申请人:——
公开号:US20040029967A1
公开(公告)日:2004-02-12
Novel mono- and dihydroxy phenylethylamine derivatives useful in treating melanoma are provided having the formulae (Ia, Ib or Ic). In the above formulae, R
a
is hydrogen or —COOR
b,
R
b
is hydrogen or C
1-6
alkyl; R
e
and R
e
independently represent hydrogen and hydroxy, R
f
is hydrogen, C
1-4? alkyl or halogen, X is —CHOH—, —CH
2
-oxygen or sulphur, m is zero or 1, W is oxygen or sulphur, and —ODrug, —NHDrug and —N(Drug)
2
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.
1
提供了用于治疗黑色素瘤的新型单氢和二羟基苯乙胺衍生物,其化学式为(Ia、Ib或Ic)。在上述化学式中,R是氢或—COORb,Rb是氢或C1-6烷基;Re和Re独立表示氢和羟基,Rf是氢、C1-4烷基或卤素,X是—CHOH—、—CH2-氧或硫,m为零或1,W是氧或硫,而—ODrug、—NHDrug和—N(Drug)2分别表示治疗活性剂的残基。上述化合物是一种前药,在被宿主黑色素瘤细胞表达的酶代谢之前是无效的。该发明允许使用更多的活性剂而减少全身副作用。