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2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors |
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| Authors: | Michael Siu 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 Deepak Sampath |
| Affiliation: | 1. Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States;2. WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, PR China;3. Argenta, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom |
| 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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