Compounds for the suppression of hiv tat transactivation

A - Human Necessities – 61 – K

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A61K 31/222 (2006.01) A61K 31/05 (2006.01) A61K 31/085 (2006.01) A61K 31/09 (2006.01) A61K 31/22 (2006.01) C07C 43/23 (2006.01)

Patent

CA 2200991

The present invention reveals the isolation, purification and characterization from the creosote bush Larrea tridentata of compounds of structural formula (I) where R1, R2, R3 and R4 are each selected from the group consisting of HO-, CH3O- and CH3(C=O)O-, provided that R1, R2, R3 and R4 are not each HO- simultaneously. Each compound is a derivative of 1,4-bis-(3,4-dihydroxyphenyl)-2, 3--dimethylbutane (nordihydroquaiaretic acid, NDGA). In addition, NDGA and each derivative can be used in a method to suppress Tat transactivation of a lentivirus, including the HIV virus, in a cell by administering NDGA or a derivative of NDGA to the cell.

L'invention porte sur l'isolement, la purification et l'identification à partir de l'arbuste générateur de créosote Larrea tridentata de composés de formule structurelle (I) dans laquelle R1, R2, R3 et R4 sont chacun sélectionnés dans un groupe consistant en HO-, CH3O- et CH3(C=C)O- sous réserve que R1, R2, R3 et R4 ne soient pas simultanément HO-. Chacun des composés est un dérivé du 1,4-bis-(3,4-dihydroxyphényl)-2,3-diméthylbutane (acide nordihydroquaiarétique, NDGA). En outre, le NDGA et chacun de ses dérivés peut être utilisé dans un procédé inhibant la transactivation par le Tat de lentivirus, y compris celui du VIH, dans une cellule par administration de NGDA ou d'un de ses dérivés à ladite cellule.

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