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Compounds, compositions, and methods for cancer imaging and therapy

  • US 5,919,934 A
  • Filed: 02/19/1997
  • Issued: 07/06/1999
  • Est. Priority Date: 02/19/1997
  • Status: Expired due to Fees
First Claim
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1. A compound, for use in radioimaging and radiotherapy, of the formula K1 ##STR36## wherein R1 and R2 are H or Me;

  • R3 is H, lower alkyl, lower alkylene, cycloalkyenyl, aryl, or arylalkane;

    R4 and R5 are independently ##STR37## --CH2 --, or ##STR38## R6 is --(CH2)j --CZ--NR10 --(CH2)m --R9 ;

    ##STR39## or hydrogen;

    R7 is ##STR40## --CH2 --, or ##STR41## R8 is --SH, or ##STR42## R9 and R15 are --N(R10)2 or a 5 to 7 membered heterocyclic ring, containing nitrogen, oxygen, or sulfur, the ring being unsubstituted or optionally substituted wi least one alkyl or arylalkyl substitutent, said heterocyclic ring containing 2-6 ring ca atoms and 1-3 ring heteroatoms;

    R10 and R14 are independently lower alkyl or hydrogen;

    R11 is hydrogen or methyl;

    Z is oxygen or 2 hydrogen atoms;

    m is an integer from 0 to 6;

    n is an integer from 1 to 6;

    and j is an integer from 0 to 6;

    whereinif R6 is hydrogen, then R8 is not --SH; and

    if R9 is --N(R10)2 or said 5 to 7 membered heterocyclic ring is linked to the --(CH2)m-- moiety by a heteroatom, then m is not 0.

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