公开(公告)号：EP1949896A2

公开(公告)日：2008-07-30

申请号：EP08150205.6

申请日：2008-01-14

申请人： The University of North Carolina At Chapel Hill ,  GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. ,  Werbovetz, Karl ,  Brun, Reto

发明人： Werbovetz, Karl ,  Brun, Reto ,  Tidwell, Richard R. ,  Boykin, David W. ,  Ismail, Mohamed A. ,  Wilson, W. David ,  Arafa, Reem K. ,  Hu, Laixing

IPC分类号： A61K31/155 ,  C07C257/18 ,  C07C259/18 ,  C07C279/18 ,  C07D213/58 ,  C07D213/26 ,  C07D213/28 ,  C07D239/26 ,  C07D239/28 ,  C07D241/12 ,  C07D241/14 ,  C07D307/46 ,  C07D307/52 ,  C07D307/68 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  A61P33/00

CPC分类号： C07C257/18 ,  C07C259/18 ,  C07C279/18 ,  C07C279/24 ,  C07D213/58 ,  C07D239/26 ,  C07D307/68 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14

摘要： Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues.

        L 1 -Ar 1 -(CH 2 ) p -Ar 2 -(CH 2 ) q -Ar 3 -L 2      (I)

摘要翻译： 新型双阳离子三联苯化合物及其杂环类似物。 用新型双阳离子三联苯化合物及其氮杂类似物对抗微生物感染的方法。 合成新型双线性三联苯化合物及其氮杂类似物的方法。 €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒL1 -Ar 1 - （CH 2）p -Ar 2 - （CH 2）q -Ar 3 -L 2€ƒ€ƒ€ƒ€ ƒ（I）

公开(公告)号：EP1792613A2

公开(公告)日：2007-06-06

申请号：EP06118366.1

申请日：2006-08-03

申请人： UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL ,  GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.

发明人： Tidwell, Richard R. ,  Boykin, David W. ,  Ismail, Mohamed A. ,  Wilson, W. David ,  White, Elizabeth W. ,  Kumar, Arvind ,  Nanjunda, Rupesh

IPC分类号： A61K31/33 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/443 ,  A61P33/02 ,  A61P35/00 ,  C07D307/68 ,  C07D329/00 ,  C07D405/14 ,  C07D421/14

CPC分类号： A61K31/341 ,  A61K31/33 ,  A61K31/381 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/443 ,  C07D345/00 ,  C07D405/14 ,  C07D421/14 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/415

摘要： Dicationic compounds that are highly selective for binding G-quadruplex DNA are described. Several compounds exhibit groove binding toward G-quadruplex DNA and in vitro and in vivo activity versus Trypanosoma brucei rhodesiense. The compounds represent novel drugs for the treatment of cancer, malaria, leishmania, and trypanosomiasis.

摘要翻译： 描述了对结合G-四链体DNA具有高选择性的二价化合物。 几种化合物显示出与G-四链体DNA结合的凹槽，并且与罗氏黑斑病相比体外和体内活性相反。 这些化合物代表用于治疗癌症，疟疾，利什曼原虫和锥虫病的新型药物。

公开(公告)号：EP1244651B1

公开(公告)日：2006-11-22

申请号：EP00989364.5

申请日：2000-12-20

申请人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL ,  GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.

发明人： Wilson, W. David ,  Boykin, David ,  Tidwell, Richard R.

IPC分类号： C07D405/04 ,  C12Q1/68 ,  A61K31/415 ,  A61P31/04 ,  A61P35/00

CPC分类号： C07D207/416 ,  C07D307/54 ,  C07D405/04 ,  C07D405/14 ,  C12Q1/6816 ,  C12Q2563/173

摘要： Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.

公开(公告)号：EP1837024A2

公开(公告)日：2007-09-26

申请号：EP07110507.6

申请日：2002-01-11

申请人： UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL ,  GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. ,  Auburn University

发明人： Boykin, David ,  Tidwell, Richard R. ,  Stringfellow, David ,  Brock, Kenny ,  Stephens, Chad E. ,  Kumar, Arvind ,  Wilson, W. David ,  Givens, Daniel ,  Dykstra, Christine

IPC分类号： A61K31/505

CPC分类号： C07D405/10 ,  C07D207/337 ,  C07D277/30 ,  C07D307/54 ,  C07D333/24

摘要： The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of virtases. Compounds of the present invention will have a structure according to Formulas (I) - (VI) as recited throughout the application.

摘要翻译： 本发明涉及新的化合物和方法可用于治疗黄病毒科的virtases的那样成员有用的。 本发明的化合物将具有雅鼎的结构式（I） - 如权利整个申请（VI）。

公开(公告)号：EP1726589A3

公开(公告)日：2006-12-13

申请号：EP06114189.1

申请日：2006-05-19

申请人： UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL ,  GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. ,  Werbovetz, Karl ,  Brun, Reto

发明人： Werbovetz, Karl ,  Brun, Reto ,  Tidwell, Richard R. ,  Boykin, David W. ,  Stephens, Chad E. ,  Ismail, Mohamed A. ,  Wilson, W. David

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

CPC分类号： C07D307/68 ,  C07D307/54 ,  C07D333/24 ,  C07D333/38 ,  C07D345/00 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D421/14

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

摘要翻译： 描述了新的式（I）的双阳离子双酚类化合物。 目前公开的新型双阳离子双苯乙烯类化合物相对于喷他脒和呋咱英表现出与布氏罗得西亚罗得西亚虫，恶性疟原虫或杜氏利什曼原虫相比的体外活性。 一些新型双阳离子双酚类化合物在布氏锥虫罗得斯菌感染的小鼠模型中显示出良好的体内活性。 其中：X 1和X 2独立地选自O，S，Se，Te和NR 1，Ar 1和Ar 2独立地选自由苯基，吡啶和苯并咪唑组成的组; Am1和Am2都是

公开(公告)号：EP1726589A2

公开(公告)日：2006-11-29

申请号：EP06114189.1

申请日：2006-05-19

申请人： UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL ,  GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. ,  Werbovetz, Karl ,  Brun, Reto

发明人： Werbovetz, Karl ,  Brun, Reto ,  Tidwell, Richard R. ,  Boykin, David W. ,  Stephens, Chad E. ,  Ismail, Mohamed A. ,  Wilson, W. David

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

CPC分类号： C07D307/68 ,  C07D307/54 ,  C07D333/24 ,  C07D333/38 ,  C07D345/00 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D421/14

摘要： Novel dicationic bichalcophene compounds 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.

摘要翻译： 描述了式（I）的新型双阳离子双生烯烃化合物。 目前公开的新型双阳离子双生命烯化合物显示体外活性与罗氏黑斑病，恶性疟原虫或杜氏不动症相当，与戊脒和呋脒相当。 一些新型双阳离子双生命烯化合物在罗氏黑斑病感染的鼠模型中在体内表现出良好的活性。 其中：X 1和X 2独立地选自O，S，Se，Te和NR 1，Ar 1和Ar 2独立地选自苯基，吡啶和苯并咪唑; Am 1和Am 2各自

公开(公告)号：EP1736466A1

公开(公告)日：2006-12-27

申请号：EP06011533.4

申请日：2006-06-02

申请人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL ,  GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. ,  Werbovetz, Karl ,  Brun, Reto

发明人： Werbovetz, Karl ,  Brun, Reto ,  Tidwell, Richard R. ,  Boykin, David W. ,  Ismail, Mohamed A. ,  Wilson, David W. ,  Arafa, Reem K.

IPC分类号： C07C257/18 ,  C07C279/18 ,  C07D307/68 ,  C07D213/58 ,  C07D405/04 ,  A61K31/435 ,  A61K31/341 ,  A61K31/155 ,  A61P31/04 ,  C07D239/26 ,  C07D405/14 ,  C07D401/14 ,  C07D213/74

CPC分类号： C07D213/58 ,  C07C257/18 ,  C07C259/18 ,  C07C279/18 ,  C07D213/74 ,  C07D213/75 ,  C07D239/26 ,  C07D307/54 ,  C07D307/68 ,  C07D401/10 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14

摘要： Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues.

摘要翻译： 新型双阳离子三联苯化合物及其杂环类似物。 用新型双阳离子三联苯化合物及其氮杂类似物对抗微生物感染的方法。 合成新型双线性三联苯化合物及其氮杂类似物的方法。

公开(公告)号：EP1244651A1

公开(公告)日：2002-10-02

申请号：EP00989364.5

申请日：2000-12-20

申请人： The University of North Carolina at Chapel Hill ,  GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.

发明人： Wilson, W. David ,  Boykin, David ,  Tidwell, Richard R.

IPC分类号： C07D405/04 ,  C12Q1/68 ,  A61K31/415 ,  A61P31/04 ,  A61P35/00

CPC分类号： C07D207/416 ,  C07D307/54 ,  C07D405/04 ,  C07D405/14 ,  C12Q1/6816 ,  C12Q2563/173

摘要： Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.

公开(公告)号：EP1726589B1

公开(公告)日：2008-10-15

申请号：EP06114189.1

申请日：2006-05-19

申请人： The University of North Carolina at Chapel Hill ,  GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. ,  Werbovetz, Karl ,  Brun, Reto

发明人： Werbovetz, Karl ,  Brun, Reto ,  Tidwell, Richard R. ,  Boykin, David W. ,  Stephens, Chad E. ,  Ismail, Mohamed A. ,  Wilson, W. David

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

CPC分类号： C07D307/68 ,  C07D307/54 ,  C07D333/24 ,  C07D333/38 ,  C07D345/00 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D421/14

公开(公告)号：EP1949896A3

公开(公告)日：2008-08-06

申请号：EP08150205.6

申请日：2008-01-14

申请人： The University of North Carolina At Chapel Hill ,  GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. ,  Werbovetz, Karl ,  Brun, Reto

发明人： Werbovetz, Karl ,  Brun, Reto ,  Tidwell, Richard R. ,  Boykin, David W. ,  Ismail, Mohamed A. ,  Wilson, W. David ,  Arafa, Reem K. ,  Hu, Laixing

IPC分类号： A61K31/155 ,  C07C257/18 ,  C07C259/18 ,  C07C279/18 ,  C07D213/58 ,  C07D213/26 ,  C07D213/28 ,  C07D239/26 ,  C07D239/28 ,  C07D241/12 ,  C07D241/14 ,  C07D307/46 ,  C07D307/52 ,  C07D307/68 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  A61P33/00

CPC分类号： C07C257/18 ,  C07C259/18 ,  C07C279/18 ,  C07C279/24 ,  C07D213/58 ,  C07D239/26 ,  C07D307/68 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14

摘要： Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues.

        L 1 -Ar 1 -(CH 2 ) p -Ar 2 -(CH 2 ) q -Ar 3 -L 2      (I)