1292300-75-4Relevant articles and documents
Discovery of N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4- methyl-1,3-thiazol-2-yl}acetamide (TASP0415914) as an orally potent phosphoinositide 3-kinase γ inhibitor for the treatment of inflammatory diseases
Oka, Yusuke,Yabuuchi, Tetsuya,Oi, Takahiro,Kuroda, Shoichi,Fujii, Yasuyuki,Ohtake, Hidenori,Inoue, Tomoyuki,Wakahara, Shunichi,Kimura, Kayo,Fujita, Kiyoko,Endo, Mayumi,Taguchi, Kyoko,Sekiguchi, Yoshinori
, p. 7578 - 7583 (2013)
Class I phosphoinositide 3-kinases (PI3Ks), particularly PI3Kγ, have become attractive drug targets for inflammatory and autoimmune disorders such as rheumatoid arthritis. Herein, we describe the synthesis and the structure-activity relationships (SAR) of a series of 2-amino-5-oxadiazolyl thiazoles, culminating in the identification of 8j (TASP0415914), an orally potent inhibitor of phosphoinositide 3-kinase γ (PI3Kγ). TASP0415914 demonstrated good potency in a cell-based assay and, furthermore, exhibited in vivo efficacy in a collagen induced arthritis (CIA) model in mice after oral administration.