公开(公告)号：EP4410307A1

公开(公告)日：2024-08-07

申请号：EP22875194.7

申请日：2022-09-30

申请人： Jiangsu Hengrui Pharmaceuticals Co., Ltd. ,  Shanghai Hengrui Pharmaceutical Co., Ltd. ,  Suncadia Pharmaceuticals Co., Ltd

发明人： XU, Jianyan ,  CAI, Xiaofeng ,  QU, Bolei ,  ZHANG, Ying ,  CHEN, Xiaoxi ,  HE, Feng ,  TAO, Weikang ,  ZHU, Lingjian ,  HONG, Min ,  HUANG, Jian ,  LI, Yanbing ,  XU, Xiaolang ,  HU, Zhipeng ,  XUE, Zhouyang ,  YOU, Lingfeng

IPC分类号： A61K39/395 ,  C07K16/46 ,  C12N5/10 ,  A61K47/68 ,  C12N15/13 ,  A61P35/00

CPC分类号： A61K47/68 ,  A61P35/00 ,  A61K47/68035 ,  A61K47/6851 ,  A61K47/6855 ,  C07K16/28 ,  C07K16/32

摘要： The present disclosure relates to a pyrrolo benzodiazepine derivative and a conjugate, preparation method and use thereof. In particular, the present disclosure relates to a compound of formula (DL) and a antibody-drug conjugate thereof, a pharmaceutical composition containing same, and a use thereof in the preparation of a medicament for the treatment of cancer. The definitions of groups in the general formula (DL) are as defined in the description.

公开(公告)号：EP3858386A1

公开(公告)日：2021-08-04

申请号：EP19866595.2

申请日：2019-09-25

申请人： Jiangsu Hengrui Medicine Co., Ltd. ,  Shanghai Hengrui Pharmaceutical Co., Ltd.

发明人： XU, Jianyan ,  ZHANG, Ying ,  CAI, Xiaofeng ,  QU, Bolei ,  LIANG, Jindong ,  ZHANG, Lianshan ,  HE, Feng ,  TAO, Weikang

IPC分类号： A61K47/68 ,  A61K47/65 ,  A61K47/54 ,  A61K38/07 ,  A61P35/00 ,  A61P37/02

摘要： The present invention relates to a ligand-drug conjugate of an exatecan analogue, a preparation method therefor and an application thereof. Specifically, the present invention provides a ligand-drug conjugate having a structure shown in formula (-D), a preparation method therefor, a pharmaceutical composition containing same, and use thereof in preparation of drugs for treating cancers by means of receptor regulation. The definition of each substituent in formula (-D) is the same as that in the description.

公开(公告)号：EP3421463A1

公开(公告)日：2019-01-02

申请号：EP17755844.2

申请日：2017-02-24

申请人： Jiangsu Hengrui Medicine Co., Ltd. ,  Shanghai Hengrui Pharmaceutical Co., Ltd.

发明人： XU, Jianyan ,  ZHANG, Ying ,  QU, Bolei ,  JIANG, Guiyang

IPC分类号： C07D403/12 ,  C07D209/02

摘要： The present invention relates to a new toxin and a method for preparing an intermediate thereof. In particular, the present invention relates to a new toxin and a method for preparating intermediates (III) and (IV) thereof, and a preparation method for synthesizing what is shown in general formula (I). The method comprises subjecting a chiral compound shown in general formula (III) to a series of protective group addition, protective group removal and amidation so as to obtain a compound as shown in general formula(I). The present method has the advantages of mild reaction condition, simple operation, high optical purity and high synthetic yield, and is suitable for large-scale production.

公开(公告)号：EP3251698A1

公开(公告)日：2017-12-06

申请号：EP16748591.1

申请日：2016-01-26

申请人： Jiangsu Hengrui Medicine Co. Ltd. ,  Shanghai Hengrui Pharmaceutical Co. Ltd.

发明人： XU, Jianyan ,  ZHANG, Ying ,  QU, Bolei ,  ZHANG, Fuyao ,  YU, Xiuzhao ,  LIANG, Jindong ,  JIANG, Guiyang ,  ZHANG, Lianshan ,  LI, Ang ,  WANG, Yali

IPC分类号： A61K47/69 ,  C07K16/30 ,  A61P35/00

CPC分类号： A61K47/6889 ,  A61K47/50 ,  A61K47/6817 ,  A61K47/6849 ,  A61K47/6855 ,  A61K47/6857 ,  A61K47/6863 ,  A61P35/00 ,  C07K7/06 ,  C07K16/2863 ,  C07K16/30 ,  C07K16/3023 ,  C07K16/32 ,  C07K2317/56 ,  C07K2317/73 ,  C07K2317/76 ,  Y02P20/55

摘要： Provide are a ligand-cytotoxicity drug conjugate with a general formula of PC-L-Dr, a preparing method thereof, and applications of the ligand-cytotoxicity drug conjugate and pharmaceutical compositions comprising the same in preparing drugs for treating cancers by means of receptor regulation.

摘要翻译： 提供具有通式PC-L-Dr的配体 - 细胞毒性药物缀合物及其制备方法，以及配体 - 细胞毒性药物缀合物和包含其的药物组合物在通过受体调节来制备用于治疗癌症的药物中的应用 。