Compounds Useful in the Treatment of Hiv
AssigneeMedivir AB
InventorsXiao-Xiong Zhou, Hong Zhang
Life of this patent
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Abstract
There is provided inter alia use of 2′,3′-dideoxy-3′-hydroxymethylcytosine or a prodrug or salt thereof in the manufacture of a medicament for the treatment of HIV infection wherein the reverse transcriptase of the HIV bears at least one mutation that allows an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.
Claims31
A method of treating HIV infection comprising administering to a patient in need thereof 2′,3′-dideoxy-3′-C-hydroxymethylcytosine or a prodrug thereof releasing 2′,3′-dideoxy-3′-C-hydroxymethylcytosine or its 5′-monophosphate in vivo;
- or a salt thereof, wherein the reverse transcriptase of the infecting HIV bears at least one mutation that allows an obligate chain terminating nucleoside- or nucleotide-phosphate to be excised from a nascent DNA strand by ATP- or pyrophosphate-mediated excision.
A method for the treatment of an HIV patient where the reverse transcriptase of the HIV bears at least one primer rescue mutation that allows an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision comprising administering to the patient an effective amount of 2′,3′-dideoxy-3′-hydroxymethylcytosine or a prodrug thereof releasing 2′,3′-dideoxy-3′-C-hydroxymethylcytosine or its 5′-monophosphate in vivo;
- or a salt thereof.
A method for inhibiting the emergence or propagation of HIV primer rescue mutants that are able to remove a chain-terminating NRTI nucleotide incorporated into an HIV primer/template complex where the removal is effected by an ATP-dependent or pyrophosphate dependent excision mechanism, comprising the simultaneous or sequential administration to an individual infected with HIV an effective amount of 2′,3′-dideoxy-3′-hydroxymethylcytosine or a prodrug thereof releasing 2′,3′-dideoxy-3′-C-hydroxymethylcytosine or its 5′-monophosphate in vivo;
- or a salt thereof, and at least one chain terminator NRTI which induces primer rescue mutants.
A compound comprising 2′,3′-dideoxy-3′-hydroxymethylcytosine or a prodrug thereof releasing 2′,3′-dideoxy-3′-C-hydroxymethylcytosine or its 5′-monophosphate in vivo;
- or a salt thereof for use in the treatment of HIV infection wherein the reverse transcriptase of the HIV bears at least one mutation that allows an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the a nascent DNA strand by ATP- or pyrophosphate-mediated excision.
A compound comprising 2′,3′-dideoxy-3′-C-hydroxymethylcytosine or a prodrug thereof releasing 2′,3′-dideoxy-3′-C-hydroxymethylcytosine or its 5′-monophosphate in vivo;
- or a salt thereof together with at least one chain terminator NRTI as active ingredients for use for simultaneous or sequential administration of said active ingredients for the inhibition of the emergence or propagation of HIV mutants in an individual infected with HIV, wherein said mutants are able to remove a chain-terminating NRTI nucleotide incorporated into an HIV primer/template complex, the removal being facilitated by an ATP-dependent or pyrophosphate dependent excision mechanism.
Dependencies are inferred from the claim text.