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。

公开(公告)号：US20150376196A1

公开(公告)日：2015-12-31

申请号：US14769921

申请日：2014-02-18

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 ,  Hartmut REHWINKEL

IPC分类号： C07D487/14 ,  C07D519/00 ,  A61K31/5517

CPC分类号： C07D487/14 ,  A61K31/5517 ,  C07D519/00

摘要： BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, 4-substituted pyrrolo- and pyrazolodiazepines of the general formula I are described, in which X, Y, n, m, p, R1, R2, R3, R4 and R5 are each as defined in the description, as are pharmaceutical compositions comprising the inventive compounds, and the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of neoplastic disorders. Also described is the use of the inventive compounds as BET protein inhibitors in benign hyperplasias, in atherosclerotic disorders, in sepsis, in autoimmune disorders, in vascular disorders, in viral infections, in neurodegenerative disorders, in inflammatory disorders and in male fertility control.

摘要翻译： 描述了通式I中的β蛋白抑制特别是BRD2-，BRD3-和BRD4抑制性4-取代的吡咯并 - 吡唑并二氮杂，其中X，Y，n，m，p，R1，R2，R3，R4 和R5各自如说明书中所定义，以及包含本发明化合物的药物组合物，以及在过度增殖性疾病的情况下的预防和治疗用途，特别是在肿瘤性疾病的情况下。 还描述了本发明化合物作为良性增生中的BET蛋白抑制剂，动脉粥样硬化病症，败血症，自身免疫性疾病，血管病症，病毒感染，神经变性疾病，炎症性疾病和雄性生育控制中的用途。