65797-52-6Relevant articles and documents
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity
Gong, Hua,Weinstein, David S.,Lu, Zhonghui,Duan, James J.-W.,Stachura, Sylwia,Haque, Lauren,Karmakar, Ananta,Hemagiri, Hemalatha,Raut, Dhanya Kumar,Gupta, Arun Kumar,Khan, Javed,Camac, Dan,Sack, John S.,Pudzianowski, Andrew,Wu, Dauh-Rurng,Yarde, Melissa,Shen, Ding-Ren,Borowski, Virna,Xie, Jenny H.,Sun, Huadong,D'Arienzo, Celia,Dabros, Marta,Galella, Michael A.,Wang, Faye,Weigelt, Carolyn A.,Zhao, Qihong,Foster, William,Somerville, John E.,Salter-Cid, Luisa M.,Barrish, Joel C.,Carter, Percy H.,Dhar, T.G. Murali
, p. 85 - 93 (2018)
We disclose the optimization of a high throughput screening hit to yield benzothiazine and tetrahydroquinoline sulfonamides as potent RORγt inverse agonists. However, a majority of these compounds showed potent activity against pregnane X receptor (PXR) and modest activity against liver X receptor α (LXRα). Structure-based drug design (SBDD) led to the identification of benzothiazine and tetrahydroquinoline sulfonamide analogs which completely dialed out LXRα activity and were less potent at PXR. Pharmacodynamic (PD) data for compound 35 in an IL-23 induced IL-17 mouse model is discussed along with the implications of a high Ymax in the PXR assay for long term preclinical pharmacokinetic (PK) studies.
Cobalt-Catalyzed Selective Functionalization of Aniline Derivatives with Hexafluoroisopropanol
Zhao, He,Zhao, Shuo,Li, Xiu,Deng, Yinyue,Jiang, Huanfeng,Zhang, Min
supporting information, p. 218 - 222 (2019/01/10)
A cobalt-catalyzed site-selective functionalization of aniline derivatives with hexafluoroisopropanol, which enables the synthesis of a wide array of fluoroalkylated anilines, a class of highly valuable building blocks for further preparation of fluorinated functional products, is reported. The developed transformation proceeds with operational simplicity, use of earth-abundant metal catalyst, broad substrate scope, good functional group tolerance, and mild reaction conditions.
ANILINO LIVER X-RECEPTOR MODULATORS
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Page 52, (2010/02/04)
The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.