公开(公告)号：US06008247A

公开(公告)日：1999-12-28

申请号：US32586

申请日：1998-02-27

Applicant: David W. Boykin ,  Richard R. Tidwell ,  W. David Wilson ,  Iris Francesconi

Inventor： David W. Boykin ,  Richard R. Tidwell ,  W. David Wilson ,  Iris Francesconi

IPC: A61K31/34 ,  A61K31/341 ,  A61P11/00 ,  A61P29/00 ,  A61P33/02 ,  C07D307/52 ,  C07D307/54 ,  C07D405/10 ,  C07D405/14 ,  C07D233/06 ,  C07D307/08

CPC classification number: C07D405/14 ,  C07D307/52 ,  C07D307/54

Abstract: Compounds according to the formula: ##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; and X and Y are located in the para or meta positions and are each 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 to C.sub.10 alkyl, hydroxyalkyl, or alkylene; and R.sub.6 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylamino, lkylarninoalkyl, cycloalkyl, hydroxycycloalkyl, alkoxycycloalkyl, aryl, or alkylaryl; or a pharmaceutically acceptable salt thereof, are disclosed. The compounds are useful for treating Pneumocystis carinii in a subject in need of such treatment.

Abstract translation: 根据下式的化合物：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，氧烷基，氧芳基或氧芳基烷基; 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，并且各自选自H，低级烷基，烷氧基，并且其中：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至C 10烷基，羟基烷基或亚烷基; 羟基烷基，氨基烷基，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; 或其药学上可接受的盐。 该化合物可用于治疗需要这种治疗的受试者的卡氏肺囊虫。

公开(公告)号：US5935982A

公开(公告)日：1999-08-10

申请号：US808321

申请日：1997-02-28

Applicant: Christine C. Dykstra ,  David Boykin ,  Richard R. Tidwell

Inventor： Christine C. Dykstra ,  David Boykin ,  Richard R. Tidwell

IPC: A61K31/4184 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61P31/18 ,  A61P37/04 ,  C07D235/20 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  A61K31/415

CPC classification number: C07D403/14 ,  C07D235/20 ,  C07D405/14 ,  C07D413/14

Abstract: The present invention provides methods for treating retroviral infection and methods of treating HIV infection. The methods of the present invention include administering compounds of the general Formula I: ##STR1## wherein L, R.sub.1, R.sub.2, R.sub.3, R.sub.4 are defined herein.

Abstract translation: 本发明提供了治疗逆转录病毒感染的方法和治疗HIV感染的方法。 本发明的方法包括施用通式I的化合物：其中L，R 1，R 2，R 3，R 4在本文中定义。

公开(公告)号：US5723288A

公开(公告)日：1998-03-03

申请号：US238766

申请日：1994-05-06

Applicant: Christine C. Dykstra ,  Richard R. Tidwell ,  David W. Boykin ,  W. David Wilson ,  Jaroslaw Spychala ,  Bijan P. Das ,  Arvind Kumar

Inventor： Christine C. Dykstra ,  Richard R. Tidwell ,  David W. Boykin ,  W. David Wilson ,  Jaroslaw Spychala ,  Bijan P. Das ,  Arvind Kumar

IPC: 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 classification number: G01N33/52 ,  A61K31/505 ,  A61K31/506 ,  C07D307/54 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C09B23/0075 ,  Y10S435/808 ,  Y10S435/81

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5686456A

公开(公告)日：1997-11-11

申请号：US564879

申请日：1995-11-28

Applicant: David W. Boykin ,  Christine C. Dykstra ,  Richard R. Tidwell ,  James E. Hall ,  W. David Wilson ,  Arvind Kumar

Inventor： David W. Boykin ,  Christine C. Dykstra ,  Richard R. Tidwell ,  James E. Hall ,  W. David Wilson ,  Arvind Kumar

IPC: 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 classification number: C07D239/26 ,  A61K31/505 ,  A61K31/506 ,  C07D307/54 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C09B23/0075 ,  G01N33/52

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5667975A

公开(公告)日：1997-09-16

申请号：US485381

申请日：1995-06-07

Applicant: Christine C. Dykstra ,  Richard R. Tidwell ,  David W. Boykin ,  W. David Wilson

Inventor： Christine C. Dykstra ,  Richard R. Tidwell ,  David W. Boykin ,  W. David Wilson

IPC: 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 classification number: A61K31/505 ,  A61K31/506 ,  C07D307/54 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C09B23/0075 ,  G01N33/52 ,  Y10S435/81

Abstract: Disclosed is a method of fluorescent detection of a nucleic acid. The method comprises contacting to the nucleic acid a bis-dicationic aryl furan 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.

Abstract translation: 公开了一种荧光检测核酸的方法。 所述方法包括使所述核酸与双阳离子芳基呋喃接触，并将所述核酸以一定频率曝光以诱导所述化合物的荧光。 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。

公开(公告)号：US5578631A

公开(公告)日：1996-11-26

申请号：US427597

申请日：1995-04-24

Applicant: Richard R. Tidwell ,  Christine C. Dykstra ,  James E. Hall

Inventor： Richard R. Tidwell ,  Christine C. Dykstra ,  James E. Hall

IPC: C07D235/14 ,  A61K31/415 ,  A61K31/4184 ,  A61P11/00 ,  A61P29/00 ,  A61P33/02 ,  A61P43/00 ,  C07D403/14 ,  A61K31/55 ,  A61K31/505

CPC classification number: C07D403/14 ,  A61K31/415

Abstract: Disclosed is a method of combating Pneumocystis carinii Pneumonia in a subject in need of such treatment. The method comprises administering to to the subject an effective Pneumocystis carinii-combating amount of a bis-benzimidazole compound such as bis[5-(2-imidazolyl)-2-benzimidazolyl]methane, 1,4-bis[5-2-imidazolyl)-2-benzimidazolyl]butane, or a pharmaceutically acceptable salt thereof. Pharmaceutical formulations for carrying out the method and novel compounds are also disclosed, along with methods of combating Giardia lamblia.

Abstract translation: 公开了一种在需要这种治疗的受试者中对抗卡氏肺囊虫肺炎的方法。 该方法包括向受试者施用有效的卡氏肺囊虫抗性量的双苯并咪唑化合物，例如双[5-（2-咪唑基）-2-苯并咪唑基]甲烷，1,4-双[5-2-咪唑基 ）-2-苯并咪唑基]丁烷或其药学上可接受的盐。 还公开了用于实施该方法和新化合物的药物制剂，以及与贾第鞭毛虫抗性的方法。

公开(公告)号：US20110257199A1

公开(公告)日：2011-10-20

申请号：US13162907

申请日：2011-06-17

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

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

IPC: 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 classification number: C07C257/18 ,  C07C259/18 ,  C07C279/18 ,  C07C279/24 ,  C07D213/58 ,  C07D239/26 ,  C07D307/68 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100331368A1

公开(公告)日：2010-12-30

申请号：US12680844

申请日：2008-10-17

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

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

IPC: A61K31/444 ,  C07D345/00 ,  A61K31/33 ,  A61K31/4427 ,  C07D421/04 ,  C07D421/14 ,  C07D409/14 ,  A61P31/00 ,  A61P33/02

CPC classification number: C07D345/00 ,  C07D409/14 ,  C07D421/04 ,  C07D421/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07825279B2

公开(公告)日：2010-11-02

申请号：US10992607

申请日：2004-11-18

Applicant: David W. Boykin ,  Richard R. Tidwell ,  W. David Wilson ,  Reto Brun ,  Reem K. Arafa ,  Chad E. Stephens

Inventor： David W. Boykin ,  Richard R. Tidwell ,  W. David Wilson ,  Reto Brun ,  Reem K. Arafa ,  Chad E. Stephens

IPC: C07C279/18 ,  C07D219/12 ,  C07D213/06 ,  A61K31/155 ,  A61K31/235 ,  A61K31/24 ,  A61K31/44

CPC classification number: C07D219/08 ,  C07C257/18 ,  C07C279/18 ,  C07C279/24 ,  C07C291/04 ,  C07C2603/18 ,  C07C2603/24

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07241795B2

公开(公告)日：2007-07-10

申请号：US10791425

申请日：2004-03-02

Applicant: David W. Boykin ,  Richard R. Tidwell ,  W. David Wilson ,  John R. Perfect ,  Chad F. Stephens

Inventor： David W. Boykin ,  Richard R. Tidwell ,  W. David Wilson ,  John R. Perfect ,  Chad F. Stephens

IPC: A61K31/40 ,  A61K31/38 ,  C07D207/04 ,  C07D333/38 ,  C07D307/34

CPC classification number: C07D307/10 ,  C07D307/14 ,  C07D307/52 ,  C07D333/20 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12

Abstract: The present invention relates to novel 2,5-bis{[alkyl (or aryl) imino]aminophenyl}furans and thiophenes of the general formula in which R1, R2, R3 and R4 are each independently selected from the group consisting of H, alkyl, alkoxy, halide, and alkylhalide groups; R5 is H, alkyl or aryl; R6 is H, alkyl, aryl, or NR7R8, in which R7 and R8 are each independently selected from the group consisting of H, alkyl and aryl; and X is O, S or NR9, in which R9 is H or alkyl, and to the use of such compounds.

Abstract translation: 本发明涉及通式的新的2,5-双{[烷基​​（或芳基）亚氨基]氨基苯基}呋喃和噻吩，其中R 1，R 2， R 3和R 4各自独立地选自H，烷基，烷氧基，卤化物和烷基卤化物基团; R 5是H，烷基或芳基; R 6是H，烷基，芳基或NR 7 R 8，其中R 7和R 7， 各自独立地选自H，烷基和芳基; 并且X是O，S或NR 9，其中R 9是H或烷基，以及这些化合物的用途。