Phenylethylamine derivatives and their use in the treatment...

Details Phenylethylamine derivatives and their use in the treatment... Phenylethylamine derivatives and their use in the treatment...

2007-02-27

2007-02-27

Richter, Johann (Department: 1621)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Radical -xh acid, or anhydride, acid halide or salt thereof...

C514S575000, C514S617000, C562S621000, C564S161000

Reexamination Certificate

active

10333933

ABSTRACT:
Novel mono- and dihydroxy phenylethylamine derivatives useful in treating melanoma are provided having the formulae (Ia, Ib or Ic). In the above formulae, Rais hydrogen or —COORb, Rbis hydrogen or C1-6alkyl; Reand Reindependently represent hydrogen and hydroxy, Rfis hydrogen, C1–4? alkyl or halogen, X is —CHOH—, —CH2-oxygen or sulphur, m is zero or 1, W is oxygen or sulphur, and —ODrug, —NHDrug and —N(Drug)2each 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

REFERENCES:
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patent: 0 584 552 (1994-03-01), None
patent: WO 98/25886 (1998-06-01), None
Hong et al.Synthesis and Biological Activity of Analogs of Naturally Occuring 6-Ureidopurines and Their Nucleosides,Journal of Medicinal Chemistry (1973) vol. 16, No. 2, pp. 139-147.

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