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    Methods of inhibiting pneumocystis carinii pneumonia and compounds useful therefor
    36.
    发明授权
    Methods of inhibiting pneumocystis carinii pneumonia and compounds useful therefor 失效
    抑制卡氏肺囊虫肺炎的方法及其有用的化合物

    公开(公告)号：US5668166A

    公开(公告)日：1997-09-16

    申请号：US474440

    申请日：1995-06-07

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

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

    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 Pneumocystis carinii pneumonia. The method 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, wherein R.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: 本发明提供了治疗卡氏肺囊虫肺炎的方法。 该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，羟基烷基，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。

    Method for treating leishmaniasis
    37.
    发明授权
    Method for treating leishmaniasis 失效
    治疗利什曼病的方法

    公开(公告)号：US5202320A

    公开(公告)日：1993-04-13

    申请号：US334730

    申请日：1989-04-06

    Applicant: Richard R. Tidwell ,  J. Dieter Geratz ,  James E. Hall ,  Dennis E. Kyle ,  Max Grogl ,  Kwasi A. Ohemeng

    Inventor： Richard R. Tidwell ,  J. Dieter Geratz ,  James E. Hall ,  Dennis E. Kyle ,  Max Grogl ,  Kwasi A. Ohemeng

    IPC: C07C257/18 ,  C07D239/22 ,  C07D239/24

    CPC classification number: C07C257/18 ,  C07D239/22 ,  C07D239/24

    Abstract: This invention relates to a method for treating leishmaniasis which comprises administering to an afflicted host patient, a therapeutically effective amount of a compound having the following structure; ##STR1## wherein X is O or NH; R.sub.1 is H or two R.sub.1 of the same amidine group together represent --(CH.sub.2).sub.m -- wherein m=2, 3 or 4; R.sub.2 is H, NH.sub.2, OCH.sub.3, Cl or NO.sub.2 ; R.sub.3 is H, CH.sub.3 or CH.sub.2 CH.sub.3 and n=2-6 or a pharmaceutical acceptable salt thereof provided that X is O both R.sub.2 and both R.sub.3 cannot be H.

    Abstract translation: 本发明涉及一种治疗利什曼病的方法，其包括对受影响的宿主患者施用治疗有效量的具有以下结构的化合物; 其中X为O或NH; R1是H或相同脒基的两个R1一起表示 - （CH 2）m - ，其中m = 2,3或4; R2是H，NH2，OCH3，Cl或NO2; R 3为H，CH 3或CH 2 CH 3且n = 2-6或其药学上可接受的盐，条件是X均为R 2且两者均不能为H.

    Inhibition of respiratory syncytial virus-induced cell fusion by amidino compounds
    39.
    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：US4324794A

    公开(公告)日：1982-04-13

    申请号：US181341

    申请日：1980-08-26

    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

    CPC classification number: A61K31/155 ,  A61K31/34 ,  A61K31/40 ,  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-amidino-phenoxy)-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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