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    Diphenyl imidazoles as potassium channel modulators
    1.
    发明授权
    Diphenyl imidazoles as potassium channel modulators 有权
    二苯基咪唑作为钾通道调节剂

    公开(公告)号：US06271249B1

    公开(公告)日：2001-08-07

    申请号：US09538520

    申请日：2000-03-29

    申请人： Jeffrey L. Romine ,  Scott W. Martin ,  Piyasena Hewawasam ,  Nicholas A. Meanwell ,  Valentin K. Gribkoff ,  John E. Starrett, Jr.

    发明人： Jeffrey L. Romine ,  Scott W. Martin ,  Piyasena Hewawasam ,  Nicholas A. Meanwell ,  Valentin K. Gribkoff ,  John E. Starrett, Jr.

    IPC分类号： A61K31402

    CPC分类号： C07D263/58 ,  C07D233/64 ,  C07D233/70 ,  C07D233/76 ,  C07D235/12 ,  C07D249/12 ,  C07D249/14 ,  C07D271/113 ,  C07D413/10

    摘要： Novel compounds of Formula 1 are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels: wherein “Het” is one of a select group of heterocyclic moieties; Z is independently for each occurrence selected from O or S; Ra, Rb and Rc each are independently selected from hydrogen, halogen, OH, CF3, NO2, or provided Rc is not hydrogen; and when Ra and Rb are hydrogen, Rc may be a heterocyclic moiety selected from the group consisting of imidazol-1-yl, morpholinomethyl, N-methylimidazol-2-yl, and pyridin-2-yl; Rd and Re each are independently selected from hydrogen, halogen, CF3, NO2 or imidazol-1-yl; m, n and p each are independently selected from an integer of 0 or 1; and Rf and Rg each are independently hydrogen; C1-4 alkyl; or Rf and Rg, taken together with the nitrogen atom to which they are attached, is a heterocyclic moiety selected from the group consisting of N-methylpiperazine, morpholine, thiomorpholine, N-benzylpiperazine and imidazolinone.

    摘要翻译： 式1的新型化合物可用于治疗对大电导钙激活钾通道的开放剂起反应的病症：其中“Het”是选择性杂环部分组之一; Z独立地选自O或S; R a，R b和R c各自独立地选自氢，卤素，OH，CF 3，NO 2，或提供的R c不是氢; 当R a和R b为氢时，R c可以是选自咪唑-1-基，吗啉代甲基，N-甲基咪唑-2-基和吡啶-2-基的杂环部分; Rd和Re各自独立地选自氢，卤素，CF 3，NO 2或咪唑-1-基; m，n和p各自独立地选自0或1的整数; Rf和Rg各自独立地为氢; C 1-4烷基 或R f和R g与它们所连接的氮原子一起是选自N-甲基哌嗪，吗啉，硫代吗啉，N-苄基哌嗪和咪唑啉酮的杂环部分。

    3-fluoro-2-oxindole modulators of KCNQ potassium channels and use thereof in treating migraine and mechanistically related disease
    6.
    发明授权
    3-fluoro-2-oxindole modulators of KCNQ potassium channels and use thereof in treating migraine and mechanistically related disease 有权
    KCNQ钾通道的3-氟-2-羟吲哚调节剂及其在治疗偏头痛和机械相关疾病中的应用

    公开(公告)号：US06855829B2

    公开(公告)日：2005-02-15

    申请号：US10075703

    申请日：2002-02-14

    申请人： Steven I. Dworetzky ,  Valentin K. Gribkoff ,  Gene G. Kinney ,  Piyasena Hewawasam

    发明人： Steven I. Dworetzky ,  Valentin K. Gribkoff ,  Gene G. Kinney ,  Piyasena Hewawasam

    IPC分类号： G01N33/50 ,  A61K31/404 ,  A61K31/506 ,  A61K45/00 ,  A61P25/06 ,  G01N33/15 ,  C07D209/34

    CPC分类号： A61K31/404 ,  A61K31/506

    摘要： Compounds which function as modulators, particularly, openers, of human KCNQ potassium channel proteins or polypeptides, particularly, central nervous system (CNS)-located KCNQ potassium channels, and heteromultimers thereof, and their use in the treatment of migraine are provided by the present invention. One novel type of potassium channel polypeptide openers provided by the present invention is the fluorooxindole compounds, described for the first time as therapeutics for the treatment of migraine by preventing the asynchronous firing of neurons. Other KCNQ potassium channel opener compounds that are also useful in the treatments of the invention include 2,4-disubstituted pyrimidine-5-carboxamide derivatives. One or more of the compounds according to the present invention may be utilized alone, in combination, or in conjunction with other treatment modalities for reducing, ameliorating and/or alleviating migraine or diseases similar to, or mechanistically related to, migraine, e.g., cluster headache.

    摘要翻译： 作为人KCNQ钾通道蛋白或多肽，特别是中枢神经系统（CNS）分配的KCNQ钾通道及其异源多肽的调节剂，特别是开放剂的化合物及其在治疗偏头痛中的用途由本发明提供 发明。 本发明提供的一种新型的钾通道多肽开放剂是氟氧吲哚化合物，首次作为通过防止神经元的异步烧制来治疗偏头痛的治疗剂。 也可用于本发明处理的其它KCNQ钾通道开放剂化合物包括2,4-二取代的嘧啶-5-甲酰胺衍生物。 根据本发明的一种或多种化合物可以单独使用，或与其它治疗方式联用，用于减少，改善和/或减轻与偏头痛相似或机械相关的偏头痛或类似疾病，例如，集群 头痛。

    Fluoro oxindole derivatives as modulators if KCNQ potassium channels
    7.
    发明授权
    Fluoro oxindole derivatives as modulators if KCNQ potassium channels 有权
    氟羟吲哚衍生物作为KCNQ钾通道的调节剂

    公开(公告)号：US06469042B1

    公开(公告)日：2002-10-22

    申请号：US10075522

    申请日：2002-02-14

    申请人： Piyasena Hewawasam ,  Pierre Dextraze ,  Valentin K. Gribkoff ,  Gene G. Kinney ,  Steven I. Dworetzky

    发明人： Piyasena Hewawasam ,  Pierre Dextraze ,  Valentin K. Gribkoff ,  Gene G. Kinney ,  Steven I. Dworetzky

    IPC分类号： A61K3405

    CPC分类号： C07D209/34

    摘要： There is provided novel 3-fluoro-3-phenyl oxindole derivatives of Formula I wherein R1, R2, R3 and R4 each are independently hydrogen, C1-4 alkyl, halogen, fluoromethyl, trifluoromethyl, phenyl, 4-methylphenyl or 4-trifluoromethylphenyl; R5 is C1-6 alkyl optionally substituted with one to three same or different groups selected from fluoro and chloro, provided R5 is not C1-6 alkyl when Y is O; Y is O or S; and R6 and R7 each are independently hydrogen, chloro, bromo or trifluoromethy; which are openers of the KCNQ potassium channels and are useful in the treatment of disorders which are responsive to the opening of the KCNQ potassium channels.

    摘要翻译： 提供式I的新型3-氟-3-苯基羟吲哚衍生物，其中R1，R2，R3和R4各自独立地为氢，C1-4烷基，卤素，氟甲基，三氟甲基，苯基，4-甲基苯基或4-三氟甲基苯基; R5为 任选被一至三个选自氟和氯的相同或不同的基团取代的C 1-6烷基，当Y是O时，R 5不是C 1-6烷基; Y是O或S; 和R6和R7各自独立地是氢，氯，溴或三氟甲基;它们是KCNQ钾通道的开放剂，并且可用于治疗响应于KCNQ钾通道开放的病症。

    3-substituted-4-arylquinolin-2-one derivatives as potassium channel modulators
    8.
    发明授权
    3-substituted-4-arylquinolin-2-one derivatives as potassium channel modulators 失效
    3-取代-4-芳基喹啉-2-酮衍生物作为钾通道调节剂

    公开(公告)号：US06184231B2

    公开(公告)日：2001-02-06

    申请号：US09452523

    申请日：1999-12-01

    申请人： Piyasena Hewawasam ,  John E. Starrett, Jr.

    发明人： Piyasena Hewawasam ,  John E. Starrett, Jr.

    IPC分类号： A61K314704

    CPC分类号： C07D215/227 ,  C07D215/54

    摘要： The present invention provides novel 3-substituted-4-arylquinolin-2-one derivatives having the general formula wherein R, R1, R2, R3, R4, R5, R6 and R7 are as defined herein, or a non-toxic pharmaceutically acceptable salt thereof which are modulators of the large conductance calcium-activated K+ channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.

    摘要翻译： 本发明提供了具有通式R，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义的新的3-取代-4-芳基喹啉-2-酮衍生物或其无毒的药学上可接受的盐 其是大电导钙激活的K +通道的调节剂，并且可用于治疗对钾通道开放有反应的病症。