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公开(公告)号：EP2885286B1
公开(公告)日：2017-03-22
申请号：EP13748072.9
申请日：2013-08-13
发明人： SIEGEL, Stephan , BÄURLE, Stefan , CLEVE, Arwed , HAENDLER, Bernard , FERNANDEZ-MONTALVAN, Amaury Ernesto , MÖNNING, Ursula , KRAUSE, Sabine , LEJEUNE, Pascale , SCHMEES, Norbert , BUSEMANN, Matthias , HOLTON, Simon , KUHNKE, Joachim
IPC分类号： C07D401/14 , C07D413/14 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/14 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/10 , C07D243/02 , A61K31/55 , A61P35/00 , A61P31/12
CPC分类号： C07D417/10 , A61K31/551 , A61K31/5513 , C07D243/02 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/14 , C07D409/10 , C07D413/04 , C07D413/10 , C07D413/14
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2.发明公开BET-PROTEININHIBITORISCHE 5-ARYL-TRIAZOLO-AZEPINE 有权BET-PROTEININHIBITORISCHE 5-ARYL-TRIZZOLO-AZEPINE
公开(公告)号：EP2900672A1
公开(公告)日：2015-08-05
申请号：EP13766962.8
申请日：2013-09-25
发明人： SCHMEES, Norbert , KUHNKE, Joachim , HAENDLER, Bernard , NEUHAUS, Roland , LEJEUNE, Pascale , SIEGEL, Stephan , KRÜGER, Martin , FERNANDEZ-MONTALVAN, Amaury Ernesto , KÜNZER, Hermann , GALLENKAMP, Daniel
IPC分类号： C07D487/04 , C07D519/00 , A61K31/55 , A61P35/00 , A61P31/12 , A61P29/00 , A61P25/28 , A61P9/10
CPC分类号： C07D487/04 , A61K31/55 , C07D519/00
摘要： The present invention relates to BET protein-inhibiting 5-aryl triazole azepines, particularly BRD4-inhibiting 5-aryl triazole azepines of general formula (I) in which R
1 , R2, R3 and R4 have the meanings indicated in general formula (I). The invention also relates to pharmaceutical agents containing the compounds according to the invention and the prophylactic and therapeutic use thereof in hyperproliferative disorders, particularly in tumorous diseases. Furthermore, this invention relates to the use of BET protein inhibitors in viral infections, in neurodegenerative diseases, in inflammatory diseases, in atherosclerotic diseases and in monitoring male fertility.摘要翻译： 本发明涉及其中R 1，R 2，R 3和R 4具有通式（I）中所示含义的通式（I）的抑制BR蛋白的5-芳基三唑吖庚因，特别是BRD4抑制性5-芳基三唑吖庚因， 。 本发明还涉及含有本发明化合物的药剂以及其在过度增殖性疾病，特别是在肿瘤疾病中的预防和治疗用途。 此外，本发明涉及BET蛋白抑制剂在病毒感染，神经退行性疾病，炎性疾病，动脉粥样硬化疾病和监测男性生育力中的用途。
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3.发明公开PYRROLO- UND PYRAZOLO-TRIAZOLODIAZEPINE ALS BET-PROTEININHIBITOREN ZUR BEHANDLUNG VON HYPER-PROLIFERATIVEN ERKRANKUNGEN 审中-公开吡咯并吡唑并和-TRIAZOLODIAZEPINE AS bet蛋白抑制剂来治疗过度增殖性病症
公开(公告)号：EP2958922A1
公开(公告)日：2015-12-30
申请号：EP14704595.9
申请日：2014-02-17
发明人： SCHMEES, Norbert , BUCHMANN, Bernd , HAENDLER, Bernard , NEUHAUS, Roland , LEJEUNE, Pascale , KRÜGER, Martin , FERNANDEZ-MONTALVÁN, Amaury Ernesto
IPC分类号： C07D487/14 , C07D487/04 , A61K31/5517 , A61P35/00
CPC分类号： C07D487/14 , A61K31/551 , C07D487/04 , C07D491/08 , C07D491/107 , C07D495/10 , C07D498/08
摘要： BET-protein-inhibiting, in particular BRD2-, BRD3- and BRD4-inhibiting bicyclo- and spiro-substituted pyrrolo- and pyrazolo-diazepines, of general formula I in which X, Y, n, m, R
1 , R
2 , R
3 , R
4 and R
5 have the meanings indicated in the description, intermediates for producing the compounds according to the invention, pharmaceutical agents containing the compounds according to the invention and the prophylactic and therapeutic use thereof for treating hyperproliferative diseases, in particular tumor diseases, are described. Furthermore, the use of the compounds according to the invention as BET-protein inhibitors in benign hyperplasias, in atherosclerotic diseases, in sepsis, in autoimmune diseases, in vascular diseases, in viral infections, in neurodegenerative diseases, in inflammatory diseases, in atherosclerotic diseases and for controlling fertility in males is described.-
公开(公告)号：EP2958923A1
公开(公告)日：2015-12-30
申请号：EP14705164.3
申请日：2014-02-18
发明人： SCHMEES, Norbert , BUCHMANN, Bernd , HAENDLER, Bernard , NEUHAUS, Roland , LEJEUNE, Pascale , KRÜGER, Martin , FERNANDEZ-MONTALVAN, Amaury, Ernesto , KÜNZER, Hermann , REHWINKEL, Hartmut
IPC分类号： C07D487/14 , A61K31/55 , A61P35/00 , A61P43/00
CPC分类号： C07D487/14 , A61K31/5517 , C07D519/00
摘要： BET-protein-inhibiting, in particular BRD2-, BRD3- and BRD4-inhibiting 4-substituted pyrrolo- and pyrazolo-diazepines, of general formula I in which X, Y, n, m, p, R
1 , R
2 , R
3 , R
4 and R
5 have the meanings indicated in the description, pharmaceutical agents containing the compounds according to the invention and the prophylactic and therapeutic use thereof for treating hyperproliferative diseases, in particular tumor diseases, are described. Furthermore, the use of the compounds according to the invention as BET-protein inhibitors in benign hyperplasias, in atherosclerotic diseases, in sepsis, in autoimmune diseases, in vascular diseases, in viral infections, in neurodegenerative diseases, in inflammatory diseases, in atherosclerotic diseases and for controlling fertility in males is described.-
公开(公告)号：EP2958909A1
公开(公告)日：2015-12-30
申请号：EP14704594.2
申请日：2014-02-17
发明人： SIEGEL, Stephan , BÄURLE, Stefan , CLEVE, Arwed , HAENDLER, Bernard , FERNÁNDEZ-MONTALVÁN, Amaury Ernesto , MÖNNING, Ursula , KRAUSE, Sabine , LEJEUNE, Pascale , BUSEMANN, Matthias , KUHNKE, Joachim
IPC分类号： C07D401/10 , C07D403/10 , C07D405/10 , A61K31/551 , A61P35/00 , A61P37/00 , A61P7/00 , A61P25/28 , A61P31/12 , C07D451/06 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/048
CPC分类号： A61K31/551 , C07D245/06 , C07D401/10 , C07D403/10 , C07D405/10 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/048 , C07D491/08 , C07D491/107 , C07D495/10 , C07D498/08 , C07D498/10
摘要： The invention relates to BET protein-inhibiting, in particular BRD4-inhibiting, bicyclo 2,3-benzodiazepines and spirocyclically substituted 2,3-benzodiazepines of the general formula (I), to the pharmaceutical agents containing the compounds according to the invention, and to the prophylactic and therapeutic use thereof against hyper-proliferative diseases, in particular tumor diseases. The invention further relates to the use of BET protein inhibitors in benign hyperplasia, atherosclerotic diseases, sepsis, autoimmune diseases, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, and male fertility control.
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公开(公告)号：EP2935260A1
公开(公告)日：2015-10-28
申请号：EP13807998.3
申请日：2013-12-17
发明人： SCHMEES, Norbert , BADER, Benjamin , HAENDLER, Bernard , STÖCKIGT, Detlef , LEJEUNE, Pascale , FERNÁNDEZ-MONTALVÁN, Amaury Ernesto , STELLFELD, Timo , GALLENKAMP, Daniel
IPC分类号： C07D471/04 , A61P25/00 , A61K31/4985
CPC分类号： A61K31/4985 , A61K31/5377 , C07D471/04 , C07D493/10 , C07D495/10
摘要： The invention concerns BET-protein-inhibiting, in particular BRD4-inhibiting, dihydropyridopyrazinones of general formula (I), in which A, X, R
1 , R
2 , R
3 , R
4 , R
5 , R
6 , R
7 and n have the meanings given in the description, intermediates for producing the compounds according to the invention, pharmaceutical agents containing the compounds according to the invention, and their prophylactic and therapeutic use in hyperproliferative diseases, in particular tumour diseases. The invention further concerns the use of BET-protein-inhibitors in viral infections, neurodegenerative diseases, inflammatory illnesses, atherosclerotic diseases, and in male fertility control.-
公开(公告)号：EP2885286A1
公开(公告)日：2015-06-24
申请号：EP13748072.9
申请日：2013-08-13
发明人： SIEGEL, Stephan , BÄURLE, Stefan , CLEVE, Arwed , HAENDLER, Bernard , FERNANDEZ-MONTALVAN, Amaury Ernesto , MÖNNING, Ursula , KRAUSE, Sabine , LEJEUNE, Pascale , SCHMEES, Norbert , BUSEMANN, Matthias , HOLTON, Simon , KUHNKE, Joachim
IPC分类号： C07D401/14 , C07D413/14 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/14 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/10 , C07D243/02 , A61K31/55 , A61P35/00 , A61P31/12
CPC分类号： C07D417/10 , A61K31/551 , A61K31/5513 , C07D243/02 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/14 , C07D409/10 , C07D413/04 , C07D413/10 , C07D413/14
摘要： What are described are BET protein-inhibitory, in particular BRD4-inhibitory, 2,3-benzodiazepines of the general formula (I) in which R
1a , R
1b , R
1c , R
2 , R
3 , R
4 , R
5 , A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumour disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.
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