405911-35-5

Upstream product

• 3963-62-0 2,2-Diphenylethylamine 
• 93118-03-7 2-chloro-3-trifluoromethylbenzaldehyde 

Downstream Products

• 609772-05-6 (S)-4-[N-(2,2-diphenylethyl)-N-(2-chloro-3-(trifluoromethyl)benzyl)amino]-butan-2-ol 
• 405911-26-4 methyl 2-{3-[3-({[2-chloro-3-(trifluoromethyl)phenyl]methyl}-(2,2-diphenylethyl)-amino)-propoxy]phenyl}acetate 
• 612494-90-3 [3-(3-bromophenoxy)propyl]({[2-chloro-3-(trifluoromethyl)phenyl]methyl})(2,2-diphenylethyl)amine 
• 848086-69-1 5-{3-[(2-chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-amino]-propoxy}-1,2,3,4-tetrahydro-naphthalene-1-carboxylic acid hydrochloride 
• 848086-64-6 N-(5-{3-[2-(chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-amino]-propoxy}-naphthalen-1-yl)-methanesulfonamide hydrochloride 
• 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 
• 848171-53-9 5-{3-[(2-chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-amino]-propoxy}-1,2,3,4-tetrahydro-naphthalene-1-carboxylic acid 
• 848171-52-8 N-(5-{3-[2-(chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-amino]-propoxy}-naphthalen-1-yl)-methanesulfonamide 
• 848086-78-2 (5-{3-[(2-chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-amino]-propoxy}-naphthalen-1-yl)-ethylamine 
• 848086-73-7 (2-chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-[3-(1,2,3,4-tetrahydro-quinolin-5-yloxy)-propyl]-amine 
• 848086-75-9 5-{3-[(2-chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-amino]-propoxy}-naphthalen-1-ylamine 
• 847990-59-4 (2-chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-[(3-(1-methanesulfonyl-1H-indol-4-yl)oxy)-propyl]-amine trifluoroacetate 

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.

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.

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.

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.

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.

COMPOUNDS AND METHODS

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

AMIDE COMPOUNDS AND METHODS OF USING THE SAME

Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.

Substitued aminopropoxyaryl derivatives useful as agonists for lxr

Disclosed is a compound of formula (I), wherein the variables are as defined herein, and pharmaceutically acceptable salts or solvates thereof. The compounds of formula (I) are useful as LXR agonists.

ACID AND ESTER COMPOUNDS AND METHODS OF USING THE SAME

Disclosed is a compound of having the formula (II-A), pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.