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    INHIBITION OF MYCOBACTERIAL TYPE VII SECRETION
    1.
    发明申请
    INHIBITION OF MYCOBACTERIAL TYPE VII SECRETION 审中-公开

    公开(公告)号：WO2021040519A1

    公开(公告)日：2021-03-04

    申请号：PCT/NL2020/050527

    申请日：2020-08-26

    Applicant: STICHTING VUMC ,  STICHTING VU

    Inventor： RUIJTER, Eelco ,  RONG, Mark Karsten ,  SPEER, Alexander ,  BITTER, Wilhelmus ,  COLE, Stewart Thomas

    IPC: C07D285/08 ,  C07D417/04 ,  A61K31/4436 ,  A61K31/42 ,  A61K31/426 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/506 ,  A61P31/04 ,  A61P31/06

    Abstract: The invention relates to compounds and pharmaceutically acceptable salts thereof, and to their medical use. Exemplary medical uses are the prevention and treatment of a bacterial infection, for example, a mycobacterial infection, such as a Mycobacterium tuberculosis infection, e.g., in a respiratory system and/or extrapulmonic. The invention further relates to a use of such compounds, pharmaceutically acceptable salts thereof or prodrugs of the compounds as chemotherapeutic agents. Also, the invention relates to a use of such compounds, pharmaceutically acceptable salts thereof or prodrugs of the compounds for inhibiting mycobacterial type VII secretion. The compounds have the following formula (Ia), wherein Q and X are, respectively, CH and C, CR2 and C, CH and N, CR2 and N, or N and C; R1 is hydrogen, halide or optionally substituted linear or branched alkoxy having 1 or 2 carbon atoms; R2 is independently selected from hydrogen, halide or optionally substituted linear or branched alkoxy having 1 or 2 carbon atoms, and R3 is optionally substituted linear or branched alkoxy having 1-6 carbon atoms, haloalkyl having 1-6 carbon atoms, n-propyl, 2-propenyl, 2-propynyl, or n-pentyl, or a pharmaceutically acceptable salt of the compound, for use in the prevention or treatment of a bacterial infection.

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