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    1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
    3.
    发明授权
    1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer 有权

    公开(公告)号：US11279689B2

    公开(公告)日：2022-03-22

    申请号：US16480195

    申请日：2018-01-24

    申请人： Araxes Pharma LLC

    发明人： Liansheng Li ,  Jun Feng ,  Yuan Liu ,  Pingda Ren ,  Yi Liu

    IPC分类号： C07D405/04 ,  C07D403/04 ,  A61P35/04 ,  A61K9/00

    摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, isotopic form or stereoisomer thereof, wherein A is a five-membered heteroaryl comprising 1 or 2 non-adjacent heteroatoms, inclusive of X and Y; W, X, Y, Z, L, L1, E, R1, R2b R2c and the dotted circle are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and compounds for use in methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided. Preferred compounds are e.g. 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and related compounds such as e.g. the corresponding derivatives with e.g. a benzoimidazole, indole, benzooxazole, imidazopyridine or imidazole core structure, substituted on ring A by e.g. azetidine, pyrrolidine, azepane or bicyclopentane-amine (L1) each substituted by e.g. propenone (E), and the core structure substituted on the six-membered ring with e.g. 3-hydroxynaphthalene or indazole or hydroxy-, alkoxy- and/or fluoro-substituted phenyl (R1).

    INHIBITORS OF KRAS G12C MUTANT PROTEINS
    5.
    发明申请
    INHIBITORS OF KRAS G12C MUTANT PROTEINS 审中-公开

    公开(公告)号：US20200062761A1

    公开(公告)日：2020-02-27

    申请号：US16374356

    申请日：2019-04-03

    申请人： Araxes Pharma LLC

    发明人： Liansheng Li ,  Jun Feng ,  Yun Oliver Long ,  Yuan Liu ,  Pingda Ren ,  Yi Liu

    IPC分类号： C07D487/04 ,  A61P35/00 ,  C07D403/04 ,  C07D471/04 ,  C07D491/04

    摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein B, W, X, Y, R1, R2a, R2b, R3a, R3b, R4a, R4b, G1, G2, m1, m2, L1, L2 and E are defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

    INHIBITORS OF KRAS G12C MUTANT PROTEINS
    7.
    发明申请
    INHIBITORS OF KRAS G12C MUTANT PROTEINS 审中-公开

    公开(公告)号：US20190092767A1

    公开(公告)日：2019-03-28

    申请号：US15764097

    申请日：2016-09-28

    申请人： Araxes Pharma LLC

    发明人： Liansheng Li ,  Jun Feng ,  Yun Oliver Long ,  Yuan Liu ,  Pingda Ren ,  Yi Liu

    IPC分类号： C07D471/04 ,  C07D243/14 ,  C07D307/82

    摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein A, B R1, R2a, R2b, R3a, R3b, R4a, R4b, G1, G2, m1, m2, L1, L2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

    COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF CANCER
    8.
    发明申请
    COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF CANCER 审中-公开

    公开(公告)号：US20190062314A1

    公开(公告)日：2019-02-28

    申请号：US15989031

    申请日：2018-05-24

    申请人： Araxes Pharma LLC

    发明人： Liansheng Li ,  Jun Feng ,  Tao Wu ,  Yuan Liu ,  Yi Wang ,  Pingda Ren ,  Yi Liu

    IPC分类号： C07D403/14 ,  C07D401/10

    摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, L1, L2, E, X, Y, Z, m1 and m2 are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.