公开(公告)号：EP2203457A2

公开(公告)日：2010-07-07

申请号：EP08845311.3

申请日：2008-10-29

申请人： Medicines For Malaria Venture MMV

发明人： VENNERSTROM, Jonathan, L. ,  DONG, Yuxiang ,  CHARMAN, Susan, A. ,  WITTLIN, Sergio ,  CHOLLET, Jacques ,  CREEK, Darren, J. ,  WANG, Xiaofang ,  SRIRAGHAVAN, Kamaraj ,  ZHOU, Lin ,  MATILE, Hugues ,  CHARMAN, William, N.

IPC分类号： C07D493/10 ,  A61K31/343 ,  A61K31/4525 ,  A61K31/496 ,  A61P33/06 ,  A61K31/553 ,  A61K31/5377 ,  A61K31/541

CPC分类号： C07D493/10 ,  C07D323/02 ,  C07D405/12 ,  C07D413/12

摘要： A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.