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    Inhibition of respiratory syncytial virus-induced cell fusion by amidino compounds
    12.
    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：US4397863A

    公开(公告)日：1983-08-09

    申请号：US366652

    申请日：1982-04-08

    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

    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。

    Dicationic 2,5-diarylfuran aza-analogs as anti-protozoan agents
    14.
    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
    16.
    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。

    2,4-bis[(4-amidino)phenyl]furans as anti-Pneumocystis carinii agents
    20.
    发明授权
    2,4-bis[(4-amidino)phenyl]furans as anti-Pneumocystis carinii agents 失效
    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：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。

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