2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors

被引：39

作者：

Siu, Michael ^{[1
]}

Pastor, Richard ^{[1
]}

Liu, Wendy ^{[1
]}

Barrett, Kathy ^{[1
]}

Berry, Megan ^{[1
]}

Blair, Wade S. ^{[1
]}

Chang, Christine ^{[1
]}

Chen, Jacob Z. ^{[1
]}

Eigenbrot, Charles ^{[1
]}

Ghilardi, Nico ^{[1
]}

Gibbons, Paul ^{[1
]}

He, Haiying ^{[2
]}

Hurley, Christopher A. ^{[3
]}

Kenny, Jane R. ^{[1
]}

Khojasteh, S. Cyrus ^{[1
]}

Le, Hoa ^{[1
]}

Lee, Leslie ^{[1
]}

Lyssikatos, Joseph P. ^{[1
]}

Magnuson, Steve ^{[1
]}

Pulk, Rebecca ^{[1
]}

Tsui, Vickie ^{[1
]}

Ultsch, Mark ^{[1
]}

Xiao, Yisong ^{[2
]}

Zhu, Bing-yan ^{[1
]}

Sampath, Deepak ^{[1
]}

机构：

[1] Genentech Inc, San Francisco, CA 94080 USA

[2] WuXi AppTec Co Ltd, Shanghai 200131, Peoples R China

[3] Argenta, Spire Green Ctr 8 9, Harlow CM19 5TR, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 17期

关键词：

JAK2; Janus kinase; Triazolopyridine; JANUS KINASE 2; MYELOPROLIFERATIVE DISORDERS; ACCURATE DOCKING; DISCOVERY; GLIDE; JAK2V617F; MUTATION; THERAPY;

D O I：

10.1016/j.bmcl.2013.06.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The advancement of a series of ligand efficient 2-amino-[1,2,4]triazolo[1,5-a]pyridines, initially identified from high-throughput screening, to a JAK2 inhibitor with pharmacodynamic activity in a mouse xenograft model is disclosed. [GRAPHICS] . (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：5014 / 5021

页数：8

共 50 条

[1] 2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors
Siu, Michael
Pastor, Richard
Liu, Wendy
Barrett, Kathy
Berry, Megan
Blair, Wade S.
Chang, Christine
Chen, Jacob Z.
Eigenbrot, Charles
Ghilardi, Nico
Gibbons, Paul
He, Haiying
Hurley, Christopher A.
Kenny, Jane R.
Khojasteh, S. Cyrus
Le, Hoa
Lee, Leslie
Lyssikatos, Joseph P.
Magnuson, Steve
Pulk, Rebecca
Tsui, Vickie
Ultsch, Mark
Xiao, Yisong
Zhu, Bing-yan
Sampath, Deepak
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2014, 247
[2] A new synthesis for 1,2,4-triazolo[1,5-a]-pyridines and 1,2,4-triazolo[1,5-a]isoquinolines
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[J]. MONATSHEFTE FUR CHEMIE, 1996, 127 (11): : 1153 - 1160
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