1426802-39-2Relevant academic research and scientific papers
Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors
Wang, Yonghui,Cai, Wei,Cheng, Yaobang,Yang, Ting,Liu, Qian,Zhang, Guifeng,Meng, Qinghua,Han, Fangbin,Huang, Yafei,Zhou, Ling,Xiang, Zhijun,Zhao, Yong-Gang,Xu, Yan,Cheng, Ziqiang,Lu, Sijie,Wu, Qianqian,Xiang, Jia-Ning,Elliott, John D.,Leung, Stewart,Ren, Feng,Lin, Xichen
supporting information, p. 787 - 792 (2015/07/15)
A novel series of biaryl amides was identified as RORγt inhibitors through core replacement of a starting hit 1. Structure-activity relationship exploration on the biaryl moiety led to discovery of potent RORγt inhibitors with good oral bioavailability and CNS penetration. Compounds 9a and 9g demonstrated excellent in vivo efficacy in EAE mice dose dependently with once daily oral administration.
NOVEL COMPOUNDS
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Page/Page column 80; 81, (2013/03/28)
Disclosed are novel retinoid-related orphan receptor gamma (RORy) modulators and their use in the treatment of diseases mediated by RORy.
