269058-49-3Relevant articles and documents
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis
Cao, Shengtian,Yang, Xinye,Zhang, Zheng,Wu, Junwen,Chi, Bo,Chen, Hong,Yu, Jianghong,Feng, Shanshan,Xu, Yulin,Li, Jing,Zhang, Yingjun,Wang, Xiaojun,Wang, Yan
supporting information, (2022/01/24)
Non-alcoholic fatty liver disease (NAFLD) is becoming the most predominant burden of chronic liver disease worldwide. Non-alcoholic steatohepatitis (NASH), the progressive form of NAFLD, can develop into cirrhosis and hepatocellular cancer. Unfortunately, current options for therapeutic treatment of NASH are very limited. Among multiple pathways in NASH, farnesoid X receptor (FXR), a nuclear bile acid receptor, is well-recognized as an important effective target. Here we report the synthesis and characterization of compound HEC96719 a novel tricyclic FXR agonist based on a prior high-affinity nonsteroidal molecule GW4064. HEC96719 exhibits excellent potency superior to GW4064 and obeticholic acid in in vitro and in vivo assays of FXR activation. It also shows higher FXR selectivity and more favorable tissue distribution dominantly in liver and intestine. Preclinical data on pharmacokinetic properties, efficacy, and safety profiles overall indicate that HEC96719 is a promising drug candidate for NASH treatment.
COMPOUNDS FOR THE INHIBITION OF INDOLEAMINE-2,3-DIOXYGENASE
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Paragraph 0570; 0574, (2016/04/09)
The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of IDO, and for the treatment of IDO-related disorders.
NAPHTHYRIDINE COMPOUNDS
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Page/Page column 29, (2010/11/25)
Certain naphthyridine compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.
A convergent approach to huperzine A and analogues
Kelly, Sean A.,Foricher, Yann,Mann, John,Bentley, Jonathan M.
, p. 2865 - 2876 (2007/10/03)
We describe a concise and convergent synthesis of (rac)-5-methoxy-6-azatricyclco[7.3.1.02,7]trideca-2(7),3,5,11-tetraen -13-ol, which has the basic ring system of huperzine A, a potent inhibitor of acetylcholinesterase. We also describe the syn
A convergent approach to huperzine A and analogues
Foricher, Yann,Mann, John
, p. 2007 - 2009 (2007/10/03)
An aldol reaction between the enolate of cyclohexenone and 3-bromo-6- methoxy-1-formylpyridine, followed by protection of the resultant alcohol and reaction with Pd(0) yielded 5-methoxy-8-tert-butyldimethylsilylanyloxy-6- azatricyclo[7.3.1.02.7