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    IMIDAZO [1,2-A]PYRIDINE COMPOUNDS FOR USE IN THERAPY
    8.
    发明申请
    IMIDAZO [1,2-A]PYRIDINE COMPOUNDS FOR USE IN THERAPY 审中-公开
    咪达唑[1,2-A]吡啶化合物用于治疗

    公开(公告)号：WO2012130322A1

    公开(公告)日：2012-10-04

    申请号：PCT/EP2011/055059

    申请日：2011-03-31

    Applicant: ELARA PHARMACEUTICALS GMBH ,  MÜLBAIER, Marcel ,  ALONSO, Jorge ,  THOMSON, Douglas ,  JANSSEN, Bernd ,  ENCINAS LOPEZ, Arantxa ,  WENDT, Bernd ,  SCHULTES, Christoph

    Inventor： MÜLBAIER, Marcel ,  ALONSO, Jorge ,  THOMSON, Douglas ,  JANSSEN, Bernd ,  ENCINAS LOPEZ, Arantxa ,  WENDT, Bernd ,  SCHULTES, Christoph

    IPC: C07D471/04 ,  A61K31/437 ,  A61P29/00

    CPC classification number: C07D471/04 ,  A61K31/496 ,  A61K31/551 ,  A61K45/06

    Abstract: The present invention provides novel imidazo[1,2-a]pyridine compounds that are useful in therapy of diseases and disorders. The novel compounds inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders. wherein X is CH 2 , CH 2 CH 2 or C=O; R 1 is phenyl or C-bound monocyclic 5- or 6-membered heteroaryl, wherein phenyl and monocyclic 5- or 6-membered heteroaryl are unsubstituted or carry 1, 2, 3, 4 or 5 radicals R 1a which are identical or different; R 2 is phenyl or C-bound monocyclic 5- or 6-membered heteroaryl, wherein phenyl and monocyclic 5- or 6-membered heteroaryl are unsubstituted or carry 1, 2, 3, 4 or 5 radicals R 2a which are identical or different; R 3 is hydrogen, C 1 -C 6 -alkyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, fluorinated C 1 -C 2 -alkyl C(O)R 4 ; where R 1a , R 2a and R 4 are as defined in the claims and the specification.

    Abstract translation: 本发明提供可用于治疗疾病和病症的新的咪唑并[1,2-a]吡啶化合物。 该新型化合物在低氧条件下抑制缺氧诱导因子（HIF）介导的转录和信号传导的活化。 一方面，本发明的化合物可用于制备用于治疗或预防选自以下的疾病或病症的药物：炎性疾病，过度增殖性疾病或病症，缺氧相关病理学和 一种以血管过度为特征的疾病。 还提供了包含本发明化合物和第二治疗剂或辐射的药物组合物，其可用于治疗或预防所述疾病或病症。 其中X是CH 2，CH 2 CH 2或C = O; R 1是苯基或C键的单环5或6元杂芳基，其中苯基和单环5或6元杂芳基是未取代的或带有相同或不同的1,2,3,4或5个基团R 1a; R 2是苯基或C结合的单环5或6元杂芳基，其中苯基和单环5或6元杂芳基是未取代的或带有相同或不同的1,2,3,4或5个基团R2a; R 3是氢，C 1 -C 6烷基，C 1 -C 4烷氧基-C 1 -C 4烷基，氟化C 1 -C 2烷基C（O）R 4; 其中R1a，R2a和R4如权利要求和说明书中所定义。

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