PHOSPHATE PRODRUGS OF FLUOROOXINDOLES
    36.
    发明申请
    PHOSPHATE PRODRUGS OF FLUOROOXINDOLES 审中-公开
    氟磷酸盐的磷酸盐

    公开(公告)号:WO2003080047A1

    公开(公告)日:2003-10-02

    申请号:PCT/US2003/008613

    申请日:2003-03-20

    CPC classification number: C07F9/5728

    Abstract: The present invention provides novel phosphate derivatives having the general Formula (I) wherein the wavy bond (b) represents the racemate, the (R)-enantiomer or the (S)-enantiomer and A, B, R 1 , R 2 , R 3 , R 4 , m and n are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.

    Abstract translation: 本发明提供具有通式(I)的新型磷酸酯衍生物,其中波状键(b)表示外消旋物,(R) - 对映异构体或(S) - 对映异构体,A,B,R 1, R 3,R 4,m和n如本文所定义,或其无毒的药学上可接受的盐或溶剂化物,并且可用于治疗对钾通道开放有反应的病症。

    MODULATORS OF KCNQ POTASSIUM CHANNELS AND USE THEREOF IN TREATING MIGRAINE AND MECHANISTICALLY RELATED DISEASES

    公开(公告)号:WO2002072088A3

    公开(公告)日:2002-09-19

    申请号:PCT/US2002/004374

    申请日:2002-02-14

    Abstract: 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.

    FLUORO OXINDOLE DERIVATIVES AS MODULATORS OF KCNQ POTASSIUM CHANNELS
    39.
    发明申请
    FLUORO OXINDOLE DERIVATIVES AS MODULATORS OF KCNQ POTASSIUM CHANNELS 审中-公开
    氟化钾衍生物作为KCNQ钾通道的调节剂

    公开(公告)号:WO2002066426A2

    公开(公告)日:2002-08-29

    申请号:PCT/US2002/004304

    申请日:2002-02-14

    CPC classification number: C07D209/34

    Abstract: There is provided novel 3-fluoro-3-phenyl oxindole derivatives of Formula I wherein R 1 , R 2 , R 3 and R 4 each are independently hydrogen, C 1-4 alkyl, halogen, fluoromethyl, trifluoromethyl, phenyl, 4-methylphenyl or 4-trifluoromethylphenyl; R 5 is C 1-6 alkyl optionally substituted with one to three same or different groups selected from fluoro and chloro, provided R 5 is not C 1-6 alkyl when Y is O; Y is O or S; and R 6 and R 7 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.

    Abstract translation: 提供式I的新的3-氟-3-苯基羟吲哚衍生物,其中R 1,R 2,R 3和R 4各自独立地为氢,C 1-4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; R 5是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为O或S; 和R 6和R 7各自独立地是氢,氯,溴或三氟甲基; 其是KCNQ钾通道的开放剂,并且可用于治疗响应于KCNQ钾通道开放的疾病。

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