公开(公告)号：EP4309675A1

公开(公告)日：2024-01-24

申请号：EP21931034.9

申请日：2021-06-08

申请人： Guangzhou Ocusun Ophthalmic Biotechnology Co., Ltd.

发明人： WANG, Yandong ,  LIU, Guoqiang ,  LIU, Wei

IPC分类号： A61K47/54 ,  A61K31/635 ,  A61K9/08 ,  A61P27/02 ,  A61P29/00

摘要： Disclosed are a prodrug of celecoxib represented by Formula I, a preparation method therefor and an application thereof. The compound has proper solubility and is relatively stable under storage conditions. Pharmacokinetic experiments show that celecoxib can be detected in ocular tissues and is distributed in cornea, conjunctiva and aqueous humor, and the celecoxib achieves a relatively high drug concentration and thus the compound of Formula I is an excellent celecoxib prodrug. Moreover, the distribution of control compound SZY1907-P4 is almost not detected, and the concentration of eye drops prepared from the celecoxib in the cornea, conjunctiva and aqueous humor is also relatively low. The compound of Formula I has a remarkable absorption advantage, the drug concentration in the ocular tissues is remarkably higher than those of the celecoxib group and control group SZY1907-P4, and thus the compound can be prepared into liquid preparations, such as eye drops and injections, for inflammatory reactions.