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    • 10. 发明公开
    • 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
    • 新型吡啶衍生物,其制备方法和含有它们的药物组合物
    • KR1020060110764A
    • 2006-10-25
    • KR1020060032449
    • 2006-04-10
    • 에스케이케미칼주식회사
    • 김형욱류제호정재윤이남규김주현김은정전선덕김지홍이해인조용백곽의종
    • C07D471/04C07D491/04
    • C07D471/04C07D491/04
    • Novel pyridine derivatives and pharmaceutical compositions containing the same compounds are provided to inhibit production of inflammation response-related cytokines, particularly TNF-alpha(tumor necrosis factor-alpha), IL-1alpha(interleukin-1alpha), IL-6, INF-gamma(interferon-gamma) and PGE2(prostaglandin E2), so that they are useful for treating inflammation disease and alleviating pain. The pyridine derivatives represented by the formula(1) or pharmaceutically acceptable salts thereof are provided, wherein R1, R2, R3, R4 and R5 are each independently hydrogen, halo, cyano, nitro, acyl, hydroxyl, amino, C1-C6 lower alkyl, C2-C6 lower alkenyl, C1-C6 lower alkoxy, C1-C6 alkylthio, C1-C10 alkylamino, C4-C9 cycloalkylamino, C4-C9 heterocycloalkylamino, arylamino, acylamino, acyloxy, C1-C6 alkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 alkylsulfonylamino, arylsulfinyl, arylsulfonyl, arylsulfonylamino, aryl, heteroaryl, C1-C10 aralkyl, C1-C10 heteroaralkyl, aryloxy or heteroaryloxy; X is oxygen or sulfur; and Y is oxygen or N-R6; R6 is hydrogen, C1-C6 lower alkyl, acyl, aryl, heteroaryl, C1-C10 aralkyl or C1-C10 heteroaralkyl.
    • 提供新的吡啶衍生物和含有相同化合物的药物组合物以抑制炎症反应相关细胞因子,特别是TNF-α(肿瘤坏死因子-α),IL-1α(白细胞介素-1α),IL-6,INF-γ (干扰素-γ)和PGE2(前列腺素E2),因此它们可用于治疗炎症疾病和缓解疼痛。 提供由式(1)表示的吡啶衍生物或其药学上可接受的盐,其中R1,R2,R3,R4和R5各自独立地为氢,卤素,氰基,硝基,酰基,羟基,氨基,C1-C6低级烷基 ,C 2 -C 6低级烯基,C 1 -C 6低级烷氧基,C 1 -C 6烷硫基,C 1 -C 10烷基氨基,C 4 -C 9环烷基氨基,C 4 -C 9杂环烷基氨基,芳基氨基,酰氨基,酰氧基,C 1 -C 6烷基亚磺酰基, C 6烷基磺酰基氨基,芳基亚磺酰基,芳基磺酰基,芳基磺酰基氨基,芳基,杂芳基,C 1 -C 10芳烷基,C 1 -C 10杂芳烷基,芳氧基或杂芳氧基; X是氧或硫; Y为氧或N-R6; R6是氢,C1-C6低级烷基,酰基,芳基,杂芳基,C1-C10芳烷基或C1-C10杂芳烷基。