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Tetrapartate prodrugs

  • US 6,720,306 B2
  • Filed: 01/12/2001
  • Issued: 04/13/2004
  • Est. Priority Date: 12/17/1997
  • Status: Expired due to Fees
First Claim
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1. A compound of formula I:

  • embedded imagewherein;

    L1 is a bifunctional linking moiety;

    D is a moiety that is a leaving group, or a residue of a compound to be delivered into a cell;

    Z is covalently linked to [D]y, wherein Z is selected from the group consisting of;

    a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof;

    Y1, Y2, Y3 and Y4 are each independently O, S, or NR12;

    R11 is a mono- or divalent polymer residue;

    R1, R4, R9, R10 and R12 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, and substituted C1-6 hetoroalkyls;

    R2, R3, R5 and R6, are independently selected from the group consisting of hydrogen, C1-6 alkyls, C1-6 alkoxy, phenoxy, C1-8 heteroalkyls, C1-8 heteroalkoxy, substituted C1-6 alkyls, C3-8 cycloalkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, halo-, nitro-, cyano-, carboxy-, C1-6 carboxyalkyls and C1-6 alkylcarbonyls;

    Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group;

    (m), (r), (s), (t), and (u) are independently zero or one;

    (p) is zero or a positive integer; and

    (y) is 1 or 2;

    wherein Z[D]y is capable of crossing the membrane of the target cell and is capable of being hydrolyzed therein to release D.

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