Synthetic ligands selective for LXRβ over LXRα, identification and methods of use thereof

US8993628B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-8993628-B2
Application numberUS-3605008-A
CountryUS
Kind codeB2
Filing dateFeb 22, 2008
Priority dateFeb 23, 2007
Publication dateMar 31, 2015
Grant dateMar 31, 2015

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Abstract

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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 LXRα subtype rather than LXRβ, which suggests that LXRβ-selective agonists are attractive candidates for modulation of human lipid metabolism. The present application provides novel LXRβ-selective ligands that preferably modulate LXRβ over LXRα. 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.

First claim

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What is claimed is: 1. An LXRβ-selective ligand having the formula: wherein R is 2. A pharmaceutical composition comprising a therapeutically effective amount of an LXRβ-selective ligand and a pharmaceutically acceptable carrier, wherein the LXRβ-s…

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What does patent US8993628B2 cover?
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 LXRα subtype rather than LXRβ, which suggests that…
Who is the assignee on this patent?
Forman Barry, Yu Donna, Hope City
What technology area does this patent fall under?
Primary CPC classification A61K31/195. Mapped technology areas include Human Necessities.
When was this patent published?
Publication date Tue Mar 31 2015 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).