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    BAK ACTIVATORS, PHARMACEUTICAL COMPOSITIONS, AND USES IN TREATING CANCER
    2.
    发明申请
    BAK ACTIVATORS, PHARMACEUTICAL COMPOSITIONS, AND USES IN TREATING CANCER 审中-公开

    公开(公告)号：WO2023003990A1

    公开(公告)日：2023-01-26

    申请号：PCT/US2022/037783

    申请日：2022-07-21

    申请人： EMORY UNIVERSITY

    发明人： DENG, Xingming

    IPC分类号： A61K31/33 ,  A61K31/4375 ,  A61K31/4353

    摘要： This disclosure relates to activators of Bak, pharmaceutical compositions, and uses in treating cancer. In certain embodiments, this disclosure relates to methods of treating cancer comprising administering an effective amount of a Bak activator as disclosed herein to a human subject in need thereof. In certain embodiments, this disclosure relates to pharmaceutical compositions comprising a Bak activator which is 1-((2-((2-methoxyacridin-9-yl)amino)ethyl)amino)propan-2-ol (BKA-073), derivative, ester, or salt thereof and a pharmaceutically acceptable excipient.

    PROCESSES FOR PREPARING PYRROLOPYRIDINE-ANILINE COMPOUNDS
    8.
    发明申请
    PROCESSES FOR PREPARING PYRROLOPYRIDINE-ANILINE COMPOUNDS 审中-公开

    公开(公告)号：WO2022159600A1

    公开(公告)日：2022-07-28

    申请号：PCT/US2022/013153

    申请日：2022-01-20

    申请人： NFLECTION THERAPEUTICS, INC.

    发明人： HOUGHTON, Michael ,  KINCAID, John

    IPC分类号： A61K31/435 ,  A61K31/4353 ,  A61K31/437 ,  C07D471/00 ,  C07D471/02 ,  C07D471/04

    摘要： The present disclosure provides processes for preparing a compound of formula (I) from a compound of formula (II) via two steps: 6a) contacting 2-(aminooxy)ethanol (i.e., formula (K)) or a salt thereof (e.g., formula (K-1)), with a base and a silylating agent to form a first mixture including an O-silyl protected compound of formula (K); and 6b) adding a second mixture including a compound of formula (II) or a salt therefore, to the first mixture of step 6a) to form the compound represented by formula (I): The present processes only utilize less than 1.5 equivalents of 2-(aminooxy)ethanol or the salt thereof relative to the compound of formula (II), and therefore reduce the burden to remove excess 2-(aminooxy)ethanol on a large manufacturing scale. Also provided are processes for preparing the compound of formula (K) or (K-1).

    METHODS FOR TREATING CANCER
    10.
    发明申请
    METHODS FOR TREATING CANCER 审中-公开

    公开(公告)号：WO2022094271A1

    公开(公告)日：2022-05-05

    申请号：PCT/US2021/057348

    申请日：2021-10-29

    申请人： SCORPION THERAPEUTICS, INC.

    发明人： MILGRAM, Benjamin C. ,  GUZMAN-PEREZ, Angel ,  WHITE, Ryan D. ,  ST. JEAN, David, Jr. ,  BROOIJMANS, Natasja

    IPC分类号： C07D471/04 ,  C07D471/16 ,  A61K31/4353 ,  A61K31/438 ,  A61P35/00

    摘要： This disclosure provides chemical entities of formula (I) (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/ or cocrystal, and/or drug combination of the compound) that inhibit epidermal growth factor receptor (EGFR, ERBB 1) and/or Human epidermal growth factor receptor 2 (HER2, ERBB2). These chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) EGFR and/or HER2 activation contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also provides compositions containing the same as well as methods of using and making the same.