1162675-66-2

Upstream product

• 74-11-3 para-chlorobenzoic acid 
• 23860-35-7 cyclohexylacetic acid chloride 
• 76179-40-3 2-amino-4,5-difluoroaniline 
• 90085-61-3 2-bromocyclohexylacetylchloride 
• 42716-73-4 ethyl 2-bromo-2-cyclohexylacetate 
• 5292-21-7 Cyclohexylacetic acid 
• 1162675-80-0 [2-(4-chloro-phenyl)-5,6-difluoro-benzoimidazol-1-yl]-cyclohexyl-acetic acid ethyl ester 
• 1265885-77-5 [2-(4-chloro-phenyl)-5,6-difluoro-benzoimidazol-1-yl]-cyclohexyl-acetic acid methyl ester 

Downstream Products

• 1265885-77-5 [2-(4-chloro-phenyl)-5,6-difluoro-benzoimidazol-1-yl]-cyclohexyl-acetic acid methyl ester 
• 1162676-63-2 2-(4-{2-[2-(4-chloro-phenyl)-5,6-difluoro-benzoimidazol-1-yl]-2-cyclohexyl-acetylamino}-3-fluoro-phenoxy)-2-methyl-propionic acid ethyl ester 
• 1162675-78-6 4-{2-[2-(4-chloro-phenyl)-5,6-difluoro-benzoimidazol-1-yl]-2-cyclohexyl-acetylamino}-benzoic acid ethyl ester 

Relevant academic research and scientific papers

Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties

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.

NEW BENZIMIDAZOLE DERIVATIVES

The invention is concerned with novel benzimidazole derivatives of Formula (I) wherein A, n and R1 to R7 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds act on Farnesyl X receptor (FXR) and against cholesterol and lipid illnesses, diabetes, obesity, psoriasis, cancer, osteoporosis, Parkinson's and Alzheimer's disease.

CARBOXYL- OR HYDROXYL-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES

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.