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72 条记录 (耗时 0.045 秒)

    Process for the synthesis of bis-aryl diamidoxime compounds
    42.
    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

    申请人： David W. Boykin ,  Mariappan Anbazhagan ,  Richard R. Tidwell

    发明人： David W. Boykin ,  Mariappan Anbazhagan ,  Richard R. Tidwell

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

    CPC分类号： C07D307/54

    摘要： 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.

    摘要翻译： 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。

    Dicationic 2,5-diarylfuran aza-analogs as anti-protozoan agents
    44.
    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

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

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

    IPC分类号： A61K31/44 ,  C07D401/02

    CPC分类号： C07D307/38 ,  C07D307/54 ,  C07D333/08 ,  C07D405/04 ,  C07D405/14 ,  C07D407/04 ,  C07D407/14 ,  C07D409/04 ,  C07D409/14

    摘要： 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.

    2,4-bis[(4-amidino)phenyl]furans as anti-Pneumocystis carinii agents
    46.
    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

    申请人： David W. Boykin ,  Richard R. Tidwell ,  W. David Wilson ,  Iris Francesconi

    发明人： David W. Boykin ,  Richard R. Tidwell ,  W. David Wilson ,  Iris Francesconi

    IPC分类号： A61K31/34 ,  A61K31/341 ,  A61P11/00 ,  A61P29/00 ,  A61P33/02 ,  C07D307/52 ,  C07D307/54 ,  C07D405/10 ,  C07D405/14 ,  C07D233/06 ,  C07D307/08

    CPC分类号： C07D405/14 ,  C07D307/52 ,  C07D307/54

    摘要： 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.

    摘要翻译： 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。