公开(公告)号：EP2328903B1

公开(公告)日：2014-03-05

申请号：EP09737222.1

申请日：2009-09-11

申请人： Amgen Inc.

发明人： WHITE, Ryan ,  AMEGADZIE, Albert ,  BRYAN, Marian C. ,  CHEN, Jian J. ,  CHENG, Alan C. ,  DINEEN, Thomas ,  EPSTEIN, Oleg ,  GORE, Vijay Keshav ,  HUA, Zihao ,  HUMAN, Jason B. ,  HUANG, Hongbing ,  KREIMAN, Charles ,  LA, Daniel ,  LIU, Qingyian ,  MA, Vu Van ,  MARX, Isaac ,  PATEL, Vinod F. ,  QIAN, Wenyuan ,  WEISS, Matthew ,  YUAN, Chester C.

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

CPC分类号： C07D498/10 ,  C07D513/10

公开(公告)号：EP2430013A1

公开(公告)日：2012-03-21

申请号：EP10719514.1

申请日：2010-05-12

申请人： Amgen, Inc

发明人： BODE, Christiane ,  BOEZIO, Alessandro ,  CHENG, Alan, C. ,  CHOQUETTE, Deborah ,  COATS, James, R. ,  COPELAND, Katrina, W. ,  HUANG, Hongbing ,  LA, Daniel ,  LEWIS, Richard ,  LIAO, Hongyu ,  POTASHMAN, Michele ,  STELLWAGEN, John ,  YI, Shuyan ,  NORMAN, Mark ,  STEC, Markian ,  PETERSON, Emily, A. ,  GRACEFFA, Russell

IPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/506 ,  A61K31/437 ,  A61K31/52 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

摘要： The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3Kα kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3Kα, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：EP2328903A1

公开(公告)日：2011-06-08

申请号：EP09737222.1

申请日：2009-09-11

申请人： Amgen Inc.

发明人： WHITE, Ryan ,  AMEGADZIE, Albert ,  BRYAN, Marian C. ,  CHEN, Jian J. ,  CHENG, Alan C. ,  DINEEN, Thomas ,  EPSTEIN, Oleg ,  GORE, Vijay Keshav ,  HUA, Zihao ,  HUMAN, Jason B. ,  HUANG, Hongbing ,  KREIMAN, Charles ,  LA, Daniel ,  LIU, Qingyian ,  MA, Vu Van ,  MARX, Isaac ,  PATEL, Vinod F. ,  QIAN, Wenyuan ,  WEISS, Matthew ,  YUAN, Chester C.

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

CPC分类号： C07D498/10 ,  C07D513/10

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 , T
1 , T
2 , W, 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).

公开(公告)号：EP2822944A1

公开(公告)日：2015-01-14

申请号：EP13710236.4

申请日：2013-03-01

申请人： AMGEN, INC.

发明人： BREGMAN, Howard ,  BUCHANAN, John, L. ,  CHAKKA, Nagasree ,  DIMAURO, Erin ,  GUNAYDIN, Hakan ,  GUZMAN PEREZ, Angel ,  HUA, Zihao ,  HUANG, Hongbing ,  HUANG, Xin ,  MARTIN, Matthew, W. ,  PATEL, Vinod

IPC分类号： C07D413/14 ,  C07D413/08 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07D263/34 ,  C07D519/00 ,  A61K31/4166 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D263/34 ,  C07D413/08 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D519/00

摘要： Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.

公开(公告)号：EP2430013B1

公开(公告)日：2014-10-15

申请号：EP10719514.1

申请日：2010-05-12

申请人： Amgen Inc.

发明人： BODE, Christiane ,  BOEZIO, Alessandro ,  CHENG, Alan, C. ,  CHOQUETTE, Deborah ,  COATS, James, R. ,  COPELAND, Katrina, W. ,  HUANG, Hongbing ,  LA, Daniel ,  LEWIS, Richard ,  LIAO, Hongyu ,  POTASHMAN, Michele ,  STELLWAGEN, John ,  YI, Shuyan ,  NORMAN, Mark ,  STEC, Markian ,  PETERSON, Emily, A. ,  GRACEFFA, Russell

IPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/506 ,  A61K31/437 ,  A61K31/52 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

公开(公告)号：EP2398791A1

公开(公告)日：2011-12-28

申请号：EP10704074.3

申请日：2010-02-10

申请人： Amgen, Inc

发明人： BOEZIO, Alessandro ,  CHENG, Alan, C. ,  COATS, James, R. ,  COPELAND, Katrina, W. ,  GRACEFFA, Russell ,  HARMANGE, Jean-Christophe ,  HUANG, Hongbing ,  LA, Daniel ,  OLIVIERI, Philip, R. ,  PETERSON, Emily, A. ,  SCHENKEL, Laurie

IPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/53 ,  A61K31/506 ,  A61K31/5355 ,  A61P35/00

CPC分类号： C07D403/14 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides compounds that are kinase inhibitors, specifically PIK kinase inhibitors, more specifically, mTOR inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PIK kinase inhibitors, more specifically, mTOR such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.