The discovery of (R)-2-(sec-butylamino)-N(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994) -: A potent and efficacious p38α MAP kinase inhibitor

被引：23

作者：

Hynes, John, Jr. ^{[1
]}

Wu, Hong ^{[1
]}

Pitt, Sidney ^{[1
]}

Shen, Ding Ren ^{[1
]}

Zhang, Rosemary ^{[1
]}

Schieven, Gary L. ^{[1
]}

Gillooly, Kathleen M. ^{[1
]}

Shuster, David J. ^{[1
]}

Taylor, Tracy L. ^{[1
]}

Yang, XiaoXia ^{[1
]}

McIntyre, Kim W. ^{[1
]}

McKinnon, Murray ^{[1
]}

Zhang, Hongjian ^{[1
]}

Marathe, Punit H. ^{[1
]}

Doweyko, Arthur M. ^{[1
]}

Kish, Kevin ^{[1
]}

Kiefer, Susan E. ^{[1
]}

Sack, John S. ^{[1
]}

Newitt, John A. ^{[1
]}

Barrish, Joel C. ^{[1
]}

Dodd, John ^{[1
]}

Leftheris, Katerina ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 06期

关键词：

D O I：

10.1016/j.bmcl.2008.02.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel structural class of p38 alpha MAP kinase inhibitors has been identified via iterative SAR studies of a focused deck screen hit. Optimization of the lead series generated 6e, BMS-640994, a potent and selective p38 alpha inhibitor that is orally efficacious in rodent models of acute and chronic inflammation. (C) 2008 Elsevier Ltd. All rights reserved.

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收藏

页码：1762 / 1767

页数：6

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