1426804-84-3Relevant academic research and scientific papers
BIARYL UREA DERIVATIVE OR SALT THEREOF, AND MANUFACTURING AND APPLICATION OF SAME
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, (2019/05/10)
The present invention discloses a biaryl urea RORγt inhibitor, and specifically relates to a biaryl urea derivative, as represented by formula I, with an RORγt inhibiting activity, and a preparation process thereof, and a pharmaceutical composition comprising the compound. Further disclosed is use of the compound for treating an RORγt-related disease.
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.
