公开(公告)号：EP2361625A1

公开(公告)日：2011-08-31

申请号：EP10195408.9

申请日：2005-09-19

申请人： Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences

发明人： Jiang, Jian-Dong ,  Kong, Wei-Jia ,  Zhao, Li-Xun ,  Song, Dan-Qing ,  Wei, Jing

IPC分类号： A61K31/4375 ,  A61K31/4725 ,  A61P3/06 ,  A61P9/10

CPC分类号： A61K31/4375

摘要： Methods and compositions containing a berberine compound or berberine related or derivative compound are provided for the prevention and treatment of hyperlipidemia, elevated cholesterol, and/or cardiovascular disease in mammalian subjects. The methods and compositions of the invention are effective for prevention and treatment of atherosclerosis, coronary artery disease, angina pectoris, carotid artery disease, stroke, cerebral arteriosclerosis, high blood pressure, myocardial infarction, cerebral infarction, restenosis following balloon angioplasty, intermittent claudication, dyslipidemia post-prandial lipidemia or xanthoma. Additional compositions and methods are provided which employ a berberine compound or berberine related or derivative compound in combination with a second anti-hyperlipidemia agent, or a different therapeutic agent to yield more effective treatment tools against hyperlipidemia and/or cardiovascular disease, and/or dual activity therapeutic methods and formulations useful to prevent or reduce hyperlipidemia and one or more causal or related symptoms or conditions associated with hyperlipidemia in mammalian subjects.

摘要翻译： 提供含有小檗碱化合物或小檗碱相关或衍生化合物的方法和组合物用于预防和治疗哺乳动物受试者中的高脂血症，升高的胆固醇和/或心血管疾病。 本发明的方法和组合物可有效预防和治疗动脉粥样硬化，冠状动脉疾病，心绞痛，颈动脉疾病，中风，脑动脉硬化，高血压，心肌梗塞，脑梗死，球囊血管成形术后的再狭窄，间歇性跛行， 餐后血脂异常或血清白血病。 提供了另外的组合物和方法，其使用小檗碱化合物或小檗碱相关或衍生化合物与第二抗高脂血症药物或不同治疗剂组合以产生更有效的治疗工具来抵抗高脂血症和/或心血管疾病，和/或双重 用于预防或减少哺乳动物受试者中与高脂血症相关的高脂血症和一种或多种因果或相关症状或状况的活性治疗方法和制剂。

公开(公告)号：EP3556769B1

公开(公告)日：2023-06-14

申请号：EP17880389.6

申请日：2017-12-15

发明人： CUI, Along ,  LI, Zhuorong ,  JIN, Jie ,  GAO, Yan ,  HU, Xinxin ,  YOU, Xuefu ,  CHEN, Yang ,  HE, Qiyang

IPC分类号： C07K7/62 ,  A61K38/12 ,  A61P31/04 ,  A61K38/00

公开(公告)号：EP2796442B1

公开(公告)日：2019-03-27

申请号：EP12859858.8

申请日：2012-12-18

申请人： Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences

发明人： LI, Zhuorong ,  JI, Xingyue ,  XUE, Situ ,  ZHENG, Guanghui ,  LI, Yuhuan ,  TAO, Peizhen ,  JIANG, Jiandong

IPC分类号： C07C65/03 ,  C07C65/05 ,  C07C65/28 ,  C07C69/78 ,  C07C69/88 ,  C07C69/92 ,  C07C51/09 ,  C07C67/14 ,  C07C67/16 ,  A61K31/192 ,  A61P3/06 ,  A61P3/10 ,  A61P3/14 ,  A61P25/28 ,  A61P25/00 ,  A61P31/04 ,  A61P31/12

公开(公告)号：EP2796442A1

公开(公告)日：2014-10-29

申请号：EP12859858.8

申请日：2012-12-18

申请人： Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences

发明人： LI, Zhuorong ,  JI, Xingyue ,  XUE, Situ ,  ZHENG, Guanghui ,  LI, Yuhuan ,  TAO, Peizhen ,  JIANG, Jiandong

IPC分类号： C07C65/03 ,  C07C65/05 ,  C07C65/28 ,  C07C69/78 ,  C07C69/88 ,  C07C69/92 ,  C07C51/09 ,  C07C67/14 ,  C07C67/16 ,  A61K31/192 ,  A61P3/06 ,  A61P3/10 ,  A61P3/14 ,  A61P25/28 ,  A61P25/00 ,  A61P31/04 ,  A61P31/12

CPC分类号： C07D213/30 ,  C07C39/21 ,  C07C41/18 ,  C07C43/215 ,  C07C43/23 ,  C07C51/09 ,  C07C51/353 ,  C07C51/36 ,  C07C65/105 ,  C07C65/19 ,  C07C65/28 ,  C07C67/30 ,  C07C69/157 ,  C07C69/36 ,  C07C69/92 ,  C07C217/20 ,  C07C217/22 ,  C07C229/08 ,  C07C231/12 ,  C07C235/46 ,  C07C235/62 ,  C07C235/64 ,  C07C275/00 ,  C07C275/54 ,  C07C279/22 ,  C07C281/02 ,  C07C2601/02 ,  C07C2601/14 ,  C07D207/16 ,  C07D211/58 ,  C07D213/55 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/69 ,  C07D213/80 ,  C07D233/60 ,  C07D233/90 ,  C07D241/04 ,  C07D311/58 ,  C07D333/16 ,  C07D333/24 ,  C07C65/24

摘要： Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.

摘要翻译： 本发明提供cajanine结构类似化合物的合成方法和药理作用物，其具有结构通式I，II，III，IV和V.因此提供了含有所述化合物作为活性成分的药物组合物作为代表的本发明的化合物中， 及其用途; 如抗病毒，抗病毒感染，神经保护，抗代谢疾病等：具有药理活性的本发明的化合物。 这样提供了一种天然产物cajanine，cajanine A的化学全合成制备方法和cajanine C.本发明奠定了所述化合物作为药物的临床在未来的深入研究和发展的基础。

公开(公告)号：EP2581376A1

公开(公告)日：2013-04-17

申请号：EP11774274.2

申请日：2011-04-29

申请人： Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences

发明人： JIANG, Jiandong ,  SONG, Danqing ,  DU, Nana ,  PENG, Zonggen ,  WANG, Yuping ,  GAO, Limei ,  HAN, Yanxing ,  LI, Xin ,  LI, Chunxin

IPC分类号： C07D471/16 ,  C07D471/22 ,  A61K31/4375 ,  A61P31/14

CPC分类号： C07D471/16 ,  C07D471/22

摘要： The present invention relates to a N-substituted matrinic acid derivative or matrine derivative, and its preparation method and uses. Specifically, the present invention relates to a compound of Formula (I) or (II) (wherein all the definitions of substituted groups are those mentioned in the specification), or a pharmaceutically acceptable salt, geometric isomer, stereoisomer, solvate, ester or prodrug thereof. The present invention further relates to a method for preparing the compound of the present invention, a pharmaceutical composition containing the compound, and uses thereof in manufacture of a medicament. The compound of the present invention can be used for prophylaxis and/or treatment of a disease or disorder associated with viral infection such as hepatitis B and/orhepatitis C and/orAIDS.

摘要翻译： N-取代的甘草酸衍生物或苦参碱衍生物及其制备方法和用途。 具体而言，本发明涉及式（I）或（II）的化合物（其中所有取代基的定义均为说明书中提及的那些），或其药学上可接受的盐，几何异构体，立体异构体，溶剂化物，酯或前药 它们。 本发明进一步涉及制备本发明化合物的方法，含有该化合物的药物组合物及其在制备药物中的用途。 本发明的化合物可以用于预防和/或治疗与病毒感染有关的疾病或病症，例如乙型和/或丙型肝炎和/或艾滋病。

公开(公告)号：EP2351731B1

公开(公告)日：2016-02-10

申请号：EP09817185.3

申请日：2009-09-28

申请人： Institute Of Medicinal Biotechnology, Chinese Academy of Medical Sciences

发明人： JIANG, Jiandong ,  YU, Liyan ,  CEN, Shan ,  LI, Zhuorong ,  LI, Yanping ,  XU, Jian

IPC分类号： C07C237/44 ,  C07C309/76 ,  C07C311/46 ,  A61K31/167 ,  A61K31/16 ,  A61P31/12 ,  C07C327/28 ,  C07D207/36 ,  C07D213/75 ,  C07D239/47 ,  C07D239/52 ,  C07D307/66 ,  C07C233/43 ,  C07C233/54 ,  C07C255/57 ,  C07C229/60

CPC分类号： C07C327/28 ,  C07C229/60 ,  C07C233/25 ,  C07C233/33 ,  C07C233/43 ,  C07C233/54 ,  C07C237/42 ,  C07C237/44 ,  C07C255/57 ,  C07C309/76 ,  C07C311/08 ,  C07C311/29 ,  C07C311/44 ,  C07C311/46 ,  C07D207/36 ,  C07D213/75 ,  C07D239/42 ,  C07D239/47 ,  C07D239/52 ,  C07D307/66

公开(公告)号：EP2351731A1

公开(公告)日：2011-08-03

申请号：EP09817185.3

申请日：2009-09-28

申请人： Institute Of Medicinal Biotechnology, Chinese Academy of Medical Sciences

发明人： JIANG, Jiandong ,  YU, Liyan ,  CEN, Shan ,  LI, Zhuorong ,  LI, Yanping ,  XU, Jian

IPC分类号： C07C237/44 ,  C07C233/12 ,  C07C229/54 ,  C07C327/16 ,  C07C307/02 ,  C07C303/26 ,  C07D239/52 ,  A61K31/21 ,  A61K31/165 ,  A61K31/255 ,  A61P31/12

CPC分类号： C07C327/28 ,  C07C229/60 ,  C07C233/25 ,  C07C233/33 ,  C07C233/43 ,  C07C233/54 ,  C07C237/42 ,  C07C237/44 ,  C07C255/57 ,  C07C309/76 ,  C07C311/08 ,  C07C311/29 ,  C07C311/44 ,  C07C311/46 ,  C07D207/36 ,  C07D213/75 ,  C07D239/42 ,  C07D239/47 ,  C07D239/52 ,  C07D307/66

摘要： A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.

摘要翻译： 一组氨基取代的苯甲酰基衍生物，其制备及其用途。 以hA3G / Vif为靶点的抗病毒药物的筛选和研究证明，3-氨基苯甲酰基衍生物不仅具有hA3G / Vif的组合活性，而且具有抑制病毒复制的功能。 本发明提供了HIV耐药性问题可能的突破性进展，从而提供了具有更高效率的新型临床抗病毒药物。

公开(公告)号：EP2253621A1

公开(公告)日：2010-11-24

申请号：EP09703551.3

申请日：2009-01-19

申请人： Institute Of Medicinal Biotechnology, Chinese Academy of Medical Sciences

发明人： LI, Zhuorong ,  PENG, Zonggen ,  LI, Yanping ,  ZHU, Jianhua ,  TAO, Peizhen ,  FAN, Bo ,  WANG, Yuping ,  SHAN, Guangzhi ,  WANG, Shuqin ,  ZHANG, Tian ,  JIANG, Jiandong

IPC分类号： C07D225/06 ,  C07H19/06 ,  C07D401/12 ,  A61K31/395 ,  A61K31/4427 ,  A61P31/12 ,  A61P35/00

CPC分类号： C07D225/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07H19/067

摘要： A set of geldanamycin derivatives and their preparation methods. Pharmaceutical compositions comprising the said compounds as an active ingredient which are used as antivirus and antitumor agents. The said derivatives are used in the manufacture of heat shock protein 90(Hsp 90) inhibiting agents which have the utility as antivirus and antitumor agents.

摘要翻译： 一组格尔德霉素衍生物及其制备方法。 药物组合物，其包含所述化合物作为活性成分，用作抗病毒剂和抗肿瘤剂。 所述衍生物用于制造具有抗病毒和抗肿瘤剂作用的热休克蛋白90（Hsp90）抑制剂。

公开(公告)号：EP4431113A1

公开(公告)日：2024-09-18

申请号：EP21963512.5

申请日：2021-11-09

申请人： Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences ,  Guangzhou HC New Drug Research Co., Ltd.

发明人： SONG, Danqing ,  JIANG, Jiandong ,  WANG, Yanxiang ,  YOU, Xuefu ,  FENG, Shengxi ,  LI, Yinghong ,  LU, Xi ,  LIN, Lidong ,  FAN, Tianyun ,  PANG, Jing ,  GUO, Zhihao ,  LI, Zhiwen ,  LIU, Yonghua ,  WANG, Xiukun

IPC分类号： A61K45/06 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/55 ,  A61K31/551 ,  A61K31/58 ,  A61K31/69 ,  A61K38/05 ,  A61P31/04

CPC分类号： Y02A50/30 ,  A61K31/427 ,  A61K31/55 ,  A61K31/4375 ,  A61K38/05 ,  A61K45/06 ,  A61K31/69 ,  A61K31/58 ,  A61P31/04 ,  A61K31/551

摘要： The present invention relates to a pharmaceutical composition comprising a β-lactam compound of formula (I), or a stereoisomer, a solvate or a pharmaceutically acceptable salt or ester thereof, and a lactamase inhibitor or an efflux pump inhibitor, and the use thereof for inhibiting microorganisms, particularly bacteria, especially Gram-negative bacteria, wherein each symbol in formula (I) is as defined in the description.

公开(公告)号：EP3669875A1

公开(公告)日：2020-06-24

申请号：EP19843169.4

申请日：2019-06-19

申请人： Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences

发明人： CEN, Shan ,  LI, Quanjie ,  YI, Dongrong ,  SHI, Yi ,  WANG, Han ,  ZHOU, Jinming

IPC分类号： A61K31/472 ,  A61P31/14

摘要： The present invention provides use of berbamine dihydrochloride in preparation of an Ebola virus inhibitor. In the present invention, the primed glycoprotein of the Ebola virus (EBOV-GPcl) is taken as a target site, and an antiviral active compound with the capability of binding to the EBOV-GPcl, i.e., berbamine dihydrochloride, is obtained through structure-based virtual screening. Berbamine dihydrochloride can specifically inhibit the entry of an Ebola recombinant virus by binding to the target protein EBOV-GPcl, thereby achieving the effect of anti-Ebola virus infection. The half-maximum effect concentration (EC50) of berbamine dihydrochloride against EBOV is 0.49 µM, which indicates that berbamine dihydrochloride has a strong inhibition effect on EBOV.