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：EP4159733A1

公开(公告)日：2023-04-05

申请号：EP21818212.9

申请日：2021-04-30

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

发明人： SONG, Danqing ,  TANG, Sheng ,  YOU, Xuefu ,  LI, Zhiwen ,  WANG, Yanxiang ,  LU, Xi ,  LI, Yinghong ,  HU, Xinxin ,  GUO, Zhihao ,  WANG, Xiukun

IPC分类号： C07D417/12 ,  A61K31/427 ,  A61K31/433 ,  A61P31/04

摘要： The present invention relates to a compound as shown in general formula (I) below (in formula (I), each of R 1 and R 2 independently represents a hydrogen atom or a C1-10 linear or branched alkyl optionally having a substituent, or the two together form a cycloalkyl with 3 to 8 ring carbon atoms; each of R 3 and R 4 independently represents a hydrogen atom or a C1-10 linear or branched alkyl optionally having a substituent or a C6-12 aryl optionally having a substituent, or the two together form a cycloalky with 3 to 8 ring carbon atoms; X represents C or N; and Y represents a linear or branched alkenyl or alkynyl with 2 to 6 carbon atoms and optionally having a substituent, or carboxyl). The compound has good antibacterial properties against bacteria, especially gram-negative bacteria, has low drug resistance, and has good prospects for the effective treatment of various conditions.