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    Method for treating leishmaniasis
    41.
    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
    43.
    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。

    Dicationic 2,5-diarylfuran aza-analogs as anti-protozoan agents
    45.
    发明授权
    Dicationic 2,5-diarylfuran aza-analogs as anti-protozoan agents 失效

    公开(公告)号：US07256203B2

    公开(公告)日：2007-08-14

    申请号：US10721525

    申请日：2003-11-25

    Applicant: David W. Boykin ,  Richard R. Tidwell ,  Mohamed A. Ismail ,  Reto Brun

    Inventor： David W. Boykin ,  Richard R. Tidwell ,  Mohamed A. Ismail ,  Reto Brun

    IPC: A61K31/44 ,  C07D401/02

    CPC classification number: C07D307/38 ,  C07D307/54 ,  C07D333/08 ,  C07D405/04 ,  C07D405/14 ,  C07D407/04 ,  C07D407/14 ,  C07D409/04 ,  C07D409/14

    Abstract: A compound of Formula (I): wherein: X is selected from the group consisting of O, S, and NR17, where R17 is hydrogen or lower alkyl; A and Y are CH, N, NR17, O, or S; C1 and C2 are each C or N, wherein C1 and C2 are the same or different; D1 and D2 are each C or N, wherein D1 and D2 are the same or different; B and Z are CH, N, or NR17, provided that B, Z, or both B and Z are not present when A, Y, or both A and Y are O, S, or NR17; R13, R14, R1 and R8 can be present or absent, and when present are selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R15 and Rare selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R3 and R6 are each independently selected from the group consisting of H, hydroxy, lower alkyl, cycloalkyl, aryl, aralkyl, alkoxyl, hydroxycycloalkyl, alkoxycycloalkyl, hydroxyalkyl, aminoalkyl, acyloxy, acetoxy, and alkylaminoalkyl; and R2, R4, R5 and R7 are each independently selected from the group consisting of H, lower alkyl, alkoxyalkyl, cycloalkyl, aryl, aralkyl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl, or R2 and R4 together or R5 and R7 together represent a C2 to C10 alkyl, hydroxyalkyl, or alkylene, or R3 and R4 together or R6 and R7 together are: wherein n is a number from 1 to 3, and R9 is H or —CONHR10NR11R12, wherein R10 is lower alkyl and R11 and R12 are each independently selected from the group consisting of H and lower alkyl.

    Method of inhibiting retroviral integrase
    47.
    发明授权
    Method of inhibiting retroviral integrase 失效
    抑制逆转录病毒整合酶的方法

    公开(公告)号：US06815461B1

    公开(公告)日：2004-11-09

    申请号：US08185079

    申请日：1994-01-20

    Applicant: Christine C. Dykstra ,  Ronald I. Swanstrom ,  Richard R. Tidwell

    Inventor： Christine C. Dykstra ,  Ronald I. Swanstrom ,  Richard R. Tidwell

    IPC: A61F31415

    CPC classification number: A61K31/415

    Abstract: Disclosed is a method of inhibiting retroviral integrase in a subject in need of such treatment. The method comprises administering to the subject an effective retroviral integrase inhibiting amount of a bis-benzimidazole compound such as bis[5-amidino-2-benzimidazolyl]methane, 1,2-bis[5-amidino-2-benzimidazolyl]ethane, 1,2-bis[5-amidino-2-benzimidazolyl]ethene or a pharmaceutically acceptable salt thereof. A method for combatting retroviral infections is also disclosed.

    Abstract translation: 公开了在需要这种治疗的受试者中抑制逆转录病毒整合酶的方法。 该方法包括向受试者施用抑制有效量的双苯并咪唑化合物如双[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，1 ，2-双[5-脒基-2-苯并咪唑基]乙烯或其药学上可接受的盐。 还公开了一种抗逆转录病毒感染的方法。

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