Aryl phosphate derivatives of d4t

Details Aryl phosphate derivatives of d4t Aryl phosphate derivatives of d4t

C - Chemistry, Metallurgy

07

F

C07F 9/6512 (2006.01) C07F 9/655 (2006.01) C07F 9/6558 (2006.01)

Patent

CA 2428808

Specific aryl phosphate nucleoside derivatives show activity against HIV without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. Examples of aryl phosphate nucleotide nucleoside derivatives include aryl phosphate derivatives of d4T having one or more substituents on the aryl group, and wherein the phosphorus of the aryl phosphate group is attached to an amino acid residue that may be esterified or substituted, such as a methoxyalaninyl group.

Des dérivés nucléosides arylphosphate spécifiques présentent une activité contre HIV sans présenter un niveau indésirable d'activité cytotoxique. Ces dérivés sont notamment des inhibiteurs puissants de la transcriptase inverse de HIV. Lesdits dérivés nucléosides arylphosphate comportent des dérivés arylphosphate de D4T portant un ou plusieurs substituants sur le groupe aryle, le phosphore du groupe arylphosphate étant attaché à un résidu d'acide aminé pouvant être estérifié ou substitué, tel qu'un groupe méthoxyalaninyle.

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