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    Process for the synthesis of bis-aryl diamidoxime compounds
    21.
    发明授权
    Process for the synthesis of bis-aryl diamidoxime compounds 失效
    双芳基二肟化合物的合成方法

    公开(公告)号：US07071338B2

    公开(公告)日：2006-07-04

    申请号：US10722085

    申请日：2003-11-25

    Applicant: David W. Boykin ,  Mariappan Anbazhagan ,  Richard R. Tidwell

    Inventor： David W. Boykin ,  Mariappan Anbazhagan ,  Richard R. Tidwell

    IPC: C07D207/335 ,  C07D307/52 ,  C07D333/22

    CPC classification number: C07D307/54

    Abstract: Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl] furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans, are useful as therapeutic compounds. The disclosed process is scalable, simpler, more economic and more feasible than other presently known methods of preparing 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans and other bis-aryl diamidoxime compounds.

    Abstract translation: 双芳基二肟化合物，如2,5-双[4-羟基和4-O-烷基脒基苯基]呋喃，可以通过一步钯催化的交叉反应由2,5-双三烷基锡烷制备。 双芳基二肟化合物，例如2,5-双[4-羟基和4-O-烷基脒基苯基]呋喃，可用作治疗化合物。 所公开的方法比其它目前已知的制备2,5-双[4-羟基和4-O-烷基脒基苯基]呋喃和其它双芳基二肟基化合物的方法是可扩展的，更简单的，更经济的和更可行的。

    Prodrugs for antimicrobial amidines
    22.
    发明授权
    Prodrugs for antimicrobial amidines 失效
    抗生素脒类药物

    公开(公告)号：US06503940B2

    公开(公告)日：2003-01-07

    申请号：US09918787

    申请日：2001-07-31

    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: A61K3140

    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
    26.
    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：US5843980A

    公开(公告)日：1998-12-01

    申请号：US751171

    申请日：1996-11-15

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

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

    IPC: C07D307/52 ,  A61K31/00 ,  A61K31/15 ,  A61K31/155 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61P11/00 ,  A61P31/00 ,  A61P31/04 ,  A61P43/00 ,  C07C257/18 ,  C07C259/18 ,  C07D235/24 ,  C07D307/54 ,  C07D307/68 ,  C07D333/24 ,  C07D333/20

    CPC classification number: A61K31/15 ,  A61K31/155 ,  A61K31/341 ,  C07C257/18 ,  C07C259/18 ,  C07D307/54 ,  C07D307/68 ,  C07D333/24

    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 of Formula II ##STR1## wherein: R.sub.1 and R.sub.2 are each independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl or alkylaminoalkyl; R.sub.3 is H, loweralkyl, oxyalkyl, alkoxyalkyl, hydroxyalkyl, cycloalkyl, aryl, aminoalkyl, alkylaminoalkyl or halogen; R.sub.4 is --OY, or R.sub.1 and R.sub.4 together represent, ##STR2## wherein R.sub.5 is ##STR3## Y is H or loweralkyl; n is an integer from 0 to 2; and A is a heterocyclic aromatic group selected from the group consisting of: ##STR4## wherein R.sub.6 and R.sub.7 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, or oxyarylalkyl, 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。 该方法包括向受试者口服施用式II的双 - 苯甲脒肟（II），其中：R 1和R 2各自独立地选自H，低级烷基，烷氧基烷基，烷氧基烷基，环烷基，芳基，羟烷基，氨基烷基 或烷基氨基烷基; R3是H，低级烷基，氧烷基，烷氧基烷基，羟基烷基，环烷基，芳基，氨基烷基，烷基氨基烷基或卤素; R 4是-OY，或者R 1和R 4一起表示，其中R 5是H或低级烷基; n为0〜2的整数; 并且A是选自以下的杂环芳族基团：其中R 6和R 7各自独立地选自H，低级烷基，卤素，氧烷基，氧芳基或氧芳基烷基，或其药学上可接受的盐， 在受试者中减少以产生具有抗-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。

    Inhibition of respiratory syncytial virus-induced cell fusion by amidino compounds
    29.
    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。

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