Medicines for Malaria Venture, ICC, Route de Pre-Bois 20, PO Box 1826, 1215 Geneva 15, Switzerland.
Expert Opin Ther Pat. 2012 Jun;22(6):607-43. doi: 10.1517/13543776.2012.691967.
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.
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.
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.
疟疾造成了巨大的人道主义和经济负担。寄生虫对现有和最近推出的抗疟药物的耐药性是一个主要问题,再加上消除疟疾的议程,这意味着我们非常需要新的小分子抗疟药物。最近疟疾药物发现和开发的资金大量增加,推动了这一领域的发展,使得抗疟药物管道中有越来越多的化合物。
本文综述了 2010 年 1 月至 2011 年 6 月期间以治疗疟疾的小分子为特色的英文专利,描述了约 50 个系列的化合物。不包括涉及临床应用、诊断试剂盒或疫苗的专利,也不包括主要疾病焦点不是疟疾的专利。
疟疾小分子领域的活动相当多,而且可能会继续下去。最终目标是确定新型药物来支持消除疟疾的议程。这需要安全有效的化合物,来自新颖的化学类型,这些化合物可以从廉价的起始材料中快速合成,并且对寄生虫具有快速杀伤作用。此外,与针对寄生虫无性血阶段的现有抗疟系列相关的类似物相比,具有肝脏阶段或阻断传播活性的化合物可能会被优先开发。