Compounds and methods to increase plasma hdl cholesterol...

C - Chemistry – Metallurgy – 07 – C

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C07C 323/20 (2006.01) A61K 31/10 (2006.01) G01N 33/92 (2006.01)

Patent

CA 2404044

It has been discovered that certain selected ethers of probucol, 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.

Selon l'invention, certains éthers de probucol, et leurs sels ou promédicaments pharmaceutiquement acceptables, sont utiles pour accroître le HDL cholestérol en circulation. Ces composés peuvent également améliorer la fonctionnalité de HDL par (a) augmentation de la clairance des esters de cholestéryle; (b) augmentation de l'affinité des particules HDL pour les récepteurs de surfaces cellulaires hépatiques ou (c) augmentation de la demi-vie de apoAI-HDL.

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