2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors

被引：20

作者：

Gerspacher, Marc ^{[1
]}

Furet, Pascal ^{[1
]}

Pissot-Soldermann, Carole ^{[1
]}

Gaul, Christoph ^{[1
]}

Holzer, Philipp ^{[1
]}

Vangrevelinghe, Eric ^{[1
]}

Lang, Marc ^{[1
]}

Erdmann, Dirk ^{[1
]}

Radimerski, Thomas ^{[1
]}

Regnier, Catherine H. ^{[1
]}

Chene, Patrick ^{[1
]}

De Pover, Alain ^{[1
]}

Hofmann, Francesco ^{[1
]}

Baffert, Fabienne ^{[1
]}

Buhl, Thomas ^{[1
]}

Aichholz, Reiner ^{[1
]}

Blasco, Francesca ^{[1
]}

Endres, Ralf ^{[1
]}

Trappe, Joerg ^{[1
]}

Drueckes, Peter ^{[1
]}

机构：

[1] Novartis Pharma AG, Novartis Inst BioMed Res, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 05期

关键词：

Janus kinase; JAK1; JAK2; JAK3; Tyk2; Kinase inhibitors; inhibitor; ADHESION KINASE INHIBITORS; DESIGN;

D O I：

10.1016/j.bmcl.2010.01.069

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel benzoxazole derivatives has been designed and shown to exhibit attractive JAK2 inhibitory profiles in biochemical and cellular assays, capable of delivering compounds with favorable PK properties in rats. Synthesis and structure-activity relationship data are also provided. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：1724 / 1727

页数：4

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