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1.发明授权Fused multi-cyclic sulfone compounds as inhibitors of beta-secretase and methods of use thereof 有权熔融多环砜化合物作为β-分泌酶的抑制剂及其使用方法公开(公告)号：US09309263B2
公开(公告)日：2016-04-12
申请号：US14166012
申请日：2014-01-28
Applicant: AMGEN INC.
Inventor： Ryan White , Jennifer R. Allen , Oleg Epstein , Fang-Tsao Hong , Zihao Hua , Jason Brooks Human , Patricia Lopez , Philip R. Olivieri , Karina Romero , Laurie Schenkel , John Stellwagen , Nuria A. Tamayo , Xiao Mei Zheng
IPC: C07D417/10 , C07D417/14 , C07D513/04 , C07D513/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/10 , C07D513/20 , C07D519/00
CPC classification number: C07D513/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/10 , C07D513/14 , C07D513/20 , C07D519/00
Abstract: 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 A5, A6, A8, R1, R2, R3, R7, 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.
Abstract translation: 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。 本发明还提供式II化合物及其次级实施方案，式III化合物，可用于制备式I-III化合物的中间体和方法和方法及其分式。
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2.发明授权Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof 有权作为β-分泌酶抑制剂的桥连双环氨基噻嗪二氧化物化合物及其使用方法公开(公告)号：US09096615B2
公开(公告)日：2015-08-04
申请号：US14445498
申请日：2014-07-29
Applicant: AMGEN INC.
Inventor： Richard T. Lewis , Jennifer R. Allen , James Brown , Angel Guzman-Perez , Zihao Hua , Ted Judd , Qingyian Liu , Philip R. Olivieri , Karina Romero , Laurie Schenkel , John Stellwagen , Ryan White
IPC: C07D513/06 , C07D513/08 , C07D519/00
CPC classification number: C07D513/08 , C07D513/06 , C07D519/00
Abstract: 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 A4, A5, A6, A8, R1, R2, R3, R7 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, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
Abstract translation: 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，式III化合物，可用于制备式I-III化合物的中间体和方法和方法及其分式。
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3.发明申请AMINO-DIHYDROTHIAZINE AND AMINO-DIOXIDO DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE 有权氨基二苯并恶嗪和氨基二氧化二硅杂环化合物作为β-分泌酶拮抗剂及其使用方法公开(公告)号：US20150259308A1
公开(公告)日：2015-09-17
申请号：US14433769
申请日：2013-10-10
Applicant: AMGEN INC.
Inventor： Richard T. Lewis , Jennifer R. Allen , Yuan Cheng , Deborah Choquette , Oleg Epstein , Angel Guzman-Perez , Paul E. Harrington , Zihao Hua , Randall W. Hungate , Jason Brooks Human , Ted Judd , Qingyian Liu , Patricia Lopez , Ana Elena Minatti , Philip Olivieri , Karina Romero , Shannon Rumfelt , Robert M. Rzasa , Laurie Schenkel , John Stellwagen , Ryan White , Qiufen Xue , Xiao Mei Zheng , Wenge Zhong
IPC: C07D279/12 , C07D471/04 , C07D239/74 , C07D495/04 , C07D213/79 , C07D513/10 , C07D417/12 , C07D417/14 , C07D513/04 , C07D498/04 , C07D279/14 , C07D417/04 , C07D241/44
CPC classification number: 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
Abstract: 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 A4, A5, A6, A8, R1, R2, R3, R7 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.
Abstract translation: 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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Patent Agency Ranking
公开(公告)号：US09242961B2
公开(公告)日：2016-01-26
申请号：US14045715
申请日：2013-10-03
Applicant: Amgen Inc.
Inventor： Victor J. Cee , Karina Romero
IPC: C07D237/30 , C07D239/42 , C07D401/04 , C07D409/04 , C07D409/14 , C07D401/14 , C07D417/14 , C07D471/04 , C07D497/04 , C07D491/048 , C07D495/04
CPC classification number: C07D401/14 , C07D237/30 , C07D239/42 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04 , C07D497/04
Abstract: 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.
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公开(公告)号：US09212182B2
公开(公告)日：2015-12-15
申请号：US14302337
申请日：2014-06-11
Applicant: AMGEN INC.
Inventor： Matthew Weiss , Alessandro Boezio , Christiane Boezio , John R. Butler , Margaret Yuhua Chu-Moyer , Erin F. Dimauro , Thomas Dineen , Russell Graceffa , Angel Guzman-Perez , Hongbing Huang , Charles Kreiman , Daniel La , Isaac E. Marx , Benjamin Charles Milgrim , Hanh Nho Nguyen , Emily Peterson , Karina Romero , Brian Sparling
IPC: A61K31/00 , C07D215/00 , C07D471/04 , C07D413/12 , C07D401/12 , C07D413/14 , C07D417/12 , C07C53/18 , C07D215/227 , C07D403/12 , C07D215/36 , C07D241/44
CPC classification number: C07D417/14 , C07C53/18 , C07D215/227 , C07D215/36 , C07D241/44 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.
Abstract translation: 本发明提供式I化合物及其药学上可接受的盐，其是电压门控钠通道的抑制剂，特别是Nav1.7。 该化合物可用于治疗与钠通道活性相关的疾病，例如疼痛障碍和瘙痒。 还提供含有本发明化合物的药物组合物。
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公开(公告)号：US20130303529A1
公开(公告)日：2013-11-14
申请号：US13916984
申请日：2013-06-13
Applicant: Amgen Inc.
Inventor： Brian K. ALBRECHT , David Bauer , Steven Bellon , Christiane M. Bode , Shon Booker , Alessandro Boezio , Deborah Choquette , Derin D'Amico , Jean-Christophe Harmange , Satoko Hirai , Randall W. Hungate , Tae-Seong Kim , Richard T. Lewis , Longbin Liu , Julia W. Lohman , Mark H. Norman , Michele Potashman , Aaron C. Siegmund , Stephanie K. Springer , Markian Stec , Ning Xi , Kevin Yang , Karina Romero , Katrina Woodin Copeland , Emily A. Peterson
IPC: C07D487/04 , A61K31/5377 , A61K31/5025 , A61K31/497 , A61K31/52 , A61K31/437 , A61K45/06 , C07D473/34 , C07D471/04 , A61K31/538 , A61K31/506
CPC classification number: A61K31/538 , A61K31/437 , A61K31/497 , A61K31/5025 , A61K31/506 , A61K31/52 , A61K31/5377 , A61K45/06 , C07D403/12 , C07D471/04 , C07D473/34 , C07D487/04 , C07D493/04 , C07D495/04 , C07D498/04 , C07D519/00
Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Abstract translation: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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7.发明授权Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use 有权氨基二氢噻嗪和氨基二氧化二氢噻嗪化合物作为β-分泌酶拮抗剂和使用方法公开(公告)号：US09556135B2
公开(公告)日：2017-01-31
申请号：US14433769
申请日：2013-10-10
Applicant: Amgen Inc.
Inventor： Richard T. Lewis , Jennifer R. Allen , Yuan Cheng , Deborah Choquette , Oleg Epstein , Angel Guzman-Perez , Paul E. Harrington , Zihao Hua , Randall W. Hungate , Jason Brooks Human , Ted Judd , Qingyian Liu , Patricia Lopez , Ana Elena Minatti , Philip Olivieri , Karina Romero , Shannon Rumfelt , Robert M. Rzasa , Laurie Schenkel , John Stellwagen , Ryan White , Qiufen Xue , Xiao Mei Zheng , Wenge Zhong
IPC: C07D279/12 , C07D417/04 , C07D471/04 , C07D239/74 , C07D495/04 , C07D213/79 , C07D241/44 , C07D417/12 , C07D417/14 , C07D513/04 , C07D498/04 , C07D513/10 , C07D279/14 , C07D519/00
CPC classification number: 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
Abstract: 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 A4, A5, A6, A8, R1, R2, R3, R7 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.
Abstract translation: 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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公开(公告)号：US20160046625A1
公开(公告)日：2016-02-18
申请号：US14828928
申请日：2015-08-18
Applicant: AMGEN INC.
Inventor： Christiane M. Boezio , Alan C. Cheng , Deborah Choquette , Richard T. Lewis , Michele H. Potashman , Karina Romero , John C. Stellwagen , Douglas A. Whittington
IPC: C07D471/04 , C07D519/00 , C07D417/12 , C07D403/06 , C07D235/32 , C07D401/06
CPC classification number: C07D471/04 , C07D235/30 , C07D235/32 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D519/00
Abstract: Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein.
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