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：US11591301B2

公开(公告)日：2023-02-28

申请号：US16967077

申请日：2019-01-31

Applicant: HINOVA PHARMACEUTICALS INC.

Inventor： Wu Du ,  Wen Ren ,  Haibin Lv ,  Haibo Li ,  Kun Wen ,  Jinyun He ,  Dekun Qin ,  Xinghai Li ,  Yuanwei Chen

IPC: C07D271/08 ,  C07D413/12

Abstract: A compound is represented by formula (I). A pharmaceutical composition contains the compound of formula (I). The compound is used in the preparation of an indoleamine-2,3-dioxygenase (IDO) inhibitor drug. The compound exhibits inhibition effect on IDO protease and metabolizes stably in the body. The compound or pharmaceutical composition thereof can be used for preparing an IDO inhibitor drug, and can also be used for preparing a drug for preventing and/or treating diseases having IDO-mediated tryptophan metabolic pathway pathological features.

公开(公告)号：US11447477B2

公开(公告)日：2022-09-20

申请号：US16956581

申请日：2018-12-20

Applicant: HINOVA PHARMACEUTICALS INC.

Inventor： Wu Du ,  Chaowu Ai ,  Yu Li ,  Kun Wen ,  Haibin Lv ,  Wen Ren ,  Jinyun He ,  Dekun Qin ,  Xinghai Li ,  Yuanwei Chen

IPC: A61P35/00 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P27/12 ,  A61P31/18 ,  A61P37/02 ,  C07D413/12 ,  C07D413/14 ,  A61P3/00

Abstract: Provided is a compound represented by formula (I). Also provided are a pharmaceutical composition containing the compound of formula (I) and use of the compound in preparing indoleamine-2,3-dioxygenase (IDO) inhibitor drugs. The compound or the pharmaceutical composition thereof can be used for preparing drugs for preventing and/or treating diseases having pathological features of IDO-mediated tryptophan metabolic pathways.