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    Thieno[2,3-b]pyridines as Potassium Channel Inhibitors
    1.
    发明申请
    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：US20100041695A1

    公开(公告)日：2010-02-18

    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： A61K31/4436 ,  A61P9/06 ,  A61P19/02 ,  A61P29/00 ,  A61P1/00 ,  A61P3/10

    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, trifluoromethyl, 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。

    Thieno[3,2-c]pyridine potassium channel inhibitors
    2.
    发明授权
    Thieno[3,2-c]pyridine potassium channel inhibitors 有权
    噻吩并[3,2-c]吡啶钾通道抑制剂

    公开(公告)号：US09216992B2

    公开(公告)日：2015-12-22

    申请号：US11635786

    申请日：2006-12-08

    申请人： John Ford ,  David John Madge ,  Helen Jane Payne ,  Jamie David Knight

    发明人： John Ford ,  David John Madge ,  Helen Jane Payne ,  Jamie David Knight

    IPC分类号： C07D495/04 ,  A61K31/4365

    CPC分类号： C07D495/04

    摘要： The present invention provides thienopyridine compounds which are potassium channel inhibitors. In another embodiment, the invention provides pharmaceutical compositions comprising thienopyridines. In another embodiment, the invention provides methods of using thienopyridines in the treatment or prevention of cancer, arrhythmias, autoimmune diseases and inflammatory diseases, including gastric cancer, atrial fibrillation, type-2 diabetes mellitus, rheumatoid arthritis, type-1 diabetes, inflammatory bowel disorder and demyelinating disorders such as multiple sclerosis.

    摘要翻译： 本发明提供作为钾通道抑制剂的噻吩并吡啶化合物。 在另一个实施方案中，本发明提供了包含噻吩并吡啶的药物组合物。 在另一个实施方案中，本发明提供了使用噻吩并吡啶治疗或预防癌症，心律失常，自身免疫性疾病和炎性疾病的方法，包括胃癌，心房颤动，2型糖尿病，类风湿性关节炎，1型糖尿病，炎性肠 紊乱和脱髓鞘疾病如多发性硬化。

    Thieno[2,3-B] pyridines as potassium channel inhibitors
    3.
    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
    4.
    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
    5.
    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。