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1. 发明申请

WO2014078314A1 AMINO-OXAZINE AND AMINO-DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译：氨基氧化胺和氨基二氢化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：WO2014078314A1
公开(公告)日：2014-05-22
申请号：PCT/US2013/069697
申请日：2013-11-12
申请人： AMGEN INC.
发明人： WHITE, Ryan , EPSTEIN, Oleg , HUMAN, Jason, Brooks , ZHENG, Xiao Mei , SHAM, Kelvin , LIU, Qingyian , CHEN, Ning , CHENG, Yuan
IPC分类号： C07D498/10 , C07D498/20 , A61K31/537 , A61P25/28
CPC分类号： C07D519/00 , C07D311/80 , C07D491/052 , C07D498/10 , C07D498/20 , C07D513/10 , 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 , L, 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中的A1，A2，A3，A4，A5，A6，L，R2，R7，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。

2. 发明申请

WO2007024680A1 PYRAZOLOPYRIDINE AND PYRAZOLOPYRIMIDINE COMPOUNDS USEFUL AS KINASE ENZYMES MODULATORS 审中-公开
标题翻译：用作激酶酶调节剂的吡唑并吡啶和吡唑并嘧啶化合物有用
公开(公告)号：WO2007024680A1
公开(公告)日：2007-03-01
申请号：PCT/US2006/032314
申请日：2006-08-18
申请人： AMGEN INC. , BUCHANAN, John L. , BUCKNER, William H. , CARDOZO, Mario G. , DIMAURO, Erin F. , FU, Jiasheng , HAO, Xiaolin , JIAO, XianYun , KAYSER, Frank , KOPECKY, David J. , MASSE, Craig E. , TOMLINSON, Susan A. , WHITE, Ryan , ZHU, Xiaotian
发明人： BUCHANAN, John L. , BUCKNER, William H. , CARDOZO, Mario G. , DIMAURO, Erin F. , FU, Jiasheng , HAO, Xiaolin , JIAO, XianYun , KAYSER, Frank , KOPECKY, David J. , MASSE, Craig E. , TOMLINSON, Susan A. , WHITE, Ryan , ZHU, Xiaotian
IPC分类号： C07D487/04 , C07D231/56 , C07D403/06 , C07D405/06 , C07D401/14 , A61K31/519 , A61K31/416 , A61P19/00 , A61P17/00 , A61P35/00
CPC分类号： C07D403/06 , C07D231/56 , C07D401/14 , C07D405/06 , C07D487/04
摘要： The present invention relates to compounds of Formula (I) or a stereomer, a tautomer, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof, pharmaceutical formulations containing the compounds, methods of treatments using the compounds, for example, protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders and methods of preparing medicaments comprising the compounds.
摘要翻译：本发明涉及式（I）的化合物或立体异构体，互变异构体，溶剂化物，药学上可接受的盐或其前药，含有该化合物的药物制剂，使用该化合物的治疗方法，例如蛋白酪氨酸激酶 - 相关疾病如免疫学和肿瘤学疾病以及制备包含该化合物的药物的方法。

3. 发明申请

WO2012071279A1 SPIRO-AMINO-IMIDAZOLONE AND SPIRO-AMINO-DIHYDRO-PYRIMIDINONE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译： SPIRO-AMINO-IMIDAZOLONE和SPIRO-AMINO-DIHYDRO-PYRIMIDINONE化合物作为β-分泌酶调节剂及其使用方法
公开(公告)号：WO2012071279A1
公开(公告)日：2012-05-31
申请号：PCT/US2011/061473
申请日：2011-11-18
申请人： AMGEN INC. , MINATTI, Ana Elena , EPSTEIN, Oleg , WHITE, Ryan , WEISS, Matthew , ZHONG, Wenge , LOW, Jonathan
发明人： MINATTI, Ana Elena , EPSTEIN, Oleg , WHITE, Ryan , WEISS, Matthew , ZHONG, Wenge , LOW, Jonathan
IPC分类号： C07D491/20 , A61K31/527 , A61P25/28
CPC分类号： C07D491/107 , C07D491/20
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 , L, R 2 , R 7 , R 9 , W 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 plaque formation and deposition, resulting from the 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 (III), sub-Formula embodiments of Formulas (I), (II) and (III), intermediates and processes and methods useful for the preparation of compounds of Formulae (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，L，R2，R7，R9，W和Y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）和（III）的化合物，式（I），（II）和（III）的分式实施方案，可用于制备式（I-III）化合物的中间体和方法和方法）。

4. 发明申请

WO2008124083A3 AURORA KINASE MODULATORS AND METHOD OF USE 审中-公开
公开(公告)号：WO2008124083A3
公开(公告)日：2008-10-16
申请号：PCT/US2008/004432
申请日：2008-04-03
申请人： AMGEN INC. , CEE, Victor, J. , DEAK, Holly, L. , GEUNS-MEYER, Stephanie, D. , DU, Bingfan , HODOUS, Brian, L. , MARTIN, Mathew, W. , NGUYEN, Hanh, Nho , OLIVIERI, Philip, R. , PANTER, Kathleen , ROMERO, Karina , SCHENKEL, Laurie , WHITE, Ryan
发明人： CEE, Victor, J. , DEAK, Holly, L. , GEUNS-MEYER, Stephanie, D. , DU, Bingfan , HODOUS, Brian, L. , MARTIN, Mathew, W. , NGUYEN, Hanh, Nho , OLIVIERI, Philip, R. , PANTER, Kathleen , ROMERO, Karina , SCHENKEL, Laurie , WHITE, Ryan
IPC分类号： C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/04 , C07D471/04 , C07D487/04 , C07D493/04 , C07D495/04 , A61K31/502 , A61P35/00
摘要： The present invention relates to chemical compounds having a general formula (I), wherein A 1-8 , D , , L 1 , L 2 , R 1 , R 6-8 and n 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.

5. 发明申请

WO2014120658A1 FUSED MULTICYCLIC 3-AMINO-5,6-DIHYDRO-2H-1,4-THIAZINE DERIVATIVES AND THEIR USE AS BETA-SECRETASE INHIBITORS 审中-公开
标题翻译：熔融多金属3-氨基-5,6-二氢-2H-1,4-THIAZINE衍生物及其作为β-分泌酶抑制剂的用途
公开(公告)号：WO2014120658A1
公开(公告)日：2014-08-07
申请号：PCT/US2014/013340
申请日：2014-01-28
申请人： AMGEN INC.
发明人： WHITE, Ryan , ALLEN, Jennifer R. , EPSTEIN, Oleg , HONG, Fang-Tsao , HUA, Zihao , HUMAN, Jason Brooks , LOPEZ, Patricia , OLIVIERI, Philip R. , ROMERO, Karina , SCHENKEL, Laurie , STELLWAGEN, John , TAMAYO, Nuria A. , ZHENG, Xiao Mei
IPC分类号： C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04 , C07D513/10 , C07D513/14 , C07D513/20 , C07D519/00 , A61K31/5415 , A61K31/542 , A61K31/547 , A61K31/55 , A61P25/00 , A61P25/28
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 A 5 , A 6 , A 8 , R 1 , R 2 , R 3 , R 7 , 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。本发明进一步提供式II化合物及其分式实施方案，式III化合物，可用于制备式I-III化合物及其分式的中间体和方法和方法。

6. 发明申请

WO2013044092A1 AMINO-OXAZINES AND AMINO-DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译：氨基氧化合物和氨基二氢化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：WO2013044092A1
公开(公告)日：2013-03-28
申请号：PCT/US2012/056658
申请日：2012-09-21
申请人： AMGEN INC. , WHITE, Ryan , CHENG, Yuan , MINATTI, Ana Elena , YANG, Bryant , ZHENG, Xiao Mei , LOPEZ, Patricia , HUMAN, Jason B. , EPSTEIN, Oleg , JUDD, Ted , SHAM, Kelvin , XUE, Qiufen
发明人： WHITE, Ryan , CHENG, Yuan , MINATTI, Ana Elena , YANG, Bryant , ZHENG, Xiao Mei , LOPEZ, Patricia , HUMAN, Jason B. , EPSTEIN, Oleg , JUDD, Ted , SHAM, Kelvin , XUE, Qiufen
IPC分类号： C07D498/10 , A61K31/537 , A61P25/28
CPC分类号： C07D498/10 , C07D498/20 , C07D513/10 , 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 , L, 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中的A1，A2，A3，A4，A5，A6，L，R2，R7，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。

7. 发明申请

WO2009058267A2 BENZOMORPHOLINE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：苯并吡喃衍生物及其使用方法
公开(公告)号：WO2009058267A2
公开(公告)日：2009-05-07
申请号：PCT/US2008/012224
申请日：2008-10-28
申请人： AMGEN INC. , HARMANGE, Jean-christophe , WILLIAM, Matthew W. , TEFFERA, Yohannes , SUBRAMANIAN, Raju , WHITE, Ryan , ZANON, Roger , LARROW, Jay , PAYACK, Joseph F. , DILMEGHANI SERAN, Mina
发明人： HARMANGE, Jean-christophe , WILLIAM, Matthew W. , TEFFERA, Yohannes , SUBRAMANIAN, Raju , WHITE, Ryan , ZANON, Roger , LARROW, Jay , PAYACK, Joseph F. , DILMEGHANI SERAN, Mina
IPC分类号： C07D413/14 , A61K31/536 , A61P35/00
CPC分类号： C07D413/14
摘要： Selected benzomorpholine compounds are effective for prophylaxis and treatment of diseases, such as VEGF 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.
摘要翻译：选择的苯并吗啉化合物对于预防和治疗诸如VEGF介导的疾病的疾病是有效的。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。

8. 发明申请

WO2008011109A2 SUBSTITUTED PYRIDONE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：取代的吡咯烷酮化合物及其使用方法
公开(公告)号：WO2008011109A2
公开(公告)日：2008-01-24
申请号：PCT/US2007/016382
申请日：2007-07-17
申请人： AMGEN INC. , HU, Essa , HUMAN, Jason, Brooks , KUNZ, Roxanne , TASKER, Andrew , WHITE, Ryan
发明人： HU, Essa , HUMAN, Jason, Brooks , KUNZ, Roxanne , TASKER, Andrew , WHITE, Ryan
IPC分类号： C07D401/04 , C07D471/04 , A61P35/00 , A61K31/517 , A61K31/4709
CPC分类号： C07D471/04 , C07D401/04
摘要： The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula: (I); wherein A0-3 and R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译：本发明包括能够调节c-kit受体的新一类化合物，因此可用于治疗c-kit介导的疾病，包括各种炎性，纤维化和/或肥大细胞介导的疾病如肥大细胞增多症。该化合物具有通式：（I）; 其中A0-3和R1-6在本文中定义。本发明还包括药物组合物，用于治疗c-kit介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

9. 发明申请

WO2006130160A2 FURANOPYRIDINE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：呋喃并吡啶衍生物及其使用方法
公开(公告)号：WO2006130160A2
公开(公告)日：2006-12-07
申请号：PCT/US2005/025725
申请日：2005-07-19
申请人： AMGEN INC. , NUNES, Joseph, J. , MARTIN, Matthew, W. , WHITE, Ryan , MCGOWAN, David , BEMIS, Jean, E. , KAYSER, Frank , FU, Jiasheng , LIU, Jinqian , JIAO, XianYun
发明人： NUNES, Joseph, J. , MARTIN, Matthew, W. , WHITE, Ryan , MCGOWAN, David , BEMIS, Jean, E. , KAYSER, Frank , FU, Jiasheng , LIU, Jinqian , JIAO, XianYun
CPC分类号： C07D491/04 , C07D491/14
摘要： The present invention relates to furanopyridine compounds having the general Formula I (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of modulating Lck and ACK-1 enzymes and of treating various related diseases and conditions, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, comprising administering to the mammal a therapeutically effective amount a compound of Formula I, as described above, and methods of manufacturing medicaments comprising the compound of Formula I.
摘要翻译：本发明涉及具有通式I（I）的呋喃并吡啶化合物及其立体异构体，互变异构体，溶剂合物，药学上可接受的盐和衍生物及其前药。本发明还包括药物组合物，其包含式I化合物，调节Lck和ACK-1酶的方法以及治疗各种相关疾病和病症，包括炎症，T细胞活化抑制，增殖，关节炎，器官移植，缺血或再灌注损伤，心肌梗塞，中风，多发性硬化，炎性肠病，克罗恩病，狼疮，超敏反应，1型糖尿病，牛皮癣，皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进，艾迪生病，自身免疫性疾病，肾小球肾炎，过敏性疾病，哮喘，干草组织，湿疹，癌症，结肠癌，胸腺瘤，仅举几个例子，在哺乳动物中，包括向哺乳动物施用治疗有效量的如上所述的式I化合物和制备包含以下化合物的药物的方法：一级方程式

10. 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.

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