Naphthoquinone derivatives as hiv matrix protein tyrosine...

Details Naphthoquinone derivatives as hiv matrix protein tyrosine... Naphthoquinone derivatives as hiv matrix protein tyrosine...

C - Chemistry, Metallurgy

07

C

C07C 69/738 (2006.01) A61K 31/216 (2006.01) A61P 31/18 (2006.01) C07C 323/52 (2006.01)

Patent

CA 2300876

There is disclosed a structural genus of compounds, defined according to coordinates in three--dimensional space, that binds amino moieties on neighboring lysine residues in a tyrosine residue 29 pocket of the matrix protein component of the HIV preintegration complex (PIC), and having the following formula I: Image wherein R is -X-CO-Z, wherein Z is C1-6 (straight or branched) alkoxy, wherein X is (CH2) n or -S- (CH2)n, wherein n is an integer from 0 to 6, and wherein Y is H or C1-6 alkyl (straight or branched chain). The compounds and pharmaceutical compositions prevent the PIC from binding to karyopherin .alpha. and prevent nuclear importation and integration of the HIV viral genome into the host cell DNA. Thus, the inventive compounds and pharmaceutical compositions prevent HIV viral infection.

La présente invention a trait à un genre de composés de type structural, défini en fonction de coordonnées dans l'espace, qui fixe des fractions aminées sur des résidus de lysine voisins dans une poche en position 29 de résidus de tyrosine du constituant porine du complexe de préintégration du VIH (PIC). Ces composés et ces compositions pharmaceutiques empêchent le PIC de se fixer sur la Karyophérine alpha , ainsi que l'importation et l'intégration nucléaires du génome viral du VIH dans l'ADN de la cellule hôte. Ainsi, les composés et les compositions de cette invention empêchent l'infection virale par le HIV.

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