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Elongated and multiple spacers in activatible prodrugs

  • US 7,223,837 B2
  • Filed: 03/25/2002
  • Issued: 05/29/2007
  • Est. Priority Date: 03/23/2001
  • Status: Expired due to Term
First Claim
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1. A compound of the formula:


  • V—

    (W)k

    (X)l

    A—

    Zwherein;

    V is an enzymatically removable specifier, optionally being removable after prior binding to a receptor;

    (W)k

    (X)l

    A is an elongated self-eliminating spacer system;

    W and X are each a 1,(4+2n) electronic cascade self-eliminating spacer, being the same or different;

    A is either a spacer group of formula (Y)m, wherein Y is a 1,(4+2n) electronic cascade self-eliminating spacer, or a group of formula U being a cyclisation self-elimination spacer;

    Z is a therapeutic or diagnostic moiety;

    k and l are independently an integer from 0 (included) to 5 (included);

    m is an integer from 1 (included) to 5 (included);

    n is an integer from 0 (included) to 10 (included), and k+1>

    0.

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