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1. 发明授权

US08735384B2 Amino heteroaryl compounds as beta-secretase modulators and methods of use 有权
标题翻译：氨基杂芳基化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US08735384B2
公开(公告)日：2014-05-27
申请号：US13522823
申请日：2011-01-14
申请人： Nick A. Paras , James Brown , Yuan Cheng , Stephen A. Hitchcock , Ted Judd , Patricia Lopez , Ana Elena Minatti , Thomas Nixey , Timothy Powers , Christopher M. Tegley , Qiufen Xue , Bryant Yang , Wenge Zhong
发明人： Nick A. Paras , James Brown , Yuan Cheng , Stephen A. Hitchcock , Ted Judd , Patricia Lopez , Ana Elena Minatti , Thomas Nixey , Timothy Powers , Christopher M. Tegley , Qiufen Xue , Bryant Yang , Wenge Zhong
IPC分类号： A61K31/535 , A01N57/00 , A61K31/675
CPC分类号： C07D401/10 , C07D215/38 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D413/10 , C07D471/04 , C07D471/08 , C07D498/08
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 ring A, B1, B2, B3, L, R1, R2, ring Z, m and n 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 (AD), 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中的环A，B1，B2，B3，L，R1，R2，环Z，m和n定义在本文中。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病症和病症的用途。这些疾病包括例如阿尔茨海默氏病（AD），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. 发明授权

US08921363B2 Derivatives of 1 H-isoindol-3-amine, 1 H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as beta-secretase inhibitors 有权
标题翻译： 1H-异吲哚-3-胺，1H-异氮杂 - 吲哚-3-胺，3,4-二氢异喹啉-1-胺和1,4-二氢异喹啉-3-胺的衍生物作为β-分泌酶抑制剂
公开(公告)号：US08921363B2
公开(公告)日：2014-12-30
申请号：US13814232
申请日：2011-08-04
申请人： Ana Elena Minatti , Yuan Cheng , Wenge Zhong
发明人： Ana Elena Minatti , Yuan Cheng , Wenge Zhong
IPC分类号： C07D491/20 , A61K31/436 , A61K31/437 , A61K31/537 , C07D491/22 , C07D498/20 , C07D498/22
CPC分类号： C07D491/20 , A61K31/436 , A61K31/437 , A61K31/537 , C07D491/22 , C07D498/20 , C07D498/22
摘要： The present invention relates to a compound represented by general formula I: or a stereoisomer, tautomer, hydrate, solvate or pharmaceutically acceptable salt thereof, wherein A1, A2, A3, A4, A5, A6, R2, R7, W, X, Y and Z are defined within. These compounds are useful for the modulation of β-secretase enzyme activity and for the treatment of β-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions.
摘要翻译：本发明涉及由通式I表示的化合物或其立体异构体，互变异构体，水合物，溶剂化物或药学上可接受的盐，其中A1，A2，A3，A4，A5，A6，R2，R7，W，X，Y 和Z在其中定义。这些化合物可用于调节分泌酶活性和用于治疗分泌型介导的疾病，包括阿尔茨海默病（AD）和相关病症。

3. 发明申请

US20130172343A1 Derivatives of 1H-isoindol-3-amine, 1H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as Beta-secretase Inhibitors 有权
标题翻译： 1H-异吲哚-3-胺的衍生物，1H-异氮杂 - 吲哚-3-胺，3,4-二氢异喹啉-1-胺和1,4-二氢异喹啉-3-胺作为β-分泌酶抑制剂
公开(公告)号：US20130172343A1
公开(公告)日：2013-07-04
申请号：US13814232
申请日：2011-08-04
申请人： Ana Elena Minatti , Yuan Cheng , Wenge Zhong
发明人： Ana Elena Minatti , Yuan Cheng , Wenge Zhong
IPC分类号： C07D491/20 , C07D498/20 , C07D498/22 , C07D491/22
CPC分类号： C07D491/20 , A61K31/436 , A61K31/437 , A61K31/537 , C07D491/22 , C07D498/20 , C07D498/22
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: (I). In another embodiment, the compounds have a general Formula II: (II). In another embodiment, the compounds have a general Formula III: (III). Variables A1, A2, A3, A4, A5, A6, R2, R7, V, W, X, Y and Z of Formulas I, II and III 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 Formulas I, II and III, intermediates and processes useful for the preparation of compounds of Formulas I, II and III.
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：（I）。在另一个实施方案中，化合物具有通式II：（II）。在另一个实施方案中，化合物具有通式III：（III）。式I，II和III的变量A1，A2，A3，A4，A5，A6，R2，R7，V，W，X，Y和Z在本文中定义。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，II和III的其它实施方案，可用于制备式I，II和III化合物的中间体和方法。

4. 发明申请

US20130040931A1 Amino Heteroaryl Compounds as Beta-Secretase Modulators and Methods of Use 有权
标题翻译：氨基杂芳基化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US20130040931A1
公开(公告)日：2013-02-14
申请号：US13522823
申请日：2011-01-14
申请人： Nick A. Paras , James Brown , Yuan Cheng , Stephen A. Hitchcock , Ted Judd , Patricia Lopez , Ana Elena Minatti , Thomas Nixey , Timothy Powers , Christopher M. Tegley , Qiufen Xue , Bryant Yang , Wenge Zhong
发明人： Nick A. Paras , James Brown , Yuan Cheng , Stephen A. Hitchcock , Ted Judd , Patricia Lopez , Ana Elena Minatti , Thomas Nixey , Timothy Powers , Christopher M. Tegley , Qiufen Xue , Bryant Yang , Wenge Zhong
IPC分类号： A61K31/5377 , C07D413/04 , C07D471/04 , A61P25/16 , A61K31/4709 , C07D417/14 , A61P25/28 , A61P25/00 , C07D413/14 , C07D405/14
CPC分类号： C07D401/10 , C07D215/38 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D413/10 , C07D471/04 , C07D471/08 , C07D498/08
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 ring A, B1, B2, B3, L, R1, R2, ring Z, m and n 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 (AD), 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中的环A，B1，B2，B3，L，R1，R2，环Z，m和n定义在本文中。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病症和病症的用途。这些疾病包括例如阿尔茨海默氏病（AD），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。

5. 发明授权

US08957083B2 Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use 有权
标题翻译：螺 - 氨基 - 咪唑啉酮和螺 - 氨基 - 二氢 - 嘧啶酮化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US08957083B2
公开(公告)日：2015-02-17
申请号：US13988745
申请日：2011-11-18
申请人： Ana Elena Minatti , Oleg Epstein , Ryan White , Matthew Weiss , Wenge Zhong , Jonathan D. Low
发明人： Ana Elena Minatti , Oleg Epstein , Ryan White , Matthew Weiss , Wenge Zhong , Jonathan D. Low
IPC分类号： C07D491/107 , C07D491/20
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 A1, A3, A4, A5, A6, A8, L, R2, R7, R9, 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，以及用于治疗由于BACE的活性而导致的斑块形成和沉积相关疾病和/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的次级实施方案，可用于制备式I-III化合物的中间体和方法和方法。

6. 发明申请

US20130338177A1 Spiro-Amino-Imidazolone and Spiro-Amino-Dihydro-Pyrimidinone Compounds as Beta-Secretase Modulators and Methods of Use 有权
标题翻译：螺氨基 - 咪唑啉酮和螺 - 氨基 - 二氢 - 嘧啶酮化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US20130338177A1
公开(公告)日：2013-12-19
申请号：US13988745
申请日：2011-11-18
申请人： Ana Elena Minatti , Oleg Epstein , Ryan White , Matthew Weiss , Wenge Zhong , Jonathan D. Low
发明人： Ana Elena Minatti , Oleg Epstein , Ryan White , Matthew Weiss , Wenge Zhong , Jonathan D. Low
IPC分类号： C07D491/107 , C07D491/20
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 A1, A3, A4, A5, A6, A8, L, R2, R7, R9, 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的活性而导致的斑块形成和沉积相关疾病和/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）。

7. 发明授权

US08497264B2 Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use 有权
公开(公告)号：US08497264B2
公开(公告)日：2013-07-30
申请号：US13047693
申请日：2011-03-14
申请人： Jian J. Chen , Wenge Zhong , Bryant Yang , Ryan White , Matthew Weiss , Timothy Powers , Yuan Cheng
发明人： Jian J. Chen , Wenge Zhong , Bryant Yang , Ryan White , Matthew Weiss , Timothy Powers , Yuan Cheng
IPC分类号： C07D513/10 , C07D498/20 , A61K31/547 , A61K31/5386
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 A1, A2, A3, A4, A5, A6, R2, R7, 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.

8. 发明申请

US20110251190A1 SPIRO-TETRACYCLIC RING COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 有权
标题翻译：作为β-分泌酶调节剂的螺环四环化合物及其使用方法
公开(公告)号：US20110251190A1
公开(公告)日：2011-10-13
申请号：US13047734
申请日：2011-03-14
申请人： Yuan CHENG , Ryan White , Albert Amegadzie , James Brown , Alan C. Cheng , Erin F. Dimauro , Thomas Dineen , Oleg Epstein , Vijay Keshav Gore , Jason Brooks Human , Ted Judd , Charles Kreiman , Qingyian Liu , Patricia Lopez , Vu Van Ma , Isaac Marx , Ana Minatti , Hanh Nho Nguyen , Nick A. Paras , Vinod F. Patel , Wenyuan Qian , Matthew Weiss , Qiufen Xue , Xiao Mei Zheng , Wenge Zhong
发明人： Yuan CHENG , Ryan White , Albert Amegadzie , James Brown , Alan C. Cheng , Erin F. Dimauro , Thomas Dineen , Oleg Epstein , Vijay Keshav Gore , Jason Brooks Human , Ted Judd , Charles Kreiman , Qingyian Liu , Patricia Lopez , Vu Van Ma , Isaac Marx , Ana Minatti , Hanh Nho Nguyen , Nick A. Paras , Vinod F. Patel , Wenyuan Qian , Matthew Weiss , Qiufen Xue , Xiao Mei Zheng , Wenge Zhong
IPC分类号： A61K31/538 , A61K31/436 , C07D413/14 , C07D417/14 , A61K31/444 , A61P25/00 , C07D513/10 , A61K31/4545 , C07D498/10 , A61K31/497 , A61P25/28 , A61P25/16 , C07D513/20 , A61K31/506
CPC分类号： C07D491/10 , A61K31/42 , A61K31/422 , A61K31/4439 , A61K31/506 , A61K31/5377 , C07D221/20 , C07D235/02 , C07D263/08 , C07D295/135 , C07D498/10 , C07D498/20 , C07D513/10 , C09B11/28
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 other related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R2, R7, X and Y 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（包括阿尔茨海默氏病（AD））和其它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，R2，R7，X和Y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。

9. 发明申请

US20110118250A1 BETA-SECRETASE MODULATORS AND METHODS OF USE 有权
标题翻译： BETA-SECRETASE调制器和使用方法
公开(公告)号：US20110118250A1
公开(公告)日：2011-05-19
申请号：US12909566
申请日：2010-10-21
申请人： Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Wenge Zhong
发明人： Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Wenge Zhong
IPC分类号： A61K31/538 , C07D405/12 , A61K31/4433 , A61K31/444 , C07D405/14 , A61K31/4439 , A61K31/506 , A61K31/497 , C07D413/12 , A61K31/5377 , A61K31/4178 , A61K31/4545 , A61K31/453 , C07D311/96 , A61K31/352 , C07D407/12 , A61K31/4709 , C07D401/12 , C07D409/12 , A61K31/422 , A61K31/4025 , C07D471/04 , A61K31/501 , A61P25/28 , A61P25/00 , A61P25/16
CPC分类号： C07D405/12 , C07D413/12
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, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
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（包括阿尔茨海默氏病（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A，B，R 3，R 4，R 5，i和j在本文中定义。本发明还包括药物组合物，其包括一种或多种式I化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过给受试者施用式I化合物或包含它们的组合物。本发明还包括式II和III的其它实施方案，可用于制备本发明化合物的中间体和方法。

10. 发明申请

US20090036478A1 Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use 有权
标题翻译：取代的羟乙基胺化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US20090036478A1
公开(公告)日：2009-02-05
申请号：US12154497
申请日：2008-05-23
申请人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Daniel Horne , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Lewis Pennington , Qiufen Xue , Bryant Yang , Yuan Cheng
发明人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Daniel Horne , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Lewis Pennington , Qiufen Xue , Bryant Yang , Yuan Cheng
IPC分类号： A61K31/438 , C07D221/20 , C07D233/54 , A61K31/4178 , A61P25/28 , A61P25/00
CPC分类号： C07D491/107 , C07D221/06 , C07D311/96 , C07D471/10 , C07D491/10 , C07D493/10 , C07D495/10
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 R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z 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 (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.
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R 1a，R 1b，R 1c，B，W，R 3，R 4和R 5在本文中定义。在另一个实施方案中，本发明提供通式II的化合物，其中A1，A2，A3，A4，R1a，R1b，R1c，R2，R4，R5，W，X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病症和病症的用途。这些疾病包括例如阿尔茨海默病（AD），认知缺陷和损伤，精神分裂症和其他类似的中枢神经系统疾病。本发明还包括式II的其它实施方案，可用于制备式I和II化合物的中间体和方法。

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