Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants-Reference-Cited by-同舟云学术

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

Published:2016-01-28 Issue:5 Volume:59 Page:2005-2024
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Cheng Hengmiao¹,Nair Sajiv K.¹,Murray Brion W.¹,Almaden Chau¹,Bailey Simon¹,Baxi Sangita¹,Behenna Doug¹,Cho-Schultz Sujin¹,Dalvie Deepak¹,Dinh Dac M.¹,Edwards Martin P.¹,Feng Jun Li¹,Ferre Rose Ann¹,Gajiwala Ketan S.¹,Hemkens Michelle D.¹,Jackson-Fisher Amy¹,Jalaie Mehran¹,Johnson Ted O.¹,Kania Robert S.¹,Kephart Susan¹,Lafontaine Jennifer¹,Lunney Beth¹,Liu Kevin K.-C.¹,Liu Zhengyu¹,Matthews Jean¹,Nagata Asako¹,Niessen Sherry¹,Ornelas Martha A.¹,Orr Suvi T. M.¹,Pairish Mason¹,Planken Simon¹,Ren Shijian²,Richter Daniel¹,Ryan Kevin¹,Sach Neal¹,Shen Hong¹,Smeal Tod¹,Solowiej Jim¹,Sutton Scott¹,Tran Khanh¹,Tseng Elaine¹,Vernier William¹,Walls Marlena¹,Wang Shuiwang²,Weinrich Scott L.¹,Xin Shuibo²,Xu Haiwei²,Yin Min-Jean¹,Zientek Michael¹,Zhou Ru¹,Kath John C.¹

Affiliation:

1. La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, California 92121, United States

2. Wuxi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.5b01633

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