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公开(公告)号：US20150203483A1
公开(公告)日：2015-07-23
申请号：US14421994
申请日：2013-08-13
发明人： Stephan Siegel , Stefan Bäurle , Arwed Cleve , Bernard Haendler , Amaury Ernesto Fernandiez-Montalvan , Ursula Mönning , Sabine Krause , Pascale Lejeune , Norbert Schmees , Matthias Busemann , Simon Holton , Joachim Kuhnke
IPC分类号： C07D417/10 , A61K31/551 , C07D413/10 , C07D403/10 , C07D413/14 , C07D409/10 , C07D401/04 , C07D401/14 , A61K31/5513 , C07D401/12 , C07D243/02 , C07D401/10
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 is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, 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.
摘要翻译： 描述了通式（I）的BET蛋白抑制性特别是BRD4抑制性2,3-苯二氮卓类，其中R1a，R1b，R1c，R2，R3，R4，R5，A和X具有 描述，用于制备根据本发明的化合物的中间体，包含根据本发明的化合物的药物组合物及其对过度增殖性疾病，特别是肿瘤病症的预防和治疗用途。 还描述了BET蛋白抑制剂用于良性增生，动脉粥样硬化性疾病，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，动脉粥样硬化性疾病和用于控制雄性生育力的用途。
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公开(公告)号：US09890147B2
公开(公告)日：2018-02-13
申请号：US14421994
申请日：2013-08-13
发明人： Stephan Siegel , Stefan Bäurle , Arwed Cleve , Bernard Haendler , Amaury Ernesto Fernandez-Montalvan , Ursula Mönning , Sabine Krause , Pascale Lejeune , Norbert Schmees , Matthias Busemann , Simon Holton , Joachim Kuhnke
IPC分类号： A61K31/551 , C07D243/02 , C07D401/04 , C07D403/04 , C07D417/10 , C07D401/14 , C07D413/14 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/14 , C07D409/10 , C07D413/04 , C07D413/10 , A61K31/5513
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 is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, 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 tumor 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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公开(公告)号：US09714266B2
公开(公告)日：2017-07-25
申请号：US14770444
申请日：2014-02-18
发明人： Ulrich Bothe , Matthias Busemann , Naomi Barak , Andrea Rotgeri , Oliver Martin Fischer , Tobias Marquardt
CPC分类号： C07J43/003 , A61K31/58 , A61K45/06
摘要： The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of bleeding disorders and endometriosis.
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4.发明授权3-substituted estra-1,3,5(10),16-tetraene derivatives, methods for the production thereof, pharmaceutical preparations containing same, and use thereof for the production of medicaments 有权3-取代的雌-1,3,5（10），16-四烯衍生物，其制备方法，含有它们的药物制剂及其用于生产药物的用途公开(公告)号：US09512169B2
公开(公告)日：2016-12-06
申请号：US14414386
申请日：2013-07-05
发明人： Ulrich Bothe , Matthias Busemann , Oliver Martin Fischer , Naomi Barak , Andrea Rotgeri , Tobias Marquardt , Christian Stegmann
CPC分类号： C07J43/003 , A61K31/58
摘要： The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.
摘要翻译： 本发明涉及AKR1C3抑制剂及其制备方法，其用于治疗和/或预防疾病的用途，以及其用于制备用于治疗和/或预防疾病，特别是出血性疾病和子宫内膜异位症的药物的用途。
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5.发明授权Estra-1,3,5(10),16-tetraene-3-carboxamide derivatives, processes for their preparation, pharmaceutical preparations comprising them and their use for preparing medicaments 有权Estra-1,3,5（10），16-四烯-3-甲酰胺衍生物，其制备方法，包含它们的药物制剂及其制备药物的用途公开(公告)号：US09487554B2
公开(公告)日：2016-11-08
申请号：US14348645
申请日：2012-09-24
发明人： Ulrich Bothe , Naomi Barak , Matthias Busemann , Oliver Martin Fischer , Andrea Rotgeri , Isabella Gashaw , Ingo Hartung , Tobias Marquardt
CPC分类号： C07J43/003 , A61K31/58 , A61K45/06
摘要： The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.
摘要翻译： 本发明涉及AKR1C3抑制剂及其制备方法，其用于治疗和/或预防疾病的用途，以及其用于制备用于治疗和/或预防疾病，特别是出血性疾病和子宫内膜异位症的药物的用途。
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6.发明申请3-SUBSTITUTED ESTRA-1,3,5(10),16-TETRAENE DERIVATIVES, METHODS FOR THE PRODUCTION THEREOF, PHARMACEUTICAL PREPARATIONS CONTAINING SAME, AND USE THEREOF FOR THE PRODUCTION OF MEDICAMENTS 有权3-取代的ESTRA-1,3,5（10），16-四烯衍生物，其生产方法，含有它们的药物制剂及其用于生产药物的用途公开(公告)号：US20150210734A1
公开(公告)日：2015-07-30
申请号：US14414386
申请日：2013-07-05
发明人： Ulrich Bothe , Matthias Busemann , Oliver Martin Fischer , Naomi Barak , Andrea Rotgeri , Tobias Marquardt , Christian Stegmann
CPC分类号： C07J43/003 , A61K31/58
摘要： The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.
摘要翻译： 本发明涉及AKR1C3抑制剂及其制备方法，其用于治疗和/或预防疾病的用途，以及其用于制备用于治疗和/或预防疾病，特别是出血性疾病和子宫内膜异位症的药物的用途。
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7.发明申请Estra-1,3,5(10),16-tetraene-3-carboxamide derivatives, processes for their preparation, pharmaceutical preparations comprising them and their use for preparing medicaments 有权Estra-1,3,5（10），16-四烯-3-甲酰胺衍生物，其制备方法，包含它们的药物制剂及其制备药物的用途公开(公告)号：US20140249119A1
公开(公告)日：2014-09-04
申请号：US14348645
申请日：2012-09-24
发明人： Ulrich Bothe , Naomi Barak , Matthias Busemann , Oliver Martin Fischer , Andrea Rotgeri , Isabella Gashaw , Ingo Hartung , Tobias Marquardt
CPC分类号： C07J43/003 , A61K31/58 , A61K45/06
摘要： The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.
摘要翻译： 本发明涉及AKR1C3抑制剂及其制备方法，其用于治疗和/或预防疾病的用途，以及其用于制备用于治疗和/或预防疾病，特别是出血性疾病和子宫内膜异位症的药物的用途。
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