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1. 发明申请

WO2011115928A1 AMINO -DIHYDROOXAZINE AND AMINO - DIHYDROTHIAZINE SPIRO COMPOUNDS AS BETA - SECRETASE MODULATORS AND THEIR MEDICAL USE 审中-公开
标题翻译：作为β-分泌酶调节剂的氨基 - 二氢X嗪和氨基 - 二氢哒嗪类化合物及其医疗用途
公开(公告)号：WO2011115928A1
公开(公告)日：2011-09-22
申请号：PCT/US2011/028401
申请日：2011-03-14
申请人： AMGEN INC. , CHEN, Jian, J. , ZHONG, Wenge , YANG, Bryant , QIAN, Wenyuan , LOPEZ, Patricia , WHITE, Ryan , WEISS, Matthew , JUDD, Ted , POWERS, Timothy , CHENG, Yuan , DINEEN, Thomas , EPSTEIN, Oleg , LOW, Jonathan , MARX, Isaac , MINATTI, Ana Elena , PARAS, Nick, A. , POTASHMAN, Michele
发明人： CHEN, Jian, J. , ZHONG, Wenge , YANG, Bryant , QIAN, Wenyuan , LOPEZ, Patricia , WHITE, Ryan , WEISS, Matthew , JUDD, Ted , POWERS, Timothy , CHENG, Yuan , DINEEN, Thomas , EPSTEIN, Oleg , LOW, Jonathan , MARX, Isaac , MINATTI, Ana Elena , PARAS, Nick, A. , POTASHMAN, Michele
IPC分类号： C07D498/10 , C07D498/20 , C07D513/10 , C07D513/20 , A61K31/537 , A61K31/5386 , A61K31/547 , A61P25/28
CPC分类号： C07D513/10 , C07D498/10 , C07D498/20 , C07D513/20
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I): wherein A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , R 2 , R 7 , X, Y and Z of Formula (I) are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).
摘要翻译：本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。在一个实施方案中，化合物具有通式（I）：其中式（I）的A1，A2，A3，A4，A5，A6，R2，R7，X，Y和Z在本文中定义。本发明还包括这些化合物在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。本发明还包括式（I）的其它实施方案，可用于制备式（I）化合物的中间体和方法。

2. 发明申请

WO2013044092A1 AMINO-OXAZINES AND AMINO-DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译：氨基氧化合物和氨基二氢化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：WO2013044092A1
公开(公告)日：2013-03-28
申请号：PCT/US2012/056658
申请日：2012-09-21
申请人： AMGEN INC. , WHITE, Ryan , CHENG, Yuan , MINATTI, Ana Elena , YANG, Bryant , ZHENG, Xiao Mei , LOPEZ, Patricia , HUMAN, Jason B. , EPSTEIN, Oleg , JUDD, Ted , SHAM, Kelvin , XUE, Qiufen
发明人： WHITE, Ryan , CHENG, Yuan , MINATTI, Ana Elena , YANG, Bryant , ZHENG, Xiao Mei , LOPEZ, Patricia , HUMAN, Jason B. , EPSTEIN, Oleg , JUDD, Ted , SHAM, Kelvin , XUE, Qiufen
IPC分类号： C07D498/10 , A61K31/537 , A61P25/28
CPC分类号： C07D498/10 , C07D498/20 , C07D513/10 , C07D513/20
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , L, R 2 , R 7 , X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译：本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。在一个实施方案中，化合物具有通式I，其中式I中的A1，A2，A3，A4，A5，A6，L，R2，R7，X，Y和Z如本文所定义。本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的疾病和病症的用途。这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。本发明还包括式I的其它实施方案，可用于制备式I化合物的中间体和方法。

3. 发明申请

WO2010030954A1 SPIRO-TETRACYCLIC RING COMPOUNDS AS BETASECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译： SPIRO-TETRACYCLING环化合物作为BETASECRETASE调节剂和使用方法
公开(公告)号：WO2010030954A1
公开(公告)日：2010-03-18
申请号：PCT/US2009/056748
申请日：2009-09-11
申请人： AMGEN INC. , WHITE, Ryan , AMEGADZIE, Albert , BRYAN, Marian C. , CHEN, Jian J. , CHENG, Alan C. , DINEEN, Thomas , EPSTEIN, Oleg , GORE, Vijay Keshav , HUA, Zihao , HUMAN, Jason B. , HUANG, Hongbing , KREIMAN, Charles , LA, Daniel , LIU, Qingyian , MA, Vu Van , MARX, Isaac , PATEL, Vinod F. , QIAN, Wenyuan , WEISS, Matthew , YUAN, Chester C.
发明人： WHITE, Ryan , AMEGADZIE, Albert , BRYAN, Marian C. , CHEN, Jian J. , CHENG, Alan C. , DINEEN, Thomas , EPSTEIN, Oleg , GORE, Vijay Keshav , HUA, Zihao , HUMAN, Jason B. , HUANG, Hongbing , KREIMAN, Charles , LA, Daniel , LIU, Qingyian , MA, Vu Van , MARX, Isaac , PATEL, Vinod F. , QIAN, Wenyuan , WEISS, Matthew , YUAN, Chester C.
IPC分类号： C07D498/10 , C07D513/10 , A61K31/424 , A61K31/429 , A61P25/28
CPC分类号： C07D498/10 , C07D513/10
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , T 1 , T 2 , W, X, Y and Z of Formula (I) are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula (I).
摘要翻译：本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。在一个实施方案中，化合物具有通式（I）; 其中本文定义式（I）的A1，A2，A3，A4，A5，A6，T1，T2，W，X，Y和Z。本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的疾病和病症的用途。这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。本发明还包括式I的其它实施方案，可用于制备式（I）化合物的中间体和方法。

4. 发明申请

WO2012071279A1 SPIRO-AMINO-IMIDAZOLONE AND SPIRO-AMINO-DIHYDRO-PYRIMIDINONE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译： SPIRO-AMINO-IMIDAZOLONE和SPIRO-AMINO-DIHYDRO-PYRIMIDINONE化合物作为β-分泌酶调节剂及其使用方法
公开(公告)号：WO2012071279A1
公开(公告)日：2012-05-31
申请号：PCT/US2011/061473
申请日：2011-11-18
申请人： AMGEN INC. , MINATTI, Ana Elena , EPSTEIN, Oleg , WHITE, Ryan , WEISS, Matthew , ZHONG, Wenge , LOW, Jonathan
发明人： MINATTI, Ana Elena , EPSTEIN, Oleg , WHITE, Ryan , WEISS, Matthew , ZHONG, Wenge , LOW, Jonathan
IPC分类号： C07D491/20 , A61K31/527 , A61P25/28
CPC分类号： C07D491/107 , C07D491/20
摘要： The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I), wherein variables A 1 , A 3 , A 4 , A 5 , A 6 , A 8 , L, R 2 , R 7 , R 9 , W and Y of Formula (I) are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas (II) and (III), sub-Formula embodiments of Formulas (I), (II) and (III), intermediates and processes and methods useful for the preparation of compounds of Formulae (I-III).
摘要翻译：本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。化合物具有通式（I），其中式（I）的变量A1，A3，A4，A5，A6，A8，L，R2，R7，R9，W和Y如本文所定义。本发明还提供包含该化合物的药物组合物，以及用于治疗由于BACE的活性而导致的与斑块形成和沉积有关的疾病和/或病症的化合物和组合物的相应用途。这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。本发明还提供式（II）和（III）的化合物，式（I），（II）和（III）的分式实施方案，可用于制备式（I-III）化合物的中间体和方法和方法）。

5. 发明申请

WO2012112462A1 SPIRO-AMINO-IMIDAZO-FUSED HETEROCYCLIC COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译：作为β-分泌酶调节剂的螺旋 - 氨基 - 咪唑 - 稠合的杂环化合物及其使用方法
公开(公告)号：WO2012112462A1
公开(公告)日：2012-08-23
申请号：PCT/US2012/024918
申请日：2012-02-13
申请人： AMGEN INC. , EPSTEIN, Oleg , WHITE, Ryan , PATEL, Vinod F. , HUMAN, Jason
发明人： EPSTEIN, Oleg , WHITE, Ryan , PATEL, Vinod F. , HUMAN, Jason
IPC分类号： C07D491/00 , A61K31/353 , A61P25/00
CPC分类号： C07D491/20 , A61K31/353
摘要： The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A 1 , A 3 , A 4 , A 5 , A 6 , A 8 , R 2 , R 7 , X, Y and Z of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.
摘要翻译：本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。化合物具有通式I，其中式I的变量A1，A3，A4，A5，A6，A8，R2，R7，X，Y和Z如本文所定义。本发明还提供包含该化合物的药物组合物，以及用于治疗由于BACE的活性而导致的与斑块形成和沉积有关的疾病和/或病症的化合物和组合物的相应用途。这种BACE介导的病症包括例如阿尔茨海默病，认知缺陷和损伤，精神分裂症和其他中枢神经系统病症和障碍。本发明还提供了式II和III的化合物和式I，II和III的分子式，可用于制备式I-III化合物的中间体和方法和方法。

6. 发明申请

WO2014078314A1 AMINO-OXAZINE AND AMINO-DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译：氨基氧化胺和氨基二氢化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：WO2014078314A1
公开(公告)日：2014-05-22
申请号：PCT/US2013/069697
申请日：2013-11-12
申请人： AMGEN INC.
发明人： WHITE, Ryan , EPSTEIN, Oleg , HUMAN, Jason, Brooks , ZHENG, Xiao Mei , SHAM, Kelvin , LIU, Qingyian , CHEN, Ning , CHENG, Yuan
IPC分类号： C07D498/10 , C07D498/20 , A61K31/537 , A61P25/28
CPC分类号： C07D519/00 , C07D311/80 , C07D491/052 , C07D498/10 , C07D498/20 , C07D513/10 , C07D513/20
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A 1, A 2 , A 3 , A 4 , A 5 , A 6 , L, R 2 , R 7 , X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译：本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。在一个实施方案中，化合物具有通式I，其中式I中的A1，A2，A3，A4，A5，A6，L，R2，R7，X，Y和Z如本文所定义。本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的疾病和病症的用途。这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。本发明还包括式I的其它实施方案，可用于制备式I化合物的中间体和方法。

7. 发明申请

WO2014120658A1 FUSED MULTICYCLIC 3-AMINO-5,6-DIHYDRO-2H-1,4-THIAZINE DERIVATIVES AND THEIR USE AS BETA-SECRETASE INHIBITORS 审中-公开
标题翻译：熔融多金属3-氨基-5,6-二氢-2H-1,4-THIAZINE衍生物及其作为β-分泌酶抑制剂的用途
公开(公告)号：WO2014120658A1
公开(公告)日：2014-08-07
申请号：PCT/US2014/013340
申请日：2014-01-28
申请人： AMGEN INC.
发明人： WHITE, Ryan , ALLEN, Jennifer R. , EPSTEIN, Oleg , HONG, Fang-Tsao , HUA, Zihao , HUMAN, Jason Brooks , LOPEZ, Patricia , OLIVIERI, Philip R. , ROMERO, Karina , SCHENKEL, Laurie , STELLWAGEN, John , TAMAYO, Nuria A. , ZHENG, Xiao Mei
IPC分类号： C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04 , C07D513/10 , C07D513/14 , C07D513/20 , C07D519/00 , A61K31/5415 , A61K31/542 , A61K31/547 , A61K31/55 , A61P25/00 , A61P25/28
CPC分类号： C07D513/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/10 , C07D513/14 , C07D513/20 , C07D519/00
摘要： The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A 5 , A 6 , A 8 , R 1 , R 2 , R 3 , R 7 , X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
摘要翻译：本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。化合物具有通式I：其中式I的变量A5，A6，A8，R1，R2，R3，R7，X，Y，n和o独立地在本文中定义。本发明还提供包含该化合物的药物组合物，以及用于治疗由BACE的生物学活性产生的A-β斑块形成和沉积相关的病症和/或病症的化合物和组合物的相应用途。这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。本发明进一步提供式II化合物及其分式实施方案，式III化合物，可用于制备式I-III化合物及其分式的中间体和方法和方法。

8. 发明公开

EP2675810A1 SPIRO-AMINO-IMIDAZO-FUSED HETEROCYCLIC COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译：螺氨基咪唑缩合杂环化合物作为β-分泌调节剂和其使用方法
公开(公告)号：EP2675810A1
公开(公告)日：2013-12-25
申请号：EP12704644.9
申请日：2012-02-13
申请人： Amgen Inc.
发明人： EPSTEIN, Oleg , WHITE, Ryan , PATEL, Vinod F. , HUMAN, Jason
IPC分类号： C07D491/00 , A61K31/353 , A61P25/00
CPC分类号： C07D491/20 , A61K31/353
摘要： The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A1, A3, A4, A5, A6, A8, R2, R7, X, Y and Z of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.

9. 发明申请

WO2015129926A1 PYRAZOLE AMIDE DERIVATIVE 审中-公开
标题翻译：吡唑酰胺衍生物
公开(公告)号：WO2015129926A1
公开(公告)日：2015-09-03
申请号：PCT/JP2015/056584
申请日：2015-02-27
申请人： TEIJIN PHARMA LIMITED , AMGEN INC.
发明人： BECK, Hilary Plake , BOOKER, Shon Keith , BREGMAN, Howard , CEE, Victor J. , CHAKKA, Nagasree , CUSHING, Timothy D. , EPSTEIN, Oleg , FOX, Brian M. , GEUNS-MEYER, Stephanie , HAO, Xiaolin , HIBIYA, Kenta , HIRATA, Jun , HUA, Zihao , HUMAN, Jason , KAKUDA, Shinji , LOPEZ, Patricia , NAKAJIMA, Ryota , OKADA, Kazuhisa , OLSON, Steven H. , OONO, Hiroyuki , PENNINGTON, Lewis D. , SASAKI, Kosuke , SHIMADA, Keiko , SHIN, Youngsook , WHITE, Ryan D. , WURZ, Ryan P. , YI, Shuyan , ZHENG, Xiao Mei
IPC分类号： C07D403/12 , C07D401/14 , C07D405/14 , C07D231/14 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/14 , C07D493/08 , A61K31/4155 , A61P29/00
CPC分类号： C07D231/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/14 , C07D493/08
摘要： The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.
摘要翻译：本发明涉及具有抑制RORγ活性的新型化合物。本发明还涉及包含该化合物的药物组合物，该化合物在治疗或预防自身免疫疾病，炎性疾病，代谢疾病或癌症疾病中的用途。

10. 发明申请

WO2014059185A1 AMINO - DIHYDROTHIAZINE AND AMINO - DIOXIDO DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE 审中-公开
标题翻译：氨基 - 二氢INE嗪和氨基 - 二氧化二吖啶化合物作为β-分泌酶拮抗剂及其使用方法
公开(公告)号：WO2014059185A1
公开(公告)日：2014-04-17
申请号：PCT/US2013/064400
申请日：2013-10-10
申请人： AMGEN INC.
发明人： LEWIS, Richard T. , CHOQUETTE, Deborah , EPSTEIN, Oleg , GUZMAN-PEREZ, Angel , HUA, Zihao , HUMAN, Jason Brooks , JUDD, Ted , LIU, Qingyian , LOPEZ, Patricia , MINATTI, Ana Elena , OLIVIERI, Philip R. , ROMERO, Karina , SCHENKEL, Laurie , STELLWAGEN, John , WHITE, Ryan , ZHENG, Xiao Mei , ALLEN, Jennifer R. , CHENG, Yuan , HARRINGTON, Paul E. , HUNGATE, Randall W. , RUMFELT, Shannon , RZASA, Robert M. , XUE, Qiufen , ZHONG, Wenge
IPC分类号： C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D498/04 , C07D279/12 , C07D279/14 , C07D513/04 , C07D513/10 , C07D519/00 , A61P25/18 , A61P25/28 , A61K31/54 , A61K31/541 , A61K31/547
CPC分类号： C07D279/12 , C07D213/79 , C07D239/74 , C07D241/44 , C07D279/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D513/10 , C07D519/00
摘要： The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A 4 , A 5 , A 6 , A 8 , R 1 , R 2 , R 3 , R 7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.
摘要翻译：本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。化合物具有通式I：其中式I的变量A4，A5，A6，A8，R1，R2，R3，R7和n独立地在本文中定义。本发明还提供包含该化合物的药物组合物，以及用于治疗由BACE的生物学活性产生的A-β斑块形成和沉积相关的病症和/或病症的化合物和组合物的相应用途。这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。本发明还提供式II化合物及其次级实施方案，可用于制备式I-II化合物的中间体和方法和方法。

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