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公开(公告)号：US07825279B2
公开(公告)日：2010-11-02
申请号：US10992607
申请日：2004-11-18
申请人： David W. Boykin , Richard R. Tidwell , W. David Wilson , Reto Brun , Reem K. Arafa , Chad E. Stephens
发明人： David W. Boykin , Richard R. Tidwell , W. David Wilson , Reto Brun , Reem K. Arafa , Chad E. Stephens
IPC分类号： C07C279/18 , C07D219/12 , C07D213/06 , A61K31/155 , A61K31/235 , A61K31/24 , A61K31/44
CPC分类号： C07D219/08 , C07C257/18 , C07C279/18 , C07C279/24 , C07C291/04 , C07C2603/18 , C07C2603/24
摘要： Novel fused ring dicationic anti-protozoan compounds. Representative protozoan species include but are not limited to Trypanosoma brucei rhodesiense (T.b.r.) and Plasmodium falciparum. Prodrugs of these compounds can be used as an oral treatment for malaria and human African trypanosomiasis.
摘要翻译： 新型稠环双阳离子抗原生动物化合物。 代表性的原生动物物种包括但不限于罗非鱼锥虫（T.b.r.）和恶性疟原虫。 这些化合物的前药可用作疟疾和人类非洲锥虫病的口服治疗。
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公开(公告)号：US07964619B2
公开(公告)日：2011-06-21
申请号：US11698257
申请日：2007-01-25
申请人： Richard R. Tidwell , David W. Boykin , W. David Wilson , Reto Brun , Laixing Hu , Karl Werbovetz , Mohamed A. Ismail , Reem K. Arafa
发明人： Richard R. Tidwell , David W. Boykin , W. David Wilson , Reto Brun , Laixing Hu , Karl Werbovetz , Mohamed A. Ismail , Reem K. Arafa
IPC分类号： A61K31/44
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： Disclosed herein are novel dicationic teraryl compounds and their aza analogues, including compounds of Formula (IIe): wherein p and q are each 0 and each A, Y and Z is CR4. An exemplary compound of Formula (IIe) is: Methods for combating microbial infections, such as parasitic Leishmania species, with novel dicationic terphenyl compounds and their aza analogues are included. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues are disclosed along with methods for evaluation of the compounds as potential anti-protozoan agents.
摘要翻译： 本文公开的是新型二次辛基化合物及其氮杂类似物，包括式（IIe）的化合物：其中p和q各自为0，并且每个A，Y和Z为CR 4。 式（IIe）的示例性化合物是：包括用于防治微生物感染的方法，例如寄生的利什曼原虫属物种，具有新型双阳离子三联苯化合物及其氮杂类似物。 公开了用于合成新型双阳离子三联苯化合物及其氮杂类似物的方法以及用于评估化合物作为潜在的抗原生动物剂的方法。
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公开(公告)号：US08188121B2
公开(公告)日：2012-05-29
申请号：US13162907
申请日：2011-06-17
申请人： Richard R. Tidwell , David W. Boykin , W. David Wilson , Reto Brun , Karl Werbovetz , Mohamed A. Ismail , Reem K. Arafa , Laixing Hu
发明人： Richard R. Tidwell , David W. Boykin , W. David Wilson , Reto Brun , Karl Werbovetz , Mohamed A. Ismail , Reem K. Arafa , Laixing Hu
IPC分类号： A61K31/44
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 aza analogues of dicationic terphenyl compounds for use in combating microbial infections are described. The compounds include those of Formula (III): wherein one of A1, Y1, and Z1 is N; Ar1 is phenylene; and Ar3 is a nitrogen-containing aromatic group. An exemplary compound of Formula (III) is:
摘要翻译： 描述了用于防治微生物感染的双阳离子三联苯化合物的新型氮杂类似物。 化合物包括式（III）的化合物：其中A1，Y1和Z1中的一个为N; Ar1为亚苯基; 而Ar 3为含氮芳族基团。 式（III）的示例性化合物是：
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4.发明授权Linear dicationic terphenyls and their aza analogues as antiparasitic agents 失效线性双阳离子三联苯及其氮杂类似物作为抗寄生虫剂公开(公告)号：US08101636B2
公开(公告)日：2012-01-24
申请号：US11436045
申请日：2006-05-17
申请人： Richard R. Tidwell , David W. Boykin , W. David Wilson , Reto Brun , Karl Werbovetz , Mohamed A. Ismail , Reem K. Arafa
发明人： Richard R. Tidwell , David W. Boykin , W. David Wilson , Reto Brun , Karl Werbovetz , Mohamed A. Ismail , Reem K. Arafa
IPC分类号： C07D213/76 , A61K31/4418 , A61K31/443 , C07D405/04 , A61P33/00
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 aza analogues of dicationic terphenyl compounds for use in combating microbial infections are described. Also described are processes for synthesizing the compounds. The presently disclosed compounds can include those of the formulas: and wherein L1 and L2 are selected from the group consisting of:
摘要翻译： 描述了用于防治微生物感染的双阳离子三联苯化合物的新型氮杂类似物。 还描述了合成化合物的方法。 目前公开的化合物可以包括下式的化合物：其中L1和L2选自：
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公开(公告)号：US20110257199A1
公开(公告)日：2011-10-20
申请号：US13162907
申请日：2011-06-17
申请人： Richard R. Tidwell , David W. Boykin , W. David Wilson , Reto Brun , Karl Werbovetz , Mohamed A. Ismail , Reem K. Arafa , Laixing Hu
发明人： Richard R. Tidwell , David W. Boykin , W. David Wilson , Reto Brun , Karl Werbovetz , Mohamed A. Ismail , Reem K. Arafa , Laixing Hu
IPC分类号： A61K31/506 , A61K31/444 , C07D239/42 , A61K31/505 , C07D213/87 , A61P33/00 , C07D401/14 , C07D401/10 , C07C279/18 , A61K31/155 , C07D405/14 , A61K31/4178 , C07D401/04 , A61K31/4418
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.
摘要翻译： 新型的二联三联苯化合物及其杂环类似物。 用新型双极化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。
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6.发明申请2,5-DIARYL SELENOPHENE COMPOUNDS, AZA 2,5-DIARYL THIOPHENE COMPOUNDS, AND THEIR PRODRUGS AS ANTIPROTOZOAL AGENTS 审中-公开2,5-DIARYL SELENOPHENE化合物，AZA 2,5-二异噻唑化合物及其作为抗真菌药物的产品公开(公告)号：US20100331368A1
公开(公告)日：2010-12-30
申请号：US12680844
申请日：2008-10-17
申请人： Richard R. Tidwell , David W. Boykin , Chad E. Stephens , Mohamed A. Ismail , Arvind Kumar , W. David Wilson , Reto Brun , Karl Werbovetz
发明人： Richard R. Tidwell , David W. Boykin , Chad E. Stephens , Mohamed A. Ismail , Arvind Kumar , W. David Wilson , Reto Brun , Karl Werbovetz
IPC分类号： A61K31/444 , C07D345/00 , A61K31/33 , A61K31/4427 , C07D421/04 , C07D421/14 , C07D409/14 , A61P31/00 , A61P33/02
CPC分类号： C07D345/00 , C07D409/14 , C07D421/04 , C07D421/14
摘要： Novel dicationic 2,5-diaryl selenophene compounds are described. Also described are novel aza analogues of dicationic 2,5-diaryl thiophenes. The presently disclosed dicationic compounds exhibit in vitro activity versus Trypanosoma brucei rhodesiense, Plasmodium falciparum, and/or Leishmania donovani comparable to that of pentamidine and furamidine. Some of the novel dicationic compounds display good activity in vivo in a murine model of a Trypanosoma brucei rhodesiense infection.
摘要翻译： 描述了新型的阳离子2,5-二芳基硒吩化合物。 还描述了双阳离子2,5-二芳基噻吩的新型氮杂类似物。 目前公开的阳离子化合物显示体外活性与罗氏黑斑病，恶性疟原虫和/或与烟脒和呋脒类似的杜氏利什曼原虫的体外活性。 一些新型阳离子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。
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公开(公告)号：US07517893B2
公开(公告)日：2009-04-14
申请号：US11435323
申请日：2006-05-16
申请人： Richard R. Tidwell , David W. Boykin , Chad Stephens , Mohamed A. Ismail , W. David Wilson , Reto Brun , Karl Werbovetz
发明人： Richard R. Tidwell , David W. Boykin , Chad Stephens , Mohamed A. Ismail , W. David Wilson , Reto Brun , Karl Werbovetz
IPC分类号： C07D401/02 , A61K31/44
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烯烃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。
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8.发明授权Methods of combatting infectious diseases using dicationic bis-benzimidazoles 失效使用双极化双苯并咪唑来防治传染病的方法公开(公告)号：US06294565B1
公开(公告)日：2001-09-25
申请号：US09544643
申请日：2000-04-06
IPC分类号： A61K31415
CPC分类号： A61K31/427 , A61K31/4184 , A61K31/422 , A61K31/4439 , A61K31/497 , A61K31/506
摘要： The present invention provides methods for treating Crytococcus neoformans and Candida albicans in a subject in need of such treatment. The methods comprises administering to the subject a dicationic bis-benzimidazole in an amount effective to treat the conditions.
摘要翻译： 本发明提供了在需要这种治疗的受试者中治疗新型隐球菌和白色假丝酵母的方法。 所述方法包括以有效治疗病症的量给予受试者双阳离子双苯并咪唑。
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9.发明授权
公开(公告)号：US6017941A
公开(公告)日：2000-01-25
申请号：US145368
申请日：1998-09-01
IPC分类号： C07D401/14 , A61K31/415 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/445 , A61K31/497 , A61K31/505 , A61K31/506 , A61P31/04 , C07D403/14 , C07D405/14
CPC分类号： A61K31/427 , A61K31/4184 , A61K31/422 , A61K31/4439 , A61K31/497 , A61K31/506
摘要： The present invention provides methods for treating Cryptococcus neoformans and Candida albicans in a subject in need of such treatment. The methods comprises administering to the subject a dicationic bis-benzimidazole in an amount effective to treat the conditions.
摘要翻译： 本发明提供了在需要这种治疗的受试者中治疗新型隐球菌和白色念珠菌的方法。 所述方法包括以有效治疗病症的量给予受试者双阳离子双苯并咪唑。
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公开(公告)号：US5939440A
公开(公告)日：1999-08-17
申请号：US130496
申请日：1998-08-07
IPC分类号： C07D401/14 , A61K31/415 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/445 , A61K31/497 , A61K31/505 , A61K31/506 , A61P31/04 , C07D403/14 , C07D405/14 , C07D235/06
CPC分类号： A61K31/427 , A61K31/4184 , A61K31/422 , A61K31/4439 , A61K31/497 , A61K31/506
摘要： The present invention provides methods for treating Cryptococcus neoformans and Candida albicans in a subject in need of such treatment. The methods comprises administering to the subject a dicationic bis-benzimidazole in an amount effective to treat the conditions.
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