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公开(公告)号：US08772480B2
公开(公告)日：2014-07-08
申请号：US13681230
申请日：2012-11-19
申请人： Amgen Inc.
发明人： Kristin L. Andrews , Yunxin Y. Bo , Shon Booker , Victor J. Cee , Noel D'Angelo , Bradley J. Herberich , Fang-Tsao Hong , Claire L. M. Jackson , Brian Alan Lanman , Hongyu Liao , Longbin Liu , Nobuko Nishimura , Mark H. Norman , Liping H. Pettus , Anthony B. Reed , Adrian Leonard Smith , Seifu Tadesse , Nuria A. Tamayo , Bin Wu , Ryan Wurz , Kevin C. Yang
IPC分类号： C07D401/04 , C07D401/14 , A61K31/444 , A61K31/53 , A61P35/00
CPC分类号： C07D473/00 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐; 使用该化合物治疗疾病或病症如癌症的方法; 和含有这些化合物的药物组合物，其中变量如本文所定义。
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公开(公告)号：US11643440B2
公开(公告)日：2023-05-09
申请号：US16619874
申请日：2018-06-01
申请人： AMGEN INC.
发明人： Irwin Chen , Su Chong , Essa Hu Harrington , Fang-Tsao Hong , Jason C. Long , Leslie P. Miranda
CPC分类号： C07K14/001 , A61P25/06 , A61K38/00
摘要： Novel peptides that bind to human PAC1 are provided. These peptides that are antagonists of PAC1 are useful in a number of PAC1 related disorders, including the treatment and/or prevention of headache disorders, including migraine, such as acute migraine.
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3.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
申请人： AMGEN INC.
发明人： 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分类号： C07D417/10 , C07D417/14 , C07D513/04 , C07D513/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/10 , C07D513/20 , C07D519/00
CPC分类号： C07D513/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/10 , C07D513/14 , C07D513/20 , 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 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.
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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公开(公告)号：US20130079303A1
公开(公告)日：2013-03-28
申请号：US13681230
申请日：2012-11-19
申请人： Amgen Inc.
发明人： Kristin L. ANDREWS , Yunxin Y. Bo , Shon Booker , Victor J. Cee , Noel D'Angelo , Bradley J. Herberich , Fang-Tsao Hong , Claire I.M. Jackson , Brian Alan Lanman , Hongyu Liao , Longbin Liu , Nobuko Nishimura , Mark H. Norman , Liping H. Pettus , Anthony B. Reed , Adrian Leonard Smith , Seifu Tadesse , Nuria A. Tamayo , Bin Wu , Ryan Wurz , Kevin C. Yang
IPC分类号： C07D473/00 , C07D417/14 , C07D405/14 , C07D413/14 , C07D401/14
CPC分类号： C07D473/00 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐; 使用该化合物治疗疾病或病症如癌症的方法; 和含有这些化合物的药物组合物，其中变量如本文所定义。
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