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    Thieno[2,3-B] pyridines as potassium channel inhibitors
    1.
    发明授权
    Thieno[2,3-B] pyridines as potassium channel inhibitors 失效
    噻吩并[2,3-B]吡啶作为钾通道抑制剂

    公开(公告)号：US07576212B2

    公开(公告)日：2009-08-18

    申请号：US11297330

    申请日：2005-12-09

    申请人： John Ford ,  Nicholas John Palmer ,  John Frederick Atherall ,  David John Madge ,  Derek John

    发明人： John Ford ,  Nicholas John Palmer ,  John Frederick Atherall ,  David John Madge ,  Derek John

    IPC分类号： C07D513/02

    CPC分类号： C07D495/04 ,  C07D333/36 ,  C07D333/38 ,  C07D409/12

    摘要： The invention provides compounds of the formula: wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, CO2R7, CONR5R6 or halo; R3 and R4 are H, NR5R6, NC(O)R7, halo, trifluromethyl, alkyl, CONR5R6, CO2R7, nitrile or alkoxy; R5 and R6 may be the same or different and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R5 and R6 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; R7 is H or alkyl; A is H, halo, or a group of formula X-L-Y; X is O, S or NR8; R8 is H or alkyl; L is (CH2)n, where n is 0, 1, 2, 3 or 4; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; the products of mono- and di-oxidation of sulphur and/or mono-oxidation of nitrogen moieties in compounds of formula I; or a pharmaceutically acceptable salt thereof. These compounds find use as inhibitors of potassium ion channels and thus are useful in the treatment of various conditions including arrhythmia and type-2 diabetes mellitus.

    摘要翻译： 本发明提供下式的化合物：其中R1是芳基，杂芳基，环烷基或烷基; R2是H，烷基，硝基，CO 2 R 7，CONR 5 R 6或卤素; R3和R4是H，NR5R6，NC（O）R7，卤素，三氟甲基，烷基，CONR5R6，CO2R7，腈或烷氧基; R5和R6可以相同或不同，可以是H，烷基，芳基，杂芳基或环烷基; 或R 5和R 6可以一起形成饱和的，不饱和的或部分饱和的4至7元环，其中所述环可任选地包含一个或多个选自N，O或S的其它杂原子; R7是H或烷基; A是H，卤素或式X-L-Y基团; X是O，S或NR8; R8是H或烷基; L是（CH 2）n，其中n是0,1,2,3或4; Y为芳基，杂环基，烷基，链烯基或环烷基; 式I化合物中硫的单和二氧化和/或氮部分的单氧化的产物; 或其药学上可接受的盐。 这些化合物可用作钾离子通道的抑制剂，因此可用于治疗各种病症，包括心律失常和2型糖尿病。

    Furanopyrimidine compounds as potassium ion channel inhibitors
    2.
    发明授权
    Furanopyrimidine compounds as potassium ion channel inhibitors 失效
    呋喃并嘧啶化合物作为钾离子通道抑制剂

    公开(公告)号：US07456187B2

    公开(公告)日：2008-11-25

    申请号：US11148991

    申请日：2005-06-10

    申请人： John Ford ,  Nicholas John Palmer ,  John Frederick Atherall ,  David John Madge

    发明人： John Ford ,  Nicholas John Palmer ,  John Frederick Atherall ,  David John Madge

    IPC分类号： C07D491/048 ,  A61K31/519 ,  A61P9/06

    CPC分类号： C07D491/04

    摘要： A compound of formula (I) wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, —CO2R7, CONR4R5 or halo; R3 is H, NR4R5, NC(O)R8, halo, trifluoromethyl, alkyl, nitrile or alkoxy; R4 and R5 may be the same or different, and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R4 and R5 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; X is O, S or NR6; R6 is H or alkyl; R7 is hydrogen, methyl or ethyl; R8 is methyl or ethyl; L is (CH2)n, where n is 1, 2 or 3; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; together with pharmaceutically acceptable salts thereof. The use of these compounds as potassium channel inhibitors is also described.

    摘要翻译： 式（I）化合物，其中R 1是芳基，杂芳基，环烷基或烷基; R 2是H，烷基，硝基，-CO 2 R 7，CONR 4 R 5 /或卤素; R 3是H，NR 4 R 5，NC（O）R 8，卤素，三氟甲基，烷基 ，腈或烷氧基; R 4和R 5可以相同或不同，并且可以是H，烷基，芳基，杂芳基或环烷基; 或R 4和R 5可以一起形成饱和的，不饱和的或部分饱和的4至7元环，其中所述环可以任选地包含一个或多个其它选自N ，O或S; X是O，S或NR 6; R 6是H或烷基; R 7是氢，甲基或乙基; R 8是甲基或乙基; L是（CH 2 CH 2）n N，其中n是1,2或3; Y为芳基，杂环基，烷基，链烯基或环烷基; 以及其药学上可接受的盐。 还描述了这些化合物作为钾通道抑制剂的用途。

    Thieno[2 3-b]pyridines as potassium channel inhibitors
    3.
    发明授权
    Thieno[2 3-b]pyridines as potassium channel inhibitors 有权
    噻吩并[2,3-b]吡啶作为钾通道抑制剂

    公开(公告)号：US08193215B2

    公开(公告)日：2012-06-05

    申请号：US12543151

    申请日：2009-08-18

    申请人： John Ford ,  Nicholas John Palmer ,  John Frederick Atherall ,  David John Madge ,  Derek John

    发明人： John Ford ,  Nicholas John Palmer ,  John Frederick Atherall ,  David John Madge ,  Derek John

    IPC分类号： A01N43/42

    CPC分类号： C07D495/04 ,  C07D333/36 ,  C07D333/38 ,  C07D409/12

    摘要： The invention provides compounds of the formula: wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, CO2R7, CONR5R6 or halo; R3 and R4 are H, NR5R6, NC(O)R7, halo, trifluromethyl, alkyl, CONR5R6, CO2R7, nitrile or alkoxy; R5 and R6 may be the same or different and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R5 and R6 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; R7 is H or alkyl; A is H, halo, or a group of formula X-L-Y; X is O, S or NR8; R8 is H or alkyl; L is (CH2)n, where n is 0, 1, 2, 3 or 4; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; the products of mono- and di-oxidation of sulphur and/or mono-oxidation of nitrogen moieties in compounds of formula I; or a pharmaceutically acceptable salt thereof. These compounds find use as inhibitors of potassium ion channels and thus are useful in the treatment of various conditions including arrhythmia and type-2 diabetes mellitus.

    摘要翻译： 本发明提供下式的化合物：其中R1是芳基，杂芳基，环烷基或烷基; R2是H，烷基，硝基，CO 2 R 7，CONR 5 R 6或卤素; R3和R4是H，NR5R6，NC（O）R7，卤素，三氟甲基，烷基，CONR5R6，CO2R7，腈或烷氧基; R5和R6可以相同或不同，可以是H，烷基，芳基，杂芳基或环烷基; 或R 5和R 6可以一起形成饱和的，不饱和的或部分饱和的4至7元环，其中所述环可任选地包含一个或多个选自N，O或S的其它杂原子; R7是H或烷基; A是H，卤素或式X-L-Y基团; X是O，S或NR8; R8是H或烷基; L是（CH 2）n，其中n是0,1,2,3或4; Y为芳基，杂环基，烷基，链烯基或环烷基; 式I化合物中硫的单和二氧化和/或氮部分的单氧化的产物; 或其药学上可接受的盐。 这些化合物可用作钾离子通道的抑制剂，因此可用于治疗各种病症，包括心律失常和2型糖尿病。