公开(公告)号：US20130165445A1

公开(公告)日：2013-06-27

申请号：US13757438

申请日：2013-02-01

申请人： AMGEN INC.

发明人： Ryan WHITE ,  Jason HUMAN

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to chemical compounds having a general formula I wherein A1-5 and 7-8, D′, L1, L2, R1, R3, R6-8, n and o are defined herein, and synthetic intermediates, which are capable of modulating the activity of Aurora kinase proteins and, thereby, influencing various disease states and conditions related to the activities of Aurora kinases. 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, 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A1-5和7-8，D'，L1，L2，R1，R3，R6-8，n和o如本文所定义，和合成中间体，其能够 调节极光激酶蛋白的活性，从而影响与极光激酶活性相关的各种疾病状态和状况。 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，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。

公开(公告)号：US20140045828A1

公开(公告)日：2014-02-13

申请号：US13929483

申请日：2013-06-27

申请人： AMGEN INC.

发明人： Jian CHEN ,  Wenge ZHONG ,  Bryant YANG ,  Wenyuan QIAN ,  Patricia LOPEZ ,  Ryan WHITE ,  Matthew WEISS ,  Tedd JUDD ,  Timothy POWERS ,  Yuan CHENG ,  Thomas DINEEN ,  Oleg EPSTEIN ,  Jason HUMAN ,  Jonathan D. LOW ,  Isaac E. MARX ,  Ana Elena MINATTI ,  Michele POTASHMAN ,  Nick A. PARAS ,  Qingyian LIU

IPC分类号： C07D513/10 ,  C07D498/20

CPC分类号： C07D513/10 ,  C07D498/10 ,  C07D498/20 ,  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 A1, A2, A3, A4, A5, A6, R2, R7, 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，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。