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    WNT PATHWAY MODULATORS
    1.
    发明申请
    WNT PATHWAY MODULATORS 审中-公开

    公开(公告)号：US20190185478A1

    公开(公告)日：2019-06-20

    申请号：US16226398

    申请日：2018-12-19

    Applicant: Agency for Science, Technology and Research

    Inventor： Jenefer Alam ,  Soo Yei Ho ,  Wei Ling Wang ,  Athisayamani Jeyaraj Duraiswamy

    IPC: C07D487/04

    CPC classification number: C07D487/04

    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents H; optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); —C(O)Oalkyl; haloalkyl; haloalkoxy; or -alkylaryl; each R2 independently represents H; optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); -alkylaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); —NHalkyl; —N(alkyl)2; amino; hydroxyl; alkoxy or halo; n represents 0, 1 or 2; R3 represents H or alkyl; R4 represents H or alkyl; R5 represents H or alkyl; W and X each independently represent C═O; C═S; or CH2; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); and Z represents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); aryl; heteroaryl; -alkylaryl;-alkylheteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); -alkylcarbocyclyl wherein carbocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkoxy and halo); -alkylheterocyclyl wherein heterocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); -arylcarbocyclyl wherein carbocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkoxy and halo); or -arylheterocyclyl wherein heterocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl).

    WNT PATHWAY MODULATORS
    7.
    发明申请
    WNT PATHWAY MODULATORS 有权

    公开(公告)号：US20210047336A1

    公开(公告)日：2021-02-18

    申请号：US17084507

    申请日：2020-10-29

    Applicant: Agency for Science, Technology and Research

    Inventor： Jenefer Alam ,  Soo Yei Ho ,  Wei Ling Wang ,  Athisayamani Jeyaraj Duraiswamy

    IPC: C07D487/04 ,  A61K31/519 ,  A61P35/04 ,  A61P35/00

    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents H; optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); —C(O)Oalkyl; haloalkyl; haloalkoxy; or -alkylaryl; each R2 independently represents H; optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); -alkylaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); —NHalkyl; —N(alkyl)2; amino; hydroxyl; alkoxy or halo; n represents 0, 1 or 2; R3 represents H or alkyl; R4 represents H or alkyl; R5 represents H or alkyl; W and X each independently represent C═O; C═S; or CH2; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); and Z represents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); aryl; heteroaryl; -alkylaryl; -alkylheteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); -alkylcarbocyclyl wherein carbocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkoxy and halo); -alkylheterocyclyl wherein heterocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); -arylcarbocyclyl wherein carbocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkoxy and halo); or -arylheterocyclyl wherein heterocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl).

    Maleimide derivatives as modulators of wnt pathway
    9.
    发明授权
    Maleimide derivatives as modulators of wnt pathway 有权

    公开(公告)号：US09981964B2

    公开(公告)日：2018-05-29

    申请号：US15105312

    申请日：2014-12-17

    Applicant: Agency for Science, Technology and Research

    Inventor： Jenefer Alam ,  Anders Poulsen ,  Soo Yei Ho ,  Wei Ling Wang ,  Athisayamani Jeyaraj Duraiswamy

    IPC: C07D471/04 ,  C07D487/04

    CPC classification number: C07D471/04 ,  C07D487/04

    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy); optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or -alkylaryl; R2 represents H; or alkyl; R3 represents H; or alkyl; U, V and W represent —(CH2)—; or U and V together represent —CH═CH— and W represents C═O; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); and Z represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl).

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