sub.-4 alkyl, (C.sub.1.sub.-4 alkoxy)C.sub.1.sub.-4 alkyl, (C.sub.1.sub.-4 alkylthio)C.sub.1.sub.-4 alkyl, hydroxy-C.sub.1.sub.-4 alkyl or C.sub.2.sub.-5 alkanoyloxy-C.sub.1.sub.-4 alkyl; Y is oxygen, or a group of the formula N - R.sub.5, wherein R.sub.5 is hydrogen or C.sub.1.sub.-4 alkyl; and Z is C.sub.2.sub.-5 alkylene or alkenylene, are prepared by reacting a trihaloacetamidophenyl ketone derivative of the formula, ##SPC3##Wherein R.sub.1, R.sub.2, R.sub. 3 and R are as defined above; and X.sub.1, X.sub.2 and X.sub.3 are halogen, with an amine of the formula, HY - Z - NH.sub.

Abstract: A process for producing butyrophenone derivatives of the formula: ##EQU1## which comprises reacting a compound of the formula: ##SPC1##With an amine of the formulaH-W(wherein Ar represents a group of either one of the formulas: ##SPC2##Z is a secondary amino group and W is the residue of an amine excluding a hydrogen atom therefrom). The said butyrophenone derivatives and their salts exhibit a variety of beneficial pharmacological activities including a central and autonomic nervous system depressing activity.

Abstract: Method and burner apparatus for burning fuels wherein an air-fuel premixture of a low fuel concentration formed by premixing a fuel with combustion air in an amount larger than the theoretical air amount necessary for combustion of said fuel is fed and burnt in a combustion zone, and simultaneously, a fuel and combustion air in an amount smaller than the theoretical air amount necessary for combustion of said fuel are fed separately and burnt in the vicinity of said combustion zone or an air-fuel premixture formed by premixing a fuel with a part of combustion air supplied in said amount and the remainder of said combustion air are fed separately in the vicinity of said combustion zone.

Abstract: Novel indolylacetic acid derivatives, which have excellent anti-inflammatory, antipyretic and analgesic activities, represented by the formula, ##SPC1##Wherein X.sub.1 and X.sub.2 each is a member selected from the group consisting of oxygen and methylene; A is a member selected from the group consisting of unsubstituted saturated hydrocarbon chain having up to 5 carbon atoms, unsubstituted unsaturated hydrocarbon chain having up to 5 carbon atoms and substituted saturated or substituted ethylenically unsaturated hydrocarbon chain having up to 5 carbon atoms, in which the substituents are selected from the group consisting of halogen or phenyl, the hydrocarbon chain being straight or blanched one; m is 0 or 1; n is 1 or 2; R.sub.1 and R.sub.2 each is a member selected from the group consisting of hydrogen and alkyl having up to 4 carbon atoms; R.sub.

Abstract: Quinazolinone derivatives of the formula, ##SPC1##Wherein R is a polyalicyclic hydrocarbon group; R.sup.1 and R.sup.2 are independently a hydrogen atom, a nitro group, a trifluoromethyl group or a methylsulfonyl group; R.sup.3 is a phenyl group, a substituted phenyl group, a pyridyl group or a thienyl group; and n is 0 or an integer of 1 to 3, have potent antiviral activity with low toxicities. These compounds can be prepared using a variety of processes analogous to known methods, for example, by oxidizing a 3,4-dihydro-2(1H)-quinazolinone having a polyalicyclic hydrocarbon group bonded through an alkylene group at the 1 position.

Abstract: Novel 2-substituted 6,7-benzomorphan derivatives of the formula: ##SPC1##And acid addition salts thereof, which are useful as non-addicting analgesics, pain relieving agents and antitussives and can be prepared by reacting 6,7-benzomorphan derivatives of the formula: ##SPC2##With the reactive derivatives of alcohols of the formula: ##EQU1## [wherein R is a hydrogen atom, a hydroxyl group, an alkoxy group or an alkanoyloxy group; R.sub.1 is a hydrogen atom, an alkyl group, an alkoxyalkyl group or a substituted or unsubstituted aryl group; R.sub.3 is a hydrogen atom or a hydroxyl group; R.sub.4 is a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, or R.sub.3 and R.sub.4 may form an alkylidene group or a carbonyl group together with the carbon atom to which these substituents are bonded; R.sub.2, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are each a hydrogen atom or an alkyl group; A is an alkylene group; and m is an integer of 0 to 2].

Abstract: A 3-phenoxypropylamine derivative of the formula: ##SPC1##Wherein Y is ##SPC2##(wherein R.sub.1 is a halogen atom or a trifluoromethyl group) or ##SPC3##(wherein R.sub.2 is a lower alkyl group) and its pharmaceutically acceptable salts which are useful as central nervous system depressing agents.

Abstract: An analgesic composition comprising an analgesically effective amount of at least one 6,7-benzomorphan derivative of the formula: ##SPC1##Wherein R is a hydrogen atom, a hydroxyl group, a C.sup.1 - C.sup.3 alkoxy group or a C.sup.1 - C.sup.8 alkanoyloxy group; R.sub.1 is a hydrogen atom, a C.sup.1 - C.sup.5 alkyl group, a phenyl group, a halophenyl group, an alkylphenyl group wherein the alkyl moiety has 1 to 3 carbon atoms, an alkoxyphenyl group wherein the alkoxy moiety has 1 to 3 carbon atoms, a trifluoromethylphenyl group, an alkylthiophenyl group wherein the alkylthio moiety has 1 to 3 carbon atoms or a group of the formula (C.sub.m H.sub.2m.sub.-p.sub.+1) - (R.sub.9).sub.p wherein m is an integer of 1 - 6, p is an integer of 1 - 2 and R.sub.9 is a C.sup.1 - C.sup.3 alkoxy group; R.sub. 2 is a hydrogen atom or a C.sup.1 - C.sup.3 alkyl group; R.sub.3 is a hydrogen atom, a C.sup.1 - C.sup.3 alkyl group, a phenyl group or an alkoxyphenyl group wherein the alkoxy moiety has 1 to 3 carbon atoms; R.sub.

Abstract: Novel N-substituted heterocyclic derivatives represented by the formula, ##SPC1##Wherein R.sub.1 is hydrogen atom, lower alkyl, lower alkoxy, nitro, halogen or trifluoromethyl group; R.sub.2 is hydrogen atom or lower alkyl group; X is sulfur atom, sulfinyl or sulfonyl group; Y is ##EQU1## group (wherein R.sub.3 is phenyl or substituted phenyl group; R.sub.4 is hydrogen atom, hydroxy, lower alkyl, lower alkoxy, lower alkanoyl, lower alkanoyloxy, carbamoyl, N-(lower alkyl)-carbamoyl or N,N-di(lower akyl)-carbamoyl group; R.sub.5 is hydrogen atom, morpholino, pyrrolidinyl, piperidinyl, hexamethylenimino, lower alkyl, cyclo(lower alkyl), cyclo(lower alkyl)-(lower alkyl), hydroxy-(lower alkyl), (lower alkoxy)-(lower alkyl), phenyl or substituted phenyl group; k is 0 or 1 and m is 0, 1 or 2); and n is 3 or 4, and pharmaceutically acceptable salts thereof, which have excellent tranquillizing, anti-psychotonic, anti-emotional, anti-convulsive, anti-psychosis, sedative, analgesic or anti-hypertensive activities.

Abstract: A novel 2-substituted-6,7-benzomorphan derivative of the formula: ##SPC1##And its acid addition salts, which are useful as non-addicting analgesics and antitussives and can be prepared by reacting a 2-unsubstituted-6,7-benzomorphan derivative of the formula: ##SPC2##With the reactive derivative of an alcohol of the formula:HOA',optionally followed by elimination of the protective group in the resulting product, wherein R.sub.1 is hydrogen, lower alkyl or acyl; R.sub.2 and R.sub.3 are each lower alkyl; A is lower alkyl, cyano(lower)alkyl, benzoyl(lower)alkyl, ar(lower)alkyl, lower alkenyl or cyclo(lower)alkyl(lower)alkyl; and A' is a group as mentioned in A or benzoyl(lower)alkyl of which the carbonyl group is masked with a suitable protective group.

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.

Abstract: A novel process for preparing 2-benzoylalkylbenzomorphan derivatives and salts thereof, represented by the formula ##SPC1##Wherein n, R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification. The process comprises reacting a pyridinium derivative of the formula, ##SPC2##Wherein X is a halogen atom and Y' is an ethylenedioxy group; with a Grignard reagent of the formula, ##SPC3##Wherein R' is a hydrogen atom or a C.sub.1 -C.sub.3 alkoxy group and Z is a halogen atom, to yield a 1,2-dihydropyridine derivative of the formula; ##SPC4##And then reducing the said 1,2-dihydropyridine derivative to give a 1,2,5,6-tetrahydropyridine derivative of the formula, ##SPC5##Wherein Y is an oxygen atom or an ethylenedioxy group, and further cyclizing the obtained 1,2,5,6-tetrahydropyridine derivative.

Abstract: Quinazoline derivatives which have anti-inflammatory, antiviral, uricosuric activities are prepared by reacting an indole-2-carbonylazide derivative with an oxidizing agent under mild conditions.

Abstract: 2-Propanol derivatives of the formula: ##SPC1##And their pharmaceutically acceptable acid addition salts, which are useful as medicaments and can be produced by reacting a compound of the formula: A-CH.sub.2 -Z with a compound of the formula: A'-H [wherein R is hydrogen or lower alkanoyl; R.sub.1 is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; W is oxygen, sulfur, sulfinyl or sulfonyl; Y is a group of either one of the formulae: ##SPC2##(wherein R.sub.2 is hydrogen, halogen, lower alkyl or lower alkoxy and R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl); A and A' are each a group of either one of the formulae: ##SPC3##(wherein R.sub.1, W and Y are each as defined above), provided that A and A' are different each other; and Z is a group of either one of the formulae: ##EQU1## (wherein X is halogen, alkylsulfonyloxy or arylsulfonyloxy and R is as defined above)].

Abstract: A 3-benzazocine compound of the formula: ##SPC1##Wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5 and R.sub.8 are each hydrogen or lower alkyl, R.sub.2 is hydrogen, lower alkyl or phenyl and R.sub.6 and R.sub.7 are each lower alkyl, and its pharmaceutically acceptable acid addition salts, which are useful as analgesics and can be produced by reacting a tetrahydropyridine compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are each as defined above or its salt with a Lewis acid.

Abstract: Quinazoline derivatives represented by the formula ##SPC1##Wherein R.sub.1 and R.sub.2 are individually a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, a lower alkylthio group or a lower alkylsulfonyl group; R.sub.3 is a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, a napthyl group, a furyl group or a thienyl group; R.sub.4 is a lower cycloalkyl group or a trihalomethyl group; and n is an integer of 1 to 3, are novel compounds and have excellent pharmacological properties, particularly as anti-inflammatory and analgesic effects with low toxicity. They can be prepared by treating with ammonia a trihaloacetamidophenylketone derivative of the formula, ##SPC2##Wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above; R is a hydrogen atom or a group of the formula --C.sub.n H.sub.2n --R.sub.4 ; and X is a halogen atom.

Abstract: 2-Ketoethyl-6,7-benzomorphan derivatives of the formula: ##SPC1##And their pharmaceutically acceptable non-toxic salts, which are useful as non-addictive analgesics and pain-relieving agents and can be prepared by reacting the corresponding 6,7-benzomorphan derivative of the formula: ##SPC2##With a vinyl carbonyl compound of the formula: ##EQU1## [wherein R' is a hydrogen atom or a group of the formula: --OR" (wherein R" is a hydrogen atom, an alkanoyl group, an alkyl group, an aralkyl group, an alkoxycarbonylmethyl group or a tetrahydropyranyl group), R.sub.1 is a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, R.sub.2 is a hydrogen atom or an alkyl group and A is an alkyl group, an alkoxy group, a substituted or unsubstituted aryl group or a substituted or unsubstituted amino group].

Abstract: Butyrophenone derivatives having excellent psychotropic activity and represented by the formula, ##SPC1##Wherein A represents a single or double bond linkage; R.sub.1 represents a hydrogen atom or a C.sub.1 - C.sub.4 alkyl group; R.sub.2, which is present only in case A represents a single bond linkage, represents a hydrogen atom, or a hydroxyl, C.sub.1 - C.sub.4 alkyl, or C.sub.1 - C.sub.4 alkoxy group; R.sub.3 represents a hydrogen atom, or a piperidino, pyrrolidino, morpholino, furyl, thienyl, C.sub.1 - C.sub.4 alkylamino, benzylamino, unsubstituted or halogen-substituted phenyl group, etc.; and X represents a hydrogen or halogen atom, or a C.sub.1 - C.sub.4 alkyl, C.sub.1 - C.sub.4 alkoxy, or trifluoromethyl group, can be prepared by reducing a benzoylpropionamide derivative of the formula, ##SPC2##Wherein A, R.sub.1, R.sub.2, R.sub.

Abstract: Central nervous system active butyrophenone derivatives in which .gamma. -piperazinobutyrophenone derivatives of the formula, ##SPC1##Wherein R.sup.1 is hydrogen, amino, C.sub.1 -C.sub.5 alkanoylamino, C.sub.1 -C.sub.4 alkylamino or N-(C.sub.1 -C.sub.4 alkyl)(C.sub.1 -C.sub.5 alkanoyl) amino; R.sup.2 is hydrogen or halogen; R.sup.3 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or trifluoromethyl; and m is 0, 1 or 2, and acid addition salts thereof, can be prepared by reacting an indole derivative of the formula, ##SPC2##Wherein R.sup.2, R.sup.3 and m are the same as defined above, and R.sup.4 and R.sup.5 are hydrogen or C.sub.1 -C.sub.4 alkyl respectively, with an oxidizing agent to yield an o-alkanoylamino-.gamma.-piperazinobutyrophenone derivative of the formula, ##SPC3##Wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5 and m are the same as defined above, and further, if necessary, hydrolyzing the product to yield an o-amino-.gamma.