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公开(公告)号：US20210179590A1
公开(公告)日：2021-06-17
申请号：US16758744
申请日：2018-10-17
发明人： Marie-Pierre COLLIN-KROEPELIN , Peter KOLKHOF , Thomas NEUBAUER , Chantal FUERSTNER , Elisabeth POOK , Hanna TINEL , Carsten SCHMECK , Pierre WASNAIRE , Heiko SCHIRMER , Klemens LUSTIG
IPC分类号： C07D403/14 , C07D403/06 , C07D405/14 , C07D401/14 , C07D413/14 , A61P9/10 , A61K45/06
摘要： The present invention relates to novel substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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公开(公告)号：US20200017473A1
公开(公告)日：2020-01-16
申请号：US16579341
申请日：2019-09-23
发明人： Marie-Pierre COLLIN , Peter KOLKHOF , Thomas NEUBAUER , Chantal FUERSTNER , Elisabeth POOK , Matthias Beat WITTWER , Klemens LUSTIG , Anja BUCHMUELLER , Hanna TINEL , Karoline DROEBNER , Thomas MONDRITZKI , Heiko SCHIRMER , Axel KRETSCHMER , Carsten SCHMECK , Pierre WASNAIRE , Hana CERNECKA
IPC分类号： C07D401/14 , A61P9/04 , A61P13/12 , A61P3/10 , A61P9/10 , A61K45/06 , A61K31/4439
摘要： The present invention relates to novel 5-(carboxamide)-1-pyridinyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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![SUBSTITUTED 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRIDINE-3(2H)-ONES AND 2,5,6,7-TETRAHYDRO-3H-PYRROLO[2,1-C][1,2,4]TRIAZOL-3-ONES, AND USE THEREOF](/abs-image/US/2019/05/30/US20190160048A1/abs.jpg.150x150.jpg)
公开(公告)号：US20190160048A1
公开(公告)日：2019-05-30
申请号：US16300480
申请日：2017-05-08
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 , Steven MOORE , Alexander SCHULZ
IPC分类号： A61K31/437 , A61P29/00 , A61P11/00 , C07D471/04 , A61K31/506
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, 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.
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公开(公告)号：US20200375986A1
公开(公告)日：2020-12-03
申请号：US16761713
申请日：2018-10-31
发明人： Nicole BIBER , Damian BROCKSCHNIEDER , Florian KÖLLING , Jörg MEDING , Hideki MIYATAKE ONDOZABAL , Thomas NEUBAUER , Martina SCHÄFER , Dmitry ZUBOV , Carsten TERJUNG
IPC分类号： A61K31/4985 , A61K45/06 , C07D487/04 , A61P11/00
摘要： The invention relates to prolyl endopeptidase (PREP) inhibitors which contain a condensed 2,4-dihydro-3H-1,2,4-triazol-3-one ring system, methods for producing same, the use thereof alone or in combinations for treating and/or preventing diseases, and the use thereof for producing drugs for treating and/or preventing diseases, in particular for treating and/or preventing inflammatory lung diseases (COPD).
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公开(公告)号：US20200338096A1
公开(公告)日：2020-10-29
申请号：US16758742
申请日：2018-10-17
发明人： Marie-Pierre COLLIN-KROEPELIN , Peter KOLKHOF , Thomas NEUBAUER , Chantal FUERSTNER , Elisabeth POOK , Matthias Beat WITTWER , Carsten SCHMECK , Pierre WASNAIRE , Heiko SCHIRMER , Hana CERNECKA , Karoline DROEBNER , Hanna TINEL , Anja BUCHMUELLER , Thomas MONDRITZKI , Axel KRETSCHMER , Klemens LUSTIG , Robert FRICKE , Guillaume LEVILAIN , Ursula KRENZ , Norbert WITOWSKI
IPC分类号： A61K31/675 , A61K45/06 , C07F9/6558 , A61P13/12
摘要： The present invention relates to prodrugs of 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-[3-(trifluoromethyl)-pyridin-2-yl]-1H-1,2,4-triazole-5-carboxamide, 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-[2-(trifluoromethyl)-phenyl]-1H-1,2,4-triazole-5-carboxamide and 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-(3-chloropyridin-2-yl)-1H-1,2,4-triazole-5-carboxamide, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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公开(公告)号：US20190315720A1
公开(公告)日：2019-10-17
申请号：US16343150
申请日：2017-10-16
发明人： Chantal FUERSTNER , Marie-Pierre COLLIN-KROEPELIN , Peter KOLKHOF , Thomas NEUBAUER , Elisabeth POOK , Heiko SCHIRMER , Carsten SCHMECK , Pierre WASNAIRE , Matthias Beat WITTWER
IPC分类号： C07D403/06 , C07D403/14 , A61P13/12
摘要： The present invention relates to novel 3-(hydroxyalkyl)-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and/or cardiovascular diseases.
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公开(公告)号：US20190144431A1
公开(公告)日：2019-05-16
申请号：US16098238
申请日：2017-05-02
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).
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公开(公告)号：US20240010684A1
公开(公告)日：2024-01-11
申请号：US18035493
申请日：2021-10-29
发明人： Donald BIERER , Ingo FLAMME , Dmitry ZUBOV , Thomas NEUBAUER , Adrian TERSTEEGEN , Lars BAUMANN , Cathleen JUHL , Marie GLATZ , Jan DREHER , Simon HOLTON , Jiancheng XIONG , Jianchao XU
摘要： The present invention relates to novel Mannose-binding lectin (MBL)-associated serine protease (MASP) inhibitory bicyclic compounds, as well as to processes for the preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of renal and cardiovascular disorders and of ischemia reperfusion injuries.
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公开(公告)号：US20210253557A1
公开(公告)日：2021-08-19
申请号：US16758741
申请日：2018-10-17
发明人： Marie-Pierre COLLIN-KROEPELIN , Peter KOLKHOF , Thomas NEUBAUER , Chantal FUERSTNER , Elisabeth POOK , Hanna TINEL , Carsten SCHMECK , Pierre WASNAIRE , Heiko SCHIRMER , Klemens LUSTIG , Nils GRIEBENOW
摘要： The present invention relates to novel substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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公开(公告)号：US20200316045A1
公开(公告)日：2020-10-08
申请号：US16756623
申请日：2018-10-17
发明人： Marie-Pierre COLLIN-KROEPELIN , Peter KOLKHOF , Thomas NEUBAUER , Chantal FUERSTNER , Elisabeth POOK , Matthias Beat WITTWER , Klemens LUSTIG , Hanna TINEL , Niels LINDNER , Heiko SCHIRMER
IPC分类号： A61K31/4439 , A61K45/06 , C07D401/14 , A61K31/496 , C07D403/14 , C07D417/14 , A61K31/541 , A61K31/5377 , C07D413/14 , C07D409/14 , A61K31/4188 , C07D487/10 , A61K31/4196 , C07D403/06 , C07D405/14 , A61K31/551
摘要： The present invention relates to novel substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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