公开(公告)号：US20250051347A1

公开(公告)日：2025-02-13

申请号：US18293289

申请日：2022-07-29

Applicant: Hinova Pharmaceuticals, Inc.

Inventor： Wu Du ,  Xinghai Li ,  Kun Wen ,  Dekun Qin ,  Shaohua Zhang ,  Song Chen ,  Jingyi Duan ,  Haibin Lv ,  Haibo Li ,  Yu Li ,  Jinyun He ,  Muyang Chen ,  Shijuan Liu ,  Yiwei Fu ,  Yikai Guan ,  Zhilin Tu

IPC: C07D491/107 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D519/00

Abstract: A compound as shown in formula I, or an optical isomer thereof, a solvate thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, a tautomer thereof, a mesomer thereof, a racemate thereof, an enantiomer thereof, a diastereomer thereof, a mixture form thereof, a metabolite thereof, a metabolic precursor thereof, or an isotope substitute form thereof. TB is a target recognition/binding portion, L is a linking portion, and U is a ubiquitin protease recognition/binding portion, the three portions being connected by means of chemical bonds. The compound can significantly down-regulate mutated androgen receptor (AR) proteins, and has good inhibitory activity on prostate cancer cell lines. The compound of formula I can be used for preparation of a protein degradation targeted chimera for targeted regulation of androgen receptors, and a drug for treating diseases correlated with regulation by androgen receptors, and has particularly good application prospects in drugs for treating prostate cancers and breast cancers.