Small molecule inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase

US8703811B2 · kind B2 · utility

Assignees

• Genzyme Corporation · US
• Massachusetts Institute of Technology · US
• President and Fellows of Harvard College · US

Inventors

• Cecilia M. Bastos · Grafton, US
• Michael L. Booker · Bridgewater, US
• Cassandra Celatka · Hull, US
• Jon Clardy · Ithaca, US
• Joseph Cortese · Quincy, US
• Vishal P. Patel · Washington, US
• Renato Skerlj · Vancouver, CA
• Roger C. Wiegand · Chesterfield, US
• Dyann F. Wirth · Boston, US

Key dates

• Filing date: May 7, 2009
• Grant date: Apr 22, 2014
• Expiry date: Nov 7, 2029

Classification

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

Abstract

Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.