Discovery of potent, selective, and orally bioavailable inhibitors of interleukin-1 receptor-associate kinase-4
摘要:
In this Letter, we report the continued optimization of the N-acyl-2-aminobenzimidazole series, focusing in particular on the N-alkyl substituent and 5-position of the benzimidazole based on the binding mode and the early SAR. These efforts led to the discovery of 16, a highly potent, selective, and orally bioavailable inhibitor of IRAK-4. (C) 2015 Elsevier Ltd. All rights reserved.
[EN] CAFFEINE INHIBITORS OF MTHFD2 AND USES THEREOF<br/>[FR] INHIBITEURS DE CAFÉINE DE MTHFD2 ET LEURS UTILISATIONS
申请人:RAZE THERAPEUTICS INC
公开号:WO2017106352A1
公开(公告)日:2017-06-22
The present invention provides compounds, compositions thereof, and methods of using the same.
本发明提供了化合物、其组合物以及使用方法。
[EN] S1P MODULATING AGENTS<br/>[FR] AGENTS MODULATEURS DE S1P
申请人:BIOGEN IDEC INC
公开号:WO2014120764A1
公开(公告)日:2014-08-07
Compounds of formula (I) can modulate the activity of one or more S 1P receptors. Sphingosine 1-phosphate (S IP) is a lysophospholipid mediator that evokes a variety of cellular responses by stimulation of five members of the endothelial cell differentiation gene (EDG) receptor family, namely S1P1, S1P2, S1P3, S1P4, and S1P5 (formerly EDG1, EDG5, EDG3, EDG6 and EDG8). The EDG receptors are G-protein coupled receptors (GPCRs) and on stimulation propagate second messenger signals via activation of heterotrimeric G-protein alpha (Ga.) subunits and beta-gamma (G()y) dimers.
[EN] S1P AND/OR ATX MODULATING AGENTS<br/>[FR] AGENTS DE MODULATION DE S1P ET/OU ATX
申请人:BIOGEN IDEC INC
公开号:WO2014081756A1
公开(公告)日:2014-05-30
Compounds of formula (I), and pharmaceutically acceptable salts thereof, can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).
化合物的结构式(I)及其药用盐可以调节一个或多个SIP受体的活性和/或自体毒素酶(ATX)的活性。
S1P AND/OR ATX MODULATING AGENTS
申请人:BIOGEN IDEC MA INC.
公开号:US20150299123A1
公开(公告)日:2015-10-22
Compounds of formula (I), and pharmaceutically acceptable salts thereof, can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).