Probucol monoesters and their use to increase plasma hdl...

A - Human Necessities – 61 – K

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A61K 31/216 (2006.01) A61K 31/225 (2006.01) A61P 3/06 (2006.01)

Patent

CA 2444429

It has been discovered that certain selected probucol monoesters, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.

La présente invention se rapporte à certains monoesters de probucol sélectionnés ainsi qu'à des sels ou promédicaments pharmaceutiquement acceptables de ces monoesters, qui sont utiles pour accroître le cholestérol des lipoprotéines de haute densité (HDL) circulantes. Ces composés peuvent également améliorer la fonctionnalité des HDL par (a) accroissement de la suppression des esters de cholestéryle, (b) accroissement de l'affinité des particules-HDL pour les récepteurs de surface des cellules hépatiques ou (c) accroissement de la demi-vie de l'apoAI-HDL.

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