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1. 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。

2. 发明公开

EP3110810A1 PYRAZOLE AMIDE DERIVATIVE 有权转让
标题翻译：吡唑酰胺衍生物
公开(公告)号：EP3110810A1
公开(公告)日：2017-01-04
申请号：EP15713244.0
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活性功能的新型化合物。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性疾病，炎性疾病，代谢性疾病或癌症疾病中的用途。

3. 发明授权

EP3110810B1 PYRAZOLE AMIDE DERIVATIVE 有权转让
标题翻译：吡唑酰胺衍生物
公开(公告)号：EP3110810B1
公开(公告)日：2018-05-02
申请号：EP15713244.0
申请日：2015-02-27
申请人： Teijin Pharma Limited
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.

4. 发明申请

WO2018119183A2 KRAS G12C INHIBITORS AND METHODS OF USING THE SAME 审中-公开
公开(公告)号：WO2018119183A2
公开(公告)日：2018-06-28
申请号：PCT/US2017/067801
申请日：2017-12-21
申请人： AMGEN INC.
发明人： LANMAN, Brian Alan , CEE, Victor J. , PICKRELL, Alexander J. , REED, Anthony B. , YANG, Kevin C. , KOPECKY, David John , WANG, Hui-Ling , LOPEZ, Patricia , ASHTON, Kate , BOOKER, Shon , TEGLEY, Christopher M.
IPC分类号： C07D275/04 , C07D417/04 , C07D471/08 , C07D513/04 , C07D487/10 , C07D487/04 , C07D239/80 , C07D471/04 , C07D401/04 , C07D403/04 , A61K31/428 , A61K31/429 , A61K31/437 , A61K31/517 , A61K31/519 , A61K31/498 , A61K31/4985 , A61P35/00
摘要： Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

5. 发明申请

WO2008147547A1 SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译：取代的羟基乙胺化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：WO2008147547A1
公开(公告)日：2008-12-04
申请号：PCT/US2008/006644
申请日：2008-05-23
申请人： AMGEN INC. , ZHONG, Wenge , HITCHCOCK, Stephen , PATEL, Vinod F. , CROGHAN, Michael , DINEEN, Thomas , HARRIED, Scott , HORNE, Daniel , JUDD, Ted , KALLER, Matthew , KREIMAN, Charles , LOPEZ, Patricia , MONENSCHEIN, Holger , NGUYEN, Thomas , WEISS, Matthew , XUE, Qiufen , YANG, Bryant
发明人： ZHONG, Wenge , HITCHCOCK, Stephen , PATEL, Vinod F. , CROGHAN, Michael , DINEEN, Thomas , HARRIED, Scott , HORNE, Daniel , JUDD, Ted , KALLER, Matthew , KREIMAN, Charles , LOPEZ, Patricia , MONENSCHEIN, Holger , NGUYEN, Thomas , WEISS, Matthew , XUE, Qiufen , YANG, Bryant
IPC分类号： C07D221/06 , C07D311/96 , C07D471/10 , C07D491/10 , C07D493/10 , C07D495/10 , A61P25/28 , A61K31/438
CPC分类号： 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 or Formula II wherein RIa, RIb, RIc, B, R3, R4, R5 and W of Formula I, and RIa, RIb, RIc, R2, R2a, R3, R4, R5, R6, Al, A2, A3, A4, W, X, Z, m and n of Formula II are defined herein.
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或式II，其中式I的RIa，RIb，RIc，B，R3，R4，R5和W以及RIa，RIb，RIc，R2，R2a，R3，R4，R5 ，式II的R6，A1，A2，A3，A4，W，X，Z，m和n定义。

6. 发明申请

WO2007061930A1 BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译： BETA-SECRETASE调制器和使用方法
公开(公告)号：WO2007061930A1
公开(公告)日：2007-05-31
申请号：PCT/US2006/044833
申请日：2006-11-17
申请人： AMGEN INC. , XUE, Qiufen , ALBRECHT, Brian K. , ANDERSEN, Denise Lyn , BARTBERGER, Michael , BROWN, James , BROWN, Ryan , CHAFFEE, Stuart C. , CHENG, Yuan , CROGHAN, Michael , GRACEFFA, Russell , HARRIED, Scott , HITCHCOCK, Stephen , HUNGATE, Randall , JUDD, Ted , KALLER, Matthew , KREIMAN, Charles , LA, Daniel , LOPEZ, Patricia , MASSE, Craig E. , MONENSCHEIN, Holger , NGUYEN, Thomas , NIXEY, Thomas , PATEL, Vinod F. , PENNINGTON, Lewis , WEISS, Matthew , YANG, Bryant , ZHONG, Wenge
发明人： XUE, Qiufen , ALBRECHT, Brian K. , ANDERSEN, Denise Lyn , BARTBERGER, Michael , BROWN, James , BROWN, Ryan , CHAFFEE, Stuart C. , CHENG, Yuan , CROGHAN, Michael , GRACEFFA, Russell , HARRIED, Scott , HITCHCOCK, Stephen , HUNGATE, Randall , JUDD, Ted , KALLER, Matthew , KREIMAN, Charles , LA, Daniel , LOPEZ, Patricia , MASSE, Craig E. , MONENSCHEIN, Holger , NGUYEN, Thomas , NIXEY, Thomas , PATEL, Vinod F. , PENNINGTON, Lewis , WEISS, Matthew , YANG, Bryant , ZHONG, Wenge
IPC分类号： C07D405/12 , C07D413/12 , A61K31/44 , A61P25/28
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 R 1 , W, B, R 3 , R 4 , R 5 , 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 1，W，B，R 3，R 4，R 4， SUP> 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，通过施用式（I）化合物或其组合物，包括它们，到一个主题。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。

7. 发明申请

WO2006004702A1 CONDENSED TRIAZOLES AND INDAZOLES USEFUL IN TREATING CITOKINES MEDIATED DISEASES AND OTHER DISEASES 审中-公开
标题翻译：浓缩的三唑和吲哚有用的治疗介质性疾病和其他疾病
公开(公告)号：WO2006004702A1
公开(公告)日：2006-01-12
申请号：PCT/US2005/022835
申请日：2005-06-24
申请人： AMGEN INC.
发明人： ANDERSON, Denise, Lyn , FROHN, Michael, J. , HONG, Fang-Tsao , LIU, Longin , LOPEZ, Patricia
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to triazolopyrimidines, imidazolopyrimidines and derivatives thereof of Formula (I), and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shack syndrome, fever, myalgias due to HIV-l, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
摘要翻译：本发明涉及式（I）的三唑并嘧啶，咪唑并嘧啶及其衍生物及其药学上可接受的盐。还包括治疗炎症，类风湿性关节炎，佩吉特病，骨质疏松症，多发性骨髓瘤，葡萄膜炎，急性或慢性骨髓性白血病，胰腺β细胞破坏，骨关节炎，类风湿性脊椎炎，痛风性关节炎，炎性肠病，成人呼吸窘迫综合征（ARDS），牛皮癣，克罗恩病，过敏性鼻炎，溃疡性结肠炎，过敏反应，接触性皮炎，哮喘，肌肉退化，恶病质，赖特综合征，I型糖尿病，II型糖尿病，骨吸收疾病，移植物抗宿主反应，阿尔茨海默病，中风，心肌梗死，缺血再灌注损伤，动脉粥样硬化，脑外伤，多发性硬化，脑疟疾，败血症，脓毒性休克，毒性综合症，发热，HIV-1，HIV-3，巨细胞病毒（CMV）），流感病毒，腺病毒，哺乳动物中的疱疹病毒或带状疱疹感染，包括给予有效量的如上所述的化合物。

8. 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。

9. 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。

10. 发明申请

WO2007062007A1 BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译： BETA-SECRETASE调制器和使用方法
公开(公告)号：WO2007062007A1
公开(公告)日：2007-05-31
申请号：PCT/US2006/045004
申请日：2006-11-20
申请人： AMGEN INC. , ALBRECHT, Brian, K , ANDERSEN, Denise, Lyn , BARTBERGER, Michael , BROWN, James , BROWN, Ryan , CHAFFEE, Stuart, C. , CHENG, Yuan , CROGHAN, Michael , GRACEFFA, Russell , HARRIED, Scott , HITCHCOCK, Stephen , HUNGATE, Randall , JUDD, Ted , KALLER, Matthew , KREIMAN, Charles , LA, Daniel , LOPEZ, Patricia , MASSE, Craig, E. , MONENSCHEIN, Holger , NGUYEN, Thomas , NIXEY, Thomas , PATEL, Vinod, F. , PENNINGTON, Lewis , WEISS, Matthew , XUE, Qiufen , YANG, Bryant , ZHONG, Wenge
发明人： ALBRECHT, Brian, K , ANDERSEN, Denise, Lyn , BARTBERGER, Michael , BROWN, James , BROWN, Ryan , CHAFFEE, Stuart, C. , CHENG, Yuan , CROGHAN, Michael , GRACEFFA, Russell , HARRIED, Scott , HITCHCOCK, Stephen , HUNGATE, Randall , JUDD, Ted , KALLER, Matthew , KREIMAN, Charles , LA, Daniel , LOPEZ, Patricia , MASSE, Craig, E. , MONENSCHEIN, Holger , NGUYEN, Thomas , NIXEY, Thomas , PATEL, Vinod, F. , PENNINGTON, Lewis , WEISS, Matthew , XUE, Qiufen , YANG, Bryant , ZHONG, Wenge
IPC分类号： C07D405/12 , C07D413/12 , A61K31/44 , A61P25/28
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, R 3 , R 4 , R 5 , 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分别为本文定义。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。

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