Nucleobase phosphonate analogs for antiviral treatment

C - Chemistry – Metallurgy – 07 – F

Patent

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Details

C07F 9/6512 (2006.01) A61K 31/675 (2006.01) C07F 9/653 (2006.01)

Patent

CA 2533966

The present invention provides novel compounds with activity against infectious viruses. The compounds of the invention may inhibit retroviral reverse transcriptases and thus inhibit the replication of the virus. They are useful for treating human patients infected with a human retrovirus, such as human immunodeficiency virus (strains of HIV-1 or HIV-2) or human T-cell leukemia viruses (HTLV-I or HTLV-II) which results in acquired immunodeficiency syndrome (AIDS) and/or related diseases. The present invention also relates generally to the accumulation or retention of therapeutic compounds inside cells. The invention is more particularly related to attaining high concentrations of active metabolite molecules in HIV infected cells. Intracellular targeting may be achieved by methods and compositions which allow accumulation or retention of biologically active agents inside cells. Such effective targeting may be applicable to a variety of therapeutic formulations and procedures.

L'invention concerne des nouveaux composés présentant une activité contre les virus infectieux. Les composés de l'invention peuvent inhiber des transcriptases inverses rétrovirales et ainsi inhiber la réplication du virus. Ces composés s'avèrent utiles pour traiter des patients humains infectés par un rétrovirus humain, de type virus de l'immunodéficience humaine (souches de HIV-1 ou de HIV-2) ou virus de type leucémie à lymphocytes T (HTLV-I ou HTLV-II) qui entraîne le syndrome d'immunodéficience acquise (SIDA) et/ou des maladies associées. L'invention concerne également en général l'accumulation ou la rétention de composés thérapeutiques à l'intérieur de cellules. L'invention concerne plus particulièrement l'atteinte de concentrations élevées de molécules de métabolite actif dans des cellules infectées par le virus HIV. Le ciblage intracellulaire peut être obtenu par des procédés et des compositions qui permettent l'accumulation ou la rétention d'agents actifs sur le plan biologique à l'intérieur des cellules. Ce ciblage actif peut être applicable à une variété de formulations et de procédures thérapeutiques.

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