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    • 22. 发明申请
      WO2010139967A1 DIHYDROINDOLE AND TETRAHYDROISOQUINOLINE DERIVATIVES USEFUL AS POTASSIUM CHANNEL INHIBITORS 审中-公开
    • DIHYDROINDOLE AND TETRAHYDROISOQUINOLINE DERIVATIVES USEFUL AS POTASSIUM CHANNEL INHIBITORS
    • 用作钾通道抑制剂的二氢吲哚衍生物和四氢喹啉衍生物
    • WO2010139967A1
    • 2010-12-09
    • PCT/GB2010/001123
    • 2010-06-04
    • XENTION LIMITED , HAMLYN, Richard, John , MADGE, David , MULLA, Mushtaq
    • MADGE, David , MULLA, Mushtaq
    • C07D401/12 , C07D403/12 , A61K31/4155 , A61K31/4178 , A61K31/47 , A61P9/00 , A61P17/00
    • C07D401/12 , C07D403/12
    • A compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein; A represents a chemical moiety with the general formula (II); X and Y are independently selected from a group consisting of CH 2 , CH(R 5 ) or C(R 5 )(R 6 ); R 1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R 2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR 7 R 8 ; R 3 is selected from the group consisting of hydrogen, halogen, hydroxyl, alkoxy, aryloxy, optionally substituted alkyl, optionally substituted amino, optionally substituted amino sulfonyl or nitrile; R 4 is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted acyl, optionally substituted sulfonyl, optionally substituted sulfamoyl, optionally substituted aryl, optionally substituted arylalkyl, and optionally substituted heteroaryl; R 5 and R 6 for each occurrence is optionally substituted alkyl; R 7 and R 8 are the same or different and each represents hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; n = 0, 1, 2 or 3; o = 0, 1 or 2 with the proviso that when o = 0, n is 1, 2 or 3 and when o = 1, n is 1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. These compounds are useful in the treatment of various disorders including arrhythmia.
    • 式（I）化合物或其盐或其药学上可接受的衍生物，其中： A表示具有通式（II）的化学部分; X和Y独立地选自由CH 2，CH（R 5）或C（R 5）（R 6）组成的组。 R 1选自任选取代的芳烷基和任选取代的杂芳基烷基; R 2选自任选取代的芳基或任选取代的杂芳基或NR 7 R 8; R 3选自氢，卤素，羟基，烷氧基，芳氧基，任选取代的烷基，任选取代的氨基，任选取代的氨基磺酰基或腈; R 4选自氢，任选取代的烷基，任选取代的环烷基，任选取代的杂环烷基，任选取代的酰基，任选取代的磺酰基，任选取代的氨磺酰基，任选取代的芳基，任选取代的芳基烷基和任选取代的杂芳基; R5和R6各为任意取代的烷基; R7和R8相同或不同，各自表示氢，任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或任选取代的杂芳基; n = 0,1,2或3; o = 0,1或2，条件是当o = 0时，n为1,2或3，当o = 1时，n为1或2。 还提供了包含该化合物的药物组合物。 这些化合物可用于治疗各种疾病，包括心律失常。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 24. 发明申请
      WO2010023446A1 NOVEL POTASSIUM CHANNEL BLOCKERS 审中-公开
    • NOVEL POTASSIUM CHANNEL BLOCKERS
    • 新型钾通道阻塞剂
    • WO2010023446A1
    • 2010-03-04
    • PCT/GB2009/002076
    • 2009-08-27
    • XENTION LIMITED , JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , JONES, Simon, Mark , HARTZOULAKIS, Basil , MADGE, David , FORD, John
    • JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , JONES, Simon, Mark , HARTZOULAKIS, Basil , MADGE, David , FORD, John
    • C07C311/21 , C07D213/71 , C07D231/18 , C07D233/84 , C07D233/90 , C07D403/12 , C07D413/12 , C07D295/135 , C07D207/27 , A61K31/18 , A61P29/00
    • C07C311/21 , C07D207/27 , C07D213/71 , C07D231/18 , C07D233/84 , C07D233/90 , C07D295/135 , C07D403/12 , C07D413/12
    • The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein; X 1 is selected from a group consisting of CH, O or N; R 1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R 2 is selected from the group consisting of optionally substituted aryl, optionally substituted heteroaryl or NR 6 R 7 ; R 3 is selected from the group consisting of hydrogen, halogen, hydroxyl, alkoxy, aryloxy, optionally substituted alkyl, optionally substituted amino, optionally substituted amino sulphonyl or nitrile; R 4 is selected from the group consisting of optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted acyl, optionally substituted sulfonyl, optionally substituted sulfamoyl, optionally substituted aryl, optionally substituted arylalkyl, and optionally substituted heteroaryl R 5 may be hydrogen or may, together with R 4 and X 1 (when X 1 = N), form an optionally substituted saturated or partially saturated 5-7 membered ring with the general formula (II). X 2 is C(=O), C(R 8 ) 2 ; X 3 is, C(R 9 ) 2 , N(R 9b ), O or S; R 6 and R 7 are the same or different and each represents hydrogen, optioanally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; R 8a and R 8b for each occurence is independently hydrogen, halogen, optionally substituted amino, optionally substituted amino carbonyl, hydroxyl, optionally substituted acyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalky, optionally substituted aryl or optionally substituted heteroaryl; R 9a R 9b for each occurence is independently hydrogen, halogen, optionally substituted amino, optionally substituted amino carbonyl, hydroxyl, optionally substituted acyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalky, optionally substituted aryl or optionally substituted heteroaryl; R 9c is optionally substituted acyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalky, optionally substituted aryl or optionally substituted heteroaryl; With the proviso that: When X 1 is O then j = 0 When X 1 is N or CH then j =1 n = 1,2 or 3. The compounds are useful as potassium ion channel inhibitors.
    • 本发明提供式（I）化合物或其盐或其药学上可接受的衍生物，其中： X1选自CH，O或N; R 1选自任选取代的芳基烷基和任选取代的杂芳基烷基; R 2选自任选取代的芳基，任选取代的杂芳基或NR 6 R 7; R 3选自氢，卤素，羟基，烷氧基，芳氧基，任选取代的烷基，任选取代的氨基，任选取代的氨基磺酰基或腈; R 4选自任选取代的烷基，任选取代的环烷基，任选取代的杂环烷基，任选取代的酰基，任选取代的磺酰基，任选取代的氨磺酰基，任选取代的芳基，任选取代的芳烷基和任选取代的杂芳基R 5可以是氢或可以 与R4和X1一起（当X1 = N时）与通式（II）形成任选取代的饱和或部分饱和的5-7元环。 X2为C（= O），C（R8）2; X3为，C（R9）2，N（R9b），O或S; R6和R7相同或不同，各自代表氢，视黄醛取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或任选取代的杂芳基; R8a和R8b各自独立地为氢，卤素，任选取代的氨基，任选取代的氨基羰基，羟基，任选取代的酰基，任选取代的烷氧基，任选取代的芳氧基，任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或 任选取代的杂芳基; R9a R9b各自独立地为氢，卤素，任选取代的氨基，任选取代的氨基羰基，羟基，任选取代的酰基，任选取代的烷氧基，任选取代的芳氧基，任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或 任选取代的杂芳基; 任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或任选取代的杂芳基; 条件是：当X1为O时，j = 0当X1为N或CH时，则j = 1 n = 1,2或3.该化合物可用作钾离子通道抑制剂。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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