DRUG WITH ANTIVIRAL ACTIVITY (VARIANTS)
    10.
    发明公开
    DRUG WITH ANTIVIRAL ACTIVITY (VARIANTS) 审中-公开
    具有抗病毒活性的药物(变体)

    公开(公告)号:EP3315501A1

    公开(公告)日:2018-05-02

    申请号:EP16773558.8

    申请日:2016-04-06

    摘要: The invention relates to the field of organic chemistry and medicine, and more particularly to synthetic substances of the pyrimidine series, namely 2-chloro-5-phenyl-5 H- pyrimido[5',4':5,6]pyrano[2,3-d]pyrimidine-4-ol derivatives, having antiviral activity. Claimed are a drug with antiviral activity against HIV infection and hepatitis B virus, containing 2-chloro-5-phenyl-5H-pyrimido[5',4':5,6]pyrano[2,3-d]pyrimidine-4-ol derivatives of the general formula shown, where: X is selected from the group: H, NO 2 , Hal, OMe; R1 is selected from the group: Cl, OH; and R2 is selected from the group: Cl, SH, OH; and a drug with antiviral activity against HIV infection, containing a 2-chloro-5-phenyl-5H-pyrimido[5',4':5,6]pyrano[2,3-d]pyrimidine-4-ol derivative of the general formula shown, where: X is selected from the group: H, NO 2 , Hal, OMe; R1 is selected from the group: Cl, OH; and R2 is selected from the group: Cl, SH, OH in combination with a reverse transcriptase inhibitor selected from Retrovir, or in combination with a protease inhibitor selected from Lopinavir, in an effective amount. The result is an effective drug with antiviral activity.

    摘要翻译: 本发明涉及有机化学和医药领域,更具体地涉及嘧啶系列的合成物质,即2-氯-5-苯基-5H-嘧啶并[5',4':5,6]吡喃并[2,1- 3-d]嘧啶-4-醇衍生物,具有抗病毒活性。 声称含有2-氯-5-苯基-5H-嘧啶并[5',4':5,6]吡喃并[2,3-d]嘧啶-4-酮的抗HIV感染和乙型肝炎病毒的抗病毒活性的药物, 其中:X选自:H,NO 2,Hal,OMe; R1选自:Cl,OH; 并且R2选自:Cl,SH,OH; 和一种具有抗HIV感染的抗病毒活性的药物,该药物含有2-氯-5-苯基-5H-嘧啶并[5',4':5,6]吡喃并[2,3-d]嘧啶-4-醇衍生物 所示通式表示,其中:X选自:H,NO 2,Hal,OMe; R1选自:Cl,OH; R2选自:Cl,SH,OH与选自Retrovir的逆转录酶抑制剂或与选自洛匹那韦的蛋白酶抑制剂组合的有效量的组合。 其结果是具有抗病毒活性的有效药物。