-
公开(公告)号:US07371778B2
公开(公告)日:2008-05-13
申请号:US11121451
申请日:2005-05-04
申请人: Jonathan L. Vennerstrom , Yuxiang Dong , Jacques Chollet , Hugues Matile , Xiaofang Wang , Kamaraj Spiraghavan , William N. Chapman
发明人: Jonathan L. Vennerstrom , Yuxiang Dong , Jacques Chollet , Hugues Matile , Xiaofang Wang , Kamaraj Spiraghavan , William N. Chapman
IPC分类号: A61K31/357 , C07D323/02
CPC分类号: A61K31/335 , C07D323/02 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , C07D417/06 , C07D417/12 , C07D491/10 , C07D493/10 , C07D495/10 , Y02A50/411 , Y02A50/423
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, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.
摘要翻译: 描述了使用螺或二脱氧-1,2,4-三恶烷来治疗疟疾,血吸虫病和癌症的方法和方法。 优选的1,2,4-三氧杂环戊烷在三氧杂环戊烷基的一侧包括一个双金刚烷基,在三氧杂环戊烷基的另一侧包括一个螺环己基,因此螺环己基环优选在4位被取代。 与青蒿素半合成衍生物相比,本发明的化合物在结构上简单,易于合成,无毒,对抗疟疾寄生虫有效。
-
公开(公告)号:US08067620B2
公开(公告)日:2011-11-29
申请号:US11930606
申请日:2007-10-31
申请人: Jonathan L. Vennerstrom , Yuxiang Dong , Susan A. Charman , Sergio Wittlin , Jacques Chollet , Darren J. Creek , Xiaofang Wang , Kamaraj Spiraghavan , Lin Zhou , Hugues Matile , William N. Charman
发明人: Jonathan L. Vennerstrom , Yuxiang Dong , Susan A. Charman , Sergio Wittlin , Jacques Chollet , Darren J. Creek , Xiaofang Wang , Kamaraj Spiraghavan , Lin Zhou , Hugues Matile , William N. Charman
IPC分类号: A61K31/357 , C07D323/02
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.
摘要翻译: 描述了使用螺或二脱氧-1,2,4-三恶烷来治疗疟疾,血吸虫病和癌症的方法和方法。 优选的1,2,4-三氧杂环戊烷在三氧杂环戊烷基的一侧包括一个双金刚烷基,在三氧杂环戊烷基的另一侧包括一个螺环己基。 与青蒿素半合成衍生物相比,本发明的化合物在结构上简单,易于合成,无毒,对抗疟疾寄生虫有效。 本发明的化合物意外地提供了用于疟疾的单剂量治疗,以及针对其的预防活性。 这些化合物对抗血吸虫病和癌症也是有效的。
-