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1. 发明申请

WO2010023448A1 NOVEL POTASSIUM CHANNEL BLOCKERS 审中-公开
标题翻译：新型钾通道阻塞剂
公开(公告)号：WO2010023448A1
公开(公告)日：2010-03-04
申请号：PCT/GB2009/002078
申请日：2009-08-27
申请人： XENTION LIMITED , JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , GARRETT, Sarah, Louise , HARTZOULAKIS, Basil , MADGE, David , FORD, John
发明人： JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , GARRETT, Sarah, Louise , HARTZOULAKIS, Basil , MADGE, David , FORD, John
IPC分类号： C07C311/21 , C07D205/04 , C07D211/08 , C07D213/04 , C07D231/00 , C07D233/54 , C07D265/28 , C07D271/12 , C07D277/32 , C07D307/79 , C07D311/70 , C07D317/62 , C07D319/18 , A61K31/18 , A61P29/00
CPC分类号： C07C311/21 , C07C311/46 , C07C317/32 , C07C317/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D207/12 , C07D209/08 , C07D211/16 , C07D211/34 , C07D211/44 , C07D213/36 , C07D213/40 , C07D213/71 , C07D231/12 , C07D231/18 , C07D231/56 , C07D233/61 , C07D233/64 , C07D233/84 , C07D265/30 , C07D265/36 , C07D271/08 , C07D277/28 , C07D277/36 , C07D277/46 , C07D285/12 , C07D285/135 , C07D307/79 , C07D311/70 , C07D317/62 , C07D319/18 , C07D401/12 , C07D403/12 , C07D413/12
摘要： 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 2 , C(=O), C(=NH), NC(=O), 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 alkyl, optionally substituted aryl or heteroaryl or NR 24 R 25 , 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 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, an optionally substituted alkyl, preferably CH 3 or, NR 4 R 5 may form an optionally substituted saturated or partially saturated 4-7 membered ring with the general formula (II). Wherein; X 2 is C(=O), CH 2 , CH(R 6 ) or C(R 6 )(R 6 ), X 3 is CH 2 , CH(R 7 ), C(R 7 )(R 7 ), NH, N(R 8 ), O or S Each R 6 independently represents 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; Each R 7 independently represents 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 8 is optionally substituted acyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; R 24 and R 25 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 = 1 or 2 m = 1, 2 or 3 With the proviso that when X 1 is C=O and R 5 is H then R 4 is not (a) or (b) or (c). Where R 4 a, R 5 a and R 6 a are each independently H, C 1-6 alkyl, aryl, heteroaryl, cycloalkyl, or aryl-C 1-6 alkyl; R 10 a is H or C 1-6 alkyl; and R 11 a is C 1-6 alkyl or aryl-C 1-6 alkyl and when X 1 is C=O or CH 2 and R 5 is H then R 4 is not (d) Where q is 0 to 5, R 3 b is H, OH or alkoxy and R 4 b is NH 2 , phenyl or a C 3-10 heterocycle. The compounds are useful as potassium ion channel inhibitors.
摘要翻译：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： X 1选自CH 2，C（= O），C（= NH），NC（= O），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选自基团由任选取代的烷基，任选取代的芳基或杂芳基或NR 24 R 25组成，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，任选取代的芳基烷基和任选取代的杂芳基R 5可以是氢，任选取代的烷基，优选CH 3或NR 4 R 5可以形成具有通式（II）的任选取代的饱和或部分饱和的4-7元环。其中： X2是C（= O），CH2，CH（R6）或C（R6）（R6），X3是CH2，CH（R7），C（R7）（R7），NH，N（R8）每个R 6独立地表示任选取代的氨基，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; 每个R 7独立地表示任选取代的氨基，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R 8是任选取代的酰基，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; R 24和R 25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 = 1或2 m = 1,2或3，条件是当 X1为C = O，R5为H，R4不为（a）或（b）或（c）。其中R 4a，R 5a和R 6a各自独立地为H，C 1-6烷基，芳基，杂芳基，环烷基或芳基-C 1-6烷基; R10a是H或C1-6烷基; R 11a为C 1-6烷基或芳基-C 1-6烷基，当X 1为C = O或CH 2且R 5为H时，R 4不为（d）其中q为0至5，R 3b为H，OH或烷氧基，R 4b为NH 2 ，苯基或C 3-10杂环。该化合物可用作钾离子通道抑制剂。

2. 发明申请

WO2010023445A1 NOVEL POTASSIUM CHANNEL BLOCKER 审中-公开
标题翻译：新型通道阻塞器
公开(公告)号：WO2010023445A1
公开(公告)日：2010-03-04
申请号：PCT/GB2009/002075
申请日：2009-08-27
申请人： XENTION LIMITED , JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , JONES, Simon, Mark , POLLARD, Derek, Roland , HARTZOULAKIS, Basil , PAYNE, Helen , MADGE, David , FORD, John
发明人： JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , JONES, Simon, Mark , POLLARD, Derek, Roland , HARTZOULAKIS, Basil , PAYNE, Helen , MADGE, David , FORD, John
IPC分类号： C07D211/08 , C07D217/16 , C07D231/18 , C07D233/84 , C07D265/30 , C07D277/36 , C07D307/64 , C07D311/58 , C07D333/34 , C07D401/12 , C07D403/12 , C07D413/12 , C07D295/192 , A61K31/18 , A61P29/00
CPC分类号： C07D295/18 , C07D207/12 , C07D211/10 , C07D211/16 , C07D211/22 , C07D211/48 , C07D211/52 , C07D217/20 , C07D231/18 , C07D233/84 , C07D241/04 , C07D265/30 , C07D277/36 , C07D307/64 , C07D311/58 , C07D333/34
摘要： The present invention provides a compound of formula (I):or its salts or pharmaceutically acceptable derivatives wherein; R 1 is selected from the group consisting of optionally substituted arylalkyl, optionally substituted aryl, optionally substituted heteroarylalkyl and optionally substituted heteroaryl; R 2 is selected from the group consisting of optionally substituted acyl, optionally substituted sulfonyl and optionally substituted sulfamoyl; R 3 is selected from the group consisting of hydrogen, halogen, hydroxyl, alkoxy, aryloxy, optionally substituted alkyl, optionally substituted amino, optionally substituted amino carbonyl, optionally substituted amino sulfonyl or nitrile; X 1 is selected from a group consisting of a chemical bond, CR 7 R 8 , C(=O), C(=NH), NR 9 , NHC(O), and SO 2 wherein; R 7 and R 8 are independently selected from hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl and optionally substituted heteroaryl or; R 7 and R 8 together form an optionally substituted C 4-6 cycloalkyl ring; R 9 is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted aryl and optionally substituted heteroaryl; A represents an optionally substituted saturated or partially saturated 4-7 membered ring with the general formula (A): or is selected from formula (B): For each occurrence; X 2 is CH or N; X 3 is CH 2 , CH(R 5a ), C(R 5a )(R 5b ), NH, N(R 5c ), O or S; X 4 is independently selected from C(=O), CH 2 , CH(R 4a ) or C(R 4a )(R 4b ); R 4a and R 4b for each occurrence is independently halogen, optionally substituted amino, hydroxyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; R 5a and R 5b for each occurrence is independently, halogen, optionally substituted amino, hydroxyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted alkanoyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; R 5c is optionally substituted acyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; n = 1 or 2. The compounds are useful as potassium ion channel inhibitors.
摘要翻译：本发明提供式（I）化合物或其盐或药学上可接受的衍生物，其中： R 1选自任选取代的芳基烷基，任选取代的芳基，任选取代的杂芳基烷基和任选取代的杂芳基; R 2选自任选取代的酰基，任选取代的磺酰基和任选取代的氨磺酰基; 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，任选取代的氨基羰基，任选取代的氨基磺酰基或腈; X 1选自由化学键，CR 7 R 8，C（= O），C（= NH），NR 9，NHC（O）和SO 2组成的组。 R 7和R 8独立地选自氢，任选取代的烷基，任选取代的环烷基，任选取代的芳基和任选取代的杂芳基;或 R7和R8一起形成任选取代的C 4-6环烷基环; R9选自氢，任选取代的烷基，任选取代的芳基和任选取代的杂芳基; A表示任选取代的具有通式（A）的饱和或部分饱和的4-7元环：或选自式（B）：每次出现; X2是CH或N; X3是CH2，CH（R5a），C（R5a）（R5b），NH，N（R5c），O或S; X4独立地选自C（= O），CH2，CH（R4a）或C（R4a）（R4b）; R4a和R4b各自独立地为卤素，任选取代的氨基，羟基，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; R5a和R5b各自独立地为卤素，任选取代的氨基，羟基，任选取代的烷氧基，任选取代的芳氧基，任选取代的烷基，任选取代的烷酰基，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，任选取代的芳烷基，任选取代的芳基或任选取代的杂芳基; n = 1或2.化合物可用作钾离子通道抑制剂。

3. 发明申请

WO2010139953A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2010139953A1
公开(公告)日：2010-12-09
申请号：PCT/GB2010/001092
申请日：2010-06-04
申请人： XENTION LIMITED , HAMLYN, Richard, John , MADGE, David , MULLA, Mushtaq
发明人： HAMLYN, Richard, John , MADGE, David , MULLA, Mushtaq
IPC分类号： C07D209/46 , C07D217/24 , C07D401/12 , C07D403/12
CPC分类号： C07D209/46 , C07D217/24 , C07D401/12 , C07D403/12
摘要： 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 is selected from a group consisting of CH 2 , C(=O), CH(R 5 ), C(R 5 )(R 6 ) or C(R 5 )(R 6 )CH 2 ; 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; R4 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 = 1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. The compounds are useful in treating various conditions including arrhythmia.
摘要翻译：式（I）的化合物或其盐或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选自CH 2，C（= O），CH（R 5），C（R 5）（R 6）或C（R 5）（R 6）CH 2 ; 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，任选取代的芳烷基和任选取代的杂芳基; R5和R6每次出现是任选取代的烷基; R 7和R 8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，任选取代的芳烷基，任选取代的芳基或任选取代的杂芳基; 提供n = 1或2。还提供了包含该化合物的药物组合物。该化合物可用于治疗各种病症，包括心律失常。

4. 发明申请

WO2010139967A1 DIHYDROINDOLE AND TETRAHYDROISOQUINOLINE DERIVATIVES USEFUL AS POTASSIUM CHANNEL INHIBITORS 审中-公开
标题翻译：用作钾通道抑制剂的二氢吲哚衍生物和四氢喹啉衍生物
公开(公告)号：WO2010139967A1
公开(公告)日：2010-12-09
申请号：PCT/GB2010/001123
申请日：2010-06-04
申请人： XENTION LIMITED , HAMLYN, Richard, John , MADGE, David , MULLA, Mushtaq
发明人： MADGE, David , MULLA, Mushtaq
IPC分类号： C07D401/12 , C07D403/12 , A61K31/4155 , A61K31/4178 , A61K31/47 , A61P9/00 , A61P17/00
CPC分类号： C07D401/12 , C07D403/12
摘要： 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.
摘要翻译：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。

5. 发明申请

WO2010023446A1 NOVEL POTASSIUM CHANNEL BLOCKERS 审中-公开
标题翻译：新型钾通道阻塞剂
公开(公告)号：WO2010023446A1
公开(公告)日：2010-03-04
申请号：PCT/GB2009/002076
申请日：2009-08-27
申请人： XENTION LIMITED , JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , JONES, Simon, Mark , HARTZOULAKIS, Basil , MADGE, David , FORD, John
发明人： JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , JONES, Simon, Mark , HARTZOULAKIS, Basil , MADGE, David , FORD, John
IPC分类号： C07C311/21 , C07D213/71 , C07D231/18 , C07D233/84 , C07D233/90 , C07D403/12 , C07D413/12 , C07D295/135 , C07D207/27 , A61K31/18 , A61P29/00
CPC分类号： C07C311/21 , C07D207/27 , C07D213/71 , C07D231/18 , C07D233/84 , C07D233/90 , C07D295/135 , C07D403/12 , C07D413/12
摘要： 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.
摘要翻译：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。

6. 发明公开

EP2438055A1 DIHYDROINDOLE AND TETRAHYDROISOQUINOLINE DERIVATIVES USEFUL AS POTASSIUM CHANNEL INHIBITORS 有权转让
标题翻译： AS钾通道阻断剂合适的和二氢吲哚啉
公开(公告)号：EP2438055A1
公开(公告)日：2012-04-11
申请号：EP10725248.8
申请日：2010-06-04
申请人： Xention Limited
发明人： MADGE, David , MULLA, Mushtaq , JONES, Simon, Mark , HARTZOULAKIS, Basil , JOHN, Derek, Edward , HAMLYN, Richard, John
IPC分类号： C07D401/12 , C07D403/12 , A61K31/4155 , A61K31/4178 , A61K31/47 , A61P9/00 , A61P17/00
CPC分类号： C07D401/12 , C07D403/12
摘要： 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 CH2, CH(R5) or C(R5)(R6); R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR7R8; R3 R4 R5 R6 R7 and R8 are as defined herein, n=0, 1, 2 or 3; o=0, 1 or 2, with the proviso that when o=0, then n is 1, 2 or 3 and when o=1, then 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.

7. 发明公开

EP2334637A1 NOVEL POTASSIUM CHANNEL BLOCKERS 有权转让
标题翻译： NEUE KALIUMKANALBLOCKER
公开(公告)号：EP2334637A1
公开(公告)日：2011-06-22
申请号：EP09785010.1
申请日：2009-08-27
申请人： Xention Limited
发明人： JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , JONES, Simon, Mark , HARTZOULAKIS, Basil , MADGE, David , FORD, John
IPC分类号： C07C311/21 , C07D213/71 , C07D231/18 , C07D233/84 , C07D233/90 , C07D403/12 , C07D413/12 , C07D295/135 , C07D207/27 , A61K31/18 , A61P29/00
CPC分类号： C07C311/21 , C07D207/27 , C07D213/71 , C07D231/18 , C07D233/84 , C07D233/90 , C07D295/135 , C07D403/12 , C07D413/12
摘要： 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.
摘要翻译：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R1，R2，R3，R4，R5，X1和j如本文所定义。该化合物可用作钾离子通道抑制剂。

8. 发明公开

EP2342177A1 NOVEL POTASSIUM CHANNEL BLOCKERS 有权转让
标题翻译：新型钾通道阻滞剂
公开(公告)号：EP2342177A1
公开(公告)日：2011-07-13
申请号：EP09785012.7
申请日：2009-08-27
申请人： Xention Limited
发明人： JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , GARRETT, Sarah, Louise , HARTZOULAKIS, Basil , MADGE, David , FORD, John
IPC分类号： C07C311/21 , C07D205/04 , C07D211/08 , C07D213/04 , C07D231/00 , C07D233/54 , C07D265/28 , C07D271/12 , C07D277/32 , C07D307/79 , C07D311/70 , C07D317/62 , C07D319/18 , A61K31/18 , A61P29/00
CPC分类号： C07C311/21 , C07C311/46 , C07C317/32 , C07C317/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D207/12 , C07D209/08 , C07D211/16 , C07D211/34 , C07D211/44 , C07D213/36 , C07D213/40 , C07D213/71 , C07D231/12 , C07D231/18 , C07D231/56 , C07D233/61 , C07D233/64 , C07D233/84 , C07D265/30 , C07D265/36 , C07D271/08 , C07D277/28 , C07D277/36 , C07D277/46 , C07D285/12 , C07D285/135 , C07D307/79 , C07D311/70 , C07D317/62 , C07D319/18 , C07D401/12 , C07D403/12 , C07D413/12
摘要： 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
2 , C(=O), C(=NH), NC(=O), 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 alkyl, optionally substituted aryl or heteroaryl or NR
24 R
25 , 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 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, an optionally substituted alkyl, preferably CH
3 or, NR
4 R
5 may form an optionally substituted saturated or partially saturated 4-7 membered ring with the general formula (II). Wherein; X
2 is C(=O), CH
2 , CH(R
6 ) or C(R
6 )(R
6 ), X
3 is CH
2 , CH(R
7 ), C(R
7 )(R
7 ), NH, N(R
8 ), O or S Each R
6 independently represents 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; Each R
7 independently represents 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
8 is optionally substituted acyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; R
24 and R
25 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 = 1 or 2 m = 1, 2 or 3 With the proviso that when X
1 is C=O and R
5 is H then R
4 is not (a) or (b) or (c). Where R
4 a, R
5 a and R
6 a are each independently H, C
1-6 alkyl, aryl, heteroaryl, cycloalkyl, or aryl-C
1-6 alkyl; R
10 a is H or C
1-6 alkyl; and R
11 a is C
1-6 alkyl or aryl-C
1-6 alkyl and when X
1 is C=O or CH
2 and R
5 is H then R
4 is not (d) Where q is 0 to 5, R
3 b is H, OH or alkoxy and R
4 b is NH
2 , phenyl or a C
3-10 heterocycle. The compounds are useful as potassium ion channel inhibitors.
摘要翻译：本发明提供了式（I）化合物或其盐或其药学上可接受的衍生物，其中： X 1选自CH 2，C（= O），C（= NH），NC（= O），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为选自任选取代的烷基，任选取代的芳基或杂芳基或NR 24 R 25，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基; 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，任选取代的芳基烷基和任选取代的杂芳基R 5可以是氢，任选取代的烷基，优选CH 3或NR 4 R 5可以与通式（II）形成任选取代的饱和或部分饱和的4-7元环。其中： X 2为C（= O），CH 2，CH（R 6）或C（R 6）（R 6），X 3为CH 2，CH（R 7），C（R 7） NH，N（R 8），O或S各R 6独立地表示任选取代的氨基，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，，任选取代的芳基或任选取代的杂芳基; 每个R7独立地表示任选取代的氨基，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，任选取代的芳基或任选取代的杂芳基，任选取代的酰基，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; R 24和R 25相同或不同并且各自表示氢，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 = 1或2 m = 1,2或3。当X 1是C = O且R 5是H时，则R 4不是（a）或（b）或（c）。其中R 4a，R 5a和R 6a各自独立地为H，C 1-6烷基，芳基，杂芳基，环烷基或芳基-C 1-6烷基; R 10a是H或C 1-6烷基; 并且R 11a是C 1-6烷基或芳基-C 1-6烷基，并且当X 1是C = O或CH 2并且R 5是H时，则R 4不是（d）其中q是0至5，R 3b是H ，OH或烷氧基，并且R 4b是NH 2，苯基或C 3-10杂环。这些化合物可用作钾离子通道抑制剂。

9. 发明公开

EP2438044A1 COMPOUNDS 有权转让
标题翻译：化合物
公开(公告)号：EP2438044A1
公开(公告)日：2012-04-11
申请号：EP10722754.8
申请日：2010-06-04
申请人： Xention Limited
发明人： HAMLYN, Richard, John , MADGE, David , MULLA, Mushtaq , JONES, Simon, mark , HARTZOULAKIS, Basil , JOHN, Derek, Edward
IPC分类号： C07D209/46 , C07D217/24 , C07D401/12 , C07D403/12
CPC分类号： C07D209/46 , C07D217/24 , C07D401/12 , C07D403/12
摘要： 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 is selected from a group consisting of CH2, C(═O), CH(R5), C(R5)(R6) or C(R5)(R6)CH2; R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR7R8; R3 R4 R5 R6 R7 and R8 are as defined herein; and n=1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. The compounds are useful in treating various conditions including arrhythmia.
摘要翻译：式（I）化合物或其盐或其药学上可接受的衍生物，其中： A代表具有通式（II）的化学部分：X选自CH 2，C（= O），CH（R 5），C（R 5）（R 6）或C（R 5 ）（R 6）CH 2; 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; 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; R 5和R 6每次出现都是任选取代的烷基; R 7和R 8相同或不同，并且各自表示氢，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; 提供了n = 1或2。还提供了包含这些化合物的药物组合物。该化合物可用于治疗包括心律不齐在内的各种疾病。

10. 发明公开

EP2344456A1 NOVEL POTASSIUM CHANNEL BLOCKER 有权转让
标题翻译：中性糖尿病患者
公开(公告)号：EP2344456A1
公开(公告)日：2011-07-20
申请号：EP09785009.3
申请日：2009-08-27
申请人： Xention Limited
发明人： JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , JONES, Simon, Mark , POLLARD, Derek, Roland , HARTZOULAKIS, Basil , PAYNE, Helen , MADGE, David , FORD, John
IPC分类号： C07D211/08 , C07D217/16 , C07D231/18 , C07D233/84 , C07D265/30 , C07D277/36 , C07D307/64 , C07D311/58 , C07D333/34 , C07D401/12 , C07D403/12 , C07D413/12 , C07D295/192 , A61K31/18 , A61P29/00
CPC分类号： C07D295/18 , C07D207/12 , C07D211/10 , C07D211/16 , C07D211/22 , C07D211/48 , C07D211/52 , C07D217/20 , C07D231/18 , C07D233/84 , C07D241/04 , C07D265/30 , C07D277/36 , C07D307/64 , C07D311/58 , C07D333/34
摘要： The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives wherein R1, R2, R3, X1, and A are defined herein. The compounds are useful as potassium ion channel inhibitors.
摘要翻译：本发明提供式（I）化合物或其盐或药学上可接受的衍生物，其中R 1，R 2，R 3，X 1和A如本文所定义。该化合物可用作钾离子通道抑制剂。

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