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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:US20190241562A1
公开(公告)日:2019-08-08
申请号:US16317322
申请日:2017-07-04
发明人: Henrik TELLER , Melissa BOULTADAKIS ARAPINIS , Alexandros VAKALOPOULOS , Anne-Sophie REBSTOCK , Alexander STRAUB , Hanna TINEL , Markus BRECHMANN , Matthias Beat WITTWER , Maximillian Andreas KULLMANN , Klaus MÜNTER , Thomas MONDRITZKI , Tobias MARQUARDT
IPC分类号: C07D471/04 , A61P9/04 , A61P13/12 , A61P9/06
摘要: The present application relates to novel 7-substituted 1-pyridylnaphthyridine-3-carboxamides, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prevention of diseases, and to their use for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders and/or renal disorders.
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公开(公告)号:US20210261541A1
公开(公告)日:2021-08-26
申请号:US17161201
申请日:2021-01-28
发明人: Henrik TELLER , Alexandros VAKALOPOULOS , Melissa BOULTADAKIS ARAPINIS , Alexander STRAUB , Hanna TINEL , Markus BRECHMANN , Matthias Beat WITTWER , Maximillian Andreas KULLMANN , Till FREUDENBERGER , Thomas MONDRITZKI , Tobias MARQUARDT
IPC分类号: C07D471/04 , A61P9/06 , A61K31/4375 , A61K31/551 , A61K45/06 , C07D491/107 , C07D519/00 , A61P9/00 , A61P13/00
摘要: The present application relates to novel 7-substituted 1-arylnaphthyridine-3-carboxamides, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prevention of diseases, and to their use for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders and/or renal disorders.
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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:US20220089591A1
公开(公告)日:2022-03-24
申请号:US17161186
申请日:2021-01-28
发明人: Henrik TELLER , Alexandros VAKALOPOULOS , Melissa BOULTADAKIS ARAPINIS , Alexander STRAUB , Hanna TINEL , Markus BRECHMANN , Matthias Beat WITTWER , Maximillian Andreas KULLMANN , Till FREUDENBERGER , Thomas MONDRITZKI , Tobias MARQUARDT
IPC分类号: C07D471/04 , A61P9/06 , A61K31/4375 , A61K31/551 , A61K45/06 , C07D491/107 , C07D519/00 , A61P9/00 , A61P13/00
摘要: The present application relates to novel 7-substituted 1-arylnaphthyridine-3-carboxamides, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prevention of diseases, and to their use for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders and/or renal disorders.
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公开(公告)号:US20190263805A1
公开(公告)日:2019-08-29
申请号:US16333079
申请日:2017-09-06
发明人: Henrik TELLER , Alexandros VAKALOPOULOS , Melissa BOULTADAKIS ARAPINIS , Alexander STRAUB , Hanna TINEL , Markus BRECHMANN , Matthias Beat WITTWER , Maximilian Andreas KULLMANN , Till FREUDENBERGER , Thomas MONDRITZKI , Tobias MARQUARDT
IPC分类号: C07D471/04 , A61K45/06 , C07D519/00 , C07D491/107 , A61P9/06 , A61K31/551 , A61K31/4375
摘要: The present application relates to novel 7-substituted 1-arylnaphthyridine-3-carboxamides, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prevention of diseases, and to their use for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders and/or renal disorders.
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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:US20180141931A1
公开(公告)日:2018-05-24
申请号:US15847684
申请日:2017-12-19
发明人: Eva Maria BECKER-PELSTER , Philipp BUCHGRABER , Anja BUCHMÜLLER , Karen ENGEL , Volker GEISS , Andreas GÖLLER , Herbert HIMMEL , Raimund KAST , Andreas KNORR , Dieter LANG , Gorden REDLICH , Carsten SCHMECK , Hanna TINEL , Frank WUNDER
IPC分类号: C07D401/14 , A61K45/06 , A61K31/541 , A61K31/5377 , C07D491/107 , C07D417/14 , C07D413/14 , A61K31/506
摘要: The present application relates to novel substituted piperidinyltetrahydroquinolines, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardial vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.
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公开(公告)号:US20170020875A1
公开(公告)日:2017-01-26
申请号:US15288982
申请日:2016-10-07
发明人: Chantal FÜRSTNER , Jens ACKERSTAFF , Alexander STRAUB , Heinrich MEIER , Hanna TINEL , Katja ZIMMERMANN , Adrian TERSTEEGEN , Dmitry ZUBOV , Raimund KAST , Jens SCHAMBERGER , Martina SCHÄFER , Kirsten BÖRNGEN
IPC分类号: A61K31/506 , A61K45/06 , C07D405/14 , C07D413/04 , A61K31/538 , C07D401/04 , A61K31/536 , C07D409/14 , C07D417/14 , C07D403/04 , C07D417/04
CPC分类号: A61K31/513 , A61K31/506 , A61K31/536 , A61K31/538 , A61K45/06 , C07D401/04 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要: The present application relates to novel bicyclically substituted uracil derivatives, 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.
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