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    TRIAZOLE DERIVATIVES AS TANKYRASE INHIBITORS
    4.
    发明申请
    TRIAZOLE DERIVATIVES AS TANKYRASE INHIBITORS 审中-公开

    公开(公告)号：WO2018118868A1

    公开(公告)日：2018-06-28

    申请号：PCT/US2017/067228

    申请日：2017-12-19

    Applicant: OSLO UNIVERSITY HOSPITAL HF ,  FORSCHUNGSVERBUND BERLIN E.V. ,  UNIVERSITY OF OULU

    Inventor： KRAUSS, Stefan ,  NAZARE, Marc ,  ANUMALA, Upendra Rao ,  LEHTIO, Lari ,  WAALER, Jo ,  HOLSWORTH, Dan ,  WEGERT, Anita ,  LEENDERS, Ruben Gerardus George

    IPC: C07D235/26 ,  C07D403/14 ,  C07D417/14 ,  A61P35/00 ,  A61K31/4196

    CPC classification number: C07D403/14 ,  A61P35/00 ,  C07D235/26 ,  C07D417/14

    Abstract: The present invention relates to compounds of formula (I'), tautomers, stereoisomers, and pharmaceutically acceptable salts thereof, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy (I') (wherein: Z represents an optionally substituted, 5- or 6-membered unsaturated heterocyclic group comprising at least one nitrogen atom; L represents a 4-, 5- or 6-membered cycloalkyl group, preferably a cyclobutyl group; each R1 independently represents F, CI, Br, I, C 1-3 alkyl, C1-3 haloalkyl (e.g. -CF 3 ), -CN, -OH or -NO2, preferably F, CI, Br or 1, e.g. CI or F; each R 2 independently represents F, CI, Br, I, C 1-3 alkyl, -CN, -OH or -NO 2 , preferably F, CI, Br, I or -CN, e.g. F or -CN; X represents -NR 3 - or -0-; R 3 represents H or a C 1-3 alkyl group (e.g. methyl); n is an integer from 0 to 5, preferably 0 to 3, more preferably 0, 1 or 2, e.g 1; and m is an integer from 0 to 5, preferably 0 to 3, more preferably 0, 1 or 2, e.g. 0 or 1). These compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the WNT pathway and increased presence of nuclear β-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas.

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