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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:US20140031391A1
公开(公告)日:2014-01-30
申请号:US13945675
申请日:2013-07-18
发明人: Michael HAHN , Markus FOLLMANN , Walter HÜBSCH , Eva-Maria BECKER , Johannes-Peter STASCH , Joerg KELDENICH , Martina DELBECK , Hanna TINEL , Frank WUNDER , Joachim MITTENDORF , Ildiko TEREBESI , Dieter LANG , René MARTIN
IPC分类号: C07D215/48 , C07D401/12 , A61K45/06 , A61K31/4706 , A61K31/4709 , C07D413/12
CPC分类号: C07D215/48 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K45/06 , C07D217/26 , C07D401/12 , C07D413/12
摘要: The present application relates to novel 5-amino-5,6,7,8-tetrahydroquinoline-2-carboxylic acids, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular and cardiopulmonary disorders.
摘要翻译: 本申请涉及新的5-氨基-5,6,7,8-四氢喹啉-2-羧酸,其制备方法,其用于治疗和/或预防疾病的用途及其用于生产 用于治疗和/或预防疾病的药物,特别是用于治疗和/或预防心血管和心肺疾病的药物。
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公开(公告)号:US20180319807A2
公开(公告)日:2018-11-08
申请号:US15596383
申请日:2017-05-16
发明人: Marcus KOPPITZ , Holger SIEBENEICHER , Holger STEUBER , Antonius TER LAAK , Reinhard NUBBEMEYER , Antje ROTTMANN , Horst IRLBACHER , Benjamin BADER , Michaele PETERS , Andrea WAGENFELD , Ildiko TEREBESI
IPC分类号: C07D487/08 , A61K31/4995 , A61K45/06
CPC分类号: C07D487/08 , A61K31/4995 , A61K45/06
摘要: The present invention covers [8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of disorders, in particular of gynecological disorders, hyperproliferative disorders, metabolic disorders, or inflammatory disorders as a sole agent or in combination with other active ingredients.
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公开(公告)号:US20170342082A1
公开(公告)日:2017-11-30
申请号:US15596383
申请日:2017-05-16
发明人: Marcus KOPPITZ , Holger SIEBENEICHER , Holger STEUBER , Antonius TER LAAK , Reinhard NUBBEMEYER , Antje ROTTMANN , Horst IRLBACHER , Benjamin BADER , Michaele PETERS , Andrea WAGENFELD , Ildiko TEREBESI
IPC分类号: C07D487/08 , A61K45/06 , A61K31/4995
CPC分类号: C07D487/08 , A61K31/4995 , A61K45/06
摘要: The present invention covers [8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of disorders, in particular of gynecological disorders, hyperproliferative disorders, metabolic disorders, or inflammatory disorders as a sole agent or in combination with other active ingredients.
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