The discovery of adamantyl-derived, inhaled, long acting β2-adrenoreceptor agonists

被引：31

作者：

Brown, Alan D. ^{[2
]}

Bunnage, Mark E. ^{[2
]}

Glossop, Paul A. ^{[2
]}

James, Kim ^{[2
]}

Jones, Rhys ^{[2
]}

Lane, Charlotte A. L. ^{[2
]}

Lewthwaite, Russell A. ^{[2
]}

Mantell, Simon ^{[2
]}

Perros-Huguet, Christelle ^{[2
]}

Price, David A. ^{[1
]}

Trevethick, Mike ^{[2
]}

Webster, Rob ^{[2
]}

机构：

[1] Pfizer Inc, Pfizer Global Res & Dev, Groton New London Labs, Groton, CT 06340 USA

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 04期

关键词：

beta(2); adrenoreceptor; adamantyl; saligenin; asthma; crystalline;

D O I：

10.1016/j.bmcl.2008.01.034

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design and pro. le of a series of adamantyl-containing long acting beta(2)-adrenoreceptor agonists are described. An optimal pharmacokinetic profile of low oral bioavailability was combined with a strong pharmacology pro. le when assessed using a guinea pig trachea tissue model. A focus was then placed on developing a robust synthetic route to ensure rapid delivery of material for clinical trials. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：1280 / 1283

页数：4

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