Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: Discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one

被引：11

作者：

Hughes, Robert O. ^{[1
]}

Walker, John K. ^{[1
]}

Rogier, D. Joseph ^{[1
]}

Heasley, Steve E. ^{[1
]}

Blevis-Bal, Rhadika M. ^{[1
]}

Benson, Alan G. ^{[1
]}

Jacobsen, E. Jon ^{[1
]}

Cubbage, Jerry W. ^{[1
]}

Fobian, Yvette M. ^{[1
]}

Owen, Dafydd R. ^{[2
]}

Freskos, John N. ^{[1
]}

Molyneaux, John M. ^{[1
]}

Brown, David L. ^{[1
]}

Acker, Brad A. ^{[1
]}

Maddux, Todd M. ^{[1
]}

Tollefson, Mike B. ^{[1
]}

Moon, Joseph B. ^{[1
]}

Mischke, Brent V. ^{[1
]}

Rumsey, Jeanne M. ^{[1
]}

Zheng, Yi ^{[1
]}

MacInnes, Alan ^{[1
]}

Bond, Brian R. ^{[1
]}

Yu, Ying ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, St Louis, MO 63017 USA

[2] Pfizer Global Res & Dev, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 17期

关键词：

PDE5; Aminopyrazinone; Pharmacokinetics;

D O I：

10.1016/j.bmcl.2009.07.019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe efforts to improve the pharmacokinetic profile of the aminopyridopyrazinone class of PDE5 inhibitors. These efforts led to the discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl) pyrido[3,4-b]pyrazin-2(1H)-one, a potent and selective inhibitor of PDE5 with an excellent PK profile. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：5209 / 5213

页数：5

共 6 条

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