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    Substituted-4-quinolones
    1.
    发明授权
    Substituted-4-quinolones 失效
    取代的4-喹诺酮

    公开(公告)号：US07482362B2

    公开(公告)日：2009-01-27

    申请号：US10450930

    申请日：2001-12-17

    申请人： David Idris Pritchard ,  Barrie Walsham Bycroft ,  Siri Ram Chhabra ,  Doreen Hooi

    发明人： David Idris Pritchard ,  Barrie Walsham Bycroft ,  Siri Ram Chhabra ,  Doreen Hooi

    IPC分类号： A01N43/42 ,  A61K31/47 ,  C07D215/00

    CPC分类号： A61K31/4709 ,  A61K31/47 ,  A61K31/496 ,  A61K2039/55511 ,  A61K2039/57

    摘要： Substituted-4-quinolones of the formula (I): wherein R1 is a straight or branched chain, saturated or ethylenically-unsaturated aliphatic hydrocarbyl group containing 1 to 18 carbon atoms which may optionally be substituted by one or more substituent groups selected from halo, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl and NR6R7, wherein each of R6 and R7 is independently selected from H and 1-6C alkyl or R6 and R7 together with the N atom to which they are attached form a saturated heterocyclic group selected from piperidino, piperazino and morpholino; R2 is a group selected from H, —OH, halo, —CHO, —CO2H and CONHR8 wherein R8 is H or a 1-6C alkyl; each of R3, R4 and R5 is independently selected form H, —CH3, —OCH3 and halo; or a non-toxic pharmaceutically-acceptable salt thereof, have use in the manufacture of a medicament for the treatment of a disease of a living animal body, including a human, which disease is responsive to the activity of an immunosuppressant. The preferred compound of the formula 1 is 2-n-heptyl-3-hydroxy-4(1H)-quinolone.

    摘要翻译： 式（I）的取代的4-喹诺酮：其中R 1是含有1至18个碳原子的直链或支链，饱和或不饱和的脂族烃基，其可任选被一个或多个选自以下的取代基取代：卤素， 1-6C烷氧基，羧基，1-6C烷氧基羰基和NR6R7，其中R6和R7各自独立地选自H和1-6C烷基或R6和R7与它们所连接的N原子一起形成饱和杂环基， 来自哌啶子基，哌嗪基和吗啉代; R2是选自H，-OH，卤素，-CHO，-CO 2 H和CONHR 8的基团，其中R 8是H或1-6 C烷基; R 3，R 4和R 5各自独立地选自H，-CH 3，-OCH 3和卤素; 或其无毒的药学上可接受的盐可用于制备用于治疗活动动物体（包括人）的疾病的药物，所述疾病对免疫抑制剂的活性有反应。 优选的式1化合物是2-正庚基-3-羟基-4（1H） - 喹诺酮。