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    Heterocyclic amide derivatives as inhibitors of glycogen phosphorylase
    1.
    发明授权
    Heterocyclic amide derivatives as inhibitors of glycogen phosphorylase 失效
    杂环酰胺衍生物作为糖原磷酸化酶的抑制剂

    公开(公告)号：US07276517B2

    公开(公告)日：2007-10-02

    申请号：US11463144

    申请日：2006-08-08

    申请人： Alan Martin Birch ,  Andrew David Morley ,  Andrew Stocker ,  Paul Robert Owen Whittamore

    发明人： Alan Martin Birch ,  Andrew David Morley ,  Andrew Stocker ,  Paul Robert Owen Whittamore

    IPC分类号： A61K31/4375 ,  C07D471/04

    CPC分类号： C07D495/04

    摘要： Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof, possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.

    摘要翻译： 式（1）的杂环酰胺其中：X是N或CH; R 4和R 5一起是-SC（R 6）-C（R 7） - 或 -C（R 7）C（R 6）-S-; R 6和R 7独立地选自，例如氢，卤素和C 1-4烷基; A是亚苯基或亚杂芳基; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代） 组）; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10） ），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR 9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前药具有糖原磷酸化酶抑制活性，因此在治疗与增加的糖原磷酸化酶活性相关的疾病状态方面具有价值。 描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。

    Heterocyclic amide derivatives as inhibitors of glycogen phoshorylase
    2.
    发明授权
    Heterocyclic amide derivatives as inhibitors of glycogen phoshorylase 失效
    杂环酰胺衍生物作为糖原磷酸化酶的抑制剂

    公开(公告)号：US07129249B2

    公开(公告)日：2006-10-31

    申请号：US10506741

    申请日：2003-03-04

    申请人： Alan Martin Birch ,  Andrew David Morley ,  Andrew Stocker ,  Paul Robert Owen Whittamore

    发明人： Alan Martin Birch ,  Andrew David Morley ,  Andrew Stocker ,  Paul Robert Owen Whittamore

    IPC分类号： A61K31/4704 ,  A61K31/4375 ,  C07D215/38 ,  C07D471/04

    CPC分类号： C07D495/04

    摘要： Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.

    摘要翻译： 式（1）的杂环酰胺其中：X是N或CH; R 4和R 5一起是-SC（R 6）-C（R 7） - 或 -C（R 7）C（R 6）-S-; R 6和R 7独立地选自，例如氢，卤素和C 1-4烷基; A是亚苯基或亚杂芳基; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代） 组）; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10） ），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR 9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前体药物; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。 描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。

    Heterocyclic Amide Derivatives Which Possess Glycogen Phosphorylase Inhibitory Activity
    3.
    发明申请
    Heterocyclic Amide Derivatives Which Possess Glycogen Phosphorylase Inhibitory Activity 审中-公开
    具有糖原磷酸化酶抑制活性的杂环酰胺衍生物

    公开(公告)号：US20080064691A1

    公开(公告)日：2008-03-13

    申请号：US10566063

    申请日：2004-08-04

    申请人： Alan Martin Birch ,  Stuart Norman Lile Bennett ,  Andrew Duncan Campbell ,  Iain Simpson ,  Paul Robert Owen Whittamore ,  David Paul Whalley ,  Linda Godfrey

    发明人： Alan Martin Birch ,  Stuart Norman Lile Bennett ,  Andrew Duncan Campbell ,  Iain Simpson ,  Paul Robert Owen Whittamore ,  David Paul Whalley ,  Linda Godfrey

    IPC分类号： A61K31/407 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/5377 ,  A61K31/541 ,  A61P3/00 ,  C07D495/04

    CPC分类号： C07D495/04

    摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; wherein, for example, Z is CH or nitrogen, R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from hydrogen, halo, nitro, cyano, hydroxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoromethoxy, carboxy and carbamoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; r is 1 or 2; R1 is halo, cyano or carboxy; Y is selected from —C(O)R2, —C(O)OR2, —C(O)NR2R3, -(1-4C)alkyl [optionally substituted] -(2-4C)alkenyl, —SO2NR2R3, and —S(O)cR2 (wherein c is 0, 1 or 2); R2 and R3 are independently selected from hydrogen, —O(1-4C)alkyl, —S(1-4C)alkyl, —N(1-4C)alkyl, heterocyclyl, aryl, and (1-4C)alkyl [optionally substituted]; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.

    摘要翻译： 式（1）的化合物或其药学上可接受的盐或其前体药物; 其中，例如，Z是CH或氮，R 4和R 5一起是-SC（R 6）-C（R 7） ） - 或-C（R 7）C（R 6）-S-; R 6和R 7独立地选自氢，卤素，硝基，氰基，羟基，氟甲基，二氟甲基，三氟甲基，三氟甲氧基，羧基和氨基甲酰基; A是亚苯基或亚杂芳基; n为0,1或2; r为1或2; R 1是卤素，氰基或羧基; 其中Y选自-C（O）R 2，-C（O）OR 2，-C（O）NR 2 R 2， （1-4C）烷基[任选取代的] - （2-4C）烯基，-SO 2 NR 2 R 3和-S（O）C R 2（其中c是0,1或2）; R 2和R 3独立地选自氢，-O（1-4C）烷基，-S（1-4C）烷基，-N（1-4C） 烷基，杂环基，芳基和（1-4C）烷基[任选取代的]; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。 描述了制备含有它们的化合物和药物组合物的方法。