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公开(公告)号：US09315543B2
公开(公告)日：2016-04-19
申请号：US14355836
申请日：2012-10-29
发明人： Ingo Flamme , Johannes Köbberling , Hans-Georg Lerchen , Nils Griebenow , Rudolf Schohe-Loop , Sven Wittrock , Ursula Krenz
CPC分类号： C07K5/0815 , A61K38/05 , A61K38/06 , A61K47/50 , A61K47/65 , C07K5/0215 , C07K5/06086
摘要： The invention relates to novel tyrosine based linkers that allow the releasable connection of peptides or proteins with other molecular entities, e.g. polyethylene glycol, to processes for their preparation and their use for preparing medicaments for the treatment and/or prophylaxis of diseases.
摘要翻译： 本发明涉及新的基于酪氨酸的接头，其允许肽或蛋白质与其他分子实体的可释放连接，例如。 聚乙二醇，其制备方法及其用于制备用于治疗和/或预防疾病的药物的用途。
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公开(公告)号：US20150051160A1
公开(公告)日：2015-02-19
申请号：US14355836
申请日：2012-10-29
发明人： Ingo Flamme , Johannes Köbberling , Hans-Georg Lerchen , Nils Griebenow , Rudolf Schohe-Lop , Sven Wittrock , Ursula Krenz
CPC分类号： C07K5/0815 , A61K38/05 , A61K38/06 , A61K47/50 , A61K47/65 , C07K5/0215 , C07K5/06086
摘要： The invention relates to novel tyrosine based linkers that allow the releasable connection of peptides or proteins with other molecular entities, e.g. polyethylene glycol, to processes for their preparation and their use for preparing medicaments for the treatment and/or prophylaxis of diseases.
摘要翻译： 本发明涉及新的基于酪氨酸的接头，其允许肽或蛋白质与其他分子实体的可释放连接，例如。 聚乙二醇，其制备方法及其用于制备用于治疗和/或预防疾病的药物的用途。
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3.发明授权公开(公告)号：US08772498B2
公开(公告)日：2014-07-08
申请号：US13801484
申请日：2013-03-13
发明人： Alexandros Vakalopoulos , Daniel Meibom , Barbara Albrecht-Küpper , Katja Zimmermann , Jörg Keldenich , Hans-Georg Lerchen , Peter Nell , Frank Süβmeier , Ursula Krenz
IPC分类号： A61K31/44 , C07D409/00
CPC分类号： C07D417/14 , A61K47/64 , C07D417/12 , C07K5/0202 , C07K5/06026 , C07K5/06034 , C07K5/06086 , C07K5/06147 , C07K5/06165
摘要： The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
摘要翻译： 本申请涉及新的6-烷基氨基取代的二氰基吡啶，其氨基酸酯前药，其制备方法，其用于治疗和/或预防疾病的用途及其用于制备用于治疗和/ 或预防疾病，优选用于治疗和/或预防心血管疾病。
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公开(公告)号：US08957017B2
公开(公告)日：2015-02-17
申请号：US14219872
申请日：2014-03-19
发明人： Hans-Georg Lerchen , Ursula Krenz , Jörg Keldenich , Nicole Diedrichs , Thomas Krahn , Claudia Hirth-Dietrich , Barbara Albrecht-Küpper
IPC分类号： A61K38/00 , A61K47/00 , C07K5/068 , C07D417/12
CPC分类号： A61K47/48246 , A61K31/4439 , A61K47/542 , A61K47/64 , C07D417/12 , C07K5/06086
摘要： The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders.
摘要翻译： 本申请涉及2-氨基-6 - （{[2-（4-氯苯基）-1,3-噻唑-4-基]甲基}硫基）-4- [4-（2-羟基乙氧基） 苯基]吡啶-3,5-二腈，其制备方法，它们用于治疗和/或预防疾病的用途，及其用于制备用于治疗和/或预防疾病，特别是心血管疾病的药物的用途。
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公开(公告)号：US09586958B2
公开(公告)日：2017-03-07
申请号：US14897951
申请日：2014-06-06
发明人： Volker Schulze , Hans-Georg Lerchen , Donald Bierer , Antje Margret Wengner , Gerhard Siemeister , Philip Lienau , Ursula Krenz , Dirk Kosemund , Detlef Stöckigt , Michael Brüning , Ulrich Lücking , Ildikó Terebesi
IPC分类号： C07D471/02 , C07D471/04 , C07F9/6561 , C07K5/062 , C07K5/068 , A61K38/00
CPC分类号： C07D471/04 , A61K38/00 , C07F9/6561 , C07K5/06052 , C07K5/06086
摘要： The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, processes for their preparation, and their use for the treatment and/or prophylaxis of diseases.
摘要翻译： 本发明涉及Mps-1激酶抑制剂的前药衍生物，其制备方法及其用于治疗和/或预防疾病的用途。
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公开(公告)号：US11298367B2
公开(公告)日：2022-04-12
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 , A61P13/12 , A61K45/06 , C07F9/6558
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：US20160207915A1
公开(公告)日：2016-07-21
申请号：US14897951
申请日：2014-06-06
发明人： Volker Schulze , Hans-Georg Lerchen , Donald Bierer , Antje Margret Wengner , Gerhard Siemeister , Philip Lienau , Ursula Krenz , Dirk Kosemund , Detlef Stockigt , Michael Bruning , Ulrich Lucking , Ildiko Terebesi
IPC分类号： C07D471/04 , C07K5/068 , C07K5/062 , C07F9/6561
CPC分类号： C07D471/04 , A61K38/00 , C07F9/6561 , C07K5/06052 , C07K5/06086
摘要： The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, processes for their preparation, and their use for the treatment and/or prophylaxis of diseases.
摘要翻译： 本发明涉及Mps-1激酶抑制剂的前药衍生物，其制备方法及其用于治疗和/或预防疾病的用途。
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