Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability

  • US 5,922,695 A
  • Filed: 07/25/1997
  • Issued: 07/13/1999
  • Est. Priority Date: 07/26/1996
  • Status: Expired due to Term
First Claim
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1. A compound having formula (1a) ##STR33## wherein Z is independently --OC(R2)2 OC(O)X(R)a, an ester, an amidate or --H, but at least one Z is --OC(R2)2 OC(O)X(R)a ;

  • A is the residue of an antiviral phosphonomethoxy nucleotide analog;

    X is N or O;

    R2 independently is --H, C1 -C12 alkyl, C5 -C12 aryl, C2 -C12 alkenyl, C2 -C12 alkynyl, C7 -C12 alkenylaryl, C7 -C12 alkynylaryl, or C6 -C12 alkaryl, any one of which is unsubstituted or is substituted with 1 or 2 halo, cyano, azido, nitro or --OR3 in which R3 is C1 -C12 alkyl, C2 -C12 alkenyl, C2-C12 alkynyl or C5 -C12 aryl;

    R is independently --H, C1 -C12 alkyl, C5 -C12 aryl, C2 -C12 alkenyl, C2 -C12 alkynyl, C7 -C12 alkyenylaryl, C7 -C12 alkynylaryl, or C6 -C12 alkaryl, any one of which is unsubstituted or is substituted with 1 or 2 halo, cyano, azido, nitro, --N(R4)2 or --OR3, where R4 independently is --H or C1 -C8 alkyl, provided that at least one R is not H; and

    a is 1 when X is O, or 1 or 2 when X is N;

    with the proviso that when a is 2 and X is N, (a) two N-linked R groups can be taken together to form a carbocycle or oxygen-containing heterocycle, (b) one N-linked R additionally can be --OR3 or (c) both N-linked R groups can be --H;

    and the salts, hydrates, tautomers and solvates thereof.

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