公开(公告)号：EP4019510A1

公开(公告)日：2022-06-29

申请号：EP20854575.6

申请日：2020-08-20

申请人： Hinova Pharmaceuticals Inc.

发明人： DU, Wu ,  LI, Yu ,  LI, Haibo ,  CHEN, Yuanwei ,  ZHANG, Chengzhi ,  LI, Xinghai

IPC分类号： C07D403/12 ,  C07D403/10 ,  C07D403/02 ,  C07D237/18 ,  C07D237/16 ,  C07D237/14 ,  A61K31/53 ,  A61K31/501 ,  A61P5/16 ,  A61P1/16 ,  A61P3/06 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10

摘要： Disclosed in the present invention are a halogen-substituted phenylate compound and applications thereof. Particularly provided are a compound shown in formula (I) or an optical isomer thereof, and pharmaceutically acceptable salts, prodrugs, aquo-complexes or non-aqueous-solvent complexes thereof. Experiments prove that, compared with a control compound MGL-3196, the compound shown in formula (I), which is obtained through specific substitution sites and specific substitution types in the present invention, is higher in agonist activity to THR-beta and significantly improved in selectivity on THR-beta/THR-alpha. Besides, the compound in the present invention is significantly enhanced in pharmacokinetic properties. The compound in the present invention has a good application prospect 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：EP3971176A1

公开(公告)日：2022-03-23

申请号：EP20809358.3

申请日：2020-05-15

申请人： Hinova Pharmaceuticals Inc.

发明人： DU, Wu ,  LV, Haibin ,  LI, Haibo ,  QIN, Dekun ,  AI, Chaowu ,  LI, Yu ,  DUAN, Jingyi ,  TU, Zhilin ,  ZHANG, Chengzhi ,  CHEN, Yuanwei ,  LI, Xinghai

IPC分类号： C07D401/04 ,  C07D307/52 ,  C07D235/06 ,  C07D207/16 ,  A61K31/4025 ,  A61P35/00

摘要： An aromatic amine androgen receptor (AR) and BET targeting protein degradation chimera compound and its use. Specifically provided is a compound represented by formula I. Experimental results show that the compound can target and degrade both AR and BRD4, and down-regulate the expression of AR and BRD4 proteins; the compound can inhibit the proliferation of a variety of prostate cancer cells; the compound can inhibit the proliferation of a prostate cancer cell line LNCaP/AR, which overexpresses the AR, and can achieve a good inhibition effect on a prostate cancer cell line 22RV1, which is resistant to a marketed prostate cancer drug (enzalutamide); the compound also shows good metabolic stability, and has a good application prospect in the preparation of an AR and/or BET protein degradation targeting chimera, and a drug for the treatment of related diseases regulated by the AR and BET.

公开(公告)号：EP3889138A1

公开(公告)日：2021-10-06

申请号：EP19888999.0

申请日：2019-11-27

申请人： Hinova Pharmaceuticals Inc.

发明人： FAN, Lei ,  WANG, Fei ,  WU, Xiaoquan ,  XU, Kexin ,  CHEN, Ke ,  LUO, Tongchuan ,  ZHANG, Shaohua ,  DU, Wu ,  ZHANG, Chengzhi ,  HUO, Yongxu ,  TU, Zhilin ,  LI, Xinghai ,  CHEN, Yuanwei

IPC分类号： C07D235/02 ,  C07D263/52 ,  C07D269/02 ,  C07D277/60 ,  C07D283/02 ,  A61P35/00 ,  A61K31/381 ,  A61K31/4184 ,  A61K31/428

摘要： Provided are a histone acetylase p300 inhibitor and a use thereof, belonging to the filed of medicinal chemistry technology. A compound represented by formula (I), or a stereochemical isomer thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof, can inhibit the activity of histone acetylase p300 and inhibit the proliferation activity of a variety of tumor cells.