1097776-74-3Relevant academic research and scientific papers
FXR agonist activity of conformationally constrained analogs of GW 4064
Akwabi-Ameyaw, Adwoa,Bass, Jonathan Y.,Caldwell, Richard D.,Caravella, Justin A.,Chen, Lihong,Creech, Katrina L.,Deaton, David N.,Madauss, Kevin P.,Marr, Harry B.,McFadyen, Robert B.,Miller, Aaron B.,Navas III, Frank,Parks, Derek J.,Spearing, Paul K.,Todd, Dan,Williams, Shawn P.,Bruce Wisely
supporting information; experimental part, p. 4733 - 4739 (2010/06/12)
Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of potent full agonists 2a and 2g.
FARNESOID X RECEPTOR AGONISTS
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Page/Page column 120-121, (2009/03/07)
The present invention relates to famesoid X receptors (FXR, NR1H4) FXR is a member of the nuclear receptor class of ligand-activate transcription factors More particularly, the present invention relates to compounds useful as agonists for FXR, pharmaceutical formulations comprising such compounds, and therapeutic use of the same Novel isoxazole compounds are disclosed as part of pharmaceutical compositions for the treatment of a condition mediated by decreased FXR activity, such as obesity, diabetes, cholestatic liver disease, liver fibrosis, and metabolic syndrome
