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1.发明申请公开(公告)号：US20140349990A1
公开(公告)日：2014-11-27
申请号：US14282515
申请日：2014-05-20
申请人： Jutta BLANK , Vincent BORDAS , Simona COTESTA , Vito GUAGNANO , Heinrich RUEEGER , Andrea VAUPEL
发明人： Jutta BLANK , Vincent BORDAS , Simona COTESTA , Vito GUAGNANO , Heinrich RUEEGER , Andrea VAUPEL
IPC分类号： A61K31/506 , A61K31/4439 , C07D471/04 , A61K45/06 , A61K31/501 , A61K31/423 , A61K31/4192 , C07D487/04 , A61K31/437
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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2.发明申请公开(公告)号：US20160108047A1
公开(公告)日：2016-04-21
申请号：US14892616
申请日：2014-05-26
申请人： Jutta BLANK , Guido BOLD , Simona COTESTA , Vito GUAGNANO , Heinrich RUEEGER , Andrea VAUPEL
发明人： Jutta BLANK , Guido BOLD , Simona COTESTA , Vito GUAGNANO , Heinrich RUEEGER , Andrea VAUPEL
IPC分类号： C07D487/04 , A61K31/444 , A61K31/5377 , A61K31/513 , A61K31/5025 , A61K31/4439 , A61K31/4192 , C07D471/04
CPC分类号： C07D487/04 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/5025 , A61K31/513 , A61K31/5377 , C07D471/04
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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3.发明申请公开(公告)号：US20160095843A1
公开(公告)日：2016-04-07
申请号：US14892613
申请日：2014-05-26
申请人： Jutta BLANK , Vincent BORDAS , Simona COTESTA , Vito NANO , Heinrich RUEEGER , Andrea VAUPEL
发明人： Jutta BLANK , Vincent BORDAS , Simona COTESTA , Vito GUAGNANO , Heinrich RUEEGER , Andrea VAUPEL
IPC分类号： A61K31/4439 , A61K31/437
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，本发明化合物的制备方法及其治疗用途。 本发明还提供药理活性剂和药物组合物的组合。
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4.发明申请PYRAZOLO-PYRROLIDIN-4-ONE DERIVATIVES AS BET INHIBITORS AND THEIR USE IN THE TREATMENT OF DISEASE 有权吡唑并吡啶-4-酮衍生物作为抑制剂及其在治疗疾病中的应用公开(公告)号：US20160102107A1
公开(公告)日：2016-04-14
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： C07D519/00 , A61K31/5025 , A61K31/4192 , A61K31/437 , C07D487/04
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; (I) 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; （I）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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5.发明申请PYRAZOLO-PYRROLIDIN-4-ONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE 有权吡咯并吡啶-4-酮衍生物及其在治疗疾病中的应用公开(公告)号：US20160096843A1
公开(公告)日：2016-04-07
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 , A61K31/444 , A61K31/506 , A61K31/4439
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.
摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐; 制备吡唑并吡咯烷-4-酮衍生物的方法及其作为治疗癌症等疾病或疾病的BET抑制剂的用途。 本发明还提供药理活性剂和药物组合物的组合。
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6.发明申请Novel Heterocyclic Derivatives and Their Use in the Treatment of Neurological Disorders 有权新型杂环衍生物及其在神经障碍治疗中的应用公开(公告)号：US20140107118A1
公开(公告)日：2014-04-17
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： C07D413/14 , C07D487/04 , C07D471/04 , A61K31/5377
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.
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，其药物组合物，其组合及其作为药物的用途，特别是用于通过BACE-抑制剂的抑制治疗阿尔茨海默病或糖尿病， 1或BACE-2。
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公开(公告)号：US20130172331A1
公开(公告)日：2013-07-04
申请号：US13592580
申请日：2012-08-23
IPC分类号： 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.
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8.发明申请Novel Heterocyclic Derivatives and Their Use in the Treatment of Neurological Disorders 审中-公开新型杂环衍生物及其在神经障碍治疗中的应用公开(公告)号：US20150203481A1
公开(公告)日：2015-07-23
申请号：US14482662
申请日：2014-09-10
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： C07D413/14 , C07D487/04 , C07D471/04 , A61K31/5377
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.
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，其药物组合物，其组合及其作为药物的用途，特别是用于通过BACE-抑制剂的抑制治疗阿尔茨海默病或糖尿病， 1或BACE-2。
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9.发明申请公开(公告)号：US20150150877A1
公开(公告)日：2015-06-04
申请号：US14615418
申请日：2015-02-05
IPC分类号： A61K31/5355
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 通过抑制BACE-1或BACE-2来治疗阿尔茨海默病或糖尿病。
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10.发明申请公开(公告)号：US20110021520A1
公开(公告)日：2011-01-27
申请号：US12842360
申请日：2010-07-23
申请人： Sangamesh BADIGER , Murali CHEBROLU , Mathias FREDERIKSEN , Philipp HOLZER , Konstanze HURTH , Rainer Martin LUEOEND , Rainer MACHAUER , Henrik MOEBITZ , Ulf NEUMANN , Rita RAMOS , Heinrich RUEEGER , Marina TINTELNOT-BLOMLEY , Siem Jacob VEENSTRA , Markus VOEGTLE
发明人： Sangamesh BADIGER , Murali CHEBROLU , Mathias FREDERIKSEN , Philipp HOLZER , Konstanze HURTH , Rainer Martin LUEOEND , Rainer MACHAUER , Henrik MOEBITZ , Ulf NEUMANN , Rita RAMOS , Heinrich RUEEGER , Marina TINTELNOT-BLOMLEY , Siem Jacob VEENSTRA , Markus VOEGTLE
IPC分类号： A61K31/5377 , C07D413/12 , C07D419/12 , C07D265/30 , A61K31/5375 , A61P25/28
CPC分类号： C07D487/04 , A61K31/5377 , A61K31/553 , A61K45/06 , C07D265/30 , C07D267/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
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 medical use 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，其医疗用途和包含它们的药物。
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