228579-12-2

Upstream product

• 42058-59-3 3-hydroxy-benzeneacetic acid, methyl ester 
• 627-18-9 1-bromo-3-propanol 
• 2446-83-5 diisopropyl (E)-azodicarboxylate 
• 109-64-8 1,3-dibromo-propane 

Downstream Products

• 405911-26-4 methyl 2-{3-[3-({[2-chloro-3-(trifluoromethyl)phenyl]methyl}-(2,2-diphenylethyl)-amino)-propoxy]phenyl}acetate 
• 930778-28-2 2-({3-[3-(Methoxycarbonylmethyl)phenoxy]propyl}N-methylamino)ethanol 
• 405911-22-0 methyl (3-{3-[(2,2-diphenylethyl)(4-methoxybenzyl)amino]propoxy}-phenyl)acetate 

Relevant academic research and scientific papers

SYNTHETIC LIGANDS SELECTIVE FOR LXRbeta OVER LXRalpha, IDENTIFICATION AND METHODS OF USE THEREOF

LXR nuclear receptor agonists have been previously shown to increase cholesterol efflux, raise plasma HDL cholesterol, stimulate cholesterol excretion, and reduce atherosclerotic lesions. However, these agonists have also been associated with the unwanted side effect of hypertriglyeridemia. This hypertriglyeridemia appears to be mediated by the LXRalpha subtype rather than LXRbeta, which suggests that LXRbeta-selective agonists are attractive candidates for modulation of human lipid metabolism. The present application provides novel LXRbeta-selective ligands that preferably modulate LXRbeta over LXRalpha. These ligands may be used to treat a variety of diseases associated with LXR, such as for example lipid metabolism disorders, atherosclerosis, Alzheimer disease, and inflammation.

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.

Synthesis and biological evaluation of phenylacetyl derivatives having low central nervous system permeability as potent and selective M2 muscarinic receptor antagonists

A series of phenylacetyl derivatives containing the 5,10-dihydro-11H- dibenzo[b,e][1,4]diazepin-11-one or 5,11-dihydro-6H-pyrido[2,3- b][1,4]benzodiazepin-6-one skeleton was prepared and evaluated for their binding affinities to muscarinic receptors in vitro and for antagonism of bradycardia, salivation and tremor in vivo. Among them, compounds 56 and 66 had high affinity for M2 muscarinic receptors in the heart (pK(i) = 8.7 and 8.9, respectively) with low affinity for M3 muscarinic receptors in the submandibular gland. A structure-activity relationship (SAR) study suggested that the high M2 selectivity over the M3 muscarinic receptors of 56 may be attributed to the direction of the carboxamide carbonyl group. In in vivo studies, 56 and 66 antagonized oxotremorine-induced bradycardia in rats on both intravenous and oral administration, and their heart rate increasing effect in dogs with nocturnal bradycardia was about 3-fold greater than that of AF-DX 116. Furthermore, they had almost no influence on oxotremorine- induced tremor in mice, presenting no evidence of central transfer.