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Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis

Jian Liu, D Guiadeen,Arto D Krikorian,Xiaolei Gao,James Wang,Sobhana Babu Boga,Abdulbasit Alhassan,Younong Yu,Henry A Vaccaro,Shilan Liu,Chundao Yang,Hao Wu,Alan B Cooper,Jos De Man,Allard Kaptein,Kevin Maloney,Viktor Hornak, Yingduo Gao, Thierry O Fischmann,Hans C A Raaijmakers,Diep Vupham,Jeremy Presland,My Mansueto,Zangwei Xu,Erica Leccese,Jie Zhanghoover,Ian Knemeyer,Charles G Garlisi,Nathan Bays,Peter Stivers,Philip E Brandish,Alexandra Hicks,Ronald Kim,Joseph A Kozlowski

ACS medicinal chemistry letters（2016）

Cited 37|Views55
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Key words
BTK,X-ray crystal structure,human peripheral blood mononuclear cells (hPBMC),kinase selectivity,pharmacokinetic,rat CIA model,rheumatoid arthritis (RA),whole blood
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