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    • 11. 发明授权
    • Thieno[2,3-B] pyridines as potassium channel inhibitors
    • 噻吩并[2,3-B]吡啶作为钾通道抑制剂
    • US07576212B2
    • 2009-08-18
    • US11297330
    • 2005-12-09
    • John FordNicholas John PalmerJohn Frederick AtherallDavid John MadgeDerek John
    • John FordNicholas John PalmerJohn Frederick AtherallDavid John MadgeDerek John
    • C07D513/02
    • C07D495/04C07D333/36C07D333/38C07D409/12
    • 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.
    • 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。
    • 12. 发明授权
    • Furanopyrimidine compounds as potassium ion channel inhibitors
    • 呋喃并嘧啶化合物作为钾离子通道抑制剂
    • US07456187B2
    • 2008-11-25
    • US11148991
    • 2005-06-10
    • John FordNicholas John PalmerJohn Frederick AtherallDavid John Madge
    • John FordNicholas John PalmerJohn Frederick AtherallDavid John Madge
    • C07D491/048A61K31/519A61P9/06
    • C07D491/04
    • 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.
    • 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。
    • 14. 发明授权
    • Thieno[2 3-b]pyridines as potassium channel inhibitors
    • 噻吩并[2,3-b]吡啶作为钾通道抑制剂
    • US08193215B2
    • 2012-06-05
    • US12543151
    • 2009-08-18
    • John FordNicholas John PalmerJohn Frederick AtherallDavid John MadgeDerek John
    • John FordNicholas John PalmerJohn Frederick AtherallDavid John MadgeDerek John
    • A01N43/42
    • C07D495/04C07D333/36C07D333/38C07D409/12
    • 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.
    • 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。