首页> 外国专利> Heterocyclic Amide Derivatives Which Possess Glycogen Phosphorylase Inhibitory Activity

Heterocyclic Amide Derivatives Which Possess Glycogen Phosphorylase Inhibitory Activity

机译:具有糖原磷酸化酶抑制活性的杂环酰胺衍生物

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.;
机译:式(1)的化合物或其药学上可接受的盐或前药;其中,例如Z为CH或氮,R 4 和R 5 共同为-SC(R 6 )═C (R7)-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为亚苯基或亚杂芳基; n为0、1或2; r是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 < Sup> 3 ,-(1-4C)烷基[可选取代]-(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,因此在与糖原磷酸化酶活性增加相关的疾病状态的治疗中具有价值。描述了制备化合物的方法和包含它们的药物组合物。

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