Inhibitor or promoter of uridinediphosphate...

A - Human Necessities – 61 – K

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A61K 31/485 (2006.01) A61K 31/352 (2006.01) A61P 25/04 (2006.01)

Patent

CA 2593140

A UGT2B inhibitor capable of increasing the bio-availability of a drug, being a compound in a free base or a pharmaceutically acceptable salt form that is selected from the group consisting of: capillarisin, isorhamnetin,.beta.- naphthoflavone, .alpha.-naphthoflavone, hesperetin, terpineol, (+)-limonene, .beta.-myrcene, swertiamarin, eriodictyol, cineole, apigenin, baicalin, ursolic acid, isovitexin, lauryl alcohol, puerarin, trans-cinnamaldehyde, 3-phenylpropyl acetate, isoliquritigenin, paeoniflorin, gallic acid, genistein, glycyrrhizin, protocatechuic acid, ethyl myristate, umbelliferone, and a combination thereof. A UGT2B enhancer capable of enhancing the liver detoxification function in a subject, being a compound in a free base or a pharmaceutically acceptable salt form that is selected from the group consisting of: mordihydroguaiaretic acid, wogonin, trans-cinnamic acid, baicalein, quercetin, daidzein, oleanolic acid, homoorientin, hesperetin, narigin, neohesperidin, (+)-epicatechin, hesperidin, liquiritin, eriodictyol, formononetin, quercitrin, genkwanin, kaempferol, isoquercitrin, (+)-catechin, naringenin, daidzin, (-)-epicatechin, luteolin-7-glucoside, ergosterol, rutin, luteolin, ethyl myristate, apigenin, 3-phenylpropyl acetate, umbelliferone, glycyrrhizin, protocatechuic acid, poncirin, isovitexin, 6-gingerol, cineole, genistein, trans-cinnamaldehyde, and a combination thereof.

La présente invention concerne un inhibiteur de l'UGT2B qui peut augmenter la biodisponibilité des médicaments. L'inhibiteur de l'UGT2B est choisi parmi la capillarisine, l'isorhamnétine ou la ß-naphtoflavone, etc., ou leurs combinaisons, sous la forme de base libre ou des sels pharmaceutiquement acceptables. La présente invention concerne également un promoteur de l'UGT2B qui peut favoriser la fonction individuelle d'élimination des toxines du foie. Le promoteur de l'UGT2B est choisi parmi l'acide nordihydroguaïarétique, la wogonine, l'acide trans-cinnamique, etc., ou leurs combinaisons, sous la forme de base libre ou des sels pharmaceutiquement acceptables.

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