Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-07-15
1999-11-16
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514183, 514220, 5142282, 5142285, 5142328, 5142345, 514248, 514249, 514250, 514259, 514267, 540461, 540471, 540473, 540495, 540510, 540517, 540557, 540567, 540569, 540573, 544 60, 544 62, 544115, 544116, 544234, 544235, 544237, 544250, 544251, 544283, 544345, 544353, A61K 3155, A61K 3133, A61K 31495, C07D24312, C07D24314, C07D24506, C07D24136, C07D23972
Patent
active
059858699
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.2 or a group: --N(R.sup.13)-- 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:
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Yoshitake Yamamura, Hidenori Ogawa, Tomihiko Chihara, Kazumi Kondo, Toshiyuki Onogawa, Shigeki Nakamura, Toyo Mori, Michiaki Tominaga and Youichi Yabucchi, OPC-21268, An Orally Effective, Nonpeptide Vasopressin V1 Receptor Antagonist, Science, vol. 252, pp. 572-574 (Apr. 1991).
Ogawa et al., CAS printout of WO 91/05549, May 1991.
Komatsu Hajime
Kondo Kazumi
Kora Shinya
Miyamoto Hisashi
Nakaya Kenji
Coleman Brenda
Otsuka Pharmaceutical Company Limited
Raymond Richard L.
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