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公开(公告)号:US20240116874A1
公开(公告)日:2024-04-11
申请号:US18506737
申请日:2023-11-10
发明人: Britta OLENIK , Birgit KEIL , Bernd RÖSLER , Peter FEY , Heiko SCHIRMER , Guido BECKER , Julian EGGER , Clemens BOTHE , Helene FABER
IPC分类号: C07D215/48 , A61K9/00 , A61P9/12 , A61P11/08
CPC分类号: C07D215/48 , A61K9/0075 , A61P9/12 , A61P11/08
摘要: The present invention relates to a novel and improved process for preparing (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluo-romethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of the formula (I) and to novel crystalline forms of it, which is i.a. the pseudopolymorphic form monohydrate I (I-M-I) or the pseudopolymorphic form monohydrate II (I-M-II), furthermore the present invention relates to a novel and selective crystallization process for preparation of the pseudopolymorphic form monohydrate I (I-M-I) or the pseudopolymorphic form monohydrate II (I-M-II), preferably monohydrate I of formula (I-M-I) and to pharmaceutical compositions comprising monohydrate I of formula (I-M-I) and to its use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of pulmonary and cardiopulmonary and cardiovascular diseases.
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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: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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公开(公告)号:US20240148715A1
公开(公告)日:2024-05-09
申请号:US18506944
申请日:2023-11-10
发明人: Eva Maria BECKER-PELSTER , Hanna TINEL , Michael HAHN , Dieter LANG , Gerrit WEIMANN , Johannes NAGELSCHMITZ , Lisa DIETZ , Soundos SALEH , David JUNG , Ildiko TEREBESI , Tobias MUNDRY , Annett RICHTER , Britta OLENIK , Birgit KEIL , Bernd RÖSLER , Peter FEY , Heiko SCHIRMER , Guido BECKER , Clemens BOTHE , Helene FABER , Julian EGGER , Mark PARRY , David WARD , Cecile VITRE
CPC分类号: A61K31/47 , A61K9/0075 , A61P9/12
摘要: The present invention relates to the use of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), prefer-ably in form of one of its salts or solvates or hydrates, preferably (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (I) of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)-ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid inform of mono hydrate (II) of formula (I-M-II), in the inhalative treatment of cardiopulmonary and pulmonary disorders, such as pulmonary arterial hypertension (P AH), chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary hypertension (PH) associated with chronic lung disease (PH group 3) such as pulmonary hypertension in chronic obstructive pulmonary disease (PH-COPD) and pulmonary hypertension with idiopathic interstitial pneumonia (PH-IIP), characterized in that an inhalative dosage form comprising 240 to 4000 μg, preferably 480 to 2000 μg of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably in form of monohydrate I of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid in form of mono hydrate (II) of formula (I-M-II), is administered to a patient in need thereof once or twice daily for a period of at least two consecutive days, preferably at least 2 to 7 consecutive days, preferably for a period of at least 14 consecutive days, in particular from after onset of treatment for the whole course of the disease, wherein the inhalative dosage form preferably comprises the combination of the active ingredient and a pharmaceutically suitable excipient or carrier, while preferably the active ingredient and a pharmaceutically suitable excipient are filled in a hard capsule.
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公开(公告)号:US20190144422A1
公开(公告)日:2019-05-16
申请号:US16098202
申请日:2017-05-02
发明人: Marie-Pierre COLLIN-KRÖPELIN , Peter KOLKHOF , Thomas NEUBAUER , Chantal FÜRSTNER , Elisabeth POOK , Matthias Beat WITTWER , Carsten SCHMECK , Pierre WASNAIRE , Hanna TINEL , Heiko SCHIRMER
IPC分类号: C07D401/14 , A61K31/4196 , C07D417/14 , C07D403/14 , A61K45/06 , A61K31/4439 , A61K31/427 , A61K31/497 , A61K31/501 , A61P13/12 , A61P9/12 , A61P9/10
CPC分类号: C07D401/14 , A61K31/4196 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K45/06 , A61P9/10 , A61P9/12 , A61P13/12 , C07D403/14 , C07D417/14
摘要: The present invention relates to novel 5-(hydroxyalkyl)-1-heteroaryl-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: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: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:US20170320854A1
公开(公告)日:2017-11-09
申请号:US15581064
申请日:2017-04-28
发明人: Marie-Pierre COLLIN , Peter KOLKHOF , Thomas NEUBAUER , Chantal FÜRSTNER , Elisabeth POOK , Matthias Beat WITTWER , Klemens LUSTIG , Anja BUCHMÜLLER , Hanna TINEL , Karoline DRÖBNER , Thomas MONDRITZKI , Heiko SCHIRMER , Axel KRETSCHMER , Carsten SCHMECK , Pierre WASNAIRE , Hana CERNECKA
IPC分类号: C07D401/14 , A61K45/06 , A61K31/4439
CPC分类号: C07D401/14 , A61K31/4439 , A61K45/06
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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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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