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1. 发明授权

US08785436B2 1,3-oxazines as BACE 1 and/or BACE2 inhibitors 失效
标题翻译：作为BACE1和/或BACE2抑制剂的1,3-恶嗪
公开(公告)号：US08785436B2
公开(公告)日：2014-07-22
申请号：US13467085
申请日：2012-05-09
申请人： Hans Hilpert , Robert Narquizian , Emmanuel Pinard , Alessandra Polara , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
发明人： Hans Hilpert , Robert Narquizian , Emmanuel Pinard , Alessandra Polara , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
IPC分类号： C07D413/04 , C07D413/10 , C07D413/12 , A61K31/5355
CPC分类号： C07D413/10 , C07D265/08 , C07D413/12
摘要： The present invention provides compounds 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：本发明提供具有BACE1和/或BACE2抑制活性的式I化合物，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。

2. 发明申请

US20120295900A1 1,3-OXAZINES AS BACE 1 AND/OR BACE2 INHIBITORS 失效
标题翻译： 1,3-氧化物作为BACE 1和/或BACE2抑制剂
公开(公告)号：US20120295900A1
公开(公告)日：2012-11-22
申请号：US13467085
申请日：2012-05-09
申请人： Hans Hilpert , Robert Narquizian , Emmanuel Pinard , Alessandra Polara , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
发明人： Hans Hilpert , Robert Narquizian , Emmanuel Pinard , Alessandra Polara , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/5355 , C07D265/08 , C07D413/14 , A61K31/538 , C07D495/04 , A61P25/28 , A61P3/10 , A61P7/02 , A61P37/00 , A61P29/00 , A61P35/00 , A61P9/10 , A61P25/00 , A61P17/00 , A61P1/00 , A61P5/16 , A61P19/02 , A61K31/535 , C07D413/10 , C07D413/04 , A61P3/00 , C07D413/12
CPC分类号： C07D413/10 , C07D265/08 , C07D413/12
摘要： The present invention provides compounds 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：本发明提供具有BACE1和/或BACE2抑制活性的式I化合物，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。

3. 发明授权

US09073909B2 [1,3]oxazines 有权
标题翻译： [1,3]恶嗪
公开(公告)号：US09073909B2
公开(公告)日：2015-07-07
申请号：US14118754
申请日：2012-06-04
申请人： Edilio Boroni , Luca Gobbi , Hans Hilpert , Michael Honer , Dieter Murl , Robert Narquizian , Alessandra Polara
发明人： Edilio Boroni , Luca Gobbi , Hans Hilpert , Michael Honer , Dieter Murl , Robert Narquizian , Alessandra Polara
IPC分类号： C07D413/12 , C07D265/06 , A61K31/535 , A61K31/5355
CPC分类号： C07D413/12
摘要： The present invention provides compounds 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. The invention further provides a radio-labelled derivative thereof.
摘要翻译：本发明提供具有BACE1和/或BACE2抑制活性的式I化合物，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。本发明还提供其放射性标记的衍生物。

4. 发明申请

US20140112867A1 [1,3]OXAZINES 有权
标题翻译： [1,3] OXAZINES
公开(公告)号：US20140112867A1
公开(公告)日：2014-04-24
申请号：US14118754
申请日：2012-06-04
申请人： Edilio Borroni , Luca Gobbi , Hans Hilpert , Michael Honer , Dieter Muri , Robert Narquizian , Alessandra Polara
发明人： Edilio Borroni , Luca Gobbi , Hans Hilpert , Michael Honer , Dieter Muri , Robert Narquizian , Alessandra Polara
IPC分类号： C07D413/12
CPC分类号： C07D413/12
摘要： The present invention provides compounds 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. The invention further provides a radio-labelled derivative thereof.
摘要翻译：本发明提供具有BACE1和/或BACE2抑制活性的式I化合物，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。本发明还提供其放射性标记的衍生物。

5. 发明申请

US20120108609A1 DIHYDROOXAZOL-2-AMINE DERIVATIVES 有权
标题翻译：二氢异喹啉-2-胺衍生物
公开(公告)号：US20120108609A1
公开(公告)日：2012-05-03
申请号：US13279362
申请日：2011-10-24
申请人： Matthias Nettekoven , Roger Norcross , Alessandra Polara
发明人： Matthias Nettekoven , Roger Norcross , Alessandra Polara
IPC分类号： A61K31/421 , A61K31/4709 , C07D263/28 , A61K31/4439 , C07D413/14 , A61K31/444 , A61K31/506 , A61K31/497 , A61P25/00 , A61P25/18 , A61P25/16 , A61P3/00 , A61P25/30 , A61P3/10 , A61P3/04 , A61P3/06 , A61P25/28 , A61P25/06 , A61P25/08 , A61P9/12 , A61P9/00 , C07D413/12
CPC分类号： C07D263/28 , C07D263/16 , C07D413/12 , C07D413/14
摘要： The invention relates to compounds of formula wherein R1, R2, R3, R4, X, Ar, and are defined herein or to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.
摘要翻译：本发明涉及下式的化合物，其中R 1，R 2，R 3，R 4，X，Ar和本文定义或其药学上合适的酸加成盐。式I化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是TAAR1。这些化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢紊乱，如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡失调和失眠，睡眠障碍和昼夜节律和心血管疾病。

6. 发明申请

US20110112080A1 OXAZOLINE DERIVATIVES 失效
标题翻译：氧杂环丁烷衍生物
公开(公告)号：US20110112080A1
公开(公告)日：2011-05-12
申请号：US12938401
申请日：2010-11-03
申请人： Guido Galley , Roger Norcross , Alessandra Polara
发明人： Guido Galley , Roger Norcross , Alessandra Polara
IPC分类号： A61K31/541 , C07D263/28 , C07D413/10 , C07D413/12 , C07D413/14 , C07D471/04 , C07D417/14 , C07D417/12 , A61K31/421 , A61K31/422 , A61K31/4439 , A61K31/506 , A61K31/454 , A61K31/5377 , A61K31/4725 , A61K31/4709 , A61K31/437 , A61K31/4375 , A61K31/497 , A61K31/427 , A61K31/444 , A61K31/4245 , A61P25/24 , A61P25/22 , A61P25/18 , A61P25/00 , A61P25/16 , A61P25/28 , A61P25/08 , A61P25/06 , A61P25/30 , A61P3/00 , A61P3/10 , A61P3/04 , A61P3/06 , A61P9/00
CPC分类号： C07D263/28 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及式I化合物，其中X，R和R 1的定义如本文所定义。式I化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是TAAR1。这些化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病。

7. 发明授权

US08673950B2 Dihydrooxazol-2-amine derivatives 有权
标题翻译：二氢恶唑-2-胺衍生物
公开(公告)号：US08673950B2
公开(公告)日：2014-03-18
申请号：US13279362
申请日：2011-10-24
申请人： Matthias Nettekoven , Roger Norcross , Alessandra Polara
发明人： Matthias Nettekoven , Roger Norcross , Alessandra Polara
IPC分类号： A61K31/421 , C07D263/28
CPC分类号： C07D263/28 , C07D263/16 , C07D413/12 , C07D413/14
摘要： The invention relates to compounds of formula wherein R1, R2, R3, R4, X, Ar, and are defined herein or to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.
摘要翻译：本发明涉及下式的化合物，其中R 1，R 2，R 3，R 4，X，Ar和本文定义或其药学上合适的酸加成盐。式I的化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是对于TAAR1。这些化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢紊乱，如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡失调和失眠，睡眠障碍和昼夜节律和心血管疾病。

8. 发明授权

US08354441B2 Oxazoline derivatives 失效
标题翻译：恶唑啉衍生物
公开(公告)号：US08354441B2
公开(公告)日：2013-01-15
申请号：US12938401
申请日：2010-11-03
申请人： Guido Galley , Roger Norcross , Alessandra Polara
发明人： Guido Galley , Roger Norcross , Alessandra Polara
IPC分类号： A61K31/42 , C07D263/08
CPC分类号： C07D263/28 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及式I化合物，其中X，R和R 1的定义如本文所定义。式I化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是TAAR1。这些化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病。

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