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.

公开(公告)号：EP4071134A1

公开(公告)日：2022-10-12

申请号：EP20866018.3

申请日：2020-09-16

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

发明人： WANG, Yucheng ,  YOU, Xuefu ,  WANG, Juxian ,  DU, Xiaonan ,  WANG, Minghua ,  ZHU, Mei ,  ZHANG, Guoning

IPC分类号： C07C259/06 ,  C07D295/195 ,  C07D295/155 ,  A61P31/04 ,  C07C45/29 ,  C07C47/37 ,  C07C41/30 ,  C07C43/192 ,  C07C67/343 ,  C07C69/78 ,  C07C51/09 ,  C07C65/28 ,  C07C269/06 ,  C07C271/22 ,  C07C231/12 ,  C07C235/42

摘要： The present disclosure is related to the field of enzyme inhibitors, and in particular to a hydroxamic acid derivative, a method for producing the same and use thereof. The hydroxamic acid group of the hydroxamic acid derivative can be chelated with zinc ions in the LpxC active area, and the derivative has a hydrophobic side chain which can bind to hydrophic channels in the enzyme LpxC. These guarantee that the hydroxamic acid derivative has good bactericidal activity against Gram-negative bacteria and low toxicity. The present disclosure also provides a method for producing the hydroxamic acid derivative, which requires a shorter reaction time and can provide the derivative with a high yield.

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.