5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4] benzodiazepine-10(11H)-YL carbonyl)-2-pyridinyl] benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists

被引:16
作者
Aranapakam, V [1 ]
Albright, JD [1 ]
Grosu, GT [1 ]
Santos, EGD [1 ]
Chan, PS [1 ]
Coupet, J [1 ]
Ru, X [1 ]
Saunders, T [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)00279-6
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 orally active arginine vasopressin (AVP) receptor antagonists are discussed. Potent and orally active AVP receptor antagonists are produced when ring A of VPA-985 (1) is replaced with a 3-pyridinyl unit (2b). (C) 1999 Elsevier Science Ltd. All rights reserved.
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收藏
页码:1737 / 1740
页数:4
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