SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors

Timothy Forsyth; Patrick C. Kearney; Byung Gyu Kim; Henry W. B. Johnson; Naing Aay; Arlyn Arcalas; David S. Brown; Vicky Chan; Jeff Chen; Hongwang Du; Sergey Epshteyn; Adam A. Galan; Tai P. Huynh; Mohamed A. Ibrahim; Brian Kane; Elena S. Koltun; Grace Mann; Lisa E. Meyr; Matthew S. Lee; Gary L. Lewis; Robin T. Noguchi; Michael Pack; Brian H. Ridgway; Xian Shi; Craig Takeuchi; Peiwen Zu; James W. Leahy; John M. Nuss; Ron Aoyama; Stefan Engst; Steven B. Gendreau; Robert Kassees; Jia Li; Shwu-Hwa Lin; Jean-Francois Martini; Thomas Stout; Philip Tong; John Woolfrey; Wentao Zhang; Peiwen Yu

doi:10.1016/j.bmcl.2012.10.007

論文・著書情報

タイトル

和文:
英文:	SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors

著者

和文:

Timothy Forsyth, Patrick C. Kearney, Byung Gyu Kim, Henry W. B. Johnson, Naing Aay, Arlyn Arcalas, David S. Brown, Vicky Chan, Jeff Chen, Hongwang Du, Sergey Epshteyn, Adam A. Galan, Tai P. Huynh, Mohamed A. Ibrahim, Brian Kane, Elena S. Koltun, Grace Mann, Lisa E. Meyr, Matthew S. Lee, Gary L. Lewis, Robin T. Noguchi, Michael Pack, Brian H. Ridgway, Xian Shi, TAKEUCHI CRAIG, Peiwen Zu, James W. Leahy, John M. Nuss, Ron Aoyama, Stefan Engst, Steven B. Gendreau, Robert Kassees, Jia Li, Shwu-Hwa Lin, Jean-Francois Martini, Thomas Stout, Philip Tong, John Woolfrey, Wentao Zhang, Peiwen Yu.

英文:

Timothy Forsyth, Patrick C. Kearney, Byung Gyu Kim, Henry W. B. Johnson, Naing Aay, Arlyn Arcalas, David S. Brown, Vicky Chan, Jeff Chen, Hongwang Du, Sergey Epshteyn, Adam A. Galan, Tai P. Huynh, Mohamed A. Ibrahim, Brian Kane, Elena S. Koltun, Grace Mann, Lisa E. Meyr, Matthew S. Lee, Gary L. Lewis, Robin T. Noguchi, Michael Pack, Brian H. Ridgway, Xian Shi, Craig Takeuchi, Peiwen Zu, James W. Leahy, John M. Nuss, Ron Aoyama, Stefan Engst, Steven B. Gendreau, Robert Kassees, Jia Li, Shwu-Hwa Lin, Jean-Francois Martini, Thomas Stout, Philip Tong, John Woolfrey, Wentao Zhang, Peiwen Yu.

言語

English

掲載誌/書名

和文:	Bioorganic & Medicinal Chemistry Letters
英文:	Bioorganic & Medicinal Chemistry Letters

巻, 号, ページ

Vol. 22 pp. 7653-7658

出版年月

2012年

出版者

和文:
英文:	Elsevier Limited

会議名称

和文:
英文:

開催地

和文:
英文:

DOI

https://doi.org/10.1016/j.bmcl.2012.10.007

アブストラクト

We report the discovery of a series of 4-aryl-2-aminoalkylpyrimidine derivatives as potent and selectiveJAK2 inhibitors. High throughput screening of our in-house compound library led to the identification ofhit 1, from which optimization resulted in the discovery of highly potent and selective JAK2 inhibitors.Advanced lead 10d demonstrated a significant dose-dependent pharmacodynamic and antitumor effectin a mouse xenograft model. Based upon the desirable profile of 10d (XL019) it was advanced into clinicaltrials.

Home

各種検索

サポート

T2R2について

関連リンク

論文・著書情報