USES OF C15-SUBSTITUTED ANDROGRAPHOLIDE DERIVATIVES IN THE PREPARATION OF ANTI-HEPATITIS B VIRUS MEDICAMENT
    3.
    发明申请
    USES OF C15-SUBSTITUTED ANDROGRAPHOLIDE DERIVATIVES IN THE PREPARATION OF ANTI-HEPATITIS B VIRUS MEDICAMENT 审中-公开
    在制备抗乙型肝炎病毒药物中使用C15取代的吡咯烷衍生物

    公开(公告)号:US20140187627A1

    公开(公告)日:2014-07-03

    申请号:US14130695

    申请日:2012-07-03

    IPC分类号: C07D307/33 A61K31/365

    CPC分类号: C07D307/33 A61K31/365

    摘要: Disclosed is a use of C15-substituted andrographolide derivatives in preparation of anti-hepatitis B virus medicaments. In the present invention, the HepG2.2.15 cells are used to measure the amount of the hepatitis B virus surface antigen (HBsAg) secretion in the supernatant of the culture; the duck hepatitis B virus (DHBV) is used to infect the model and the DHBV-DNA level in serum is measured, and the pathological change in hepatic tissue is observed. A number of andrographolide derivative compounds are screened, compounds having a good anti-HBV effect are preferred, which has a structure represented by general formula 1 set forth herein. Due to high anti-HBV activity and low toxicity, as well as good protection against hepatic injury, the compounds can be used as the active ingredient for preparing anti-HBV medicaments, thereby providing a new pharmaceutical way for treatment of hepatitis, and broadening the range of clinical medicines.

    摘要翻译: 披露了C15-取代的穿心莲内酯衍生物在制备抗乙型肝炎病毒药物中的用途。 在本发明中,HepG2.2.15细胞用于测定培养物上清液中乙型肝炎病毒表面抗原(HBsAg)分泌量; 使用鸭乙型肝炎病毒(DHBV)感染模型,测定血清中的DHBV-DNA水平,观察肝组织病理变化。 筛选多种穿心莲内酯衍生物化合物,优选具有良好抗HBV作用的化合物,其具有由本文所述的通式1表示的结构。 由于抗HBV活性高,毒性低,对肝损伤有良好的保护作用,可用作制备抗HBV药物的有效成分,从而为治疗肝炎提供新的药物治疗方法, 临床药物范围。