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![2-amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides](/abs-image/US/2013/03/05/US08389513B2/abs.jpg.150x150.jpg)
11.发明授权2-amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides 失效2-氨基-5,5-二氟-5,6-二氢-4H- [1,3]恶嗪-4-基） - 苯基] - 酰胺公开(公告)号：US08389513B2
公开(公告)日：2013-03-05
申请号：US12959412
申请日：2010-12-03
申请人： David Banner , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Eoin Power , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
发明人： David Banner , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Eoin Power , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
IPC分类号： C07D265/04 , A61K31/33
CPC分类号： C07D265/08 , C07D413/12
摘要： The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译： 本发明涉及具有BACE1和/或BACE2抑制活性的式I的2-氨基-5,5-二氟-5,6-二氢-4H- [1,3]恶嗪-4-基） - 苯基] - 酰胺 ，它们的制造，含有它们的药物组合物及其作为治疗活性物质的用途。 本发明的活性化合物可用于例如治疗和/或预防性治疗。 阿尔茨海默病和2型糖尿病。
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公开(公告)号：US07964594B1
公开(公告)日：2011-06-21
申请号：US12958436
申请日：2010-12-02
IPC分类号： C07D265/04 , A61K31/33
CPC分类号： C07D413/12 , C07D265/08 , C07D417/12 , C07D495/04 , C07D498/04
摘要： This invention relates to 5,6-dihydro-4H-[1,3]oxazin-2-ylamine compounds of the formula wherein R1 to R5 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
摘要翻译： 本发明涉及下式的5,6-二氢-4H- [1,3]恶嗪-2-基胺化合物，其中R1至R5如说明书和权利要求书中所定义，以及其药学上可接受的盐。 这些化合物是BACE2抑制剂，可用作治疗或预防糖尿病等疾病的药物。
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公开(公告)号：US08748418B2
公开(公告)日：2014-06-10
申请号：US13415873
申请日：2012-03-09
申请人： Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Mark Rogers-Evans , Didier Rombach , Andrew Thomas , Thomas Woltering , Wolfgang Wostl
发明人： Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Mark Rogers-Evans , Didier Rombach , Andrew Thomas , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/553 , C07D413/02 , C07D267/10
CPC分类号： C07D267/10 , C07D413/12
摘要： The present invention relates to 1,4-Oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译： 本发明涉及具有BACE1和/或BACE2抑制活性的式I的1,4-氧氮杂，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。 本发明的活性化合物可用于例如治疗和/或预防性治疗。 阿尔茨海默病和2型糖尿病。
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公开(公告)号：US20120238548A1
公开(公告)日：2012-09-20
申请号：US13415873
申请日：2012-03-09
申请人： Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Mark Rogers-Evans , Didier Rombach , Andrew Thomas , Thomas Woltering , Wolfgang Wostl
发明人： Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Mark Rogers-Evans , Didier Rombach , Andrew Thomas , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/553 , C07D413/12 , A61P25/28 , A61P9/00 , A61P19/02 , A61P29/00 , A61P35/00 , A61P9/10 , A61P1/00 , C07D267/10 , A61P37/06
CPC分类号： C07D267/10 , C07D413/12
摘要： The present invention relates to 1,4-Oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译： 本发明涉及具有BACE1和/或BACE2抑制活性的式I的1,4-氧氮杂，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。 本发明的活性化合物可用于例如治疗和/或预防性治疗。 阿尔茨海默病和2型糖尿病。
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![3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINES](/abs-image/US/2011/02/24/US20110046122A1/abs.jpg.150x150.jpg)
公开(公告)号：US20110046122A1
公开(公告)日：2011-02-24
申请号：US12852538
申请日：2010-08-09
申请人： Matteo Andreini , David Banner , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Roger-Evans , Massimiliano Travagli , Michela Valacchi , Thomas Woltering , Wolfgang Wostl
发明人： Matteo Andreini , David Banner , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Roger-Evans , Massimiliano Travagli , Michela Valacchi , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/5377 , C07D413/12 , C07D265/30 , C07D409/14 , A61K31/5375 , A61P3/10 , A61P25/28 , A61P29/00 , A61P35/00 , A61P9/00 , A61P19/02
CPC分类号： C07D413/12 , C07D265/30 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译： 本发明涉及具有BACE1和/或BACE2抑制活性的式I的3-氨基-5-苯基-5,6-二氢-2H- [1,4]恶嗪，其制备方法，含有它们的药物组合物及其作为 治疗活性物质。 本发明的活性化合物可用于例如治疗和/或预防性治疗。 阿尔茨海默病和2型糖尿病。
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公开(公告)号：US09242943B2
公开(公告)日：2016-01-26
申请号：US13348675
申请日：2012-01-12
申请人： Matteo Andreini , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Massimiliano Travagli , Thomas Woltering , Wolfgang Wostl , Harald Mauser
发明人： Matteo Andreini , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Massimiliano Travagli , Thomas Woltering , Wolfgang Wostl , Harald Mauser
IPC分类号： C07D265/30 , C07D413/12 , A61K31/5375 , A61K31/5377 , A61P25/28
CPC分类号： C07D265/30 , C07D413/12
摘要： The present invention relates to 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译： 本发明涉及具有BACE1和/或BACE2抑制活性的1,4型恶唑酸，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。 本发明的活性化合物可用于例如治疗和/或预防性治疗。 阿尔茨海默病和2型糖尿病。
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公开(公告)号：US20120184540A1
公开(公告)日：2012-07-19
申请号：US13348675
申请日：2012-01-12
申请人： Matteo Andreini , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Massimiliano Travagli , Thomas Woltering , Wolfgang Wostl , Harald Mauser
发明人： Matteo Andreini , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Massimiliano Travagli , Thomas Woltering , Wolfgang Wostl , Harald Mauser
IPC分类号： A61K31/5375 , C07D413/12 , A61K31/5377 , A61P25/28 , A61P9/00 , A61P7/02 , A61P37/00 , A61P29/00 , A61P35/00 , C07D265/30 , A61P3/10
CPC分类号： C07D265/30 , C07D413/12
摘要： The present invention relates to 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译： 本发明涉及具有BACE1和/或BACE2抑制活性的1,4型恶唑酸，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。 本发明的活性化合物可用于例如治疗和/或预防性治疗。 阿尔茨海默病和2型糖尿病。
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公开(公告)号：US08501940B2
公开(公告)日：2013-08-06
申请号：US12491278
申请日：2009-06-25
IPC分类号： C07D237/36 , A01N43/58
CPC分类号： C07D237/28 , C07D403/04
摘要： Provided herein are compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof, which are useful as pharmaceutical compositions for the treatment of metabolic diseases and disorders.
摘要翻译： 本文提供了式（I）化合物：及其药学上可接受的盐和酯，其可用作治疗代谢疾病和病症的药物组合物。
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19.发明授权公开(公告)号：US08129423B2
公开(公告)日：2012-03-06
申请号：US11871318
申请日：2007-10-12
申请人： Jean Ackermann , Kurt Amrein , Daniel Hunziker , Bernd Kuhn , Alexander V. Mayweg , Werner Neidhart , Tadakatsu Takahashi
发明人： Jean Ackermann , Kurt Amrein , Daniel Hunziker , Bernd Kuhn , Alexander V. Mayweg , Werner Neidhart , Tadakatsu Takahashi
IPC分类号： A61K31/4152 , A61K31/4166 , C07D233/02
CPC分类号： C07D233/02 , A61K9/2054 , A61K9/4866 , C07D233/06 , C07D233/10 , C07D233/28 , C07D471/06 , C07D471/10
摘要： Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
摘要翻译： 式的化合物及其药学上可接受的盐和酯，其中R 1至R 6具有权利要求1中给出的含义，可以以药物组合物的形式使用。
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公开(公告)号：US20130072679A1
公开(公告)日：2013-03-21
申请号：US13612956
申请日：2012-09-13
申请人： Johannes Aebi , Kurt Amrein , Benoit Hornsperger , Henner Knust , Bernd Kuhn , Yongfu Liu , Hans P. Maerki , Alexander V. Mayweg , Peter Mohr , Xuefei Tan , Mingwei Zhou
发明人： Johannes Aebi , Kurt Amrein , Benoit Hornsperger , Henner Knust , Bernd Kuhn , Yongfu Liu , Hans P. Maerki , Alexander V. Mayweg , Peter Mohr , Xuefei Tan , Mingwei Zhou
IPC分类号： C07D401/14 , C07D417/14 , C07D471/06 , C07D471/04 , C07D413/14 , C07D405/14 , C07D401/10 , C07D487/10
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/10 , C07F7/1804
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R1，R2，R3，R4，R5，R6，R7，A1，A2和A3如本文所述，包括该化合物的组合物和使用该化合物的方法。 这些化合物可用于治疗或预防哺乳动物，特别是用于治疗或预防慢性肾脏疾病，充血性心力衰竭，高血压，原发性醛固酮增多症和库兴综合征的醛固酮合酶（CYP11B2或CYP11B1）抑制剂。
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