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.

公开(公告)号：US12162878B2

公开(公告)日：2024-12-10

申请号：US17160302

申请日：2021-01-27

Applicant: HINOVA PHARMACEUTICALS INC.

Inventor： Lei Fan ,  Fei Wang ,  Xiaoquan Wu ,  Kexin Xu ,  Ke Chen ,  Tongchuan Luo ,  Shaohua Zhang ,  Yongxu Huo ,  Zhilin Tu ,  Xinghai Li ,  Yuanwei Chen

IPC: C07D471/04 ,  A61K45/06 ,  C07D519/00

Abstract: The compound of formula (I) has a good inhibitory effect on the proliferation of human prostate cancer cells CWR22RV1 and breast cancer cells; and combined use of the compound with an androgen receptor inhibitor HC-1119 significantly enhances the inhibitory effect on prostate cancer cells, and the inhibitory effect increases with increased concentration. The compound of formula (I) can not only be used independently to prepare an antineoplastic agent but can also be used in combination with other agents having antineoplastic effects, such as an androgen receptor inhibitor, or other targeting drugs etc., to prepare an antineoplastic agent having stronger therapeutic effects, especially an agent for treating prostate cancer and breast cancer.