Antimalarial compound identification and design: advances in the patent literature, 2000 – 2003

Abstract

World patents filed from 2000 to 2003 claiming specific in vitro or in vivo antimalarial activity are examined and compiled in this review in a format that allows comparison across different chemical classes or drug targets. The most over-represented classes include the 1-desoxy-D-xylulose 5-phosphate (DOXP) reductoisomerase inhibitors and novel quinoline or artemisinin analogues. This finding can be linked to important trends in the clinical development of new antimalarial drugs. Patents disclosing novel classes of antimalarial drugs were scarce. This may mean that the target-directed screening effort in malaria has not yet come to fruition, has not been commercially exploited in an appropriate manner, or that next generation compounds in known drug classes are more viable commercial entities.

• antifolate
• artemisinin
• drug discovery
• malaria
• Plasmodium falciparum
• quinoline