Inhibitors of metazoan parasite proteases

US6548521B1 · kind B1 · utility

Assignee

• The Regents of the University of California · US

Inventors

• Fred E. Cohen · Los Angeles, US
• James McKerrow · San Francisco, US
• Christine Sun Ring · San Francisco, US
• Philip Jon Rosenthal · Nicasio, US
• George L. Kenyon · San Francisco, US
• Zhe Li · Poughkeepsie, US

Key dates

• Filing date: Jul 28, 2000
• Grant date: Apr 15, 2003
• Expiry date: Jul 28, 2020

Classification

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

Abstract

Compositions and methods 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 IA—X—B wherein A is a substituted or unsubstituted homoaromatic or 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 or heteroaromatic ring system comprising one to three rings which binds to at least one of the S1′, S1 and S2 subsites; and X is —C═C—C(═O)—. These compositions and methods have particular utility in the treatment of schistosomiasis, malaria, and other infectious diseases.