Heterocyclic acetamide and benzamide derivatives as potent and selective β3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles

被引：10

作者：

Goble, Stephen D. ^{[1
]}

Wang, Liping ^{[1
]}

Howell, K. Lulu ^{[1
]}

Bansal, Alka ^{[1
]}

Berger, Richard ^{[1
]}

Brockunier, Linda ^{[1
]}

DiSalvo, Jerry ^{[1
]}

Feighner, Scott ^{[1
]}

Harper, Bart ^{[1
]}

He, Jiafang ^{[1
]}

Hurley, Amanda ^{[1
]}

Hreniuk, Donna ^{[1
]}

Parmee, Emma ^{[1
]}

Robbins, Michael ^{[1
]}

Salituro, Gino ^{[1
]}

Sanfiz, Anthony ^{[1
]}

Streckfuss, Eric ^{[1
]}

Watkins, Eloisa ^{[1
]}

Weber, Ann E. ^{[1
]}

Struthers, Mary ^{[1
]}

Edmondson, Scott D. ^{[1
]}

机构：

[1] Merck Res Labs, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 06期

关键词：

beta 3 Adrenergic receptor agonist; Overactive bladder; DISCOVERY; SUBTYPES; PHARMACOLOGY;

D O I：

10.1016/j.bmcl.2010.01.130

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of amide derived beta 3-adrenergic receptor (AR) agonists is described. The discovery and optimization of several series of compounds derived from 1, is used to lay the SAR foundation for second generation beta 3-AR agonists for the treatment of overactive bladder. (C) 2010 Elsevier Ltd. All rights reserved.

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页码：1895 / 1899

页数：5

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