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公开(公告)号：US20140256715A1
公开(公告)日：2014-09-11
申请号：US14350938
申请日：2012-10-11
申请人： Konstanze Hurth , Sebastien Jacquier , Rainer Machauer , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
发明人： Konstanze Hurth , Sebastien Jacquier , Rainer Machauer , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
IPC分类号： C07D265/30 , A61K31/5377 , C07D487/04 , A61K31/5375 , C07D471/04 , C07D417/12 , C07D413/12
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
摘要翻译： 本发明涉及式（I）的新的恶嗪衍生物及其药学上可接受的盐，其中所有变量如说明书，其药物组合物，其组合，及其作为药物的用途，特别是用于治疗 通过BACE-1或BACE-2的抑制来治疗阿尔茨海默病或糖尿病。
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公开(公告)号：US09714249B2
公开(公告)日：2017-07-25
申请号：US14892628
申请日：2014-05-27
申请人： Jutta Blank , Simona Cotesta , Vito Guagnano , Heinrich Rueeger
发明人： Jutta Blank , Simona Cotesta , Vito Guagnano , Heinrich Rueeger
IPC分类号： C07D487/04 , A61K31/4439 , A61K31/444 , A61K31/506
CPC分类号： C07D487/04 , A61K31/4439 , A61K31/444 , A61K31/506
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the pyrazolo-pyrrolidin-4-one derivatives, and their use as BET inhibitors for the treatment of conditions or diseases such as cancer. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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13.发明授权公开(公告)号：US09624247B2
公开(公告)日：2017-04-18
申请号：US14892623
申请日：2014-05-27
申请人： Jutta Blank , Guido Bold , Simona Cotesta , Vito Guagnano , Heinrich Rueeger
发明人： Jutta Blank , Guido Bold , Simona Cotesta , Vito Guagnano , Heinrich Rueeger
IPC分类号： C07D487/04 , C07D519/00 , A61K31/4192 , A61K31/437 , A61K31/5025
CPC分类号： C07D519/00 , A61K31/4192 , A61K31/437 , A61K31/5025 , C07D487/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (1) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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公开(公告)号：US09163011B2
公开(公告)日：2015-10-20
申请号：US13592580
申请日：2012-08-23
IPC分类号： A61K31/535 , C07D413/14 , A61K31/5355 , A61K45/06
CPC分类号： C07D413/14 , A61K31/5355 , A61K45/06
摘要： The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
摘要翻译： 本发明涉及式（I）的新的恶嗪衍生物及其药学上可接受的盐，其中所有变量如说明书，其药物组合物，其组合，及其作为药物的用途，特别是用于治疗 通过BACE-1或BACE-2的抑制来治疗阿尔茨海默病或糖尿病。
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公开(公告)号：US08865712B2
公开(公告)日：2014-10-21
申请号：US14136855
申请日：2013-12-20
申请人： Sangamesh Badiger , Murali Chebrolu , Konstanze Hurth , Sebastien Jacquier , Rainer Martin Lueoend , Rainer Machauer , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
发明人： Sangamesh Badiger , Murali Chebrolu , Konstanze Hurth , Sebastien Jacquier , Rainer Martin Lueoend , Rainer Machauer , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
IPC分类号： A61K31/5377 , C07D413/14 , C07D487/04 , C07D471/04
CPC分类号： C07D413/14 , A61K31/5377 , C07B59/002 , C07B2200/05 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
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16.发明授权公开(公告)号：US08093406B2
公开(公告)日：2012-01-10
申请号：US12500093
申请日：2009-07-09
申请人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
发明人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
IPC分类号： C07D335/02
CPC分类号： C07D335/02 , C07D409/10 , C07D409/12 , C07D413/12 , C07F7/0812
摘要： The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译： 本发明涉及下式的新型杂环化合物，其中所有变量如本说明书中所定义，以游离形式或盐形式，其制备方式，其用作药物和包含它们的药物。
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17.发明申请公开(公告)号：US20090054427A1
公开(公告)日：2009-02-26
申请号：US12196461
申请日：2008-08-22
申请人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
发明人： Emmanuelle Briard , Rainer Martin Lueoend , Rainer Machauer , Henrik Moebitz , Olivier Rogel , Jean-Michel Rondeau , Heinrich Rueeger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
IPC分类号： A61K31/5377 , C07D335/02 , A61K31/382 , A61P25/00 , C07D413/08
CPC分类号： C07D335/02 , C07D409/12
摘要： The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译： 本发明涉及下式的新型杂环化合物，其中所有变量如本说明书中所定义，以游离形式或盐形式，其制备方式，其用作药物和包含它们的药物。
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18.发明授权Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases 有权恶唑烷-2-酮嘧啶衍生物及其用于治疗依赖于PI3激酶的病症，疾病和病症的用途公开(公告)号：US09296733B2
公开(公告)日：2016-03-29
申请号：US14069400
申请日：2013-11-01
申请人： Robin Alec Fairhurst , Pascal Furet , Frank Stephan Kalthoff , Andreas Lerchner , Heinrich Rueeger
发明人： Robin Alec Fairhurst , Pascal Furet , Frank Stephan Kalthoff , Andreas Lerchner , Heinrich Rueeger
IPC分类号： A61K31/5377 , C07D413/14 , A61K45/06 , C07D417/14
CPC分类号： C07D417/14 , A61K31/5377 , A61K45/06 , C07D413/14
摘要： The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
摘要翻译： 本发明涉及作为PI3K（磷脂酰肌醇-3-激酶）抑制剂的恶唑烷-2-酮取代的嘧啶化合物及其药物组合物，其制备方法和用于治疗依赖于 PI3K。
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19.发明授权公开(公告)号：US08975417B2
公开(公告)日：2015-03-10
申请号：US14282515
申请日：2014-05-20
IPC分类号： C07D231/56 , A61K31/506 , C07D487/04 , A61K31/4439 , C07D471/04 , A61K31/437 , A61K31/501 , A61K31/423 , A61K31/4192 , A61K45/06
CPC分类号： A61K31/4439 , A61K31/4192 , A61K31/423 , A61K31/437 , A61K31/501 , A61K31/506 , A61K45/06 , C07D471/04 , C07D487/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐; 制备本发明化合物的方法及其治疗用途。 本发明还提供药理活性剂和药物组合物的组合。
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20.发明申请Oxazine Derivatives and their Use in the Treatment of Neurological Disorders 审中-公开恶嗪衍生物及其在神经障碍治疗中的应用公开(公告)号：US20130281449A1
公开(公告)日：2013-10-24
申请号：US13978885
申请日：2012-01-11
申请人： Konstanze Hurth , Rainer Martin Lueoend , Rainer Machauer , Ulf Neumann , Heinrich Rueeger , Michael Schaefer , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
发明人： Konstanze Hurth , Rainer Martin Lueoend , Rainer Machauer , Ulf Neumann , Heinrich Rueeger , Michael Schaefer , Marina Tintelnot-Blomley , Siem Jacob Veenstra , Markus Voegtle
IPC分类号： C07D413/12 , C07D471/04 , A61K45/06 , A61K31/5377
CPC分类号： C07D413/12 , A61K31/5377 , A61K45/06 , C07B2200/05 , C07D471/04
摘要： The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in pharmaceutically acceptable salt form, to their preparation, to their medical use and to medicaments comprising them.
摘要翻译： 本发明涉及式（I）的新型杂环化合物，其中所有变量如本说明书中所定义，以游离形式或药学上可接受的盐形式，其制备方法及其医疗用途以及包含它们的药物 。
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