Aryl phosphate derivatives of d4t having anti-hiv activity

Details Aryl phosphate derivatives of d4t having anti-hiv activity Aryl phosphate derivatives of d4t having anti-hiv activity

C - Chemistry, Metallurgy

07

H

C07H 19/10 (2006.01) A61K 31/70 (2006.01) C07H 19/20 (2006.01)

Patent

CA 2336285

Aryl phosphate nucleosise derivatives of formula (I) show potent activity against HIV without undesirable levels of cytotoxic activity. Examples of aryl phosphate nucleoside derivatives include aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group. In said formula, Y is oxygen or sulfur; R1 is unsubstituted aryl or aryl substituted with an electron- withdrawing group; R2 is a nucleoside of formula (II or III).

Dérivés de nucléosides de phosphate arylique représentés par la formule (I) et possédant une activité puissante contre VIH sans niveaux indésirables de cytotoxicité. Des exemples de ces dérivés de nucléosides de phosphate arylique consistent en des dérivés de phosphate arylique de d4T dont le groupe aryle présente une substitution para-bromo. En particulier, ces dérivés sont des inhibiteurs puissants de la transcriptase inverse de VIH. Selon un aspect préféré de l'invention, le phosphore du groupe phosphate arylique est encore substitué par un résidu aminoacide qui peut être estérifié ou substitué, tel qu'un groupe méthoxy alaninyle (I) dans laquelle Y représente oxygène ou soufre; R¿1? représente aryle non substitué ou aryle substitué par un groupe de suppression d'électrons; R¿2? représente un nucléoside de formule II ou III.

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