Aminomethylene amide analogs of pyrazinamide with intracellular antimycobacterial activity against pyrazinamide-resistant mycobacteria combined with a rifamycin

US6399607B1 · kind B1 · utility

Assignee

• Research Foundation for the State University of New York York · US

Inventors

• John T. Welch · Akron, US
• Leonid Heifets · Denver, US
• Michael Henry Cynamon · Town of DeWitt, US

Key dates

• Filing date: Jun 30, 2000
• Grant date: Jun 4, 2002
• Expiry date: Jun 30, 2020

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K31/395
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Methods for treating diseases involving pyrazinamide-resistant mycobacteria comprise administering to a mammal in need of treatment a therapeutically effective amount of a combination of rifamycin and a compound of formula I: whereinR1 is hydrogen haloalkyl, or lower alkyl;R2 and R3 are independently chosen from alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, alkylaryl and substituted alkylaryl, or R2 and R3 taken together form a five- or six-membered heterocyclic or substituted heterocyclic ring; andX is hydrogen, halogen, or lower alkyl;or a pharmaceutically acceptable salt thereof.