公开(公告)号：EP1414813A1

公开(公告)日：2004-05-06

申请号：EP02763208.2

申请日：2002-06-21

申请人： Medicines for Malaria Venture

发明人： VENNERSTROM, J.,University of Nebraska Med. Ctr. ,  CHOLLET, Jacques,Pharma Research Department ,  DONG, Y.,University of Nebraska Medical Center ,  MATILE, Hugues,Pharma Research Department ,  PADMANILAYAM, M.,University of Nebraska Med. Ctr. ,  TANG, Y.,University of Nebraska Medical Center ,  CHARMAN, William N.,Victorian College of Pharmacy

IPC分类号： C07D323/02 ,  C07D493/10 ,  C07D405/14 ,  C07D405/08 ,  C07D419/08 ,  C07D521/00 ,  A61P33/06

CPC分类号： C07D405/12 ,  A61K31/335 ,  A61K31/357 ,  C07D323/02 ,  C07D405/14 ,  C07D491/10 ,  C07D493/10 ,  C07D495/10 ,  Y02A50/411 ,  Y02A50/423 ,  A61K2300/00

摘要： A means and method for treating malaria 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 or spiropiperidyl ring on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably functionalized or substituted at the 4-position or a spiropiperidyl ring that is functionalized or substituted at the nitrogen atom. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.