Abstract: A coating dispersion soluble in the lower digestive tract which is prepared by blending a hydroxypropyl methylcellulose acetate succinate (HPMCAS) soluble at around pH 7 with a conventional plasticizer and an anion surfactant and further adding an acid, wherein the HPMCAS has an average particle size of 10 ?m or less and is dispersed at a concentration of 2 to 20% by weight, and the acid is used in an amount of 1 to 10 parts by weight per 100 parts by weight of HPMCAS, and a sustained release coated preparation capable of releasing a medicament in the large intestine at the lower digestive tract, which is prepared by coating a medicament-containing solid preparation such as a granular core with the coating dispersion.

Abstract: A new active oxygen scavenger which comprises as an active ingredient a tetrazolylalkoxy-dihydrocarbostyril compound of the formula (I): wherein R is cycloalkyl group, A is lower alkylene group, and the bond between 3- and 4-positions of the carbostyril nucleus is single bond or double bond, or a salt thereof, and an agent for the prevention or treatment of an acute cerebral infarction comprising the same active ingredient.

Abstract: A new active oxygen scavenger which comprises as an active ingredient a tetrazolylalkoxy-dihydrocarbostyril compound of the formula (I): 1

Abstract: A thiazole compound of the formula: ##STR1## wherein T is lower alkylene; u is 0 or 1; R.sup.1 and R.sup.2 are the same or different and are each H, or lower alkyl, etc.; R.sup.3 is ##STR2## R.sup.4 is H or lower alkanoyloxy-lower alkyl, which shows inhibitory activity on protein kinase C (PKC, Ca.sup.2+ /phospholipid-depending serine/threonine protein phosphatase), and are useful as a protein kinase C inhibitor.

Abstract: A benzoheterocyclic derivative of the following formula [1]: ##STR1## and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity, vasopressin agonistic activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist, vasopressin agonist or oxytocin antagonist.

Abstract: Novel benzazepine derivative of the formula [1]: ##STR1## wherein R.sup.1 is H or halogen, A is lower alkylene, R.sup.2 and R.sup.3 are the same or different and each H, lower alkoxy, lower alkyl having optionally a lower alkoxy substituent, etc., or R.sup.2 and R.sup.3 may combine together with the nitrogen to which they bond to form a 5- to 7-membered saturated heterocyclic group which may optionally be substituted by a lower alkyl, etc., R.sup.4 is H, lower alkyl, OH, etc., R.sup.5 is --NHR.sup.6 (R.sup.6 is lower alkyl) or pyrrolidinyl, or a salt thereof, which show excellent anti-vasopressin activity, oxytocin antagonistic activity and vasopressin agonistic activity, and are useful as a vasopressin antagonist, a vasopressin agonist and an oxytocin antagonist.

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, phenylalkoxy, 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 substitued 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 beign optionally replaced by O, S, SO, SO.sub.

Abstract: A method for the prophylaxis and treatment of diseases induced by accelerated INF-.alpha. secretion, such as rheumatoid arthritis, endotoxin shock, adult respiratory distress syndrome, thermal burn, asthma, myocardial infarction, acute phase of viral myocardiosis, etc. which comprises administering a carbostyril compound of the formula: ##STR1## wherein R.sup.1 is H or lower alkyl, and R.sup.2 is phenyl(lower)alkyl having optionally 1 to 3 lower alkoxy substituents on the phenyl ring, or a pharmaceutically acceptable salt thereof to a subject.

Abstract: An agent for prophylaxis or treatment of cataract, which comprises as an active ingredient at least one compound selected from a group consisting of a carbostyril compound of the formula: ##STR1## wherein R.sup.1 is a lower alkanoylamino-substituted lower alkoxy group, and the bond between the 3- and 4-positions of the carbostyril nucleus is single bond or double bond, or a salt thereof, 5-dimethylamino-1-?4-(2-methylbenzoylamino)benzoyl!-2,3,4,5-tetrahydro-1H- benzazepine and 5-hydroxy-7-chloro-1-?2-methyl-4-(2-methylbenzoylamino)benzoyl!-2,3,4,5-te trahydro-1H-benzazepine, a method for prophylaxis or treatment of cataract using the same.

Abstract: Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 is cyclopropyl which may have 1 to 3 substituents of alkyl and halogen; phenyl which may be substituted by 1 to 3 substituents of alkoxy, halogen and OH; alkyl which may be substituted by halogen, alkanoyloxy or OH; alkenyl; or thienyl, R.sup.2 is 5- to 9-membered saturated or unsaturated heterocyclic ring which may be substituted, R.sup.3 is alkyl, R is H or 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: Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 is cyclopropyl which may have 1 to 3 substituents of alkyl and halogen; phenyl which may be substituted by 1 to 3 substituents of alkoxy, halogen and OH; alkyl which may be substituted by halogen, alkanoyloxy or OH; alkenyl; or thienyl, R.sup.2 is 5- to 9-membered saturated or unsaturated heterocyclic ring which may be sustituted, R.sup.3 is alkyl, R is H or 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 carton including a front wall, a rear wall, a right and a left side walls, a bottom wall and a top wall. A longitudinal partition flap is formed by cutting an approximately central portion of the front wall in a U shape. A partition wall of a cross in a plan view consisting of a lateral partition wall, a longitudinal partition wall and the longitudinal partition flap is integrally provided inside the carton. Each side wall has a perforated cut line continuous with an outer end of the perforated tear part formed at each side of the U-shaped cutout. Contents in the carton are exposed and displayed by removing an upper part of the carton along the perforated tear part. The contents are supported by the cross-shaped partition wall and therefore prevented from lying even when decreased in number.

Abstract: This invention provides an aqueous composition wherein a hardly water-soluble active compound, 6-?3-(3,4-dimethoxybenzyl)amino-2-hydroxypropoxy!carbostyril or a salt thereof is dissolved in water in an effective amount, particularly in an amount sufficient for exhibiting the pharmacological activities, by using as a solubilizer DL-lactic acid.

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: An antiarrhythmic agent which comprises as an active ingredient a carbostyril derivative of the formula: ##STR1## wherein R.sub.1 is hydrogen atom or a lower alkyl group, and R.sub.2 is a phenyl-lower alkyl group which has optionally 1 to 3 substituents of a lower alkoxy group on the phenyl ring, or a pharmaceutically acceptable salt thereof.

Abstract: Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 is cyclopropyl which may have 1 to 3 substituents of alkyl and halogen; phenyl which may be substituted by 1 to 3 substituents of alkoxy, halogen and OH; alkyl which may be substituted by halogen, alkanoyloxy or OH; alkenyl; or thienyl, R.sup.2 is 5- to 9-membered saturated or unsaturated heterocyclic ring which may be sustituted, R.sup.3 is alkyl or halogen, R.sup.4 is alkyl or halogen, R is H or alkyl, R.sup.1 and R.sup.3 may be taken together to form ##STR2## wherein R.sup.31 is H or alkyl, and X is halogen, provided that R.sup.3 and R.sup.4 are not simultaneously halogen, and 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: Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 is cyclopropyl which may have 1 to 3 substituents of alkyl and halogen; phenyl which may be substituted by 1 to 3 substituents of alkoxy, halogen and OH; alkyl which may be substituted by halogen, alkanoyloxy or OH; alkenyl; or thienyl, R.sup.2 is 5- to 9-membered saturated or unsaturated heterocyclic ring which may be sustituted, R.sup.3 is alkyl, R is H or 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 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: Useful as intermediates for antimicrobacterial agents are compounds of the formulas ##STR1## wherein R.sup.1A is a cyclopropyl which may be substituted by 1 to 3 substituents selected from the group consisting of a C.sub.1 -C.sub.6 alkyl and a halogen atom; a phenyl which may be substituted by 1 to 3 substituents selected from the group consisting of a C.sub.1 -C.sub.6 alkoxy, a halogen atom and hydroxy on the phenyl group; a C.sub.1 -C.sub.6 alkyl which may be substituted by a halogen atom, a C.sub.1 -C.sub.6 alkanoyloxy or hydroxy; a C.sub.2 -C.sub.6 alkenyl; or thienyl,R.sup.3A is a C.sub.1 -C.sub.6 alkyl group, or a halogen atom,R.sup.4 is a C.sub.1 -C.sub.6 alkyl group,R.sup.14 is a hydrogen atom, a lower alkyl group, or a group of the formula ##STR2## R.sup.31 is hydrogen or a C.sub.1 -C.sub.6 alkyl group, and X and X.sup.4 are halogen atoms, and salts thereof.