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    DEUTERATED MGL-3196 COMPOUND AND USE THEREOF
    2.
    发明申请
    DEUTERATED MGL-3196 COMPOUND AND USE THEREOF 有权

    公开(公告)号：US20210292304A1

    公开(公告)日：2021-09-23

    申请号：US17255231

    申请日：2019-06-21

    Applicant: HINOVA PHARMACEUTICALS INC.

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

    IPC: C07D403/12

    Abstract: Disclosed are a compound as shown in formula (I) or optical isomers, pharmaceutically acceptable salts, prodrugs, hydrates or solvates thereof, wherein R1-R10 are independently selected from H and D, respectively, and not all are H. Compared to the undeuterated control compound MGL3 196, the compound of formula (I) or the optical isomers, pharmaceutically acceptable salts, prodrugs, hydrates or solvates thereof has/have better agonistic activity on thyroid hormone receptor p (THR-p), has/have a longer half-life and a lower clearance rate, has/have better metabolic stability and pharmacokinetic properties, and has/have excellent application prospects in the preparation of THR-p agonists and drugs for treating indications to which THR-p agonists are applicable, including dyslipidemia, hypercholesterolemia, nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD).

    HALOGEN-SUBSTITUTED PHENYLATE COMPOUND AND APPLICATIONS THEREOF
    5.
    发明申请
    HALOGEN-SUBSTITUTED PHENYLATE COMPOUND AND APPLICATIONS THEREOF 有权

    公开(公告)号：US20220332707A1

    公开(公告)日：2022-10-20

    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

    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.

    AROMATIC AMINE AR AHD BET TARGETING PROTEIN DEGRADATION CHIMERA COMPOUND AND USE
    6.
    发明申请
    AROMATIC AMINE AR AHD BET TARGETING PROTEIN DEGRADATION CHIMERA COMPOUND AND USE 有权

    公开(公告)号：US20220257774A1

    公开(公告)日：2022-08-18

    申请号：US17595023

    申请日：2020-05-15

    Applicant: HINOVA PHARMACEUTICALS INC.

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

    IPC: A61K47/55 ,  A61K47/54

    Abstract: An aromatic amine androgen receptor (AR) and BET targeting protein degradation chimera compound is 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.

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