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公开(公告)号：US20150005309A1
公开(公告)日：2015-01-01
申请号：US14370831
申请日：2013-01-08
发明人： Lars Bärfacker , William Scott , Andrea Hägebarth , Stuart Ince , Hartmut Rehwinkel , Oliver Politz , Roland Neuhaus , Ulf Bömer
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/4985 , A61K45/06 , A61K2300/00
摘要： Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
摘要翻译： 作为Pi3K / Akt途径的有效抑制剂的式（I）化合物，其制备方法及其作为药物的用途。
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公开(公告)号：US09260435B2
公开(公告)日：2016-02-16
申请号：US14370831
申请日：2013-01-08
发明人： Lars Bärfacker , William Scott , Andrea Hägebarth , Stuart Ince , Hartmut Rehwinkel , Oliver Politz , Roland Neuhaus , Ulf Bömer
IPC分类号： C07D487/04 , A61K45/06 , A61K31/4985
CPC分类号： C07D487/04 , A61K31/4985 , A61K45/06 , A61K2300/00
摘要： Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
摘要翻译： 作为Pi3K / Akt途径的有效抑制剂的式（I）化合物，其制备方法及其作为药物的用途。
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公开(公告)号：US09370517B2
公开(公告)日：2016-06-21
申请号：US14371567
申请日：2013-01-08
发明人： Lars Bärfacker , William Scott , Andrea Hägebarth , Hartmut Rehwinkel , Oliver Politz , Roland Neuhaus , Ulf Bömer
IPC分类号： A61K31/519 , C07D487/04 , A61K45/06
CPC分类号： A61K31/519 , A61K45/06 , C07D487/04
摘要： Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
摘要翻译： 作为Pi3K / Akt途径的有效抑制剂的式（I）化合物，其制备方法及其作为药物的用途。
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公开(公告)号：US09604989B2
公开(公告)日：2017-03-28
申请号：US14792205
申请日：2015-07-06
发明人： Lars Bärfacker , William Scott , Andrea Hägebarth , Stuart Ince , Hartmut Rehwinkel , Oliver Politz , Roland Neuhaus , Hans Briem , Ulf Bömer
IPC分类号： C07D487/04 , A61K31/5025 , A61K45/06
CPC分类号： C07D487/04 , A61K31/5025 , A61K45/06
摘要： The present invention relates to a method for the treatment of a cancer that is sensitive to Pi3K/Akt pathway inhibition by administering a therapeutically effective amount of a compound of formula (I)
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5.发明授权Substituted 4-aryl-1,4-dihydro-1,6-naphthyridine amides and their use 有权取代的4-芳基-1,4-二氢-1,6-萘啶酰胺及其用途公开(公告)号：US09051316B2
公开(公告)日：2015-06-09
申请号：US13801376
申请日：2013-03-13
发明人： Lars Bärfacker , Peter Kolkhof , Karl-Heinz Schlemmer , Rolf Grosser , Adam Nitsche , Martina Klein , Klaus Münter , Barbara Albrecht-Küpper , Elke Hartmann
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, a process 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 cardiovascular disorders.
摘要翻译： 本申请涉及新的取代的4-芳基-1,4-二氢-1,6-二氮杂萘-3-甲酰胺，其制备方法，其用于治疗和/或预防疾病的用途及其用于 制造用于治疗和/或预防疾病，特别是心血管疾病的药物。
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公开(公告)号：US09682995B2
公开(公告)日：2017-06-20
申请号：US14764853
申请日：2014-01-28
发明人： Lars Bärfacker , Stefan Prechtl , Gerhard Siemeister , Antje Margret Wengner , Jens Ackerstaff , Katrin Nowak-Reppel , Benjamin Bader , Philip Lienau , Detlef Stöckigt , Tobias Heinrich
IPC分类号： C07D417/12 , C07D417/14 , C07D495/04 , C07D487/04 , C07D513/04
CPC分类号： C07D495/04 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention relates to isothiazoles of general formula (I) which inhibit the mitotic checkpoint: in which A, R1 and R2 are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US10350206B2
公开(公告)日：2019-07-16
申请号：US15512494
申请日：2015-09-17
发明人： Anne Mengel , Hans-Georg Lerchen , Manfred Möwes , Thomas Müller , Lars Bärfacker , Marion Hitchcock , Arwed Cleve , Joachim Kuhnke , Hans Briem , Gerhard Siemeister , Wilhelm Bone , Amaury Ernesto Fernandez-Montalvan , Jens Schröder , Ursula Mönning , Simon Holton
IPC分类号： A61K31/506 , C07D401/14 , C07D403/14
摘要： Compounds of formula (I) as defined herein and their use as pharmaceuticals.
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公开(公告)号：US10428044B2
公开(公告)日：2019-10-01
申请号：US15317924
申请日：2015-06-17
发明人： Keith Graham , Ulrich Klar , Hans Briem , Marion Hitchcock , Lars Bärfacker , Knut Eis , Volker Schulze , Gerhard Siemeister , Wilhelm Bone , Jens Schröder , Simon Holton , Philip Lienau , René Tempel , Helmut Sonnenschein , Jozsef Bálint , Heinz Graubaum
IPC分类号： C07D401/04 , A61K31/4439 , C07D403/04 , A61K31/506 , C07D401/14 , A61K31/444 , C07D405/14 , C07D471/04 , A61K31/437 , A61K31/501 , A61K31/4725 , C07D409/14 , A61K31/4709 , A61K31/5377 , C07D491/056 , A61K31/436 , C07D417/14 , C07D413/14 , A61K45/06
摘要： Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.
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公开(公告)号：US10047096B2
公开(公告)日：2018-08-14
申请号：US15529043
申请日：2015-11-23
发明人： Andreas Schall , Jürgen Klar , Mario Lobell , Hartmut Schirok , Joachim Telser , Steffen Müller , Dirk Brohm , Hans Briem , Hannah Jörißen , Joerg Keldenich , Michael Böttger , Georges Von Degenfeld , Thomas Schlange , Ulf Bömer , Niels Lindner , Hanna Eilken , Dmitrij Hristodorov , Pierre Wasnaire , Kersten Matthias Gericke , Lars Bärfacker
IPC分类号： A61K31/551 , C07D471/04 , C07D487/04 , A61K31/5513 , A61K39/395
摘要： The present application relates to novel (3-hydroxyphenyl)amino-substituted pyrido[2,3-b][1,5]benzodiazepin-5-one derivatives, to processes for preparation thereof, to the use thereof alone or in combination for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially of angiogenic disorders and hyperproliferative disorders in which neovascularization plays a role, for example ophthalmological disorders and cancers and tumours. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.
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公开(公告)号：US09745285B2
公开(公告)日：2017-08-29
申请号：US14900548
申请日：2014-06-17
发明人： Anne Mengel , Marion Hitchcock , Anja Richter , Lars Bärfacker , Hans Briem , Gerhard Siemeister , Wilhelm Bone , Amaury Ernesto Fernandez-Montalvan , Jens Schröder , Simon Holton , Cornelia Preuβe , Ursula Mönning
IPC分类号： C07D401/14 , A61K31/506 , A61K45/06 , C07D413/14
CPC分类号： C07D401/14 , A61K31/506 , A61K45/06 , C07D413/14
摘要： Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.
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