公开(公告)号：US20140187627A1

公开(公告)日：2014-07-03

申请号：US14130695

申请日：2012-07-03

申请人： Guifu DAI ,  Haiwei XU ,  Zhiwen JIANG ,  Hongmin LIU ,  Yanan WANG ,  Kuicheng ZHU ,  Zhenwei WU ,  Weiyi LI ,  Fengjuan WU ,  Mengjiao LIU ,  Wei HAN

发明人： Guifu DAI ,  Haiwei XU ,  Zhiwen JIANG ,  Hongmin LIU ,  Yanan WANG ,  Kuicheng ZHU ,  Zhenwei WU ,  Weiyi LI ,  Fengjuan WU ,  Mengjiao LIU ,  Wei HAN

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。