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31. 发明申请

WO2005019172A1 INDOL-2-AMIDES AS GLYCOGEN PHOSPHORYLASE INHIBITORS 审中-公开
标题翻译：吲哚-2-酰胺作为GLYCOGEN磷酸酶抑制剂
公开(公告)号：WO2005019172A1
公开(公告)日：2005-03-03
申请号：PCT/GB2004/003552
申请日：2004-08-18
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BENNETT, Stuart, Norman, Lile , SIMPSON, Iain , WHITTAMORE, Paul, Robert, Owen
发明人： BENNETT, Stuart, Norman, Lile , SIMPSON, Iain , WHITTAMORE, Paul, Robert, Owen
IPC分类号： C07D209/42
CPC分类号： C07D405/12 , C07D209/42
摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; (1) wherein, for example, R 4 is halo or (1-4C)alkyl ; A is phenylene or heteroarylene; n is 0, 1 or 2; m is 0, 1 or 2; R 1 is halo, cyano or carboxy; R 2 is for example methyl; R 3 is for example selected from halo(1-4C)alkyl, dihalo(1-4C)alkyl, trifluoromethyl, hydroxy(1-4C)alkyl, dihydroxy(2-4C)alkyl, trihydroxy(3-4C)alkyl, cyano(1-4C)alkyl (optionally substituted on alkyl with hydroxy), (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkoxy(1-4C)alkyl, di[(1-4C)alkoxy](1-4C)alkyl, (hydroxy)[(1-4C)alkoxy](1-4C)alkyl; 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; （1）其中，例如，R 4为卤素或（1-4C）烷基; A是亚苯基或亚杂芳基; n为0,1或2; m为0,1或2; R 1是卤素，氰基或羧基; R 2例如是甲基; R 3例如选自卤素（1-4C）烷基，二卤代（1-4C）烷基，三氟甲基，羟基（1-4C）烷基，二羟基（2-4C）烷基，三羟基（3-4C）烷基，（1-4C）烷基（任选在羟基烷基上取代），（1-4C）烷氧基（1-4C）烷基，（1-4C）烷氧基（1-4C）烷氧基（1-4C）烷基，二（1-4C）烷氧基]（1-4C）烷基，（羟基）[（1-4C）烷氧基]（1-4C）烷基; 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。

32. 发明申请

WO2005013981A1 HETEROCYCLIC AMIDE DERIVATIVES WHICH POSSESS GLYCOGEN PHOSPHORYLASE INHIBITORY ACTIVITY 审中-公开
标题翻译：杂环化合物酰胺衍生物，其具有磷酸酶抑制活性
公开(公告)号：WO2005013981A1
公开(公告)日：2005-02-17
申请号：PCT/GB2004/003345
申请日：2004-08-04
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BIRCH, Alan, Martin , BENNETT, Stuart, Norman, Lile , CAMPBELL, Andrew, Duncan , SIMPSON, Iain , WHITTAMORE, Paul, Robert, Owen , WHALLEY, David, Paul , GODFREY, Linda
发明人： BIRCH, Alan, Martin , BENNETT, Stuart, Norman, Lile , CAMPBELL, Andrew, Duncan , SIMPSON, Iain , WHITTAMORE, Paul, Robert, Owen , WHALLEY, David, Paul , GODFREY, Linda
IPC分类号： A61K31/407
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, R 4 and R 5 together are either -S-C(R 6 )=C(R7)- or -C(R 7 )=C(R 6 )-S- ; R 6 and R 7 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; R 1 is halo, cyano or carboxy; Y is selected from -C(O)R 2 , -C(O)OR 2 , -C(O)NR 2 R 3 , -(1-4C)alkyl [optionally substituted] -(2-4C)alkenyl, -SO 2 NR 2 R 3 , and -S(O) c R 2 (wherein c is 0, 1 or 2); R 2 and R 3 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-; 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; R 6和R 7独立地选自氢，卤素，硝基，氰基，羟基， 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; Y选自-C（O）R 2，-C（O）OR 2，-C（O）NR 2 R 3， - （1-4C）烷基[任意取代的] （2-4C）烯基，-SO 2 NR 2 R 3和-S（O）c R 2（其中c为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。

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