Carbostyril derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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5142228, 5142352, 514 63, 514312, 514255, 514303, 514310, 514248, 514259, 536 41, 536173, 544 582, 544 62, 544128, 544363, 544333, 544284, 544406, 544235, 546 14, 546118, 546148, 546157, C07H 504, C07D215227, C07D295195, A61K 3147

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052254020

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: 4960883 (1990-10-01), Tanabe et al.
J. Med. Chem., 24(7), 777-782 (1981), "Opiate Receptor Interaction of Compounds Derived from or Structurally Related to Fentanyl".
Klein et al Arch. Pharm. 1974 307(5) 360-6 Chemical Abstracts, vol. 81, 1974 Abstract 77786r.
Lobbezoo, et al. J. Med. Chem. 1981 24 777-782.

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