Hydroxylation activated prodrugs

• US 6,214,886 B1
• Filed: 07/14/1998
• Issued: 04/10/2001
• Est. Priority Date: 02/06/1998
• Status: Expired due to Term

• Current Assignee: Spear Therapeutics Ltd. (Incanthera Ltd)
• Original Assignee: Demontfort University The Gateway
• Inventors: Patterson, Lawrence Hylton, Burke, Michael Danny, Potter, Gerald Andrew
• Primary Examiner(s): NORTHINGTON DAVIS, ZINNA
• Application Number:
  US09/115,015
• Time in Patent Office: 1,001 Days
• Field of Search: 546/330, 514/357, 514/685
• US Class Current: 514/685
• CPC Class Codes: C07C 205/35 having nitro groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
• CPC Class Codes: C07C 255/36 the carbon skeleton being further substituted by hydroxy groups
• CPC Class Codes: C07C 2602/10 the other ring being six-membered, e.g. tetraline
• CPC Class Codes: C07C 327/48 having carbon atoms of thiocarboxamide groups bound to carbon atoms of six-membered aromatic rings
• CPC Class Codes: C07C 43/215 having unsaturation outside the six-membered aromatic rings
• CPC Class Codes: C07C 49/84 containing ether groups, groups, groups, or groups
• CPC Class Codes: C07D 213/57 Nitriles

Abstract

The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumour prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.

Claims

1. A method of inhibiting growth of tumor cells containing an aromatic hydroxylase enzyme comprising contacting the tumor cells with a prodrug having the formula

2. The method of claim 1 wherein the aromatic hydroxylase enzyme is CYP1B1.