公开(公告)号：US20200299271A1

公开(公告)日：2020-09-24

申请号：US16880933

申请日：2020-05-21

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Heiko SCHIRMER ,  Philipp RUBENBAUER ,  Hans-Christian MILITZER ,  Marie-Pierre COLLIN-KROEPELIN ,  Frank SUESSMEIER ,  Kersten GERICKE ,  Thomas NEUBAUER ,  Chantal FUERSTNER

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：US20180282337A1

公开(公告)日：2018-10-04

申请号：US15524581

申请日：2015-11-05

申请人： Bayer Pharma Aktiengesellschaft

发明人： Jan-Georg PETERS ,  Philipp RUBENBAUER ,  Daniel GÖTZ ,  Danja GROßBACH ,  Franz-Josef MAIS ,  Heiko SCHIRMER ,  Juergen STIEHL ,  Kai LOVIS ,  Andreas LENDER ,  Martin SEYFRIED ,  Theodor ZWEIFEL ,  Maurus MARTY ,  Günter WEINGÄRTNER

IPC分类号： C07D487/04 ,  C07D233/24

摘要： The present invention relates to a novel method of preparing copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride. The present invention also relates to copanlisib dihydrochloride hydrates as compounds.

公开(公告)号：US20210253573A1

公开(公告)日：2021-08-19

申请号：US17271141

申请日：2019-08-22

申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

发明人： Johannes PLATZEK ,  Philipp RUBENBAUER ,  Hendricus Nicolaas Sebastiaan VAN DER HAAS ,  Sonja Elisabeth HOOGEVEEN ,  Matthijs Cornelis Maria VAN OERS ,  Reinerus Gerardus GIELING ,  Jeroen Alexander DEKKER

IPC分类号： C07D471/04

摘要： The present invention covers a method for preparing 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridine (“the compound of formula (I)” in the following) as well as intermediate compounds useful in the preparation of the compound of formula (I). The present invention also covers polymorphic form B of the compound of formula (I) with very high purity.

公开(公告)号：US20190144431A1

公开(公告)日：2019-05-16

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：US20210179541A1

公开(公告)日：2021-06-17

申请号：US16767724

申请日：2018-11-26

申请人： Bayer Pharma Aktiengesellschaft

发明人： Peter FEY ,  Philipp RUBENBAUER ,  Kai LOVIS ,  Britta OLENIK ,  Julia KUSEL ,  Felix SPINDLER

IPC分类号： C07C233/88 ,  C07C231/02 ,  C07C231/12 ,  C07C51/09 ,  C07C227/18

摘要： The present invention relates to a novel and improved process for preparing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid of the formula (I), to the compound of the formula (I) in crystalline form and to their use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular, cardiopulmonary and cardiorenal disorders.

公开(公告)号：US20200237648A1

公开(公告)日：2020-07-30

申请号：US16486449

申请日：2019-07-19

申请人： BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT

发明人： ANKE STROYER ,  Carmen LOBBACK ,  Peter SERNO ,  Kia LOVIS ,  Philipp RUBENBAUER ,  Helko SCHIRMER ,  Danja GROßBACH ,  Tia JACOBS ,  Britta OLENIK ,  Julia Küsel ,  Donald BIERER

IPC分类号： A61K9/00 ,  A61K9/20 ,  A61K31/196

摘要： The present invention relates to orally administrable modified-release pharmaceutical dosage forms comprising sodium (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoate and to processes for preparing the dosage forms and to their use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiac, renal, pulmonary and ophthalmic disorders, disorders of the central nervous system, fibrotic and inflammatory disorders and metabolic disorders.