公开(公告)号：EP2675810A1

公开(公告)日：2013-12-25

申请号：EP12704644.9

申请日：2012-02-13

申请人： Amgen Inc.

发明人： EPSTEIN, Oleg ,  WHITE, Ryan ,  PATEL, Vinod F. ,  HUMAN, Jason

IPC分类号： C07D491/00 ,  A61K31/353 ,  A61P25/00

CPC分类号： C07D491/20 ,  A61K31/353

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, R2, R7, X, Y and Z 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 and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.

公开(公告)号：EP1836174B1

公开(公告)日：2013-02-27

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 A 1 , A 2 , A 3 , B, R 1 , R 2 , R 3 and R 4 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.

公开(公告)号：EP2049115B1

公开(公告)日：2013-08-21

申请号：EP07810444.5

申请日：2007-07-13

申请人： Amgen Inc.

发明人： WHITE, Ryan

IPC分类号： A61K31/506 ,  C07D401/14 ,  C07D405/14 ,  A61P11/00 ,  A61P19/02 ,  A61P35/00

CPC分类号： C07D401/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14

公开(公告)号：EP2547686A1

公开(公告)日：2013-01-23

申请号：EP11714873.4

申请日：2011-03-14

申请人： Amgen Inc.

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

IPC分类号： C07D498/10 ,  C07D498/20 ,  C07D513/10 ,  C07D513/20 ,  A61K31/537 ,  A61K31/5386 ,  A61K31/547 ,  A61P25/28

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 A
1 , A
2 , A
3 , A
4 , A
5 , A
6 , 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).

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：EP2220078A2

公开(公告)日：2010-08-25

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

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.

公开(公告)号：EP2137177A2

公开(公告)日：2009-12-30

申请号：EP08742582.3

申请日：2008-04-03

申请人： Amgen, Inc

发明人： CEE, Victor, J. ,  DEAK, Holly, L. ,  GEUNS-MEYER, Stephanie, D. ,  DU, Bingfan ,  HODOUS, Brian, L. ,  MARTIN, Matthew, 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

CPC分类号： C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  C07D487/04 ,  C07D493/04 ,  C07D495/04

摘要： The present invention relates to chemical compounds having a general formula (I), wherein A1-8, D,, L1, L2, R1, R6-8 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.

公开(公告)号：EP2049115A2

公开(公告)日：2009-04-22

申请号：EP07810444.5

申请日：2007-07-13

申请人： Amgen Inc.

发明人： WHITE, Ryan

IPC分类号： A61K31/506 ,  C07D401/14 ,  C07D405/14 ,  A61P11/00 ,  A61P19/02 ,  A61P35/00

CPC分类号： C07D401/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14

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 A1-3, R1 and R3-6 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：EP2137177B1

公开(公告)日：2014-05-07

申请号：EP08742582.3

申请日：2008-04-03

申请人： Amgen, Inc

发明人： CEE, Victor, J. ,  DEAK, Holly, L. ,  GEUNS-MEYER, Stephanie, D. ,  DU, Bingfan ,  HODOUS, Brian, L. ,  MARTIN, Matthew, 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

CPC分类号： C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  C07D487/04 ,  C07D493/04 ,  C07D495/04

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