公开(公告)号：US09890147B2

公开(公告)日：2018-02-13

申请号：US14421994

申请日：2013-08-13

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

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.

公开(公告)号：US20160272635A1

公开(公告)日：2016-09-22

申请号：US14907367

申请日：2014-07-21

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Norbert Schmees ,  Benjamin Bader ,  Bernard Haendler ,  Volker Schulze ,  Ingo Hartung ,  Niels Bohnke ,  Florian Puehler

IPC分类号： C07D471/04 ,  A61K31/55 ,  A61K31/4985

CPC分类号： C07D471/04 ,  A61K31/4985 ,  A61K31/55

摘要： The present invention relates to substituted dihydropyrido[3,4-b]pyrazinones as dual inhibitors of BET proteins, in particular BRD4 proteins, and Polo-like kinases, in particular Plk-1 proteins of the general formula (I) in which A, X, R1, R2, R3, R4, R5, R6, R7 and n are each as defined in the description, to intermediates for preparation of the compounds according to the invention, to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of tumour disorders.Furthermore, the present invention relates to the use of the dihydropyrido[3,4-b]pyrazinones according to the invention in viral infections, in neurodegenerative disorders, in inflammation disorders, in atherosclerotic disorders and in male fertility control.

摘要翻译： 此外，本发明涉及根据本发明的二氢吡啶并[3,4-b]吡嗪酮在病毒感染，神经退行性疾病，炎性疾病，动脉粥样硬化疾病和雄性生育控制中的用途。

公开(公告)号：US20150119372A1

公开(公告)日：2015-04-30

申请号：US14396742

申请日：2013-04-19

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Norbert Schmees ,  Lars Röse ,  Tuula Valo ,  Katja Prelle ,  Reinhard Nubbemeyer ,  Henriikka Korolainen ,  Harri Jukarainen

IPC分类号： A61K31/58

CPC分类号： A61K31/58 ,  A61K9/0039

摘要： The present invention describes intrauterine use of 18-methyl-15β,16β-methylene-19-nor-20-spirox-4-en-3-ones of the general formula (1) wherein R6 and R7 are hydrogen or a methylene group, in the treatment of menorrhagia, of uterine haemorrhages in general, and an intrauterine system for said use, comprising a compound of formula 1.

摘要翻译： 本发明描述了通式（1）的18-甲基-15β，16β-亚甲基-19-去甲代螺环-4-烯-3-酮的宫内使用，其中R 6和R 7是氢或亚甲基 组，治疗月经过多，子宫出血一般，以及所述用途的子宫内系统，其包含式1的化合物。