Carbostyril derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546141, A61K 3147, C07D21700

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active

054362547

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.12 ], and the bond between 3- and 4-position of carbostyril nucleus is single or double bond, 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.

REFERENCES:
patent: 4895841 (1990-01-01), Sugimoto et al.
patent: 5100901 (1992-03-01), Sugimoto et al.
J. Med. Chem., 24(7), 777-782 (1981).
Chemical Abstracts, vol. 81, p. 450 (Abstract No. 77786r), 1974.
Chemical Abstracts, vol. 102, p. 17 (Abstract No. 143336z), 1985.
Journal of Medicinal Chemistry, vol. 24, No. 7, Jul. 1981, pp. 777-782, 1981.
Chemical Abstracts, vol. 108, p. 13 (Abstract No. 112151e), 1988.

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