发明公开
EP1726589A3 5,5'-bis-(4-amidinophenyl)-2,2'-bifuran derivatives and related compounds as antiprotozoal agent and prodrugs thereof
有权
5,5'-双 - （4-脒基苯基）-2,2'-联呋喃衍生物和作为抗原虫剂的相关化合物及其前药
- 专利标题： 5,5'-bis-(4-amidinophenyl)-2,2'-bifuran derivatives and related compounds as antiprotozoal agent and prodrugs thereof
- 专利标题（中）： 5,5'-双 - （4-脒基苯基）-2,2'-联呋喃衍生物和作为抗原虫剂的相关化合物及其前药
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申请号： EP06114189.1申请日： 2006-05-19
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公开(公告)号： EP1726589A3公开(公告)日： 2006-12-13
- 发明人: Werbovetz, Karl , Brun, Reto , Tidwell, Richard R. , Boykin, David W. , Stephens, Chad E. , Ismail, Mohamed A. , Wilson, W. David
- 申请人： UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , Werbovetz, Karl , Brun, Reto
- 申请人地址： 308 Bynum Hall, Campus Box 4105 Chapel Hill, NC 27599-4105 US
- 专利权人： UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL,GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.,Werbovetz, Karl,Brun, Reto
- 当前专利权人： UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL,GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.,Werbovetz, Karl,Brun, Reto
- 当前专利权人地址： 308 Bynum Hall, Campus Box 4105 Chapel Hill, NC 27599-4105 US
- 代理机构： Behnisch, Werner
- 优先权： US683177P 20050520
- 主分类号： C07D307/68
- IPC分类号： C07D307/68 ; C07D405/04 ; C07D307/54 ; C07D333/24 ; C07D345/00 ; C07D421/04 ; C07C257/18 ; C07C259/18 ; A61K31/341 ; A61K31/443 ; A61K31/381 ; A61K31/4436 ; A61K31/4427 ; A61K31/4184 ; A61P33/02 ; A61P33/06
摘要：
Novel dicationic bichalcophene compounds of formula (I) are described. The presently disclosed novel dicationic bichalcophene compounds exhibit in vitro activity versus Trypanosoma brucei rhodesiense, Plasmodium falciparum, or Leishmania donovani comparable to that of pentamidine and furamidine. Some of the novel dicationic bichalcophene compounds displayed good activity in vivo in a murine model of a Trypanosoma brucei rhodesiense infection.
wherein:
X 1 and X 2 are independetly selected from the group consisting of O, S, Se, Te, and NR 1 ,
Ar 1 and Ar 2 are independently selected from the group consisting of phenyl, pyridine, and benzimidazole;
Am 1 and Am 2 are each
wherein:
X 1 and X 2 are independetly selected from the group consisting of O, S, Se, Te, and NR 1 ,
Ar 1 and Ar 2 are independently selected from the group consisting of phenyl, pyridine, and benzimidazole;
Am 1 and Am 2 are each
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