公开(公告)号：EP2643325A1

公开(公告)日：2013-10-02

申请号：EP11791392.1

申请日：2011-11-18

申请人： Amgen Inc.

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 A1, A3, A4, A5, A6, A8, L, R2, R7, R9, 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).

公开(公告)号：EP2220078B1

公开(公告)日：2013-05-22

申请号：EP08845711.4

申请日：2008-10-28

申请人： Amgen, Inc

发明人： HARMANGE, Jean-christophe ,  MARTIN, 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

公开(公告)号：EP2547685A1

公开(公告)日：2013-01-23

申请号：EP11710372.1

申请日：2011-03-14

申请人： Amgen Inc.

发明人： CHENG, Yuan ,  WHITE, Ryan ,  AMEGADZIE, Albert ,  BROWN, James ,  CHENG, Alan, C. ,  DIMAURO, Erin, F. ,  DINEEN, Thomas ,  GORE, Vijay Keshav ,  HUMAN, Jason, Brooks ,  JUDD, Ted ,  KREIMAN, Charles ,  LIU, Qingyian ,  LOPEZ, Patricia ,  MA, Vu, Van ,  MARX, Isaac ,  MINATTI, Ana, Elena ,  NGUYEN, Hanh, Nho ,  PARAS, Nick, A. ,  PATEL, Vinod, F. ,  QIAN, Wenyuan ,  WEISS, Matthew ,  XUE, Qiufen ,  ZHENG, Xiao Mei ,  ZHONG, Wenge ,  EPSTEIN, Oleg

IPC分类号： C07D498/10 ,  C07D498/20 ,  C07D513/10 ,  A61K31/424 ,  A61K31/429 ,  A61P25/28

CPC分类号： C07D491/10 ,  A61K31/42 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/5377 ,  C07D221/20 ,  C07D235/02 ,  C07D263/08 ,  C07D295/135 ,  C07D498/10 ,  C07D498/20 ,  C07D513/10 ,  C09B11/28

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 other 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 , R
2 , R
7 , X and Y 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））和其它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，R2，R7，X和Y定义如下。 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。

公开(公告)号：EP2288611A1

公开(公告)日：2011-03-02

申请号：EP09723292.0

申请日：2009-03-19

申请人： Amgen Inc.

发明人： WHITE, Ryan ,  HUMAN, Jason, B.

IPC分类号： C07D487/04 ,  A61K31/437 ,  A61K31/5025 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D487/04

摘要： The present invention relates to chemical compounds having a general formula (I) wherein A
1-5 and 7-8 , D', L
1 , L
2 , R
1 , R
3 , R
6-8 , 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.

公开(公告)号：EP2079724A2

公开(公告)日：2009-07-22

申请号：EP07810612.7

申请日：2007-07-17

申请人： Amgen Inc.

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.

公开(公告)号：EP1836174A2

公开(公告)日：2007-09-26

申请号：EP05818381.5

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. ,  MASSE, Craig E. ,  BUCKNER, William H. ,  TEMPEST, Paul A. ,  HERBERICH, Bradley J. ,  GRACEFFA, Russell ,  ZHANG, Dawei ,  XU, Shimin ,  SHAM, Kelvin ,  RZASA, Robert M. ,  FALSEY, James Richard ,  CHAKRABARTI, Partha P. ,  CAO, Guo-giang ,  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

CPC分类号： C07D215/38 ,  C07C205/37 ,  C07D215/12 ,  C07D217/12 ,  C07D217/22 ,  C07D217/26 ,  C07D239/26 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

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.