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公开(公告)号：US20240124522A1
公开(公告)日：2024-04-18
申请号：US18299600
申请日：2023-04-12
发明人： Donald Bierer , Ingo Flamme , Dmitry Zubov , Thomas Neubauer , Adrian Tersteegen , Cathleen Juhl , Marie Glatz , Jan Dreher , Simon Holton , Carsten Terjung , Lars Baumann , Thorsten Poethko , Jiancheng Xiong , Yibo Qiu
摘要： The present invention relates to novel Mannose-binding lectin (MBL)-associated serine protease (MASP) inhibitory compounds, as well as analogues and derivatives thereof, 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：US11773070B2
公开(公告)日：2023-10-03
申请号：US17865236
申请日：2022-07-14
申请人： Bayer Aktiengesellschaft , Bayer Pharma Aktiengesellschaft , The Broad Institute, Inc. , Dana-Farber Cancer Institute, Inc.
发明人： Manuel Ellermann , Stefan Nikolaus Gradl , Charlotte Christine Kopitz , Martin Lange , Adrian Tersteegen , Philip Lienau , Christa Hegele-Hartung , Detlev Sülzle , Timothy A. Lewis , Heidi Greulich , Xiaoyun Wu , Matthew Meyerson , Alex Burgin
IPC分类号： C07D273/04 , C07D413/10 , C07D413/12 , C07D417/10 , C07D471/04 , C07D491/107 , C07D495/10
CPC分类号： C07D273/04 , C07D413/10 , C07D413/12 , C07D417/10 , C07D471/04 , C07D491/107 , C07D495/10
摘要： The present invention provides dihydrooxydiazinone compounds of general formula (I)
in which R1, R2, R3, and R4, 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 diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.-
3.发明申请公开(公告)号：US20200247783A1
公开(公告)日：2020-08-06
申请号：US16635513
申请日：2018-08-02
申请人： Bayer Aktiengesellschaft , Bayer Pharma Aktiengesellschaft , The Broad Institute, Inc. , Dana-Farber Cancer Institute, Inc.
发明人： Manuel Ellermann , Stefan Nikolaus Gradl , Charlotte Christine Kopitz , Martin Lange , Adrian Tersteegen , Philip Lienau , Detlev Sülzle , Timothy Lewis , Heidi Greulich , Xiaoyun Wu , Matthew Meyerson
IPC分类号： C07D403/10 , C07D405/10 , C07D401/10 , C07D237/04 , C07D413/10 , A61P35/04
摘要： The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I): The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I):
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公开(公告)号：US11667675B2
公开(公告)日：2023-06-06
申请号：US17138447
申请日：2020-12-30
发明人： Donald Bierer , Ingo Flamme , Dmitry Zubov , Thomas Neubauer , Adrian Tersteegen , Cathleen Juhl , Marie Glatz , Jan Dreher , Simon Holton , Carsten Terjung , Lars Baumann , Thorsten Poethko , Jiancheng Xiong , Yibo Qiu
摘要： The present invention relates to novel Mannose-binding lectin (MBL)-associated serine protease (MASP) inhibitory compounds, as well as analogues and derivatives thereof, 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：US20200369633A1
公开(公告)日：2020-11-26
申请号：US16635504
申请日：2018-08-02
申请人： Bayer Aktiengesellschaft , Bayer Pharma Aktiengesellschaft , The Broad Institute, Inc. , Dana-Farber Cancer Institute, Inc.
发明人： Manuel Ellermann , Stefan Nikolaus Gradl , Charlotte Christine Kopitz , Martin Lange , Adrian Tersteegen , Philip Lienau , Christa Hegele-Hartung , Detlev Sülzle , Timothy A. Lewis , Heidi Greulich , Xiaoyun Wu , Matthew Meyerson , Alex Burgin
IPC分类号： C07D273/04 , C07D413/10 , C07D413/12 , C07D417/10 , C07D491/107 , C07D495/10 , C07D471/04
摘要： The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R1, R2, R3, and R4, 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 diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US11427553B2
公开(公告)日：2022-08-30
申请号：US16635504
申请日：2018-08-02
申请人： Bayer Aktiengesellschaft , Bayer Pharma Aktiengesellschaft , The Broad Institute, Inc. , Dana-Farber Cancer Institute, Inc.
发明人： Manuel Ellermann , Stefan Nikolaus Gradl , Charlotte Christine Kopitz , Martin Lange , Adrian Tersteegen , Philip Lienau , Christa Hegele-Hartung , Detlev Sülzle , Timothy A. Lewis , Heidi Greulich , Xiaoyun Wu , Matthew Meyerson , Alex Burgin
IPC分类号： C07D273/04 , C07D413/10 , C07D413/12 , C07D417/10 , C07D471/04 , C07D491/107 , C07D495/10
摘要： The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R1, R2, R3, and R4, 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 diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US10071995B2
公开(公告)日：2018-09-11
申请号：US15513930
申请日：2015-09-22
发明人： Susanne Röhrig , Eloisa Jimenez Núnez , Karl-Heinz Schlemmer , Adrian Tersteegen , Henrik Teller , Alexander Hillisch , Stefan Heitmeier , Martina Victoria Schmidt , Jan Stampfuß
IPC分类号： C07D413/14 , C07D409/12 , C07D409/14 , A61P27/02 , A61P1/00 , A61P29/00
CPC分类号： C07D413/14 , A61P1/00 , A61P27/02 , A61P29/00 , C07D409/12 , C07D409/14
摘要： The invention relates to substituted oxopyridine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
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公开(公告)号：US09505786B2
公开(公告)日：2016-11-29
申请号：US14738148
申请日：2015-06-12
发明人： Markus Follmann , Johannes-Peter Stasch , Gorden Redlich , Nils Griebenow , Dieter Lang , Frank Wunder , Walter Hübsch , Alexandros Vakalopoulos , Adrian Tersteegen
IPC分类号： C07D471/04 , A61K31/53 , A61P9/10 , A61P9/12 , A61P7/02 , C07D519/00 , A61K31/519 , A61K45/06
CPC分类号： C07D519/00 , A61K31/519 , A61K31/53 , A61K45/06 , C07D471/04
摘要： The present application relates to novel substituted fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
摘要翻译： 本申请涉及新型取代的稠合嘧啶和三嗪，其制备方法，单独使用或组合用于治疗和/或预防疾病，以及其用于生产药物用于治疗和/或预防 疾病，特别是用于治疗和/或预防心血管疾病。
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9.发明授权Substituted oxopyridine derivatives and use thereof as factor xia/plasma 有权取代的氧代吡啶衍生物及其作为因子xia /等离子体的用途公开(公告)号：US09475809B2
公开(公告)日：2016-10-25
申请号：US14906771
申请日：2014-07-21
发明人： Susanne Röhrig , Alexander Hillisch , Julia Straβburger , Stefan Heitmeier , Martina Victoria Schmidt , Karl-Heinz Schlemmer , Anja Buchmüller , Christoph Gerdes , Henrik Teller , Martina Schäfer , Adrian Tersteegen
IPC分类号： C07D471/04 , C07D401/12 , C07D221/04 , C07D413/12 , C07D215/227
CPC分类号： A61K31/438 , A61K31/437 , C07D215/227 , C07D221/04 , C07D401/12 , C07D413/12 , C07D471/04
摘要： The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
摘要翻译： 本发明涉及取代的氧代吡啶衍生物及其制备方法，以及它们用于制备用于治疗和/或预防疾病，特别是心血管疾病，优选血栓形成或血栓栓塞性疾病，以及眼药水以及眼科疾病的药物的用途 。
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公开(公告)号：US11884660B2
公开(公告)日：2024-01-30
申请号：US17046004
申请日：2019-04-03
发明人： Mario Lobell , Hartmut Schirok , Adrian Tersteegen
CPC分类号： C07D471/04 , A01N1/00 , A61K9/0048 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2059 , A61K47/36 , A61P7/02
摘要： The invention relates to 5-({6-amino-2-[4-(5-chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1(2H)-yl]-3-methylhexanoyl}amino)pyrazolo[1,5-a]pyridine-3-carboxamide
to processes for its preparation, to its use for the treatment and/or prophylaxis of diseases and to its use for the preparation of medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and edemas, and also ophthalmic disorders, and its use to inhibit disturbing plasma kallikrein activity for the conduct of extracorporeal procedures and analytical assays.
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