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    4(1H)-quinolone derivatives and uses thereof
    4.
    发明授权
    4(1H)-quinolone derivatives and uses thereof 有权

    公开(公告)号：US11638705B2

    公开(公告)日：2023-05-02

    申请号：US16831346

    申请日：2020-03-26

    Applicant: Academia Sinica

    Inventor： Rong-Jie Chein ,  Pan-Chyr Yang ,  Chi-Huey Wong ,  Ming-Shiu Lin ,  Ting-Jen Cheng ,  Ting-Hung Chou

    IPC: A61K31/47 ,  A61P35/00 ,  A61K45/06 ,  C07D215/233

    Abstract: Compounds of Formula (I) and methods for treating, delaying, and/or preventing the adverse effects of proliferative diseases, such as cancers including, for example, lung cancer, breast cancer, ovarian cancer, prostate cancer, head cancer, neck cancer, head and neck cancer, or leukemia (e.g., cancer resistant to treatment by one or more microtubule-targeting agents, e.g., cancer resistant to multiple drugs associated with P-glycoprotein (P-gp) overexpression). Methods of inhibiting polymerization of a cancer cell microtubule in a subject in need thereof or a cell, tissue, or biological sample, binding β-tubulin, inhibiting microtubule assembly and, inducing apoptosis in a cancer cell resistant to multiple drugs in a tissue, biological sample, or subject. Pharmaceutical compositions, kits, and methods of using the compounds for treating any of the target diseases described herein.

    Methods of using 4(1
    5.
    发明授权
    Methods of using 4(1 有权

    公开(公告)号：US12109207B2

    公开(公告)日：2024-10-08

    申请号：US18184364

    申请日：2023-03-15

    Applicant: Academia Sinica

    Inventor： Rong-Jie Chein ,  Pan-Chyr Yang ,  Chi-Huey Wong ,  Ming-Shiu Lin ,  Ting-Jen Cheng ,  Ting-Hung Rachel Chou

    IPC: A61K31/47 ,  A61K45/06 ,  A61P35/00 ,  C07D215/233

    CPC classification number: A61K31/47 ,  A61K45/06 ,  A61P35/00 ,  C07D215/233 ,  A61K31/47 ,  A61K2300/00

    Abstract: Provided herein are compounds of Formula (I). The disclosure provides new compounds, compositions, and methods for treating, delaying, and/or preventing the adverse effects of proliferative diseases, such as cancers including, for example, lung cancer, breast cancer, ovarian cancer, prostate cancer, head cancer, neck cancer, head and neck cancer, or leukemia (e.g., cancer resistant to treatment by one or more microtubule-targeting agents (e.g., cancer resistant to multiple drugs associated with P-glycoprotein (P-gp) overexpression)). Provided are methods of inhibiting polymerization of a cancer cell microtubule in a subject in need thereof or a cell, tissue, or biological sample, binding β-tubulin, inhibiting microtubule assembly and, inducing apoptosis in a cancer cell resistant to multiple drugs in a tissue, biological sample, or subject. Also provided in the present disclosure are pharmaceutical compositions, kits, and methods of using the compounds for treating any of the target diseases described herein.

    Compounds and methods for treating osteoarthritis
    6.
    发明授权
    Compounds and methods for treating osteoarthritis 有权

    公开(公告)号：US11332490B1

    公开(公告)日：2022-05-17

    申请号：US17182156

    申请日：2021-02-22

    Applicant: Academia Sinica

    Inventor： Shang-Cheng Hung ,  Chi-Huey Wong ,  Ting-Jen Cheng

    IPC: C07H7/02

    Abstract: Disclosed herein are substrates and/or inhibitors of endo-O-sulfatase 1 (Sulf-1). According to some embodiments, the substrates and/or inhibitors of Sulf-1 are compounds of formula (I) or (II), In formula (I) or (II), n is 2 or 3; X is methylene, O, or N; R1 is —SO3M, or —SO2NH2; R2 is C1-6 alkyl or C1-6 alkylamine; and M is a monovalent cation selected from the group consisting of lithium, sodium, potassium, and ammonium. Also encompasses herein are methods of identifying and treating a subject having or suspected of having osteoarthritis. The method includes steps of (a) mixing a urine sample of the subject with 4-methylumbelliferyl sulfate (4-MUS) and a Sulf-1 inhibitor of formula (I) or (II); (b) determining a fluorescence intensity of the mixture of the step (a); and (c) treating the subject with an analgesic, a non-steroidal anti-inflammatory drug (NSAID), or a corticosteroid when the determined fluorescence intensity of the step (b) is smaller than that of a control sample, which is a mixture of the urine sample and 4-MUS.

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