Small molecule anti-malarial patents: a review (January 2010-June 2011)

摘要

Introduction: Malaria causes a huge humanitarian and economic burden. Parasite resistance to established and recently launched anti-malarials is a major issue which, when combined with a malaria eradication agenda, means there is a considerable need for new small molecule anti-malarials. Catalyzed by a recent surge in funding for malaria drug discovery and development, there is an increasing number of compounds in the malaria pipeline. Areas covered: This review covers patents published in English between January 2010 and June 2011, which feature small molecules for the treatment of malaria. Approximately 50 series of compounds are described. Patents covering clinical applications, diagnosis kits or vaccines are not included, nor patents where the principle disease focus is not malaria. Expert opinion: There is considerable activity in the field of small molecules for malaria which is likely to continue. The ultimate goal is to identify novel drugs to support the malaria eradication agenda. This requires safe and efficacious compounds, from novel chemotypes, which rapidly kill parasites and which are readily synthesized from cheap starting materials. In addition, compounds which have activity in the liver stages or in transmission blocking may be prioritized for development over analogs related to established anti-malarial series targeting the asexual blood stages of the parasite.