PYRIDONE DERIVATIVE, COMPOSITION THEREOF AND APPLICATION THEREOF AS ANTI-INFLUENZA DRUG
申请人:Jiangxi Caishi Pharmaceutical Technology Co., Ltd.
公开号:EP3753936A1
公开(公告)日:2020-12-23
The present disclosure belongs to the field of medicinal chemistry, and relates to a novel pyridone derivative represented by Formula (I) or a stereoisomer, a pharmaceutically acceptable salt, a solvate or a crystal thereof, and use thereof in the preparation of a drug for preventing or treating diseases such as influenza type A viral infection and/or influenza type B viral infection, particularly use thereof as a PA subunit cap-dependent endonuclease inhibitor for preventing or treating diseases such as influenza type A viral infection and/or influenza type B viral infection. The compounds of the present disclosure have significant activity in inhibiting influenza endonuclease and influenza DNA, can be used either alone or in combination with a neuraminidase inhibitor, a nucleoside drug, a PB2 inhibitor, a PB1 inhibitor, an M2 inhibitor or other anti-influenza drugs, significantly shorten the time of influenza infection and reduces mortality, and have excellent clinical application prospects.
本公开属于药物化学领域,涉及一种由式(I)或其立体异构体代表的新型吡啶酮衍生物、其药学上可接受的盐、溶液或晶体,及其在制备预防或治疗甲型流感病毒感染和/或乙型流感病毒感染等疾病的药物中的用途,特别是其作为预防或治疗甲型流感病毒感染和/或乙型流感病毒感染等疾病的PA亚基帽依赖性内切酶抑制剂的用途。本公开的化合物在抑制流感内切酶和流感DNA方面具有显著活性,可单独使用,也可与神经氨酸酶抑制剂、核苷类药物、PB2抑制剂、PB1抑制剂、M2抑制剂或其他抗流感药物联合使用,可显著缩短流感感染时间,降低死亡率,具有良好的临床应用前景。