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    PYRROLO- AND PYRAZOLO-TRIAZOLODIAZEPINES AS BET-PROTEIN INHIBITORS FOR TREATING HYPERPROLIFERATIVE DISEASES
    6.
    发明申请
    PYRROLO- AND PYRAZOLO-TRIAZOLODIAZEPINES AS BET-PROTEIN INHIBITORS FOR TREATING HYPERPROLIFERATIVE DISEASES 审中-公开
    作为用于治疗高增殖性疾病的β-蛋白酶抑制剂的吡咯并 - 吡喃并吡唑并嘧啶

    公开(公告)号：US20160009725A1

    公开(公告)日：2016-01-14

    申请号：US14770000

    申请日：2014-02-17

    申请人： BAYER PHARMA AKTIENGESELLSCHAFT

    发明人： Norbert SCHMEES ,  Bernd BUCHMANN ,  Bernard HAENDLER ,  Roland NEUHAUS ,  Pascale LEJEUNE ,  Martin KRÜGER ,  Amaury Ernesto FERNANDEZ-MONTALVAN ,  Hermann KÜNZER

    IPC分类号： C07D487/14 ,  C07D498/08 ,  C07D495/10 ,  C07D491/08 ,  C07D491/107 ,  A61K31/551

    CPC分类号： C07D487/14 ,  A61K31/551 ,  C07D487/04 ,  C07D491/08 ,  C07D491/107 ,  C07D495/10 ,  C07D498/08

    摘要： What is described are BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, bicyclo- and spino-substituted pyrrolo- and pyrazolodiazepines of the general formula I in which X, Y, n, m, R1, R2, R3, R4 and R5 are each as defined in the description, to intermediates for preparation of the inventive compounds, to pharmaceutical compositions comprising the inventive compounds, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for tumour disorders. Also described is the use of the compounds according to the invention as BET protein inhibitors for benign hyperplasias, for atherosclerotic disorders, for sepsis, for autoimmune disorders, for vascular disorders, for viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for male fertility control.

    摘要翻译： 描述了通式I的其中X，Y，n，m，R 1，R 2，R 3，R 3，R 4，R 4，R 6，R 6， ，R4和R5各自如本说明书所定义，中间体用于制备本发明化合物，包含本发明化合物的药物组合物，以及用于过度增殖性疾病，特别是肿瘤病症的预防和治疗应用。 还描述了根据本发明的化合物作为用于良性增生，动脉粥样硬化性疾病，败血症，血管疾病，病毒感染，神经变性疾病，炎症性疾病，动脉粥样硬化性疾病的BET蛋白抑制剂的用途 并为男性生育控制。