Inhibitors of metazoan parasite proteases

US6194421A · kind A · utility

Assignee

• The Regents of the University of California · US

Inventors

• Fred E. Cohen · Los Angeles, US
• James McKerrow · San Francisco, US
• George L. Kenyon · San Francisco, US
• Zhe Li · Poughkeepsie, US
• Xiaowu Chen · Hillsborough, US
• Baoqing Gong · Shoreline, US
• Rongshi Li · Omaha, US

Key dates

• Filing date: Dec 30, 1997
• Grant date: Feb 27, 2001
• Expiry date: Dec 30, 2017

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compositions and methods are disclosed for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease, wherein there is employed at least one compound of formula I EQU A--X--B wherein A is a substituted or unsubstituted heteroaromatic ring system comprising one to three rings which binds to at least one of the S2, S1 and S1' subsites; B is a substituted or unsubstituted homoaromatic ring system comprising one to three rings which binds to at least one of the S1', S1 and S2 subsites; and X is --C.dbd.C--C(.dbd.O)--. These compositions and methods have particular utility in the treatment of schistosomiasis, malaria and other infectious diseases.