| 摘要 |
Novel mono- and dihydroxy phenylethylamine derivatives useful in treating melanoma are provided having the formulae (Ia, Ib or Ic). In the above formulae, R<SUP>a </SUP>is hydrogen or -COOR<SUP>b</SUP>, R<SUP>b </SUP>is hydrogen or C<SUB>1-6 </SUB>alkyl; R<SUP>e </SUP>and R<SUP>e </SUP>independently represent hydrogen and hydroxy, R<SUP>f </SUP>is hydrogen, C<img id="CUSTOM-CHARACTER-00001" he="2.46mm" wi="1.44mm" file="US07183319-20070227-P00001.TIF" alt="custom character" img-content="character" img-format="tif"/>1-4? alkyl or halogen, X is -CHOH-, -CH<SUB>2</SUB>-oxygen or sulphur, m is zero or 1, W is oxygen or sulphur, and -ODrug, -NHDrug and -N(Drug)<SUB>2 </SUB>each represent a residue of a therapeutically active agent. The above compounds are prodrugs which are inactive until metabolised by enzymes expressed by host melanoma cells. The invention allows a greater amount of active agent to be used while reducing systemic side effects |
