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41. 发明授权

US07803809B2 Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use 有权
标题翻译：取代的吡喃并[2,3-b]吡啶胺化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US07803809B2
公开(公告)日：2010-09-28
申请号：US12291753
申请日：2008-11-12
申请人： Russell Graceffa , Matthew Kaller , Daniel La , Patricia Lopez , Vinod F. Patel , Wenge Zhong
发明人： Russell Graceffa , Matthew Kaller , Daniel La , Patricia Lopez , Vinod F. Patel , Wenge Zhong
IPC分类号： A61K31/44
CPC分类号： C07D487/04 , C07D311/96 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/052 , C07D519/00
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 R1, R2, R3, R4, R5, A1, A2, A3, A4, 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 1，R 2，R 3，R 4，R 5，A 1，A 2，A 3，A 4，X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。

42. 发明申请

US20100087429A1 SPIRO-TRICYCLIC RING COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 有权
标题翻译： SPIRO-TRICYCLIC环化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US20100087429A1
公开(公告)日：2010-04-08
申请号：US12558426
申请日：2009-09-11
申请人： Ryan White , Albert Amegadzie , Marian C. Bryan , Jian Jeffrey Chen , Alan C. Cheng , Thomas Dineen , Oleg Epstein , Vijay Keshav Gore , Zihao Hua , Jason Brooks Human , Hongbing Huang , Charles Kreiman , Daniel La , Qingyian Liu , Vu Van Ma , Isaac Marx , Vinod F. Patel , Wenyuan Qian , Matthew Weiss , Chester Chenguang Yuan
发明人： Ryan White , Albert Amegadzie , Marian C. Bryan , Jian Jeffrey Chen , Alan C. Cheng , Thomas Dineen , Oleg Epstein , Vijay Keshav Gore , Zihao Hua , Jason Brooks Human , Hongbing Huang , Charles Kreiman , Daniel La , Qingyian Liu , Vu Van Ma , Isaac Marx , Vinod F. Patel , Wenyuan Qian , Matthew Weiss , Chester Chenguang Yuan
IPC分类号： A61K31/421 , C07D498/10 , C07D513/10 , C07D498/20 , A61K31/506 , A61K31/4439 , A61K31/5377 , A61P25/00 , 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 A1, A2, A3, A4, A5, A6, T1, T2, 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，其中式I的A1，A2，A3，A4，A5，A6，T1，T2，W，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。

43. 发明申请

US20090275602A1 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：US20090275602A1
公开(公告)日：2009-11-05
申请号：US12154513
申请日：2008-05-23
申请人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Scott Harried , Daniel Horne , Ted Judd , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Matthew Weiss , Qiufen Xue , Bryant Yang
发明人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Scott Harried , Daniel Horne , Ted Judd , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Matthew Weiss , Qiufen Xue , Bryant Yang
IPC分类号： A61K31/438 , C07D491/107 , A61P25/28
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 R1a, R1b, R1c, B, R3, R4, R5 and W of Formula I, and R1a, R1b, R1c, R2, R2a, R3, R4, R5, A1, A2, A3, A4, W, X, Z, m and n of Formula II are defined herein. The invention also provides compounds of Formula III, sub-Formulas II-A-II-D, sub-Formulas III-A-III-D and Formula IV. The invention further 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, AD, cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formulas I, II, III, IV and sub-formulas thereof, intermediates and processes useful for the preparation of compounds of Formulas I, II, III, IV and sub-formulas thereof.
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R 1a，R 1b，R 1c，B，R 3，R 4，R 5和W以及R 1a，R 1b，R 1c，R 2，R 2a，R 3，R 4，R 5 ，式II中的A1，A2，A3，A4，W，X，Z，m和n定义。本发明还提供了式III化合物，分子式II-A-II-D，分子式III-A-III-D和式IV的化合物。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。这些疾病包括例如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病症。本发明还包括式I，II，III，IV及其分式的其它实施方案，可用于制备式I，II，III，IV及其子式化合物的中间体和方法。

44. 发明申请

US20080255205A1 Multi-cyclic compounds and methods of use 失效
标题翻译：多环化合物和使用方法
公开(公告)号：US20080255205A1
公开(公告)日：2008-10-16
申请号：US11977970
申请日：2007-10-25
申请人： Brian L. Hodous , Stephanie D. Geuns-Meyer , Philip R. Olivieri , Vinod F. Patel , Paul A. Tempest
发明人： Brian L. Hodous , Stephanie D. Geuns-Meyer , Philip R. Olivieri , Vinod F. Patel , Paul A. Tempest
IPC分类号： A61K31/4439 , C07D401/04 , C07D413/04 , C07D419/04 , A61K31/165 , A61K31/395 , C07D207/09 , C07C237/14
CPC分类号： C07D401/04 , C07D263/32 , C07D413/04
摘要： The present invention relates to compounds of Formulas I and II, wherein B1, B2, B3, B4, C1, C2, ring D, L1, L2 and R1-4 are defined herein, synthetic intermediates, and pharmaceutical compositions, comprising such compounds. The compounds and compositions are capable of modulating various protein kinase receptors such as Tie-2 and Aurora and, therefore, influencing kinase related disease states and conditions. The compounds, for example, are capable of treating cancer caused by unregulated angiogenesis, and inflammation as well as other proliferative disorders.
摘要翻译：本发明涉及式I和II的化合物，其中B 1，B 2，B 3，B 4， C 1，C 1，C 2，环D，L 1，L 2和R 2， 1-4本文中定义的合成中间体和包含这些化合物的药物组合物。化合物和组合物能够调节各种蛋白激酶受体如Tie-2和Aurora，因此影响激酶相关的疾病状态和状况。该化合物例如能够治疗由不受调节的血管发生，炎症以及其它增殖性疾病引起的癌症。

45. 发明申请

US20140038954A1 Spiro-Amino-Imidazo-Fused Heterocyclic Compounds as Beta-secretase Modulators and Methods of Use 有权
标题翻译：螺氨基 - 咪唑并 - 杂环化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US20140038954A1
公开(公告)日：2014-02-06
申请号：US13982096
申请日：2012-02-13
申请人： Oleg Epstein , Ryan White , Vinod F. Patel , Jason Human
发明人： Oleg Epstein , Ryan White , Vinod F. Patel , Jason Human
IPC分类号： C07D491/20
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.
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。

46. 发明授权

US08163909B2 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：US08163909B2
公开(公告)日：2012-04-24
申请号：US12154513
申请日：2008-05-23
申请人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Scott Harried , Daniel Horne , Ted Judd , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Matthew Weiss , Qiufen Xue , Bryant Yang
发明人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Scott Harried , Daniel Horne , Ted Judd , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Matthew Weiss , Qiufen Xue , Bryant Yang
IPC分类号： A61K31/438 , A61P25/28 , C07D491/107
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 R1a, R1b, R1c, B, R3, R4, R5 and W of Formula I, and R1a, R1b, R1c, R2, R2a, R3, R4, R5, A1, A2, A3, A4, W, X, Z, m and n of Formula II are defined herein. The invention also provides compounds of Formula III, sub-Formulas II-A-II-D, sub-Formulas III-A-III-D and Formula IV. The invention further 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, AD, cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formulas I, II, III, IV and sub-formulas thereof, intermediates and processes useful for the preparation of compounds of Formulas I, II, III, IV and sub-formulas thereof.
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R 1a，R 1b，R 1c，B，R 3，R 4，R 5和W以及R 1a，R 1b，R 1c，R 2，R 2a，R 3，R 4，R 5 ，式II中的A1，A2，A3，A4，W，X，Z，m和n定义。本发明还提供了式III化合物，分子式II-A-II-D，分子式III-A-III-D和式IV的化合物。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。这些疾病包括例如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病症。本发明还包括式I，II，III，IV及其分式的其它实施方案，可用于制备式I，II，III，IV及其子式化合物的中间体和方法。

47. 发明授权

US08163766B2 Beta-secretase modulators and methods of use 有权
标题翻译： β-分泌酶调节剂和使用方法
公开(公告)号：US08163766B2
公开(公告)日：2012-04-24
申请号：US12909566
申请日：2010-10-21
申请人： Wenge Zhong , Stephen A. Hitchcock , Vinod F. Patel , Yuan Cheng , Michael Croghan , Randall W. Hungate , Daniel La , Patricia Lopez , Matthew K. Kaller , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Lewis Pennington , Matthew Weiss , Ted Judd , Russell Graceffa , Qiufen Xue , Charles Kreiman , Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Scott Harried , Craig Masse , Bryant Yang
发明人： Wenge Zhong , Stephen A. Hitchcock , Vinod F. Patel , Yuan Cheng , Michael Croghan , Randall W. Hungate , Daniel La , Patricia Lopez , Matthew K. Kaller , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Lewis Pennington , Matthew Weiss , Ted Judd , Russell Graceffa , Qiufen Xue , Charles Kreiman , Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Scott Harried , Craig Masse , Bryant Yang
IPC分类号： A61K31/436
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。

48. 发明授权

US08022221B2 Aurora kinase modulators and method of use 有权
标题翻译：极光激酶调节剂和使用方法
公开(公告)号：US08022221B2
公开(公告)日：2011-09-20
申请号：US12378426
申请日：2009-02-12
申请人： Victor J. Cee , Holly L. Deak , Bingfan Du , Stephanie D. Geuns-Meyer , Brian L. Hodous , Hanh Nho Nguyen , Philip R. Olivieri , Vinod F. Patel , Karina Romero , Laurie Schenkel
发明人： Victor J. Cee , Holly L. Deak , Bingfan Du , Stephanie D. Geuns-Meyer , Brian L. Hodous , Hanh Nho Nguyen , Philip R. Olivieri , Vinod F. Patel , Karina Romero , Laurie Schenkel
IPC分类号： C07D401/14 , C07D403/14 , A61K31/53 , A61K31/4427 , A61K31/506 , A61P19/02 , A61P35/00
CPC分类号： C07D401/14 , C07D237/30 , C07D239/42 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04 , C07D497/04
摘要： The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions 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A1，A2，C1，C2，D，L1，L2，Z和R3，R4，R6，R7和R8如本文所定义，其能够调节极光激酶蛋白活动，从而影响与Aurora激酶蛋白活性相关的各种疾病状态和病症。例如，化合物能够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，制备本发明化合物的方法，合成中间体和治疗与Aurora激酶活性有关的病症的方法。

49. 发明授权

US07973047B2 Beta-Secretase modulators and methods of use 有权
标题翻译： β-分泌酶调节剂和使用方法
公开(公告)号：US07973047B2
公开(公告)日：2011-07-05
申请号：US12779858
申请日：2010-05-13
申请人： Wenge Zhong , Stephen Hitchcock , Brian K. Albrecht , Michael D. Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Dean Hickman , Daniel Horne , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig E. Masse , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Holger Monenschein , Thomas Nguyen
发明人： Wenge Zhong , Stephen Hitchcock , Brian K. Albrecht , Michael D. Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Dean Hickman , Daniel Horne , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig E. Masse , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Holger Monenschein , Thomas Nguyen
IPC分类号： A61K31/438 , C07D471/00
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, 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。

50. 发明授权

US07838676B2 Beta-secretase modulators and methods of use 有权
标题翻译： β-分泌酶调节剂和使用方法
公开(公告)号：US07838676B2
公开(公告)日：2010-11-23
申请号：US11599901
申请日：2006-11-14
申请人： Qiufen Xue , 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 , Bryant Yang , Wenge Zhong
发明人： Qiufen Xue , 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 , Bryant Yang , Wenge Zhong
IPC分类号： C07D498/02 , C07D401/00
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 R1, W, 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 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。

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