公开(公告)号：US20240124409A1

公开(公告)日：2024-04-18

申请号：US18519062

申请日：2023-11-26

申请人： NANJING UNIVERSITY OF CHINESE MEDICINE

发明人： Lihong HU ,  Jian LIU ,  Qi LV ,  Yang HU ,  Dong DONG ,  Ping WANG ,  Meng YANG

IPC分类号： C07D307/93 ,  A61P1/16 ,  A61P11/00 ,  A61P13/12 ,  A61P19/02 ,  A61P19/06 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00

CPC分类号： C07D307/93 ,  A61P1/16 ,  A61P11/00 ,  A61P13/12 ,  A61P19/02 ,  A61P19/06 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00

摘要： The present application discloses a class of guaianolide sesquiterpene lactone derivatives and pharmaceutical use thereof. The guaianolide sesquiterpene lactone derivative or a pharmaceutically acceptable salt thereof is shown as general formula I. In the present application, a class of novel guaianolide sesquiterpene lactone derivatives are found by structural optimization with abundant natural ingredients such as parthenolide and dehydrocostus lactone as raw materials, which derivatives have good inhibitory activity on the activation of the NLRP3 inflammasome, and the chemical stability, water solubility and oral bioavailability of which are significantly improved, and it is verified by experiments that the derivatives have inhibitory effects on the activity of the NLRP3 inflammasome and have potential pharmaceutical applications.