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1. 发明申请

WO2005051296A3 FUSED RING DICATIONIC ANTI-PROTOZOAN AGENTS AND THEIR PRODRUGS 审中-公开
公开(公告)号：WO2005051296A3
公开(公告)日：2005-06-09
申请号：PCT/US2004/038896
申请日：2004-11-18
申请人： UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , 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： C07C279/18
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.

2. 发明申请

WO2009051796A2 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-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：WO2009051796A2
公开(公告)日：2009-04-23
申请号：PCT/US2008/011870
申请日：2008-10-17
申请人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , 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 , C07D417/14 , C07D421/04 , C07D421/14 , A61P31/00 , A61P33/00 , A61K31/4436 , A61K31/546
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。

3. 发明申请

WO2019241566A1 AMIDINES AND AMIDINE ANALOGS FOR THE TREATMENT OF BACTERIAL INFECTIONS AND POTENTIATION ANTIBIOTICS 审中-公开
公开(公告)号：WO2019241566A1
公开(公告)日：2019-12-19
申请号：PCT/US2019/037065
申请日：2019-06-13
申请人： GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
发明人： WANG, Binghe , BOYKIN, David, W. , CHOUDHARY, Manjusha, Roy , KUMAR, Arvind , YU, Bingchen , ZHU, Mengyuan
IPC分类号： A61K31/155 , C07C257/18
摘要： Compounds and methods for the treatment of a bacterial infection or the potentiation of an antibiotic in treating a bacterial infection are described herein.

4. 发明申请

WO2004051217A2 PROCESS FOR SYNTHESIS BIS-ARYL DIAMIDOXIME COMPOUNDS 审中-公开
标题翻译：合成双 - 芳基二酰肟化合物的方法
公开(公告)号：WO2004051217A2
公开(公告)日：2004-06-17
申请号：PCT/US2003/037788
申请日：2003-11-25
申请人： UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , BOYKIN, David, W. , ANBAZHAGAN, Mariappan , TIDWELL, Richard, R.
发明人： BOYKIN, David, W. , ANBAZHAGAN, Mariappan , TIDWELL, Richard, R.
IPC分类号： G01N
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：双芳基二酰胺肟化合物，例如2,5-双[4-羟基和4-O-烷基脒基苯基]呋喃，可以由2,5-双三烷基锡烷经一步制备钯催化的交叉反应。双芳基二偕胺肟化合物如2,5-双[4-羟基和4-O-烷基脒基苯基]呋喃可用作治疗化合物。所公开的方法比其他目前已知的制备2,5-双[4-羟基和4-O-烷基脒基苯基]呋喃和其它双 - 芳基二偕胺肟化合物的方法更具可缩放性，更简单，更经济和更可行。

5. 发明申请

WO2004050018A2 DICATIONIC 2,5-DIARYLFURAN AZA-ANALOGS AS ANTI-PROTOZOAN AGENTS 审中-公开
标题翻译：作为抗原生药剂的通用2,5-二芳基氮杂-类似物
公开(公告)号：WO2004050018A2
公开(公告)日：2004-06-17
申请号：PCT/US2003/037691
申请日：2003-11-25
申请人： UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , 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： A61K
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 17, where R 17 is hydrogen or lower alkyl; C 1 , C 2 , A, and Y are CH, N, NR 17, O, or S, wherein C 1 and C 2 are the same or different; D 1 , D 2 , B, and Z are CH, N, or NR 17 wherein D 1 and D 2 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 17 ; R 13 ,R 14 , R 15 , R 16 , R 1 and R 8 are selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R 3 and R 6 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 2 , R 4 , R 5 and R 7 are each independently selected from the group consisting of H, lower alkyl, alkoxyalkyl, cycloalkyl, aryl, aralkyl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl, or R 2 and R 4 together or R 5 and R 7 together represent a C 2 to C 10 alkyl, hydroxyalkyl, or alkylene, or R 3 and R 4 together or R 6 and R 7 together are: wherein n is a number from 1 to 3, and R 9 is H or-CONHR 10 NR 11 R 12 , wherein R 10 , is lower alkyl and R 11 and R 12 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选自由O，S和NR 17组成的组，其中R 17为是氢或低级烷基; C 1，C 2，A和Y是CH，N，NR 17，O或S，其中C 1 和C ^{2 是相同的或不同的; 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两者都是O，S或NR 17时，B，Z或B和Z二者不存在; R 13，R 14，R 15，R 16，R sup 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，羟烷基，氨基烷基和烷基氨基烷基，或者R 2和R 4一起或R 5，和R 7一起代表C 2〜C 10烷基，羟烷基或亚烷基或R 3和 R 4一起或R 6和R 7一起为：其中n为1至3的数，并且R 9，其中R 10为H或-CONHR 10 NR 12 R 12，其中R 10为低级烷基和 R 11和R 12各自独立地选自H和低级烷基。}

6. 发明授权

EP0831832B1 METHODS OF COMBATTING INFECTIOUS DISEASES USING DICATIONIC BIS-BENZIMIDAZOLES 失效
标题翻译：程序对抗感染性疾病使用二价阳离子BIS的苯并咪唑
公开(公告)号：EP0831832B1
公开(公告)日：2003-12-17
申请号：EP96916817.8
申请日：1996-06-03
申请人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , DUKE UNIVERSITY , GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
发明人： DYKSTRA, Christine, C. , PERFECT, John, R. , BOYKIN, David, W. , WILSON, W., David , TIDWELL, Richard, R.
IPC分类号： A61K31/444 , A61K31/4439 , A61P31/10
CPC分类号： A61K31/427 , A61K31/4184 , A61K31/422 , A61K31/4439 , A61K31/497 , A61K31/506

8. 发明公开

EP0831813A1 METHODS OF INHIBITING PNEUMOCYSTIS CARINII PNEUMONIA AND COMPOUNDS USEFUL THEREFOR 失效
标题翻译：治疗PNEUMOCYTIS卡里尼方法会造成肺炎和合适的连接
公开(公告)号：EP0831813A1
公开(公告)日：1998-04-01
申请号：EP96919040.0
申请日：1996-06-03
申请人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
发明人： TIDWELL, Richard, R. , HALL, James, E. , BOYKIN, David, W.
IPC分类号： A61K31 , A61P11 , A61P31 , C07D209 , C07D403
CPC分类号： C07D403/14 , A61K31/403 , A61K31/4178 , C07D209/88 , Y02A50/488
摘要： The present invention provides methods for treating Pneumocystis carinii pneumonia. The method comprises administering to the subject a compound of Formula I: (I) wherein: X is located in the para or meta positions and is loweralkyl, loweralkoxy, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, alkylaryl, halogen, or wherein: each R2 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R2 groups together represent C2-C10 alkylene, or two R2 groups together represent wherein m is from 1-3 and R4 is H, or -CONHR5NR6R7, wherein R5 is loweralkyl, R6 and R7 are each independently selected from the group consisting of H and lower alkyl; each R8 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl, or two R8 groups together represent C2-C10 alkylene; R9 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl; R3 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl; R1 is H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, alkylaryl, or halogen; or a pharmaceutically acceptable salt thereof.

9. 发明申请

WO2020081829A1 TREATMENT OF ACANTHAMOEBA OR BALAMUTHIA TROPHOZOITES AND/OR CYSTS 审中-公开
公开(公告)号：WO2020081829A1
公开(公告)日：2020-04-23
申请号：PCT/US2019/056761
申请日：2019-10-17
申请人： GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC. , UNIVERSITY OF SOUTH FLORIDA
发明人： BOYKIN, David, W. , KYLE, Dennis, E. , RICE, Christopher, A. , FARAHAT, Abdelbasset, A.
IPC分类号： A61K31/4184 , A61P31/04 , C07C257/18
摘要： Compounds, compositions, and methods for the treatment of infections caused by Acanthamoeba or Balamuthia mandnllaris trophozoites and/or cysts and for the disinfection of solids and/or liquids, such as medical and personal care items, for example contact lenses, that may harbor Acanthamoeba trophozoites and/or cysts are provided.

10. 发明申请

WO2017223260A1 PU.1 INHIBITORS 审中-公开
标题翻译： PU.1抑制剂
公开(公告)号：WO2017223260A1
公开(公告)日：2017-12-28
申请号：PCT/US2017/038647
申请日：2017-06-22
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE, INC. , GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
发明人： WILSON, W., David , BOYKIN, David, W. , POON, Gregory , STEIDL, Ulrich , ANTHONY-DEBRÉ, Iléana
IPC分类号： A61K31/4439 , A61K31/4164 , C07D401/14
摘要： Disclosed herein are inhibitors of PU.1. The inhibitors are useful for treating disorders associated with abnormal PU.1 levels and function.
摘要翻译：本文公开了PU.1的抑制剂。该抑制剂可用于治疗与PU.1水平和功能异常有关的疾病。

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