452365-99-0Relevant articles and documents
FARNESOID X RECEPTOR AGONISTS AND USES THEREOF
-
Paragraph 00398, (2017/04/11)
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
FARNESOID X RECEPTOR AGONISTS AND USES THEREOF
-
Paragraph 00394, (2017/04/11)
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS
-
Page/Page column 172, (2010/05/13)
Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
NON-STEROIDAL FXR AGONISTS
-
Page 9-11; 33; 34; Sheet 12; Sheet 15, (2010/02/07)
ABSTRACT Potent non-steroidal farnesoid X receptor (FXR) agonists are N-aryl-N-arylmethyl amido and ureido compounds having the chemical structure represented by the following formula (I): INSERT FORMULA wherein E1 is (C1-C8)alkyl, cyclohexyl, 2-furyl, 3-
Discovery and optimization of non-steroidal FXR agonists from natural product-like libraries.
Nicolaou,Evans, Ronald M,Roecker,Hughes, Robert,Downes, Michael,Pfefferkorn, Jeffery A
, p. 908 - 920 (2007/10/03)
The efficient regulation of cholesterol biosynthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. Herein, we describe the development of four novel classes of potent FXR activators originating from natural product-like libraries. Initial screening of a 10,000-membered, diversity-orientated library of benzopyran containing small molecules for FXR activation utilizing a cell-based reporter assay led to the identification of several lead compounds possessing low micromolar activity (EC50's = 5-10 microM). These compounds were systematically optimized employing parallel solution-phase synthesis and solid-phase synthesis to provide four classes of compounds that potently activate FXR. Two series of compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds may find future utility as chemical tools in studies aimed at further defining the physiological role of FXR and discovering potential therapeutic agents for the treatment of diseases linked to cholesterol and bile acid metabolism and homeostasis.