1162676-06-3Relevant articles and documents
Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties
Richter, Hans G.F.,Benson,Bleicher,Blum,Chaput,Clemann,Feng,Gardes,Grether,Hartman,Kuhn,Martin,Plancher,Rudolph,Schuler,Taylor
, p. 1134 - 1140 (2011/04/16)
Structure-guided lead optimization of recently described benzimidazolyl acetamides addressed the key liabilities of the previous lead compound 1. These efforts culminated in the discovery of 4-{(S)-2-[2-(4-chloro-phenyl)-5,6- difluoro-benzoimidazol-1-yl]-2-cyclohexyl-acetylamino}-3-fluoro-benzoic acid 7g, a highly potent and selective FXR agonist with excellent physicochemical and ADME properties and potent lipid lowering activity after oral administration to LDL receptor deficient mice.
CARBOXYL- OR HYDROXYL-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES
-
Page/Page column 24-25, (2009/07/10)
This invention relates to novel carboxyl- or hydroxyl-substituted benzimidazole derivatives of formula (I) wherein R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to FXR and can be used as medicaments.