Phenylethylamine derivatives and their use in the treatment of melanoma

US7183319B2 · kind B2 · utility

Inventors

• Patrick Anthony Riley · London, GB
• Andrew Photiou · London, GB
• Tariq Hussain Khan · Hertford, GB
• Helen Mary Isted Osborn · Hertford, GB
• Hugh Malkin · Ludgershall, GB

Key dates

• Filing date: Jul 25, 2001
• Grant date: Feb 27, 2007
• Expiry date: May 2, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C333/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Novel mono- and dihydroxy phenylethylamine derivatives useful in treating melanoma are provided having the formulae (Ia, Ib or Ic). In the above formulae, Ra is hydrogen or —COORb, Rb is hydrogen or C1-6 alkyl; Re and Re independently represent hydrogen and hydroxy, Rf is 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)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