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    Uses of 15-benzylidene-14-deoxy-11,12-didehydroandrographolide derivatives in the preparation of antineoplastic drugs
    3.
    发明授权
    Uses of 15-benzylidene-14-deoxy-11,12-didehydroandrographolide derivatives in the preparation of antineoplastic drugs 有权
    使用15-亚苄基-14-脱氧-11,12-脱氢穿心莲内酯衍生物制备抗肿瘤药物

    公开(公告)号：US09198894B2

    公开(公告)日：2015-12-01

    申请号：US13823841

    申请日：2011-10-19

    申请人： Fengjuan Wu ,  Guifu Dai ,  Haiwei Xu ,  Zhiwen Jiang ,  Liping Zhu ,  Lijun Yan ,  Hongmin Liu ,  Yanan Wang ,  Weiyi Li ,  Ruijing Dong

    发明人： Fengjuan Wu ,  Guifu Dai ,  Haiwei Xu ,  Zhiwen Jiang ,  Liping Zhu ,  Lijun Yan ,  Hongmin Liu ,  Yanan Wang ,  Weiyi Li ,  Ruijing Dong

    IPC分类号： A61K31/365 ,  C07D307/33 ,  A61K31/341 ,  A61K45/06

    CPC分类号： A61K31/341 ,  A61K31/365 ,  A61K45/06 ,  C07D307/33

    摘要： The present invention relates to the preparation of anti-tumor drugs with andrographolide derivatives, which belongs to the field of pharmaceutical technology, and involves 15-benzylidene substituted derivatives of 14-deoxy-11,12-didehydro-andrographolide and their 3,19-ester derivatives. Proved by the experiments, these compounds significantly inhibited the colony formation and migration ability of various cancer cells, and also inhibited the migration ability of vascular endothelial cells in vitro. The compounds of this invention significantly inhibited the tumor growth, invasion, metastasis and angiogenesis on mouse xenograft models, and inhibited the experimental lung metastasis of B16-F10 malignant melanoma cells. Therefore, this class of compounds could be used as the active ingredients for the preparation of antineoplastic drugs, which are of efficiency and low-toxicity. Thereby it has potential to expand the selectable range of clinical drug and is of high significance to make full use of the plant resources of Andrographis paniculata.

    摘要翻译： 本发明涉及具有穿心莲内酯衍生物的抗肿瘤药物的制备，属于制药领域，涉及14-脱氧-11,12-脱氢穿心莲内酯的15-亚苄基取代衍生物及其3,19- 酯衍生物。 通过实验证明，这些化合物显着抑制了各种癌细胞的集落形成和迁移能力，并且还抑制了体外血管内皮细胞的迁移能力。 本发明化合物显着抑制小鼠异种移植模型的肿瘤生长，侵袭，转移和血管生成，并抑制B16-F10恶性黑素瘤细胞的实验性肺转移。 因此，这类化合物可用作制备有效和低毒的抗肿瘤药物的活性成分。 因此，有可能扩大临床药物的可选范围，对充分利用穿心莲的植物资源具有重要意义。

    USES OF C15-SUBSTITUTED ANDROGRAPHOLIDE DERIVATIVES IN THE PREPARATION OF ANTI-HEPATITIS B VIRUS MEDICAMENT
    4.
    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

    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。

    Uses of 15-benzylidene-14-deoxy-11,12-didehydroandrographolide Derivatives in the Preparation of Antineoplastic Drugs
    5.
    发明申请
    Uses of 15-benzylidene-14-deoxy-11,12-didehydroandrographolide Derivatives in the Preparation of Antineoplastic Drugs 有权
    15-亚苄基-14-脱氧-11,12-脱氢穿心莲内酯衍生物在制备抗肿瘤药物中的用途

    公开(公告)号：US20130237596A1

    公开(公告)日：2013-09-12

    申请号：US13823841

    申请日：2011-10-19

    申请人： Guifu Dai ,  Haiwei Xu ,  Liping Zhu ,  Ruijing Dong ,  Fengjuan Wu ,  Yanan Wang ,  Zhiwen Jiang ,  Lijun Yan ,  Weiyi Li ,  Hongmin Liu

    发明人： Guifu Dai ,  Haiwei Xu ,  Liping Zhu ,  Ruijing Dong ,  Fengjuan Wu ,  Yanan Wang ,  Zhiwen Jiang ,  Lijun Yan ,  Weiyi Li ,  Hongmin Liu

    IPC分类号： A61K31/341 ,  A61K45/06 ,  C07D307/33

    CPC分类号： A61K31/341 ,  A61K31/365 ,  A61K45/06 ,  C07D307/33

    摘要： The present invention relates to the preparation of anti-tumor drugs with andrographolide derivatives, which belongs to the field of pharmaceutical technology, and involves 15-benzylidene substituted derivatives of 14-deoxy-11,12-didehydro-andrographolide and their 3,19-ester derivatives. Proved by the experiments, these compounds significantly inhibited the colony formation and migration ability of various cancer cells, and also inhibited the migration ability of vascular endothelial cells in vitro. The compounds of this invention significantly inhibited the tumor growth, invasion, metastasis and angiogenesis on mouse xenograft models, and inhibited the experimental lung metastasis of B16-F10 malignant melanoma cells. Therefore, this class of compounds could be used as the active ingredients for the preparation of antineoplastic drugs, which are of efficiency and low-toxicity. Thereby it has potential to expand the selectable range of clinical drug and is of high significance to make full use of the plant resources of Andrographis paniculata.

    摘要翻译： 本发明涉及具有穿心莲内酯衍生物的抗肿瘤药物的制备，属于制药领域，涉及14-脱氧-11,12-脱氢穿心莲内酯的15-亚苄基取代衍生物及其3,19- 酯衍生物。 通过实验证明，这些化合物显着抑制了各种癌细胞的集落形成和迁移能力，并且还抑制了体外血管内皮细胞的迁移能力。 本发明化合物显着抑制小鼠异种移植模型的肿瘤生长，侵袭，转移和血管生成，并抑制B16-F10恶性黑素瘤细胞的实验性肺转移。 因此，这类化合物可用作制备有效和低毒的抗肿瘤药物的活性成分。 因此，有可能扩大临床药物的可选范围，对充分利用穿心莲的植物资源具有重要意义。