公开(公告)号：US10703742B2

公开(公告)日：2020-07-07

申请号：US16098238

申请日：2017-05-02

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Heiko Schirmer ,  Philipp Rubenbauer ,  Hans-Christian Militzer ,  Marie-Pierre Collin-Kröpelin ,  Frank Süßmeier ,  Kersten Matthias Gericke ,  Thomas Neubauer ,  Chantal Fürstner

IPC分类号： C07D403/06 ,  C07D249/12

摘要： The present application relates to a novel and improved process for preparing 5-(hydroxyalkyl)-1-phenyl-1,2,4-triazole derivatives of the formula (I) in which R1A and R1B are independently selected from the group consisting of hydrogen, fluorine, chlorine, methyl, monofluoromethyl, difluoromethyl, trifluoromethyl, ethyl, methoxy, difluoromethoxy and trifluoromethoxy, to novel precursors for preparation thereof, and to the preparation and use of the crystalline polymorph I of (5-(4-chlorophenyl)-2-({1-(3-chlorophenyl)-5-[(1S)-1-hydroxyethyl]-1H-1,2,4-triazol-3-yl}methyl)-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one of the formula (I-A-1).

公开(公告)号：US10047096B2

公开(公告)日：2018-08-14

申请号：US15529043

申请日：2015-11-23

申请人： Bayer Pharma Aktiengesellschaft ,  Petra Heinrich-Keldenich

发明人： Andreas Schall ,  Jürgen Klar ,  Mario Lobell ,  Hartmut Schirok ,  Joachim Telser ,  Steffen Müller ,  Dirk Brohm ,  Hans Briem ,  Hannah Jörißen ,  Joerg Keldenich ,  Michael Böttger ,  Georges Von Degenfeld ,  Thomas Schlange ,  Ulf Bömer ,  Niels Lindner ,  Hanna Eilken ,  Dmitrij Hristodorov ,  Pierre Wasnaire ,  Kersten Matthias Gericke ,  Lars Bärfacker

IPC分类号： A61K31/551 ,  C07D471/04 ,  C07D487/04 ,  A61K31/5513 ,  A61K39/395

摘要： The present application relates to novel (3-hydroxyphenyl)amino-substituted pyrido[2,3-b][1,5]benzodiazepin-5-one derivatives, to processes for preparation thereof, to the use thereof alone or in combination for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially of angiogenic disorders and hyperproliferative disorders in which neovascularization plays a role, for example ophthalmological disorders and cancers and tumours. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.

公开(公告)号：US10722501B2

公开(公告)日：2020-07-28

申请号：US16300480

申请日：2017-05-08

申请人： BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Nicole Biber ,  Damian Brockschnieder ,  Kersten Matthias Gericke ,  Florian Kölling ,  Klemens Lustig ,  Jörg Meding ,  Heinrich Meier ,  Thomas Neubauer ,  Martina Schäfer ,  Andreas Timmermann ,  Dmitry Zubov ,  Carsten Terjung ,  Niels Lindner ,  Volker Badock ,  Dieter Moosmayer ,  Hideki Miyatake Ondozabal ,  Stephen Moore ,  Alexander Schulz

IPC分类号： A61K31/437 ,  A61K31/506 ,  C07D471/04 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/497 ,  C07D519/00 ,  A61K45/06 ,  A61K31/444 ,  A61P11/00 ,  A61P29/00

摘要： The present application relates to novel substituted 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-3(2H)-ones and 2,5,6,7-tetrahydro-3H-pyrrolo[2,1-c][1,2,4]triazol-3-ones of formula (I), to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of lung inflammation disorders.

公开(公告)号：US09493472B2

公开(公告)日：2016-11-15

申请号：US14895793

申请日：2014-05-30

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Swen Allerheiligen ,  Anja Buchmüller ,  Karen Engel ,  Christoph Gerdes ,  Kersten Matthias Gericke ,  Michael Gerisch ,  Stefan Heitmeier ,  Alexander Hillisch ,  Tom Kinzel ,  Philip Lienau ,  Bernd Riedl ,  Susanne Röhrig ,  Martina Victoria Schmidt ,  Julia Strassburger ,  Adrian Tersteegen

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/495 ,  A61K31/5386 ,  A61K31/5377 ,  A61K31/423 ,  A61K31/454 ,  C07D413/06 ,  C07D263/58 ,  C07D417/06

CPC分类号： C07D487/04 ,  A61K31/423 ,  A61K31/454 ,  A61K31/495 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/5386 ,  C07D263/58 ,  C07D413/06 ,  C07D417/06

摘要： The invention relates to substituted benzoxazoles and to processes for their preparation and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders, preferably of thrombotic or thromboembolic disorders.

摘要翻译： 本发明涉及取代的苯并恶唑及其制备方法及其制备药物用途，用于治疗和/或预防疾病，特别是心血管疾病，优选血栓形成或血栓栓塞性疾病。