612499-61-3

Upstream product

• 93118-03-7 2-chloro-3-trifluoromethylbenzaldehyde 
• 3963-62-0 2,2-Diphenylethylamine 
• 405911-35-5 N-(2,2-diphenylethyl)-N-(2-chloro-trifluoromethylbenzyl)amine 
• 106-94-5 propyl bromide 
• 109-64-8 1,3-dibromo-propane 

Downstream Products

• 848086-74-8 5{3-[(chloro-trifluoromethyl-benzyl)-diphenylethyl-amino]-propoxy}-3,4-dihydro-2H-quinoline-1-carboxylic acid ter-butyl ester 
• 848086-81-7 (5-{3-[(2-chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-amino]-propoxy}-naphthalen-1-yl)-carbamic acid tert-butyl ester 
• 848086-72-6 5-{3-[(2-chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-amino]-propoxy}-1,2,3,4-tetrahydro-naphthalene-1-carboxylic acid methyl ester 
• 847990-40-3 (2-chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-[3-(1H-indol-4-yloxy)-2-methyl-propyl]-amine 
• 405911-26-4 methyl 2-{3-[3-({[2-chloro-3-(trifluoromethyl)phenyl]methyl}-(2,2-diphenylethyl)-amino)-propoxy]phenyl}acetate 

Relevant academic research and scientific papers

LXR AGONISTS AND USES THEREOF

This invention features compounds that modulate the activity of liver X receptors, pharmaceutical compositions including the compounds of the invention, and methods of utilizing those compositions for modulating the activity of liver X receptors in the treatment of cancer.

The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages

The liver X receptors (LXR) play a key role in cholesterol homeostasis and lipid metabolism. SAR studies around tertiary-amine lead molecule 2, an LXR full agonist, revealed that steric and conformational changes to the acetic acid and propanolamine groups produce dramatic effects on agonist efficacy and potency. The new analogs possess good functional activity, demonstrating the ability to upregulate LXR target genes, as well as promote cholesterol efflux in macrophages.

Synthesis and SAR of potent LXR agonists containing an indole pharmacophore

A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. Compounds from this series were potent agonists with good rat pharmacokinetic parameters. In addition, the crystal structure of an LXR agonist bound to LXRα will be disclosed.

COMPOUNDS AND METHODS

Disclosed are compounds and pharmaceutically acceptable salts thereof, useful as LXR agonists.

COMPOUNDS AND METHODS

Disclosed are compounds and pharmaceutically acceptable salts thereof, useful as LXR agonists.