Benzoheterocyclic compounds

Details Benzoheterocyclic compounds Benzoheterocyclic compounds

1993-06-10

1996-09-24

Bond, Robert T.

Organic compounds -- part of the class 532-570 series

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

540473, C07D22316, C07D24312, A61K 3155

Patent

active

055592309

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.2 or a group: --N(R).sup.12 and further these groups having optionally 1 to 3 substituents of alkyl, alkoxycarbonyl, carboxy, OH, O, alkanoyloxy, etc., 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: 3035047 (1962-05-01), Perron et al.
patent: 4582909 (1986-04-01), Butler et al.
patent: 4677112 (1987-06-01), Butler et al.
patent: 4760064 (1988-07-01), Tominaga et al.
Yoshitaka Yamamura, Hidenori Ogawa, Tomihiko Chihara, Kazumi Kondo, Toshiyuki Onogawa, Shigeki Nakamura-Toyoki Mori, Michiaki Tominaga and Youichi Yabuuchi, OPC-21268, An Orally Effective, Nonpeptide Vasopressin V1 Receptor Antagonist, Science, vol. 252, pp. 572-574 (Apr. 1991).

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