Non-steroidal farnesoid X receptor modulators and methods for the use thereof
US7671085B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Nov 14, 2003 |
| Grant date | Mar 2, 2010 |
| Priority date | — |
| Expiry date | May 9, 2026 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C2601/14
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The efficient regulation of cholesterol synthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. In accordance with the present invention, the identification of novel potent FXR activators is described. Two derivatives of invention compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds are useful as chemical tools to further define the physiological role of FXR as well as therapeutic leads for the treatment of diseases linked to cholesterol, bile acids and their metabolism and homeostasis.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.