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1. 发明申请

WO2007061670A1 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：WO2007061670A1
公开(公告)日：2007-05-31
申请号：PCT/US2006/044058
申请日：2006-11-13
申请人： AMGEN INC. , ZHONG, Wenge , HITCHCOCK, Stephen , ALBRECHT, Brian K , BARTBERGER, Michael , BROWN, James , BROWN, Ryan , CHAFFEE, Stuart C. , CHENG, Yuan , CROGHAN, Michael , GRACEFFA, Russell , HARRIED, Scott , HICKMAN, Dean , HORNE, Daniel , 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
发明人： ZHONG, Wenge , HITCHCOCK, Stephen , ALBRECHT, Brian K , BARTBERGER, Michael , BROWN, James , BROWN, Ryan , CHAFFEE, Stuart C. , CHENG, Yuan , CROGHAN, Michael , GRACEFFA, Russell , HARRIED, Scott , HICKMAN, Dean , HORNE, Daniel , 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
IPC分类号： C07D405/12 , C07D413/12 , A61K31/44 , A61P25/28
CPC分类号： C07D405/12 , C07D311/68 , C07D413/12 , C07D491/052
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, W, 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，W，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。

2. 发明申请

WO2006039718A3 ARYL NITROGEN-CONTAINING BICYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS 审中-公开
公开(公告)号：WO2006039718A3
公开(公告)日：2006-04-13
申请号：PCT/US2005/035873
申请日：2005-10-03
申请人： AMGEN INC
发明人： PATEL, Vinod F. , KIM, Joseph L. , GEUNS-MEYER, Stephanie D. , CHAFFEE, Stuart C. , CEE, Victor J. , HODOUS, Brian L. , BELLON, Steven , HARMANGE, Jean-christophe , OLIVIERI, Philip R. , THAMAN, Maya C. , DIMAURO, Erin F. , BUCHANAN, John L. , MCGOWAN, David C. , ALBRECHT, Brian K. , DEAK, Holly L. , BEMIS, Jean E. , WHITE, Ryan , MARTIN, Matthew W. , HABGOOD, Gregory J. , TEMPEST, Paul A. , MASSE, Craig E. , BUCKNER, William H. , HERBERICH, Bradley J. , GRACEFFA, Russell , ZHANG, Dawei , XU, Shimin , SHAM, Kelvin , RZASA, Robert M. , FALSEY, James Richard , CHAKRABARTI, Partha P. , CAO, Guo-qiang , TOMLINSON, Susan Ann , PETTUS, Liping H. , SMITH, Adrian Leonard , PARAS, Nick A. , LIU, Gang , DEMORIN, Frenel F. , TASKER, Andrew , REED, Anthony
IPC分类号： C07D239/84 , C07D239/95 , C07D401/12 , C07D409/04 , C07D405/12 , C07D409/14 , C07D405/04 , C07D403/10 , C07D401/04 , C07D471/04 , C07D403/12 , C07D413/12 , C07D417/12 , C07D409/12 , C07D215/12
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I, wherein A1, A2, A3, B, R1, R2, R3 and R4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

3. 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。

4. 发明申请

WO2007087276A1 AURORA KINASE MODULATORS AND METHOD OF USE 审中-公开
标题翻译： AURORA激酶调节剂及其使用方法
公开(公告)号：WO2007087276A1
公开(公告)日：2007-08-02
申请号：PCT/US2007/001714
申请日：2007-01-22
申请人： AMGEN INC. , CEE, Victor J. , DEAK, Holly L. , DU, Bingfan , GEUNS-MEYER, Stephanie D. , HODOUS, Brian L. , NGUYEN, Hanh Nho , OLIVIERI, Philip R. , PATEL, Vinod F. , ROMERO, Karina , SCHENKEL, Laurie
发明人： CEE, Victor J. , DEAK, Holly L. , DU, Bingfan , GEUNS-MEYER, Stephanie D. , HODOUS, Brian L. , NGUYEN, Hanh Nho , OLIVIERI, Philip R. , PATEL, Vinod F. , ROMERO, Karina , SCHENKEL, Laurie
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D497/04 , A61K31/502 , A61P35/00
CPC分类号： C07D401/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D497/04
摘要： The present invention relates to chemical compounds having a general formula (I) wherein A 1 , A 2 , C 1 , C 2 , D, L 1 , L 2 , Z and R 1-8 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
摘要翻译：本发明涉及具有通式（I）的化合物，其中A 1，A 2，C 1，C 2 D，L 1，L 2，Z和R 1-8均在本文中定义，合成中间体是能够调节各种蛋白激酶受体酶，从而影响与这些激酶的活性相关的各种疾病状态和状况。例如，化合物能够调节Aurora激酶，从而影响细胞周期和细胞增殖的过程，以治疗癌症和与癌症有关的疾病。本发明还包括药物组合物，包括该化合物，以及治疗与Aurora激酶活性有关的疾病状态的方法。

5. 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。

6. 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。

7. 发明申请

WO2006012374A1 SUBSTITUTED ARYL-AMINE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：取代的芳基胺衍生物及其使用方法
公开(公告)号：WO2006012374A1
公开(公告)日：2006-02-02
申请号：PCT/US2005/025800
申请日：2005-07-20
申请人： AMGEN INC. , YUAN, Chester Chenguang , YANG, Kevin , VANDERPLAS, Simon , RIAHI, Babak , POTASHMAN, Michele , PATEL, Vinod F. , NOMAK, Rana , LI, Aiwen , HUANG, Qi , HARMANGE, Jean-Christophe , ASKEW, JR., Benny C.
发明人： YUAN, Chester Chenguang , YANG, Kevin , VANDERPLAS, Simon , RIAHI, Babak , POTASHMAN, Michele , PATEL, Vinod F. , NOMAK, Rana , LI, Aiwen , HUANG, Qi , HARMANGE, Jean-Christophe , ASKEW, JR., Benny C.
IPC分类号： C07D401/12 , C07D413/14 , C07D401/14 , C07D405/12 , C07D405/14 , C07D217/02 , C07D403/12 , C07D417/14 , C07D471/04 , A61K31/443 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4725 , A61P35/00
CPC分类号： C07D401/12 , C07D217/02 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention provides classes of compounds, including-their pharmaceutically acceptable derivatives, useful for treating angiogenesis and related diseases such as cancer. Formula I and II wherein R is a 9- or 10-membered heterocyclyl ring selected from 7-isoquinolinyl,..2-methyl-3-oxo-2,3-dihydroindazol-6-yl, [1,6]-naphthydrin-3-yl, [1,7]-naphthydrin-2-yl, 1-oxo-2,3-dihydrobenzofuran-4-yl, 3-oxo - 2,3 - dihydrobenzofuran-5-yl, dihydro-benzodioxinyl, 6-quinazolinyl, 2-amino-6-quinazolinyl, 4-methylamino-6-quinazolinyl, 2,4-diamino-6 quinazolinyl, 3-oxo-3,4 - dihydro-1,4-benzoxazin-6-yl, 2,2 - difluoro-l;3-benzodioxol-5-yl and 2,2,3,3 tetrafluoro-2,3-dihydro-l,4-benzodioxin-6-yl, each of which is optionally substituted with one or more substituents selected from halo, haloakyl, C 1-6 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, N-dimethylamino-C 1-6 -alkyl, N-dimethylamino-C 1-6 -alkoxy, amino, alkyl-carbonylamino, morpholino-sulfonyl, amino-sulfonyl, oxazolyl, pyrrolyl, 4 morpholinyl, carboxyl, cyano, and acetyl; wherein R 1 in formula I is selected from unsubstituted or substituted phenyl, 5-6 membered heteroaryl, 9-10 membered bicyclic heterocyclyl and 11-14 membered tricyclic heterocyclyl, and R 1 in formula II is selected from specific bicyclic heterocycles.
摘要翻译：本发明提供了可用于治疗血管发生和相关疾病如癌症的化合物类，包括其药学上可接受的衍生物。式I和II其中R是选自7-异喹啉基，2-甲基-3-氧代-2,3-二氢吲唑-6-基，[1,6] - 萘啶-2-酮的9-或10-元杂环基环，吡啶-3-基，[1,7]萘啶-2-基，1-氧代-2,3-二氢苯并呋喃-4-基，3-氧代-2,3-二氢 - 二氢苯并二氧杂环戊烯基，6-喹唑啉基，2-氨基-6-喹唑啉基，4-甲基氨基-6-喹唑啉基，2,4-二氨基-6-喹唑啉基，3-氧代-3,4-二氢苯并呋喃-5-基二氢-1,4-苯并恶嗪-6-基，2,2 - 二氟-1,3-苯并间二氧杂环戊烯-5-基和2,2,3,3-四氟 - 2,3-二氢-1,4-苯并二恶英-6-基，其各自任选被一个或多个选自卤素，卤代烷基，C 1-6烷基，C 1 -C 6烷基， 2-8链烯基，C 2-8炔基，N-二甲基氨基-C 1-6 - 烷基，N-二甲基氨基-C1- 6 - 烷氧基，氨基，烷基 - 羰基氨基，吗啉代 - 磺酰基，氨基 - 磺酰基，恶唑基，吡咯基，吗啉基，羧基，氰基和乙酰基。其中式I中的R 1选自未取代或取代的苯基，5-6元杂芳基，9-10元双环杂环基和11-14元三环杂环基，R 1，式Ⅱ中选自具体的双环杂环。

8. 发明申请

WO2004085425A1 FUSED AZOLES SUCH AS 2,5-DISUBSTITUTED BENZIMIDAZOLES, BENZOXAZOLES AND BENZOTHIAZOLES AS KINASE INHIBITORS 审中-公开
标题翻译：作为2,5-取代苯并咪唑，苯并噻唑和苯并噻唑的熔融偶氮化物作为激酶抑制剂
公开(公告)号：WO2004085425A1
公开(公告)日：2004-10-07
申请号：PCT/US2004/008809
申请日：2004-03-22
申请人： AMGEN INC
发明人： DIPIETRO, Lucian V. , HARMANGE, Jean-Christophe , ASKEW, JR., Benny C. , ELBAUM, Daniel , GERMAIN, Julie , HABGOOD, Gregory J. , KIM, Joseph L. , PATEL, Vinod F. , POTASHMAN, Michele , VAN DER PLAS, Simon
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D235/30 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The invention relates to compounds of the formulae (I) to (III) wherein the substituents are as defined in the specification. These compounds have kinase inhibitory activity, such as VEGFR/KDR inhibitory activity. Accordingly, the compounds of the formulae (I) to (III) would be useful in the prevention and treatment of angiogenesis related disorders, ophthalmological conditions, proliferative diseases, inflammatory diseases, and other pathological conditions as described in the specification.
摘要翻译：本发明涉及式（I）至（III）的化合物，其中取代基如说明书中所定义。这些化合物具有激酶抑制活性，例如VEGFR / KDR抑制活性。因此，式（I）至（III）的化合物可用于预防和治疗血管发生相关疾病，眼科病症，增殖性疾病，炎性疾病和其他病理状况，如本说明书所述。

9. 发明申请

WO2012109165A1 5-AMINO-OXAZEPINE AND 5-AMINO-THIAZEPANE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE 审中-公开
标题翻译：作为β-分泌酶拮抗剂的5-氨基 - 氧杂环丁烯和5-氨基 - 噻唑烷酮化合物及其使用方法
公开(公告)号：WO2012109165A1
公开(公告)日：2012-08-16
申请号：PCT/US2012/024029
申请日：2012-02-06
申请人： AMGEN INC. , DINEEN, Thomas , WEISS, Matthew , PATEL, Vinod F. , ZHENG, Xiao Mei , WHITE, Ryan
发明人： DINEEN, Thomas , WEISS, Matthew , PATEL, Vinod F. , ZHENG, Xiao Mei , WHITE, Ryan
IPC分类号： C07D498/10 , C07D498/20 , C07D513/10 , A61K31/553 , A61K31/554 , A61P25/16 , A61P25/28
CPC分类号： C07D498/20 , C07D498/10 , C07D513/10
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 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 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 Formulas (II) and sub-formula embodiments of Formula (I) and (II), 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。该化合物具有通式（I）; 其中式（I）的变量A1，A3，A4，A5，A6，A8，R2，R7，X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（I）和（II）的式（II）和亚式实施方案的化合物，可用于制备式（I） - （II）化合物的中间体和方法和方法。

10. 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。

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