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    Compounds that exhibit specific molecular recognition of mixed nucleic acid sequences and bind in the DNA minor groove as a dimer
    62.
    发明授权
    Compounds that exhibit specific molecular recognition of mixed nucleic acid sequences and bind in the DNA minor groove as a dimer 失效
    显示混合核酸序列的特异性分子识别并在DNA小沟中作为二聚体结合的化合物

    公开(公告)号：US06613787B2

    公开(公告)日：2003-09-02

    申请号：US09745004

    申请日：2000-12-20

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

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

    IPC: A61K31415

    CPC classification number: C07D207/416 ,  C07D307/54 ,  C07D405/04 ,  C07D405/14 ,  C12Q1/6816 ,  C12Q2563/173

    Abstract: Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.

    Abstract translation: 已经通过定量印迹分析发现了呋喃脒苯基环之一与呋喃脒苯基环之一取代的不对称衍生物，以比纯AT序列更强地结合含DNA位点的DNA。 已经显示这些化合物以高度协同的方式作为堆叠的二聚体以特定的GC含有DNA序列在小沟中结合。 本发明化合物可用于选择性结合混合序列DNA，也可用于调节基因表达的方法，治疗机会性感染和癌症的方法，以及检测某些DNA序列的方法。

    Prodrugs for antimicrobial amidines
    63.
    发明授权
    Prodrugs for antimicrobial amidines 失效
    抗生素脒类药物

    公开(公告)号：US06486200B1

    公开(公告)日：2002-11-26

    申请号：US09612138

    申请日：2000-07-07

    Applicant: David W. Boykin ,  M. Syed Rahmathullah ,  Richard R. Tidwell ,  James E. Hall

    Inventor： David W. Boykin ,  M. Syed Rahmathullah ,  Richard R. Tidwell ,  James E. Hall

    IPC: A61K31357

    CPC classification number: C07D407/14 ,  A61K31/341 ,  A61K47/54 ,  A61K47/555 ,  C07D307/54

    Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the 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:  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.

    Abstract translation: 治疗感染的方法包括施用治疗有效量的由式（I）表示的化合物：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可以独立地选择 由H，低级烷基，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组成的组; R 3和R 4各自独立地选自H，低级烷基，卤素，烷氧基，氧基芳基和氧芳基烷基; R 5 由选自以下的式表示：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。

    Benzamidoxime prodrugs as antipneumocystic agents
    65.
    发明授权
    Benzamidoxime prodrugs as antipneumocystic agents 失效
    苯甲酰胺肟前药作为抗肺囊虫药

    公开(公告)号：US06214883B1

    公开(公告)日：2001-04-10

    申请号：US09477390

    申请日：2000-01-04

    Applicant: James E. Hall ,  Richard R. Tidwell ,  David W. Boykin

    Inventor： James E. Hall ,  Richard R. Tidwell ,  David W. Boykin

    IPC: A61K3115

    CPC classification number: A61K31/15 ,  A61K31/155 ,  A61K31/341 ,  C07C257/18 ,  C07C259/18 ,  C07D307/54 ,  C07D307/68 ,  C07D333/24 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/481 ,  Y02A50/491

    Abstract: A method of treating Pneumocystis carinii pneumonia in a subject in need of such treatment is disclosed. The method comprises orally administering to the subject a bis-benzamidoxime, or a pharmaceutically acceptable salt thereof, that is reduced in the subject to produce a benzamidine having anti-P. carinii activity. The method of the present invention may alternatively comprise intravenously administering to the subject an active compound as disclosed herein. Pharmaceutical formulations and active compounds useful in the practice of the present invention are also disclosed.

    Abstract translation: 公开了在需要这种治疗的受试者中治疗卡氏肺囊虫肺炎的方法。 该方法包括口服给予受试者的双 - 苯甲脒肟或其药学上可接受的盐，其在受试者中被还原以产生具有抗-P的苄脒。 卡里尼活动。 本发明的方法可以选择性地向受试者静脉内施用本文所公开的活性化合物。 还公开了可用于本发明实践的药物制剂和活性化合物。

    2,4-bis[(4-amidino)phenyl]furans as anti-Pneumocystis carinii agents
    66.
    发明授权
    2,4-bis[(4-amidino)phenyl]furans as anti-Pneumocystis carinii agents 有权
    2,4-二[（4-脒基）苯基]呋喃作为抗肺孢子虫卡尼氏菌剂

    公开(公告)号：US6127554A

    公开(公告)日：2000-10-03

    申请号：US311437

    申请日：1999-05-14

    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 ,  C07D307/38

    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, lkylaminoalkyl, 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; R 6为H，羟基，低级烷基，烷氧基烷基，羟基烷基，氨基烷基，烷基氨基，烷基氨基烷基，环烷基，羟基环烷基，烷氧基环烷基，芳基或烷芳基。 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。

    Methods of treating microbial infections
    67.
    发明授权
    Methods of treating microbial infections 失效
    治疗微生物感染的方法

    公开(公告)号：US5668167A

    公开(公告)日：1997-09-16

    申请号：US477876

    申请日：1995-06-07

    Applicant: Richard R. Tidwell ,  James E. Hall ,  David W. Boykin ,  Christine C. Dykstra ,  John Perfect ,  Byron L. Blagburn

    Inventor： Richard R. Tidwell ,  James E. Hall ,  David W. Boykin ,  Christine C. Dykstra ,  John Perfect ,  Byron L. Blagburn

    IPC: A61K31/40 ,  A61K31/403 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/505 ,  A61P11/00 ,  A61P31/00 ,  C07D209/86 ,  C07D209/88 ,  C07D403/14

    CPC classification number: C07D403/14 ,  A61K31/403 ,  A61K31/4178 ,  C07D209/88

    Abstract: The present invention provides methods for treating Cryptococcus neoformans, Cryptosporidium parvum, and Candida albicans in a subject in need of such treatment. The methods comprises administering to the subject a compound of Formula I: ##STR1## wherein: X is located in the para or meta positions and is loweralkyl, loweralkoxy, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, alkylaryl, halogen, or ##STR2## wherein: each R.sub.2 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R.sub.2 groups together represent C.sub.2 -C.sub.10 alkylene, or two R.sub.2 groups together represent ##STR3## wherein m is from 1-3 and R.sub.4 is H, ##STR4## or --CONHR.sub.5 NR.sub.6 R.sub.7, whereinR.sub.5 is loweralkyl, R.sub.6 and R.sub.7 are each independently selected from the group consisting of H and lower alkyl; each R.sub.8 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl, or two R.sub.8 groups together represent C.sub.2 -C.sub.10 alkylene; R.sub.9 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl;R.sub.3 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl;R.sub.1 is H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, alkylaryl, or halogen; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明提供了在需要这种治疗的受试者中治疗隐球菌新隐球蛋白，小隐孢子虫和白色念珠菌的方法。 所述方法包括向受试者施用式I化合物：其中：X位于对位或间位，且为低级烷基，低级烷氧基，烷氧基烷基，羟烷基，氨基烷基，烷基氨基烷基，环烷基，芳基，烷基芳基， 卤素或其中：每个R 2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，芳基或烷芳基，或两个R 2基团一起表示C 2 -C 10亚烷基或两个R 2 基团一起表示，其中m为1-3，R4为H，IMA或-CONHR5NR6R7，其中R5为低级烷基，R6和R7各自独立地选自H和低级烷基; 每个R 8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 8基团一起表示C 2 -C 10亚烷基; R9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; R3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; R1是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，烷基芳基或卤素; 或其药学上可接受的盐。

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