Discovery of potent, selective, and orally bioavailable inhibitors of interleukin-1 receptor-associate kinase-4
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.
Wang, Zhulun,Sun, Daqing,Johnstone, Sheree,Cao, Zhaodan,Gao, Xiong,Jaen, Juan C.,Liu, Jingqian,Lively, Sarah,Miao, Shichang,Sudom, Athena,Tomooka, Craig,Walker, Nigel P.C.,Wright, Matthew,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
p. 5546 - 5550
(2015/11/17)
Benzimidazole derivatives
Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, immune response regulation and cell proliferation. The subject compounds are 2-amino-imidazole derivatives.
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(2008/06/13)
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