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

  • Bioorg Med Chem Lett. 2013 Sep 1;23(17):5014-21. doi: 10.1016/j.bmcl.2013.06.008.
Michael Siu  1 ,  Richard Pastor ,  Wendy Liu ,  Kathy Barrett ,  Megan Berry ,  Wade S Blair ,  Christine Chang ,  Jacob Z Chen ,  Charles Eigenbrot ,  Nico Ghilardi ,  Paul Gibbons ,  Haiying He ,  Christopher A Hurley ,  Jane R Kenny ,  S Cyrus Khojasteh ,  Hoa Le ,  Leslie Lee ,  Joseph P Lyssikatos ,  Steve Magnuson ,  Rebecca Pulk ,  Vickie Tsui ,  Mark Ultsch ,  Yisong Xiao ,  Bing-yan Zhu ,  Deepak Sampath
Affiliations
  • 1. Genentech, Inc, 1 DNA Way, South San Francisco, CA 94080, United States. [email protected]
PMID: 23870430 DOI: 10.1016/j.bmcl.2013.06.008
Abstract

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.

Keywords
JAK2; Janus kinase; Triazolopyridine.
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