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公开(公告)号：US08039455B2
公开(公告)日：2011-10-18
申请号：US12159742
申请日：2006-12-28
申请人： Claudia Betschart , Manuel Koller , Kurt Laumen , Andreas Lerchner , Rainer Machauer , Clive McCarthy , Marina Tintelnot-Blomley , Siem Jacob Veenstra
发明人： Claudia Betschart , Manuel Koller , Kurt Laumen , Andreas Lerchner , Rainer Machauer , Clive McCarthy , Marina Tintelnot-Blomley , Siem Jacob Veenstra
IPC分类号： C07D245/04 , A61K31/33
CPC分类号： C07D245/04 , C07D273/00
摘要： The invention relates to novel macrocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition 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大环化合物，其中所有变量如本说明书中所定义，游离碱形式或酸加成盐形式，其制备方法，用作药物和包含它们的药物。
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公开(公告)号：US20090029960A1
公开(公告)日：2009-01-29
申请号：US12159742
申请日：2006-12-28
申请人： Claudia Betschart , Manuel Koller , Kurt Laumen , Andreas Lerchner , Rainer Machauer , Clive McCarthy , Marina Tintelnot-Blomley , Siem Jacob Veenstra
发明人： Claudia Betschart , Manuel Koller , Kurt Laumen , Andreas Lerchner , Rainer Machauer , Clive McCarthy , Marina Tintelnot-Blomley , Siem Jacob Veenstra
IPC分类号： A61K31/33 , C07D225/00 , A61P25/00
CPC分类号： C07D245/04 , C07D273/00
摘要： The invention relates to novel macrocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition 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大环化合物，其中所有变量如本说明书中所定义，游离碱形式或酸加成盐形式，其制备方法，用作药物和包含它们的药物。
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公开(公告)号：US20080132477A1
公开(公告)日：2008-06-05
申请号：US11794413
申请日：2006-01-13
申请人： Claudia Betschart , Andreas Lerchner , Rainer Machauer , Heinrich Rueger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
发明人： Claudia Betschart , Andreas Lerchner , Rainer Machauer , Heinrich Rueger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
IPC分类号： A61K31/395 , C07D487/02
CPC分类号： C07D273/00 , C07D245/04 , C07D273/02 , C07D413/04 , C07D413/12 , C07D413/14 , C07D471/08
摘要： The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译： 本发明涉及式（I）的新型大环化合物，其中所有变量如说明书中所定义，大环中包括的环原子数为14,15,16或17，游离碱形式 或以酸加成盐形式，其制备，用作药物和包含它们的药物。
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公开(公告)号：US07612055B2
公开(公告)日：2009-11-03
申请号：US10577260
申请日：2004-11-04
申请人： Yves Auberson , Claudia Betschart , Ralf Glatthar , Kurt Laumen , Rainer Machauer , Marina Tintelnot-Blomley , Thomas J. Troxler , Siem Jacob Veenstra
发明人： Yves Auberson , Claudia Betschart , Ralf Glatthar , Kurt Laumen , Rainer Machauer , Marina Tintelnot-Blomley , Thomas J. Troxler , Siem Jacob Veenstra
IPC分类号： A01N43/00 , A61K31/33 , C07D245/00
CPC分类号： C07D245/02 , C07D255/00 , C07D273/00 , C07D281/00 , C07D471/08 , C07D513/08
摘要： The present invention relates to novel macrocyclic compounds of the formula wherein R1, R2, R3, U, V, W, X, Y, Z and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
摘要翻译： 本发明涉及下式的新型大环化合物其中R1，R2，R3，U，V，W，X，Y，Z和n如说明书中所定义，大环中包括的环原子数为14 ，15,16或17，以游离碱形式或以酸加成盐形式，用于制备，用作药物和包含它们的药物组合物。
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公开(公告)号：US20100022500A1
公开(公告)日：2010-01-28
申请号：US12566928
申请日：2009-09-25
申请人： Yves AUBERSON , Claudia Betschart , Ralf Glatthar , Kurt Laumen , Rainer MacHauer , Marina Tintelnot-Blomley , Thomas J. Troxler , Siem Jacob Veenstra
发明人： Yves AUBERSON , Claudia Betschart , Ralf Glatthar , Kurt Laumen , Rainer MacHauer , Marina Tintelnot-Blomley , Thomas J. Troxler , Siem Jacob Veenstra
IPC分类号： A61K31/395 , C07D245/02 , C07D291/02 , A61P25/00
CPC分类号： C07D245/02 , C07D255/00 , C07D273/00 , C07D281/00 , C07D471/08 , C07D513/08
摘要： The present invention relates to novel macrocyclic compounds of the formula wherein R1, R2, R3, U, V, W, X, Y, Z and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
摘要翻译： 本发明涉及下式的新型大环化合物其中R1，R2，R3，U，V，W，X，Y，Z和n如说明书中所定义，大环中包括的环原子数为14 ，15,16或17，以游离碱形式或以酸加成盐形式，用于制备，用作药物和包含它们的药物组合物。
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公开(公告)号：US20090312370A1
公开(公告)日：2009-12-17
申请号：US12374467
申请日：2007-07-20
IPC分类号： A61K31/4439 , C07D211/70 , A61K31/44 , C07D413/12
CPC分类号： C07D273/00 , C07D245/06 , C07D273/02 , C07D401/12 , C07D413/12 , C07D413/14
摘要： The invention relates to novel macrocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition 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大环化合物，其中所有变量如本说明书中所定义，游离碱形式或酸加成盐形式，其制备方法，用作药物和包含它们的药物。
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公开(公告)号：US09284284B2
公开(公告)日：2016-03-15
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 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , A61K31/5375 , A61K31/5377
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.
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8.发明申请公开(公告)号：US20100056490A1
公开(公告)日：2010-03-04
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： A61K31/397 , C07D401/12 , C07D205/02 , C07D335/02 , A61K31/4535 , A61K31/382 , A61P25/00 , A61P9/10
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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![Dibenzo[b,f]oxepine-10-carboxamides and pharmaceutical uses thereof](/abs-image/US/2009/11/03/US07612054B2/abs.jpg.150x150.jpg)
9.发明授权公开(公告)号：US07612054B2
公开(公告)日：2009-11-03
申请号：US10565456
申请日：2004-07-23
申请人： Yves Auberson , Claudia Betschart , Stefanie Flohr , Ralf Glatthar , Oliver Simic , Marina Tintelnot-Blomley , Thomas J. Troxler , Eric Vangrevelinghe , Siem Jacob Veenstra
发明人： Yves Auberson , Claudia Betschart , Stefanie Flohr , Ralf Glatthar , Oliver Simic , Marina Tintelnot-Blomley , Thomas J. Troxler , Eric Vangrevelinghe , Siem Jacob Veenstra
IPC分类号： A01N43/00 , A61K31/33 , C07D313/00
CPC分类号： C07D405/12 , C07C235/82 , C07C2603/32 , C07D313/14 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04
摘要： The present invention pertains to novel dibenzo[b,f]oxepine-10-carboxamides compound to a process for the preparation of such compounds of formula I, their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula I.
摘要翻译： 本发明涉及新的二苯并[b，f]氧杂七环素-10-甲酰胺化合物，其用于制备式I化合物的方法，它们作为药物的用途，特别是用于治疗与β-谷氨酸相关的神经和血管疾病， 淀粉样蛋白生成和/或聚集，以及包含式I化合物的药物组合物和组合。
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10.发明授权Heterocyclic derivatives and their use in the treatment of neurological disorders 有权杂环衍生物及其在治疗神经系统疾病中的应用公开(公告)号：US09550758B2
公开(公告)日：2017-01-24
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： A61K31/5377 , C07D413/14 , C07D471/04 , C07D487/04 , C07B59/00
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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