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公开(公告)号：US20120196863A1
公开(公告)日：2012-08-02
申请号：US13357640
申请日：2012-01-25
申请人： Matteo Andreini , Emanuele Gabellieri , Robert Narquizian , Massimiliano Travagli , Wolfgang Wostl
发明人： Matteo Andreini , Emanuele Gabellieri , Robert Narquizian , Massimiliano Travagli , Wolfgang Wostl
IPC分类号： A61K31/5375 , C07D413/10 , A61K31/5377 , C07D413/14 , A61P3/10 , A61P25/28 , A61P29/00 , A61P37/02 , A61P35/00 , A61P9/10 , A61P25/00 , A61P17/00 , A61P1/00 , A61P5/00 , A61P19/02 , A61P21/00 , C07D265/30
CPC分类号： C07D413/10 , C07D265/30
摘要： The present invention provides 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： 本发明提供了具有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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![3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINES](/abs-image/US/2012/08/23/US20120214806A1/abs.jpg.150x150.jpg)
公开(公告)号：US20120214806A1
公开(公告)日：2012-08-23
申请号：US13460905
申请日：2012-05-01
申请人： Matteo Andreini , David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Rogers-Evans , Massimiliano Travagli , Michela Valacchi , Thomas Woltering , Wolfgang Wostl
发明人： Matteo Andreini , David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Eoin Power , Mark Rogers-Evans , Massimiliano Travagli , Michela Valacchi , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/5377 , C07D265/30 , A61K31/5375 , C07D471/04 , C07D417/12 , C07D413/14 , A61P3/10 , A61P25/28 , A61P3/00 , A61P7/02 , A61P37/00 , A61P29/00 , A61P35/00 , A61P9/10 , A61P25/00 , A61P17/00 , A61P1/00 , A61P5/16 , A61P19/04 , A61P19/02 , C07D265/32 , C07D413/12
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：US07989449B2
公开(公告)日：2011-08-02
申请号：US12369782
申请日：2009-02-12
申请人： Matteo Andreini , Emanuele Gabellieri , Wolfgang Guba , Guido Marconi , Robert Narquizian , Eoin Power , Massimiliano Travagli , Thomas Woltering , Wolfgang Wostl
发明人： Matteo Andreini , Emanuele Gabellieri , Wolfgang Guba , Guido Marconi , Robert Narquizian , Eoin Power , Massimiliano Travagli , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/421 , A61K31/506 , A61K31/4439 , A61K31/538 , C07D263/28 , C07D413/10
CPC分类号： C07D263/28 , C07D413/10
摘要： The present invention relates to a compounds of formula I wherein R1, R1′, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (β-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
摘要翻译： 本发明涉及式I化合物，其中R 1，R 1'，R 2，R 3，R 4，X，Ar和m如说明书和权利要求中所定义，及其药学上活性的酸加成盐。 本发明的化合物具有Asp2（＆bgr-分泌酶，BACE1或Memapsin-2）抑制活性，并且可用于治疗特征在于升高的淀粉样蛋白水平或淀粉样蛋白沉积物，特别是阿尔茨海默病的疾病。
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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：US08815881B2
公开(公告)日：2014-08-26
申请号：US13196933
申请日：2011-08-03
申请人： David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Benoit Hornsperger , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
发明人： David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Benoit Hornsperger , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
IPC分类号： C07D239/22 , A61K31/513
CPC分类号： C07D417/12 , A61K31/513 , C07D239/22 , C07D239/70 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
摘要翻译： 本发明涉及下式化合物或其药学上可接受的盐：其中R 1至R 9如下所述。 这些化合物是BACE2抑制剂，可用作治疗和/或预防性治疗诸如糖尿病，特别是2型糖尿病和其它代谢疾病的药物。
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公开(公告)号：US08399459B2
公开(公告)日：2013-03-19
申请号：US13357640
申请日：2012-01-25
申请人： Matteo Andreini , Emanuele Gabellieri , Robert Narquizian , Massimiliano Travagli , Wolfgang Wostl
发明人： Matteo Andreini , Emanuele Gabellieri , Robert Narquizian , Massimiliano Travagli , Wolfgang Wostl
IPC分类号： A61K31/535 , C07D265/28
CPC分类号： C07D413/10 , C07D265/30
摘要： The present invention provides 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： 本发明提供了具有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：US20120035195A1
公开(公告)日：2012-02-09
申请号：US13196933
申请日：2011-08-03
申请人： David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Benoit Hornsperger , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
发明人： David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Benoit Hornsperger , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/513 , A61P3/10 , C07D239/47
CPC分类号： C07D417/12 , A61K31/513 , C07D239/22 , C07D239/70 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
摘要翻译： 本发明涉及下式化合物或其药学上可接受的盐：其中R 1至R 9如下所述。 这些化合物是BACE2抑制剂，可用作治疗和/或预防性治疗诸如糖尿病，特别是2型糖尿病和其它代谢疾病的药物。
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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：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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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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