Discovery of aryl aminoquinazoline pyridones as potent selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit

被引：38

作者：

Hu, Essa ^{[1
,7
]}

Tasker, Andrew ^{[1
,7
]}

White, Ryan D. ^{[1
,7
]}

Kunz, Roxanne K. ^{[1
,7
]}

Human, Jason ^{[1
,7
]}

Chen, Ning ^{[1
,7
]}

Buerli, Roland ^{[1
,7
]}

Hungate, Randall ^{[1
,7
]}

Novak, Perry ^{[5
,8
]}

Itano, Andrea ^{[2
]}

Zhang, Xuxia ^{[2
]}

Yu, Violeta ^{[3
]}

Nguyen, Yen ^{[3
]}

Tudor, Yanyan ^{[3
]}

Plant, Matthew ^{[2
]}

Flynn, Shaun ^{[3
]}

Xu, Yang ^{[4
]}

Meagher, Kristin L. ^{[6
]}

Whittington, Douglas A. ^{[6
]}

Ng, Gordon Y. ^{[2
]}

机构：

[1] Amgen Inc, Dept Med Chem, Thousand Oaks, CA 91320 USA

[2] Amgen Inc, Dept Inflammat, Thousand Oaks, CA 91320 USA

[3] Amgen Inc, Dept HTS & Mol Pharmacol, Thousand Oaks, CA 91320 USA

[4] Amgen Inc, Dept Pharmacokinet & Drug Metab, Thousand Oaks, CA 91320 USA

[5] Amgen Inc, Dept Small Mol Proc Dev, Thousand Oaks, CA 91320 USA

[6] Amgen Inc, Dept Mol Struct, Thousand Oaks, CA 91320 USA

[7] Amgen Inc, Dept Med Chem, Cambridge, MA 02139 USA

[8] Amgen Inc, Dept Small Mol Proc Dev, Cambridge, MA 02139 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 11期

关键词：

D O I：

10.1021/jm800188g

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibition of c-Kit has the potential to treat mast cell associated fibrotic diseases. We report the discovery of several aminoquinazoline pyridones that are potent inhibitors of c-Kit with greater than 200-fold selectivity against KDR, p38, Lck, and Src. In vivo efficacy of pyridone 16 by dose-dependent inhibition of histamine release was demonstrated in a rodent pharmacodynamic model of mast cell activation.

引用

页码：3065 / 3068

页数：4

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