Isomers of inositol niacinate and uses thereof

C - Chemistry – Metallurgy – 07 – D

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C07D 213/80 (2006.01) A61K 31/444 (2006.01)

Patent

CA 2679403

An ester formed from an inositol or an inositol derivative and niacin, wherein the inositol or the inositol derivatives comprises a stereoisomer selected from allo-inositol, cis-inositol, epi-inositol, muco-inositol, neo-inositol, scyllo-inositol, D-chiro-inositol and L-chiro-inositol, or pharmaceutically acceptable salts thereof. Examples of esters include inositol hexaniacinates such as allo-inositol hexaniacinate and cis-inositol hexaniacinate. The esters can be used to treat any disorder that is treatable with niacin therapy such as dyslipidemia, hypercholesterolemia, hyperlipidemia or cardiovascular disease. The esters can be administered with other agents such as HMG-CoA reductase inhibitors, statins, fibrates, activators of peroxisome proliferator activated receptors policosanol, phytosterols, tocotrienols, calcium, bile acid sequestrants, guar gum and free niacin. The invention includes pharmaceutical compositions containing these compounds.

L'invention concerne un ester formé d'un inositol ou d'un dérivé d'inositol et de niacine, où l'inositol ou les dérivés d'inositol comprennent un stéréoisomère choisi parmi l'allo-inositol, le cis-inositol, l'épi-inositol, le muco-inositol, le néo-inositol, le scyllo-inositol, le D-chiro-inositol et le L-chiro inositol, ou des sels pharmaceutiquement acceptables de ceux-ci. Des exemples d'ester comprennent les hexaniacinates d'inositol tels que l'hexaniacinate d'allo-inositol et l'hexaniacinate de cis-inositol. Les esters peuvent être utilisés pour traiter toute affection qui peut être traitée avec une thérapie à niacine telle que la dyslipidémie, l'hypercholestérolémie, l'hyperlipidémie ou une maladie cardiovasculaire. Les esters peuvent être administrés avec d'autres agents tels que des inhibiteurs de la HMG-CoA réductase, des statines, des fibrates, des activateurs de polycosanol de récepteurs activés par proliférateur peroxisome, des phytostérols, des tocotriénols, du calcium, des séquestrants de l'acide biliaire, de la gomme de guar et de la niacine libre. L'invention comprend des compositions pharmaceutiques contenant ces composés.

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