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1. 发明申请

US20100331368A1 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：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。

2. 发明申请

US20100249175A1 Dicationic compounds which selectively recognize G-quadruplex DNA 审中-公开
标题翻译：选择性识别G-四链体DNA的阳离子化合物
公开(公告)号：US20100249175A1
公开(公告)日：2010-09-30
申请号：US11478453
申请日：2006-06-29
申请人： W. David Wilson , David W. Boykin , Elizabeth W. White , Mohamed A. Ismail , Arvind Kumar , Rupesh Nanjunda , Richard R. Tidwell
发明人： W. David Wilson , David W. Boykin , Elizabeth W. White , Mohamed A. Ismail , Arvind Kumar , Rupesh Nanjunda , Richard R. Tidwell
IPC分类号： A61K31/437 , C12P19/34 , C12N5/071 , C12N5/02 , A61K31/4178 , C07H21/04 , C07D471/04 , C07D405/14 , A61P35/04
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具有高度选择性的起始化合物。几种化合物表现出与G-四链体DNA结合的凹槽，并且与罗氏黑曲霉相比体外和体内活性。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。

3. 发明授权

US5622955A Methods of treating cryptosporidium parvum 失效
标题翻译：处理隐孢子虫的方法
公开(公告)号：US5622955A
公开(公告)日：1997-04-22
申请号：US456164
申请日：1995-05-31
申请人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar , Byron L. Blagburn
发明人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar , Byron L. Blagburn
IPC分类号： G01N33/50 , A61K31/505 , A61K31/506 , C07D239/26 , C07D307/52 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/01 , C12Q1/68 , G01N21/78 , G01N33/52 , G01N33/58
CPC分类号： C07D239/26 , A61K31/505 , A61K31/506 , C07D307/54 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/0075 , G01N33/52
摘要： The present invention provides methods for treating Cryptosporidium parvum in a subject in need of such treatment. The methods comprises administering to the subject a compound of Formula I: ##STR1##
摘要翻译：本发明提供了在需要这种治疗的受试者中治疗隐孢子虫的方法。所述方法包括向受试者施用式I化合物：（I）

4. 发明授权

US5594138A Method of fluorescent detection of nucleic acids and cytoskeleton elements using bis-dicationic aryl furans 失效
标题翻译：使用双阳离子芳基呋喃荧光检测核酸和细胞骨架元件的方法
公开(公告)号：US5594138A
公开(公告)日：1997-01-14
申请号：US453232
申请日：1995-05-30
申请人： Christine C. Dykstra , Richard R. Tidwell , David W. Boykin , W. David Wilson , Jaroslaw Spychala , Bijan P. Das , Arvind Kumar
发明人： Christine C. Dykstra , Richard R. Tidwell , David W. Boykin , W. David Wilson , Jaroslaw Spychala , Bijan P. Das , Arvind Kumar
IPC分类号： G01N33/50 , A61K31/505 , A61K31/506 , C07D307/52 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/01 , C12Q1/68 , G01N21/78 , G01N33/52 , G01N33/58 , C07D405/00
CPC分类号： G01N33/52 , A61K31/505 , A61K31/506 , C07D307/54 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/0075 , Y10S435/808 , Y10S435/81
摘要： Disclosed is a method of fluorescent detection of a nucleic acid. The method comprises contacting to the nucleic acid a bis-dicationic aryl furan compound, such as 2,5-bis[4-(4,5,6,7-tetrahydro-1H-1,3-diazepin-2-yl) phenyl] furan; 2,5-bis{[4-(N-isopropyl) amidino] phenyl}furan; and physiologically acceptable salts thereof, and exposing the nucleic acid to light at a frequency to induce fluorescence of the compound. A method for fluorescent detection of cytoskeleton elements, and novel bis-dicationic aryl furan compounds are also disclosed.
摘要翻译：公开了一种荧光检测核酸的方法。该方法包括使双酸性芳基呋喃化合物如2,5-双[4-（4,5,6,7-四氢-1H-1,3-二氮杂-2-基）苯基 ]呋喃 2,5-双{[4-（N-异丙基）脒基]苯基}呋喃; 和其生理上可接受的盐，并且以一定的频率使核酸暴露以诱导化合物的荧光。还公开了细胞骨架元件的荧光检测方法，以及新型的双 - 二盐酸芳基呋喃化合物。

5. 发明授权

US5627184A Methods of treating Giardia lamblia 失效
标题翻译：治疗贾第鞭毛虫的方法
公开(公告)号：US5627184A
公开(公告)日：1997-05-06
申请号：US454838
申请日：1995-05-31
申请人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar
发明人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar
IPC分类号： G01N33/50 , A61K31/505 , A61K31/506 , C07D239/26 , C07D307/52 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/01 , C12Q1/68 , G01N21/78 , G01N33/52 , G01N33/58
CPC分类号： C07D239/26 , A61K31/505 , A61K31/506 , C07D307/54 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/0075 , G01N33/52
摘要： The present invention provides methods for treating Pneumocystis carinii pneumonia and Giardia lamblia in a subject in need of such treatment. The methods comprises administering to the subject a compound of Formula I: ##STR1## wherein: X and Y are located in the para or meta positions and are selected from the group consisting of H, loweralkyl, loweralkoxy, and ##STR2## wherein: each R.sub.1 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R.sub.1 groups together represent C.sub.2 -C.sub.10 alkyl, hydroxyalkyl, or alkylene, or two R.sub.1 groups together represent ##STR3## wherein m is from 1-3 and R.sub.7 is H or --CONHCR.sub.8 NR.sub.9 R.sub.10, wherein R.sub.8 is loweralkyl, and R.sub.9 and R.sub.10 are each independently selected from the group consisting of H and lower alkyl;R.sub.2 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl;n is a number from 0 to 2;R.sub.3 and R.sub.4 are each independently selected from the group consisting of H, loweralkyl, loweralkoxy, alkylaryl, aryl, oxyaryl, aminoalkyl, aminoaryl, or halogen; andR.sub.5 and R.sub.6 are each independently selected from the group consisting of H, loweralkyl, aryl, alkylaryl, aminoalkyl, aminoaryl, halogen, oxyalkyl, oxyaryl, or oxyarylalkyl; or a phamaceutically acceptable salt thereof. The compound of Formula I is administered in an amount effective to treat the condition.The present invention also provides compounds useful for the treatment of Pneumocystis carinii pneumonia and Giardia lamblia.
摘要翻译：本发明提供了在需要这种治疗的受试者中治疗卡氏肺囊虫肺炎和贾第鞭毛虫的方法。所述方法包括向受试者施用式I化合物：其中：X和Y位于对位或间位，并且选自H，低级烷基，低级烷氧基和低级烷氧基，其中：每个R 1独立地选自H，低级烷基，烷氧基烷基，羟基烷基，氨基烷基，烷基氨基烷基，环烷基，芳基或烷基芳基，或两个R 1基团一起表示C 2 -C 10烷基，羟基烷基或亚烷基或两个R 1基团一起代表，其中m为1-3，R7为H或-CONHCR8NR9R10，其中R8为低级烷基，R9和R10各自独立地选自H和低级烷基; R2是H，羟基，低级烷基，烷氧基烷基，羟基烷基，氨基烷基，烷基氨基烷基，环烷基，芳基或烷基芳基; n是从0到2的数字; R 3和R 4各自独立地选自H，低级烷基，低级烷氧基，烷基芳基，芳基，氧芳基，氨基烷基，氨基芳基或卤素; 并且R 5和R 6各自独立地选自H，低级烷基，芳基，烷基芳基，氨基烷基，氨基芳基，卤素，氧烷基，氧芳基或氧芳基烷基; 或其药学上可接受的盐。以有效治疗病症的量施用式I化合物。本发明还提供了可用于治疗卡氏肺囊虫肺炎和贾第鞭毛虫的化合物。

6. 发明授权

US5606058A Compounds for the treatment of pneumocystis carinii Pneumonia, Giardia Lamblia, and Cryptospordium parnum 失效
标题翻译：用于治疗卡氏肺囊虫肺炎，贾第鞭毛虫和隐孢子虫的化合物
公开(公告)号：US5606058A
公开(公告)日：1997-02-25
申请号：US455047
申请日：1995-05-31
申请人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar
发明人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar
IPC分类号： G01N33/50 , A61K31/505 , A61K31/506 , C07D239/26 , C07D307/52 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/01 , C12Q1/68 , G01N21/78 , G01N33/52 , G01N33/58
CPC分类号： C07D239/26 , A61K31/505 , A61K31/506 , C07D307/54 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/0075 , G01N33/52
摘要： The present invention provides compounds useful for treating Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium parvum in a subject in need of such treatment. The compounds comprise compounds of Formula I: ##STR1##
摘要翻译：本发明提供了在需要这种治疗的受试者中可用于治疗卡氏肺囊虫肺炎，贾第鞭毛虫和隐孢子虫的化合物。化合物包括式I的化合物：（I）

7. 发明授权

US5602172A Methods of inhibiting Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium and compounds useful therefor 失效
标题翻译：抑制卡氏肺囊虫肺炎，贾第鞭毛虫和隐孢子虫的方法及其有用的化合物
公开(公告)号：US5602172A
公开(公告)日：1997-02-11
申请号：US453276
申请日：1995-05-30
申请人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar , Byron L. Blagburn
发明人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar , Byron L. Blagburn
IPC分类号： A61K31/341 , A61K31/4178 , A61K31/505 , A61K31/506 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14 , G01N33/52 , A61K31/34
CPC分类号： G01N33/52 , A61K31/341 , A61K31/4178 , A61K31/505 , A61K31/506 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14
摘要： The present invention provides methods for treating Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium parvum in a subject in need of such treatment. The methods comprise adminstering to the subject a compound of Formula (I): ##STR1## wherein: R.sub.1 and R.sub.2 are each independently selected from the group consisting of H, loweralkyl, aryl, alkylaryl, aminoalkyl, aminoaryl, halogen, oxyalkyl, oxyaryl, or oxyarylalkyl;R.sub.3 and R.sub.4 are each independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkylaryl, aryl, oxyaryl, aminoalkyl, aminoaryl, or halogen; andX and Y are located in the para or meta positions and are selected from the group consisting of H, loweralkyl, oxyalkyl, and ##STR2## wherein: each R.sub.5 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R.sub.5 groups together represent C.sub.2 -C.sub.10 alkyl, hydroxyalkyl, or alkylene; andR.sub.6 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, cycloalkyl, hydroxycycloalkyl, alkoxycycloalkyl, aryl, or alkylaryl;or a phamaceutically acceptable salt thereof. The compounds ar administered in an amount effective to treat the condition. The present invention also includes novel compounds useful in the treatment of Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium parvum.
摘要翻译：本发明提供了在需要这种治疗的受试者中治疗卡氏肺囊虫肺炎，贾第鞭毛虫和隐孢子虫的方法。所述方法包括给予受试者式（I）的化合物：其中：R 1和R 2各自独立地选自H，低级烷基，芳基，烷基芳基，氨基烷基，氨基芳基，卤素，烷氧基烷基，芳氧基或氧芳基烷基; R 3和R 4各自独立地选自H，低级烷基，烷氧基烷基，烷基芳基，芳基，氧芳基，氨基烷基，氨基芳基或卤素; 并且X和Y位于对位或间位，并且选自H，低级烷基，氧烷基和其中：每个R 5独立地选自H，低级烷基，烷氧基烷基，羟基烷基，氨基烷基，烷基氨基烷基，环烷基，芳基或烷基芳基或两个R 5基团一起表示C 2 -C 10烷基，羟基烷基或亚烷基; 烷基氨基，烷基氨基烷基，环烷基，羟基环烷基，烷氧基环烷基，芳基或烷基芳基; R 6是H，羟基，低级烷基，烷氧基烷基，羟基烷基，或其药学上可接受的盐。以有效治疗病症的量施用化合物。本发明还包括可用于治疗卡氏肺囊虫肺炎，贾第鞭毛虫和隐孢子虫的新型化合物。

8. 发明授权

US5521189A Methods of treating pneumocystis carinii pneumonia 失效
标题翻译：治疗卡氏肺囊虫肺炎的方法
公开(公告)号：US5521189A
公开(公告)日：1996-05-28
申请号：US305823
申请日：1994-09-13
申请人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar
发明人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar
IPC分类号： G01N33/50 , A61K31/505 , A61K31/506 , C07D239/26 , C07D307/52 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/01 , C12Q1/68 , G01N21/78 , G01N33/52 , G01N33/58
CPC分类号： C07D239/26 , A61K31/505 , A61K31/506 , C07D307/54 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/0075 , G01N33/52
摘要： The present invention provides methods for treating Pneumocystis carinii pneumonia and Giardia lamblia in a subject in need of such treatment. The methods comprises administering to the subject a compound of Formula I: ##STR1## wherein: X and Y are located in the para or meta positions and are selected from the group consisting of H, loweralkyl, loweralkoxy, and ##STR2## wherein: each R.sub.1 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R.sub.1 groups together represent C.sub.2 -C.sub.10 alkyl, hydroxyalkyl, or alkylene, or two R.sub.1 groups together represent ##STR3## wherein m is from 1-3 and R.sub.7 is H or --CONHCR.sub.8 NR.sub.9 R.sub.10.
摘要翻译：本发明提供了在需要这种治疗的受试者中治疗卡氏肺囊虫肺炎和贾第鞭毛虫的方法。所述方法包括向受试者施用式I化合物：其中：X和Y位于对位或间位，并且选自H，低级烷基，低级烷氧基和低级烷氧基，其中：每个R 1独立地选自H，低级烷基，烷氧基烷基，羟基烷基，氨基烷基，烷基氨基烷基，环烷基，芳基或烷基芳基，或两个R 1基团一起表示C 2 -C 10烷基，羟基烷基或亚烷基或两个R 1基团一起代表，其中m为1-3，R7为H或-CONHCR8NR9R10。

9. 发明授权

US5723288A Method of fluorescent detection of nucleic acids and cytoskeleton elements using bis-dicationic aryl furans, and kits useful therefor 失效
标题翻译：使用双阳离子芳基呋喃荧光检测核酸和细胞骨架元件的方法，以及可用于其的试剂盒
公开(公告)号：US5723288A
公开(公告)日：1998-03-03
申请号：US238766
申请日：1994-05-06
申请人： Christine C. Dykstra , Richard R. Tidwell , David W. Boykin , W. David Wilson , Jaroslaw Spychala , Bijan P. Das , Arvind Kumar
发明人： Christine C. Dykstra , Richard R. Tidwell , David W. Boykin , W. David Wilson , Jaroslaw Spychala , Bijan P. Das , Arvind Kumar
IPC分类号： G01N33/50 , A61K31/505 , A61K31/506 , C07D307/52 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/01 , C12Q1/68 , G01N21/78 , G01N33/52 , G01N33/58
CPC分类号： G01N33/52 , A61K31/505 , A61K31/506 , C07D307/54 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/0075 , Y10S435/808 , Y10S435/81
摘要： Disclosed is a method of fluorescent detection of a nucleic acid. The method comprises contacting to the nucleic acid a bis-dicationic aryl furan compound, such as 2,5-bis�4-(4,5,6,7-tetrahydro-1H-1,3-diazepin-2-yl) phenyl! furan; 2,5-bis{�4-(N-isopropyl) amidino! phenyl}furan; and physiologically acceptable salts thereof, and exposing the nucleic acid to light at a frequency to induce fluorescence of the compound. A method for fluorescent detection of cytoskeleton elements, and novel bis-dicationic aryl furan compounds are also disclosed.
摘要翻译：公开了一种荧光检测核酸的方法。该方法包括使双酸性芳基呋喃化合物如2,5-双[4-（4,5,6,7-四氢-1H-1,3-二氮杂-2-基）苯基 ]呋喃 2,5-双{[4-（N-异丙基）脒基]苯基}呋喃; 和其生理上可接受的盐，并且以一定的频率使核酸暴露以诱导化合物的荧光。还公开了细胞骨架元件的荧光检测方法，以及新型的双 - 二盐酸芳基呋喃化合物。

10. 发明授权

US5686456A Methods of treating pneumocystis carinii pneumonia 失效
标题翻译：治疗卡氏肺囊虫肺炎的方法
公开(公告)号：US5686456A
公开(公告)日：1997-11-11
申请号：US564879
申请日：1995-11-28
申请人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar
发明人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar
IPC分类号： G01N33/50 , A61K31/505 , A61K31/506 , C07D239/26 , C07D307/52 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/01 , C12Q1/68 , G01N21/78 , G01N33/52 , G01N33/58
CPC分类号： C07D239/26 , A61K31/505 , A61K31/506 , C07D307/54 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/0075 , G01N33/52
摘要： The present invention provides methods for treating Pneumocystis carinii pneumonia in a subject in need of such treatment. The methods comprise administering to a subject in need thereof, a pyrimidine of Formula I. ##STR1## wherein the variables are as defined in the specification.
摘要翻译：本发明提供了在需要这种治疗的个体中治疗卡氏肺囊虫肺炎的方法。所述方法包括向有需要的受试者施用式I的嘧啶。其中变量如说明书中所定义。

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