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1. 发明申请

WO0236588A3 REVERSED AMIDINES AND METHODS OF USING FOR TREATING, PREVENTING, OR INHIBITING LEISHMANIASIS 审中-公开
标题翻译：反转的药物及其用于治疗，预防或抑制感染的方法
公开(公告)号：WO0236588A3
公开(公告)日：2003-08-28
申请号：PCT/US0142905
申请日：2001-11-05
申请人： US ARMY MED RES MAT COMMAND , WERBOVETZ KARL A , BRENDLE JAMES J , BOYKIN DAVID W , STEPHENS CHAD E
发明人： WERBOVETZ KARL A , BRENDLE JAMES J , BOYKIN DAVID W , STEPHENS CHAD E
IPC分类号： A61K31/341 , A61K31/381 , A61K31/4184 , A61K31/444 , A61K31/4709 , C07D307/52 , C07D333/20 , C07D405/04 , C07D405/12 , C07D405/14 , C07D405/00
CPC分类号： C07D405/04 , A61K31/341 , A61K31/381 , A61K31/4184 , A61K31/444 , A61K31/4709 , C07D307/52 , C07D333/20 , C07D405/12 , C07D405/14
摘要： Methods for treating, preventing or inhibiting leishmaniasis in a subject comprising administering to the subject a therapeutically effective amount of at least one compound having the structural formula (I) wherein Y is a heteroatom; R and R are independently H or an alkyl, cycloalkyl, heterocycloalkyl, aryl, amino or heteroaryl group; and X , X , and X3 are independently H or an alkyl, alkoxy, halo, amino, alkylamino, dialkylamino acylamino, alkylthio, sulfonyl, cyano, carboxy alkoxycarbonyl, or carbamoyl group are disclosed.
摘要翻译：用于治疗，预防或抑制受试者利什曼病的方法，包括向受试者施用治疗有效量的至少一种具有结构式（I）的化合物，其中Y为杂原子; R 1和R 2独立地为H或烷基，环烷基，杂环烷基，芳基，氨基或杂芳基; X 1，X 2和X 3独立地为H或烷基，烷氧基，卤素，氨基，烷基氨基，二烷基氨基酰氨基，烷硫基，磺酰基，氰基，羧基烷氧基羰基或氨基甲酰基。

2. 发明申请

WO2009051796A3 2,5-DIARYL SELENOPHENE COMPOUNDS, AZA 2,5-DIARYL THIOPHENE COMPOUNDS, AND THEIR PRODRUGS AS ANTIPROTOZOAL AGENTS 审中-公开
标题翻译： 2,5-二芳基硒苯化合物，AZA 2,5-二芳基噻吩化合物及其作为抗原生药剂的前药
公开(公告)号：WO2009051796A3
公开(公告)日：2009-06-04
申请号：PCT/US2008011870
申请日：2008-10-17
申请人： UNIV NORTH CAROLINA , UNIV GEORGIA STATE RES FOUND , BRUN RETO , WERBOVETZ KARL , TIDWELL RICHARD R , BOYKIN DAVID W , STEPHENS CHAD E , ISMAIL MOHAMED A , KUMAR ARVIND , WILSON W DAVID
发明人： BRUN RETO , WERBOVETZ KARL , TIDWELL RICHARD R , BOYKIN DAVID W , STEPHENS CHAD E , ISMAIL MOHAMED A , KUMAR ARVIND , WILSON W DAVID
IPC分类号： C07D345/00 , A61K31/4436 , A61K31/546 , A61P31/00 , A61P33/00 , C07D417/14 , C07D421/04 , C07D421/14
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：描述了新的双阳离子2,5-二芳基硒酚化合物。还描述了双阳离子2,5-二芳基噻吩的新型氮杂类似物。目前公开的双阳离子化合物显示出与喷他脒和芬拉米丁相当的体外活性相对于布氏罗得西亚罗得西亚种，恶性疟原虫和/或杜氏利什曼原虫。一些新型双阳离子化合物在布氏罗得西亚锥虫（Rotpanosoma brucei rhodesiense）感染的小鼠模型中显示出良好的体内活性。

3. 发明申请

WO2005086754A3 DICATIONIC COMPOUNDS FOR ACTIVITY AGAINST TRICHOMONAS VAGINALIS 审中-公开
标题翻译：针对三氯乙烯VACINALIS的活性化合物
公开(公告)号：WO2005086754A3
公开(公告)日：2006-09-08
申请号：PCT/US2005007316
申请日：2005-03-07
申请人： UNIV GEORGIA STATE RES FOUND , US GOV HEALTH & HUMAN SERV , BOYKIN DAVID W , STEPHENS CHAD E , SECOR W EVAN , CROWELL ANDREA L , KUMAR ARVIND
发明人： BOYKIN DAVID W , STEPHENS CHAD E , SECOR W EVAN , CROWELL ANDREA L , KUMAR ARVIND
IPC分类号： A61K31/341
CPC分类号： A61K31/341 , A61K31/4184 , C07D235/20 , C07D413/14
摘要： Dicationic compounds for the treatment of T. vaginalis infections are described. The presently described compounds exhibit in vitro activity against metronidazole-sensitive and -resistant T. vaginalis isolates. Furthermore, the presently described compounds demonstrate IC 50 concentrations that were not elevated in the metronidazole resistant isolate, suggesting that their activity is not affected by parasite mechanisms that confer resistance to 5-nitroimidizoles.
摘要翻译：描述了用于治疗阴道炎感染的阳离子化合物。目前描述的化合物显示针对甲硝唑敏感和抗性阴道分泌物的体外活性。此外，目前描述的化合物表现出在甲硝唑抗性分离物中未升高的IC 50浓度，表明它们的活性不受赋予5-硝基亚氨基咪唑抗性的寄生虫机制的影响。

4. 发明申请

WO2005051296A2 FUSED RING DICATIONIC ANTI-PROTOZOAN AGENTS AND THEIR PRODRUGS 审中-公开
标题翻译：熔合环反应原催化剂及其产品
公开(公告)号：WO2005051296A2
公开(公告)日：2005-06-09
申请号：PCT/US2004038896
申请日：2004-11-18
申请人： UNIV NORTH CAROLINA , UNIV GEORGIA STATE RES FOUND , BOYKIN DAVID W , TIDWELL RICHARD R , WILSON DAVID W , BRUN RETO , ARAFA REEM K , STEPHENS CHAD E
发明人： BOYKIN DAVID W , TIDWELL RICHARD R , WILSON DAVID W , BRUN RETO , ARAFA REEM K , STEPHENS CHAD E
IPC分类号： A01N37/52 , A01N43/42 , A61K20060101 , A61K31/155 , A61K31/44 , A61K31/444 , A61K31/473 , C07C279/18 , C07C279/24 , C07D219/00 , C07D219/08 , A61K
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 faciparum. 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布氏罗得西亚锥虫（T.b.r）和弗氏疟原虫（Plasmodium faciparum）。这些化合物的前体药物可以用作疟疾和非洲人类锥虫病的口服治疗。

5. 发明申请

WO2004050018A3 DICATIONIC 2,5-DIARYLFURAN AZA-ANALOGS AS ANTI-PROTOZOAN AGENTS 审中-公开
标题翻译：作为抗真菌药物的二异丙基呋喃亚胺类似物
公开(公告)号：WO2004050018A3
公开(公告)日：2004-07-08
申请号：PCT/US0337691
申请日：2003-11-25
申请人： UNIV NORTH CAROLINA , UNIV GEORGIA STATE RES FOUND , BOYKIN DAVID W , TIDWELL RICHARD R , ISMAIL MOHAMED A , BRUN RETO
发明人： BOYKIN DAVID W , TIDWELL RICHARD R , ISMAIL MOHAMED A , BRUN RETO
IPC分类号： A61K20060101 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/443 , A61K31/4436 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , C07D405/04 , C07D409/04
CPC分类号： C07D307/38 , C07D307/54 , C07D333/08 , C07D405/04 , C07D405/14 , C07D407/04 , C07D407/14 , C07D409/04 , C07D409/14
摘要： A compound of Formula (I): wherein: X is selected from the group consisting of O, S, and NR where R is hydrogen or lower alkyl; C , C , A, and Y are CH, N, NR O, or S, wherein C and C are the same or different; D , D , B, and Z are CH, N, or NR wherein D and D are the same or different; provided that B, Z, or both B and Z are not present when A, Y, or both A and Y are O, S, or NR ; R ,R , R , R , R and R are selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R and R are each independently selected from the group consisting of H, hydroxy, lower alkyl, cycloalkyl, aryl, aralkyl, alkoxyl, hydroxycycloalkyl, alkoxycycloalkyl, hydroxyalkyl, aminoalkyl, acyloxy, acetoxy, and alkylaminoalkyl; and R , R , R and R are each independently selected from the group consisting of H, lower alkyl, alkoxyalkyl, cycloalkyl, aryl, aralkyl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl, or R and R together or R and R together represent a C2 to C10 alkyl, hydroxyalkyl, or alkylene, or R and R together or R and R together are: wherein n is a number from 1 to 3, and R is H or-CONHR NR R , wherein R , is lower alkyl and R and R are each independently selected from the group consisting of H and lower alkyl.
摘要翻译：式（I）的化合物：其中：X选自O，S和NR 17，其中R 17是氢或低级烷基; C 1，C 2，A和Y是CH，N，NR 17，O或S，其中C 1和C 2相同或不同; D 1，D 2，B和Z是CH，N或NR 17，其中D 1和D 2是相同或不同的; 条件是当A，Y或A和Y都为O，S或NR 17时，B，Z或两者均不存在B和Z。 R 13，R 14，R 15，R 16，R 1和R 8选自H，低级烷基，卤素，烷氧基，芳氧基，芳烷氧基和羟基 ; R 3和R 6各自独立地选自H，羟基，低级烷基，环烷基，芳基，芳烷基，烷氧基，羟基环烷基，烷氧基环烷基，羟基烷基，氨基烷基，酰氧基，乙酰氧基和烷基氨基烷基。和R 2，R 4，R 5和R 7各自独立地选自H，低级烷基，烷氧基烷基，环烷基，芳基，芳烷基，羟基烷基，氨基烷基和烷基氨基烷基，或 R 2和R 4一起或R 5和R 7一起代表C 2至C 10烷基，羟烷基或亚烷基，或R 3和R 4一起或R 6和 R 7一起是：其中n是1至3的数，R 9是H或-CONHR 10 NR 11 R 12，其中R 10是低级烷基和R <11>和R 12各自独立地选自H和低级烷基。

6. 发明申请

WO2005086808A3 NOVEL DICATIONIC IMIDAZO[1,2-a]PYRIDINES AND 5,6,7,8-TETRAHYDRO-IMIDAZO[1,2a]PYRIDINES AS ANTIPROTOZOAL AGENTS 审中-公开
标题翻译：新颖的咪唑并[1,2-a]吡啶和5,6,7,8-四氢-1H-咪唑并[1,2a]吡啶作为抗真菌剂
公开(公告)号：WO2005086808A3
公开(公告)日：2006-02-23
申请号：PCT/US2005007566
申请日：2005-03-08
申请人： UNIV NORTH CAROLINA , UNIV GEORGIA STATE RES FOUND , BOYKIN DAVID W , TIDWELL RICHARD R , WILSON W DAVID , ISMAIL MOHAMED A
发明人： BOYKIN DAVID W , TIDWELL RICHARD R , WILSON W DAVID , ISMAIL MOHAMED A
IPC分类号： A61K31/4745 , C07D471/02 , C07D471/04 , A61K31/44
CPC分类号： C07D471/04
摘要： A method for treating a microbial infection, including an infection from a protozoan pathogen, such as Trypanosoma brucei rhodesiense and Plasmodium falciparum, in a subject in need thereof by administering to the subject an effective amount of a dicationic imidazopyridine compound or a dicationic tetrahydro-imidazopyridine compound. Processes for synthesizing dicationic imidazopyridines and dicationic tetrahydro-imidazopyridines and the novel dicationic imidazopyridine and dicationic tetrahydro-imidazopyridine compounds themselves.
摘要翻译：一种用于治疗微生物感染的方法，包括通过向受试者施用有效量的双阳离子咪唑并吡啶化合物或双阳离子四氢 - 咪唑并吡啶化合物，在有需要的受试者中治疗来自原生动物病原体（例如，罗氏黑曲霉和恶性疟原虫）的感染复合。双阳离子咪唑并吡啶和双阳离子四氢 - 咪唑并吡啶的合成方法以及新型的双阳离子咪唑并吡啶和双阳离子四氢 - 咪唑并吡啶化合物本身。

7. 发明申请

WO0103685A3 NOVEL PRODRUGS FOR ANTIMICROBIAL AMIDINES 审中-公开
标题翻译：新型抗菌药物
公开(公告)号：WO0103685A3
公开(公告)日：2002-07-11
申请号：PCT/US0018499
申请日：2000-07-06
申请人： UNIV NORTH CAROLINA , BOYKIN DAVID W , RAHMATHULLAH M SYED , TIDWELL RICHARD R , HALL JAMES E
发明人： BOYKIN DAVID W , RAHMATHULLAH M SYED , TIDWELL RICHARD R , HALL JAMES E
IPC分类号： C07D307/52 , A61K31/341 , A61K31/357 , A61K47/48 , A61P31/00 , A61P31/04 , A61P31/06 , C07D307/54 , C07D407/12 , C07D407/14 , A61K31/40 , A61K31/34 , A61K31/38 , C07D207/32 , C07D333/24
CPC分类号： C07D407/14 , A61K31/341 , A61K47/54 , A61K47/555 , C07D307/54
摘要： A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by Formula (I), wherein: X may be O, S, or NR' wherein R' is H or loweralkyl; R1 and R2 may be independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl; R3 and R4 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, and oxyarylalkyl; R5 is represented by a formula selected from the group consisting of: (a) and (b), wherein: X1, X2, and X3 are independently selected from O and S; and R6 and R7 are independently selected from the group consisting of loweralkyl, aryl, alkylaryl, oxyaryl, an ester-containing substituent, and oxyalkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：治疗感染的方法包括施用治疗有效量的式（I）所述的化合物，其中：X可以是O，S或NR'，其中R'是H或低级烷基; R 1和R 2可以独立地选自H，低级烷基，烷氧基烷基，烷氧基烷基，环烷基，芳基，羟基烷基，氨基烷基和烷基氨基烷基; R 3和R 4各自独立地选自H，低级烷基，卤素，氧烷基，氧芳基和氧芳基烷基; R5由选自（a）和（b）的化合物表示，其中：X 1，X 2和X 3独立地选自O和S; R 6和R 7独立地选自低级烷基，芳基，烷芳基，氧芳基，含酯取代基和烷氧基烷基; 或其药学上可接受的盐。

8. 发明申请

WO2004051217A3 PROCESS FOR SYNTHESIS BIS-ARYL DIAMIDOXIME COMPOUNDS 审中-公开
标题翻译：合成双联氨基二异氰酸酯化合物的方法
公开(公告)号：WO2004051217A3
公开(公告)日：2004-07-08
申请号：PCT/US0337788
申请日：2003-11-25
申请人： UNIV NORTH CAROLINA , UNIV GEORGIA STATE RES FOUND , BOYKIN DAVID W , ANBAZHAGAN MARIAPPAN , TIDWELL RICHARD R
发明人： BOYKIN DAVID W , ANBAZHAGAN MARIAPPAN , TIDWELL RICHARD R
IPC分类号： C07C249/00 , C07D207/46 , C07D307/02 , C07D333/12 , C07D405/00 , G01N20060101
CPC分类号： C07D307/54
摘要： Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl] furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-0-alkylamidinophenyl] furans, are useful as therapeutic compounds. The disclosed process is scalable, simpler, more economic and more feasible than other presently known methods of preparing 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl] furans and other bis-aryl diamidoxime compounds.
摘要翻译：双芳基二肟化合物，如2,5-双[4-羟基和4-O-烷基脒基苯基]呋喃，可以通过一步钯催化的交叉反应由2,5-双三烷基锡烷制备。双芳基二肟化合物，例如2,5-双[4-羟基和4-0-烷基脒基苯基]呋喃，可用作治疗化合物。所公开的方法比其它目前已知的制备2,5-双[4-羟基和4-O-烷基脒基苯基]呋喃和其它双芳基二肟基化合物的方法是可扩展的，更简单的，更经济的和更可行的。

9. 发明申请

WO0015212A3 ANTIFUNGAL ACTIVITY OF DICATIONIC MOLECULES 审中-公开
标题翻译：定向分子的抗真菌活性
公开(公告)号：WO0015212A3
公开(公告)日：2001-08-16
申请号：PCT/US9921383
申请日：1999-09-15
申请人： UNIV NORTH CAROLINA , UNIV GEORGIA STATE RES FOUND , UNIV DUKE , TIDWELL RICHARD R , BOYKIN DAVID W , PERFECT JOHN R
发明人： TIDWELL RICHARD R , BOYKIN DAVID W , PERFECT JOHN R
IPC分类号： C07D235/20 , A61K31/00 , A61K31/155 , A61K31/341 , A61K31/343 , A61K31/4184 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/5355 , A61K31/5377 , A61P31/10 , C07D307/14 , C07D307/18 , C07D307/81 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/14 , C07D409/14
CPC分类号： A61K31/4184 , A61K31/00 , A61K31/341
摘要： Methods of treating fungal infections comprise administering a therapeutically effective amount of a compound described by Formulas (I-VI). Examples of fungal infections include Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Fusarium solani, and combinations thereof.
摘要翻译：治疗真菌感染的方法包括施用治疗有效量的式（I-VI）所述的化合物。真菌感染的实例包括白色念珠菌，新型隐球酵母，烟曲霉，茄病镰刀菌及其组合。

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