Abstract: A thiazole derivative of the general formula: ##STR1## The thiazole derivatives have an excellent inhibitory activity for superoxide radical.

Abstract: An object of the present invention is to provide a vasopressin antagonist and oxytocin antagonist.The vasopressing antagonist and oxytocin antagonist according to the present invention contain, as the active ingredient, a benzoheterocyclic compound represented by the general formula (1): ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and the carbon-carbon bond between 4- and 5-positions in the benzoazepine skeleton are the same as defined in claims 1, 2 and 3.) or salt thereof.

Abstract: Peripheral vasodilating agents containing, as the active ingredient, carbostyril derivatives represented by the general formula: ##STR1## or a salt thereof; and novel carbostyril derivatives included within the scope of the above-mentioned general formula.

Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenyialkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substituted benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups being optionally replaced by O, S, SO, SO.sub.

Abstract: An object of the invention is to provide hepatitis therapy. According to the invention, an apoptosis regulating composition is provided which comprises, as an active ingredient, at least one carbostyril derivatives of general formula (1) ##STR1## and salts thereof.

Abstract: A pharmaceutical preparation comprising at least one compound selected from the group consisting of carbostyril derivatives having the general formula: ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group optionally having hydroxy group as a substituent; R.sup.2 is a phenyl(lower alkyl) group optionally having 1 to 3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring, pyridyl(lower alkyl) group, or a group of the formula --A--NR.sup.3 R.sup.4 (wherein A is a lower alkylene group, R.sup.3 and R.sup.4 are the same or different and represent a lower alkyl group or phenyl group), and a salt thereof, which is useful as an agent for treating thrombosis, more particularly, as an agent for inhibiting platelet aggregation, an agent for platelet aggregate dissociation, an ameliorant of cerebral circulation and a phosphodiesterase inhibitor.

Abstract: Novel benzoheterocyclic compound of the formula (1): ##STR1## and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist or oxytocin antagonist.

Abstract: Apoptosis regulating compositions each comprising a member selected from a series of carbostyril derivatives and salts thereof, inclusive of carbostyril derivatives of general formula (1) ##STR1## and salts thereof, as an active ingredient are provided. The apoptosis regulating compositions of the invention are of use as anticancer agents, antiretrovirus agents, therapeutic agents for autoimmune diseases, therapeutic agents for thrombocytopenia, therapeutic agents for Alzheimer's disease, therapeutic agents for diseases of the liver, and cancer metastasis inhibitors, among others.

Abstract: Novel carbostyril derivatives of the formula: ##STR1## wherein R.sup.1 is H, NO.sub.2, alkoxy, alkoxycarbonyl, alkyl, halogen, optionally substituted amino, OH, CN, COOH, alkanoyloxy, hydrazinocarbonyl; q is 1 to 3, and R is a group of the formula: ##STR2## [wherein R.sup.2 is H, alkoxycarbonyl, optionally substituted phenoxycarbonyl, phenylalkenyl--CO--, optionally substituted phenylalkanoyl, alkanoyl, alkenyl--CO--, optionally substituted phenyl--SO.sub.2 --, --CONR.sup.8 R.sup.9, optionally substituted heterocyclic group--CO--, naphthyl--CO--, thienylalkanoyl, tricyclo[3.3.1.1]alkanoyl, ##STR3## (R.sup.13 is OH, optionally substituted alkoxy, --NR.sup.32 R.sup.33, --O--A--(E).sub.l --NR.sup.4 R.sup.5, --(B).sub.l --NR.sup.6 R.sup.7, etc.), n is 1 or 2, m is 0 or 1 to 3, R.sup.3 is alkyl, R.sup.10 is --(CO).sub.l --NR.sup.11 R.sup.

Abstract: A pharmaceutical preparation comprising at least one compound selected from the group consisting of carbostyril derivatives having the general formula: ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group optionally having hydroxy group as a substituent; R.sup.2 is a phenyl(lower alkyl) group optionally having 1 to 3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring, pyridyl(lower alkyl) group, or a group of the formula --A--NR.sup.3 R.sup.4 (wherein A is a lower alkylene group, R.sup.3 and R.sup.4 are the same or different and represent a lower alkyl group or phenyl group), and a salt thereof, which is useful as an agent for treating thrombosis, more particularly, as an agent for inhibiting platelet aggregation and as an agent for platelet aggregate dissociation.

Abstract: Method for prophylaxis and treatment of heart diseases using a carbostyril derivative-of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A--NR.sup.4 R.sup.5 (R.sup.4 and R.sup.

Abstract: Novel carbostyril derivatives of the formula: ##STR1## wherein X is 0 or S; Y is H or alkyl; R.sup.A is a group of the ##STR2## {wherein n is 1 or 2, A is alkylene, R.sup.1 is benzoyl having optionally 1-3 substituents, R.sup.2A is ##STR3## is (i) alkoxy, (ii) substituted or unsubstituted 5- or 6-membered heterocylic group, (iii) alkenylthio, (iv) pyrrolidinyl-alkyl--S--, (v) pyrrolidinyl-alkyl--SO--, (vi) pyrrolidinyl-alkyl--SO.sub.2 --, (vii) --O--B--NR.sup.4 R.sup.5 [B is alkylene having optionally OH, R.sup.4 is H, R.sup.5 is tricyclo[3.3.1.1]decanyl, tricyclo[3.3.1.1]decanylalkyl, etc., or R.sup.4 and R.sup.5 may together form a group of ##STR4## (R.sup.6 is substituted or unsubstituted amino)] or (viii) substituted alkoxy; m is 1 to 3]}, which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.

Abstract: Method for the treatment of congestive heart failure or paroxymal frequent heart pulse using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of -A-NR.sup.4 R.sup.5 (R.sup.4 and R.sup.

Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, OH, etc,; R.sup.2 is H, alkyl, halogen or alkoxy; R.sup.3 is phenyl-alkanoylamino, or ##STR2## R.sup.4 is H, --NR.sup.6 R.sup.7, alkenyloxy, HO-alkyl, --O--CO--A--NR.sup.8 R.sup.9, etc.; R.sup.5 is H, OH, etc., or a salt thereof, which have excellent vasopressin antagonistic activities and useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.

Abstract: Novel carbostyril derivatives of the formula: ##STR1## wherein R.sup.1 is H, NO.sub.2, alkoxy, alkoxycarbonyl, alkyl, halogen, optionally substituted amino, OH, CN, COOH, alkanoyloxy, hydrazinocarbonyl; q is 1 to 3, and R is a group of the formula ##STR2## [wherein R.sup.2 is H, alkoxycarbonyl, optionally substituted phenoxycarbonyl, phenylalkenyl-CO-, optionally substituted phenylalkanoyl, alkanoyl, alkenyl-CO-, optionally substituted phenyl--SO.sub.2 --, --CONR.sup.8 R.sup.9, optionally substituted heterocyclic group--CO--, naphthyl--CO--, thienylalkanoyl, tricyclo[3.3.1.1]alkanoyl, ##STR3## (R.sup.13 is OH, optionally substituted alkoxy, --NR.sup.32 R.sup.33, --O--A--(E).sub.l --NR.sup.4 R.sup.5, --(B).sub.l 'NR.sup.6 R.sup.7, etc.), n is 1 or 2, m is 0 or 1 to 3, R.sup.3 is alkyl, R.sup.10 is --(CO).sub.l --NR.sup.11 R.sup.

Abstract: Method for prophylaxis and treatment of heart diseases using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A-NR.sup.4 R.sup.5 (R.sup.4 and R.sup.

Abstract: Method for prophylaxis and treatment of heart diseases using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cyclocalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoyalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A--NR.sup.4 R.sup.5 (R.sup.4 and R.sup.

Abstract: Novel 3-formyl-4-oxoquinoline compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen atom or a lower alkanoyl, R.sup.2 is hydrogen atom or a lower alkyl, R.sup.3 is a lower alkyl, and X is halogen, and pharmaceutically acceptable salts thereof, said compounds having excellent antimicrobial activity and hence being useful as an antimicrobial agent, and a pharmaceutical composition containing said compound as an active ingredient.

Abstract: A carbostyril compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are as defined or its pharmaceutically acceptable salt, composition containing the compound and processes for preparing the same are disclosed.The compound is useful as a cardiotonic agent.

Abstract: Novel carbostyril derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen atom or a lower alkyl group, R.sup.2 is a lower alkyl group or a group of the formula: ##STR2## R.sup.3 is a lower alkylthio group, a lower alkyl group, a lower alkoxy group, phenoxy group, a phenyl(lower)alkoxy group, a lower alkenyloxy group, a phenyl group which may have a substituent selected from a lower alkoxy and a lower alkylenedioxy group on the phenyl ring, or a group of the formula: --NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are the same or different and are each hydrogen atom or a lower alkyl group), and X is oxygen atom or sulfur atom, provided that when R.sup.1 is hydrogen atom and R.sup.2 is the group of the formula: ##STR3## X is not oxygen atom and R.sup.