公开(公告)号：US11926618B2

公开(公告)日：2024-03-12

申请号：US17753162

申请日：2020-08-20

Applicant: HINOVA PHARMACEUTICALS INC.

Inventor： Wu Du ,  Yu Li ,  Haibo Li ,  Yuanwei Chen ,  Chengzhi Zhang ,  Xinghai Li

IPC: C07D403/12 ,  A61K31/53 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/14 ,  A61P5/16 ,  A61P9/10 ,  C07D253/075

CPC classification number: C07D403/12 ,  C07B2200/05

Abstract: A compound of formula (I) or an optical isomer thereof, and pharmaceutically acceptable salts, prodrugs, aquo-complexes or non-aqueous-solvent complexes thereof are provided. Experiments prove that, compared with a control compound MGL-3196, the compound of formula (I), which is obtained through specific substitution sites and specific substitution types, is higher in agonist activity to THR-beta and significantly improved in selectivity on THR-beta/THR-alpha. The compound can be used in preparing THR-beta agonist and drugs for treating adaption diseases (including dyslipidemia, hypercholesteremia, non-alcoholic steatohepatitis and non-alcoholic fatty liver disease) applicable to the THR-beta agonist.

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：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：US11753392B2

公开(公告)日：2023-09-12

申请号：US17047380

申请日：2019-04-12

Applicant: HINOVA PHARMACEUTICALS INC.

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

IPC: C07D401/04 ,  C07C231/24 ,  C07D233/02 ,  C07D401/06

CPC classification number: C07D401/04 ,  C07C231/24 ,  C07D233/02 ,  C07D401/06 ,  C07C2601/14 ,  C07C2601/16

Abstract: A novel method for synthesizing deuterated amides and deuterated sulfonamides includes the following steps: (1) adding a compound M, DMAP, R3—X to a solvent to obtain a compound N after a reaction is complete; and (2) adding the compound N, R4—NH—R5, or a salt and base thereof to a solvent, and purifying after a reaction is complete to obtain a compound I.