Patent Evaluation: Novel Compositions for the Treatment of HIV Infections

Summary

Novelty: Novel 5-thiolated oligo- and polynucleotide compositions which are potentially useful for treating HIV infections are disclosed. The nucleotides may be therapeutically effective agents for inhibiting HIV-infections.

Biology: The anti-HIV activity of 5-thiolated oligo- and polynucleotides were evaluted in vivo against Hg human lymphocytes and human peripheral blood mononuclear cells (PBM cells). Although all compositions showed anti-HIV activity, the most active include mercaptopolydeoxy-cytidylate (MPdC) in PBM cells (EC₅₀ = 2.42 g/ml).

Chemistry: The synthesis of one compound is described with four compounds exemplified. All compounds are prepared by conventional synthetic or enzymatic methods. Six compounds are specifically claimed including 5-mercaptopolycytidylic acid.