4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists

被引:13
|
作者
Aranapakam, V [1 ]
Albright, JD [1 ]
Grosu, GT [1 ]
Chan, PS [1 ]
Coupet, J [1 ]
Saunders, T [1 ]
Ru, X [1 ]
Mazandarani, H [1 ]
机构
[1] Wyeth Ayerst Res, Pearl River, NY 10965 USA
关键词
D O I
10.1016/S0960-894X(99)00278-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Synthesis and structure-activity relationships (SAR) of arginine vasopressin receptor (AVP) antagonists are described. Potent and orally active compounds are prepared when tricyclic 10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine moiety in VPA-985 1 is replaced with a compound 7 or 12. (C) 1999 Elsevier Science Ltd. All rights reserved.
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页码:1733 / 1736
页数:4
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