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    FAK inhibitor and drug combination thereof
    2.
    发明申请
    FAK inhibitor and drug combination thereof 有权

    公开(公告)号：US20220125788A1

    公开(公告)日：2022-04-28

    申请号：US17418678

    申请日：2019-12-24

    Applicant: HINOVA PHARMACEUTICALS INC.

    Inventor： Wu DU ,  Yu LI ,  Kun WEN ,  Xinghai LI ,  Yuanwei CHEN

    IPC: A61K31/506 ,  A61K39/395 ,  A61P35/00 ,  C07D403/12

    Abstract: A deuterated compound as represented by formula (I) or an optical isomer, a tautomer, a pharmaceutically acceptable salt, a prodrug, a hydrate, or a solvate thereof are presented. Compared with a compound before deuteration, the deuterated compound shows better pharmacokinetics, higher maximum plasma drug concentration, higher exposure, and longer half-life, and has more excellent metabolic performance. The deuterated compound can effectively inhibit FAK activity, and has good application prospect in preparation of FAK inhibitors and/or drugs for treating cancer. In addition, the use of the deuterated compound in combination with an anti-cancer drug (such as a PD-1 inhibitor) can achieve a synergistic effect, thereby significantly improving the tumor suppression effect, and providing a better choice for clinical cancer treatment.

    DEUTERATED MGL-3196 COMPOUND AND USE THEREOF
    3.
    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).

    Deuterated Defactinib compound and use thereof
    5.
    发明授权
    Deuterated Defactinib compound and use thereof 有权

    公开(公告)号：US11891379B2

    公开(公告)日：2024-02-06

    申请号：US17054080

    申请日：2019-05-06

    Applicant: HINOVA PHARMACEUTICALS INC.

    Inventor： Wu Du ,  Yu Li ,  Kun Wen ,  Xinghai Li ,  Yuanwei Chen

    IPC: A61K31/506 ,  C07D403/12

    CPC classification number: C07D403/12 ,  C07B2200/05

    Abstract: This disclosure provides a compound as shown in formula (I) or optical isomers, pharmaceutically acceptable salts, hydrates or solvates thereof. In formula (I), R1-R18 are independently selected from hydrogen and deuterium respectively, but not all are hydrogen at the same time. The compound and salts, hydrates or solvates thereof can be used as FAK inhibitors, and used in the preparation of anti-cancer drugs, and compared with the undeuterated control compound Defactinib, the compound has significantly improved metabolic stability and pharmacokinetic properties.

    DEUTERATED DEFACTINIB COMPOUND AND USE THEREOF
    6.
    发明申请
    DEUTERATED DEFACTINIB COMPOUND AND USE THEREOF 有权

    公开(公告)号：US20210238166A1

    公开(公告)日：2021-08-05

    申请号：US17054080

    申请日：2019-05-06

    Applicant: HINOVA PHARMACEUTICALS INC.

    Inventor： Wu DU ,  Yu LI ,  Kun WEN ,  Xinghai LI ,  Yuanwei CHEN

    IPC: C07D403/12

    Abstract: This disclosure provides a compound as shown in formula (I) or optical isomers, pharmaceutically acceptable salts, hydrates or solvates thereof. In formula (I). R1-R18 are independently selected from hydrogen and deuterium respectively, but not all are hydrogen at the same time. The compound and salts, hydrates or solvates thereof can be used as FAR inhibitors, and used in the preparation of anti-cancer drugs, and compared with the undeuterated control compound Defactinib, the compound has significantly improved metabolic stability and pharmacokinetic properties.

    DEUTERATED IMIDAZOLIDINEDIONE COMPOUNDS AND THEIR USES
    7.
    发明申请
    DEUTERATED IMIDAZOLIDINEDIONE COMPOUNDS AND THEIR USES 有权

    公开(公告)号：US20210137890A1

    公开(公告)日：2021-05-13

    申请号：US17142440

    申请日：2021-01-06

    Applicant: Hinova Pharmaceuticals Inc.

    Inventor： Xinghai Li ,  Yuanwei Chen

    IPC: A61K31/4166 ,  A61P35/00

    Abstract: Provided herein is a compound of Formula I having androgen receptor antagonistic properties and methods of using the compound to more efficiently and efficaciously reduce the concentration of prostate specific antigen (PSA) and treat male hormone-related diseases such as prostate cancer, breast cancer, alopecia, hair loss, acne and adolescent acne. Also provided are methods of reducing the plasma concentration of prostate specific antigen (PSA) in a subject with elevated PSA comprising administering to the subject a therapeutically effective amount of the compound.

    Imidazole diketone compound and use thereof
    9.
    发明授权
    Imidazole diketone compound and use thereof 有权

    公开(公告)号：US09708289B2

    公开(公告)日：2017-07-18

    申请号：US14889032

    申请日：2014-05-27

    Applicant: HINOVA PHARMACEUTICALS INC.

    Inventor： Yuanwei Chen ,  Yu Gong

    IPC: A61K31/44 ,  C07D211/00 ,  C07D401/04

    CPC classification number: C07D401/04

    Abstract: Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds possess androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne.

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