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    Dicationic dibenzofuran and dibenzothiophene compounds and methods of use thereof
    11.
    发明授权
    Dicationic dibenzofuran and dibenzothiophene compounds and methods of use thereof 有权
    二次二苯并呋喃和二苯并噻吩化合物及其使用方法

    公开(公告)号：US06172104B2

    公开(公告)日：2001-01-09

    申请号：US09344143

    申请日：1999-06-24

    Applicant: Richard R. Tidwell ,  James Edwin Hall

    Inventor： Richard R. Tidwell ,  James Edwin Hall

    IPC: A61K3138

    CPC classification number: C07D307/91 ,  C07D333/76

    Abstract: Methods of treating Pneumocystis carinii pneumonia comprise administering a therapeutically effective amount of a dicationic dibenzofuran compound described by Formula (I). Methods of treating Pneumocystis carinii pneumonia also comprise administering a therapeutically effective amount of a dicationic dibenzothiophene compound described by Formula (II). Novel compounds are also disclosed, and are represented by the Formulae (I) and (II).

    Abstract translation: 治疗卡氏肺囊虫肺炎的方法包括施用治疗有效量的式（I）所述的二氢二苯并呋喃化合物。 治疗卡氏肺囊虫肺炎的方法还包括施用治疗有效量的式（II）所述的二重阳离子二苯并噻吩化合物。 还公开了新的化合物，并且由式（I）和（II）表示。

    2,4-bis[(4-amidino)phenyl]furans as anti-Pneumocystis carinii agents
    12.
    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
    13.
    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。

    Inhibition of Respiratory Syncytial virus-induced cell fusion by amidino compounds
    18.
    发明授权
    Inhibition of Respiratory Syncytial virus-induced cell fusion by amidino compounds 失效
    通过脒基化合物抑制呼吸道合胞病毒诱导的细胞融合

    公开(公告)号：US4619942A

    公开(公告)日：1986-10-28

    申请号：US521084

    申请日：1983-08-08

    Applicant: Richard R. Tidwell ,  Edward J. Dubovi ,  Joachim D. Geratz

    Inventor： Richard R. Tidwell ,  Edward J. Dubovi ,  Joachim D. Geratz

    IPC: A61K31/155 ,  A61K31/34 ,  A61K31/40 ,  A61K31/415 ,  A61K31/405

    CPC classification number: A61K31/40 ,  A61K31/155 ,  A61K31/34 ,  A61K31/415

    Abstract: A number of aromatic mono- and bis-amidines are capable of blocking cell fusion induced by Respiratory Syncytial (RS) virus. Suitable amidino compounds include those selected from the group consisting of 1-4-di(4-amidinophenoxy)-2-butanol; bis(5-amidino-2-benzimidazolyl)methane; 1,2-bis(5-amidino-2-benzimidazolyl)ethane; 5-amidino-indole; 5-amidinobenzimidazole, 5-amidino-1-methylindole and 5-amidino-1-(4-amidinobenzyl)indole. The most powerful of the compounds, bis(5-amidino-2-benzimidazolyl)methane (BABIM), is able to achieve complete suppression of syncytium formation at a concentration of 1 .mu.M. Inhibition occurs in RS virus-infected Hep-2 cells as well as CV-1 cells. BABIM also causes a significant retardation of RS virus penetration, but does not interfere with adsorption. Addition of the amidines after the penetration of RS virus does not affect single cycle yields. The compounds may be used in the prophylactic control of RS virus in man.

    Abstract translation: 许多芳香单和双脒能够阻断呼吸道合胞病毒（RS）病毒诱导的细胞融合。 合适的脒基化合物包括选自1-4-二（4-脒基苯氧基）-2-丁醇; 双（5-脒基-2-苯并咪唑基）甲烷; 1,2-双（5-脒基-2-苯并咪唑基）乙烷; 5-脒基 - 吲哚; 5-脒基苯并咪唑，5-脒基-1-甲基吲哚和5-脒基-1-（4-脒基苄基）吲哚。 最强大的双（5-脒基-2-苯并咪唑基）甲烷（BABIM）化合物能够在1μM的浓度下完全抑制合胞体形成。抑制发生在RS病毒感染的Hep-2细胞中 以及CV-1细胞。 BABIM还引起RS病毒渗透的显着延迟，但不影响吸附。 RS病毒渗透后添加脒不影响单循环产量。 该化合物可用于人类对RS病毒的预防性控制。

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