公开(公告)号：EP1963312B1

公开(公告)日：2014-07-02

申请号：EP06838016.1

申请日：2006-11-17

申请人： Amgen Inc.

发明人： XUE, Qiufen ,  ALBRECHT, Brian K. ,  ANDERSEN, Denise Lyn ,  BARTBERGER, Michael ,  BROWN, James ,  BROWN, Ryan ,  CHAFFEE, Stuart C. ,  CHENG, Yuan ,  CROGHAN, Michael ,  GRACEFFA, Russell ,  HARRIED, Scott ,  HITCHCOCK, Stephen ,  HUNGATE, Randall ,  JUDD, Ted ,  KALLER, Matthew ,  KREIMAN, Charles ,  LA, Daniel ,  LOPEZ, Patricia ,  MASSE, Craig E. ,  MONENSCHEIN, Holger ,  NGUYEN, Thomas ,  NIXEY, Thomas ,  PATEL, Vinod F. ,  PENNINGTON, Lewis ,  WEISS, Matthew ,  YANG, Bryant ,  ZHONG, Wenge

IPC分类号： C07D405/12 ,  C07D413/12 ,  A61K31/44 ,  A61P25/28

CPC分类号： C07D405/12 ,  C07D413/12

公开(公告)号：EP1773817B1

公开(公告)日：2009-08-26

申请号：EP05791799.9

申请日：2005-07-20

申请人： Amgen Inc.

发明人： YUAN, Chester Chenguang ,  YANG, Kevin ,  VANDERPLAS, Simon ,  RIAHI, Babak ,  POTASHMAN, Michele ,  PATEL, Vinod F. ,  NOMAK, Rana ,  LI, Aiwen ,  HUANG, Qi ,  HARMANGE, Jean-Christophe ,  ASKEW, JR., Benny C.

IPC分类号： C07D401/12 ,  C07D413/14 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D217/02 ,  C07D403/12 ,  C07D417/14 ,  C07D471/04 ,  A61K31/443 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4725 ,  A61P35/00

CPC分类号： C07D401/12 ,  C07D217/02 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： The present invention provides classes of compounds, including-their pharmaceutically acceptable derivatives, useful for treating angiogenesis and related diseases such as cancer. Formula I and II wherein R is a 9- or 10-membered heterocyclyl ring selected from 7-isoquinolinyl,..2-methyl-3-oxo-2,3-dihydroindazol-6-yl, [1,6]-naphthydrin-3-yl, [1,7]-naphthydrin-2-yl, 1-oxo-2,3-dihydrobenzofuran-4-yl, 3-oxo-2,3-dihydrobenzofuran-5-yl, dihydro-benzodioxinyl, 6-quinazolinyl, 2-amino-6-quinazolinyl, 4-methylamino-6-quinazolinyl, 2,4-diamino-6 quinazolinyl, 3-oxo-3,4-dihydro-1,4-benzoxazin-6-yl, 2,2-difluoro-l;3-benzodioxol-5-yl and 2,2,3,3 tetrafluoro-2,3-dihydro-l,4-benzodioxin-6-yl, each of which is optionally substituted with one or more substituents selected from halo, haloakyl, C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, N-dimethylamino-C1-6-alkyl, N-dimethylamino-C1-6-alkoxy, amino, alkyl-carbonylamino, morpholino-sulfonyl, amino-sulfonyl, oxazolyl, pyrrolyl,4 morpholinyl, carboxyl, cyano, and acetyl; wherein R1 in formula I is selected from unsubstituted or substituted phenyl, 5-6 membered heteroaryl, 9-10 membered bicyclic heterocyclyl and 11-14 membered tricyclic heterocyclyl, and R1 in formula II is selected from specific bicyclic heterocycles.

公开(公告)号：EP1218360B1

公开(公告)日：2008-05-28

申请号：EP00972036.8

申请日：2000-10-06

申请人： Amgen Inc.,

发明人： ARMISTEAD, David, M. ,  BEMIS, Jean, E. ,  BUCHANAN, John, L. ,  DIPIETRO, Lucian, V. ,  ELBAUM, Daniel ,  HABGOOD, Gregory, J. ,  KIM, Joseph, L. ,  MARSHALL, Teresa, L. ,  GEUNS-MEYER, Stephanie, D. ,  NOVAK, Perry, M. ,  NUNES, Joseph, J. ,  PATEL, Vinod F. ,  TOLEDO-SHERMAN, Leticia, M. ,  ZHU, Xiaotian

IPC分类号： C07D251/22 ,  C07D403/12 ,  A61P43/00 ,  C07D251/16 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D405/04 ,  C07D401/14 ,  C07D405/14

CPC分类号： C07D401/04 ,  C07D251/18 ,  C07D251/22 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The invention relates to inhibitors of formula (I) of enzymes that bind to ATP or GTP and/or catalyze phosphoryl transfer, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making phosphoryl transferase inhibitor compounds, methods of inhibiting phosphoryl transferase activity, and methods for treating disease or disease symptoms. In formula (I), each R?1 and R2¿ is independently R?3; R8; NHR3; NHR5; NHR6; NR5R5; NR5R6; SR5; SR6; SR3; OR5; OR6; OR3; C(O)R3¿; heterocyclyl optionally substituted with 1-4 independent R4 on each ring; or C1-C10 alkyl substituted with 1-4 independent R?4; R3, R4, R5, R6, R8¿ are as defined in the application.

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：EP2167471A1

公开(公告)日：2010-03-31

申请号：EP08754710.5

申请日：2008-05-23

申请人： Amgen Inc.

发明人： ZHONG, Wenge ,  HITCHCOCK, Stephen ,  PATEL, Vinod F. ,  CROGHAN, Michael ,  DINEEN, Thomas ,  HORNE, Daniel ,  KALLER, Matthew ,  KREIMAN, Charles ,  LOPEZ, Patricia ,  MONENSCHEIN, Holger ,  NGUYEN, Thomas ,  PENNINGTON, Lewis ,  XUE, Qiufen ,  YANG, Bryant

IPC分类号： C07D221/06 ,  C07D311/96 ,  C07D471/10 ,  C07D491/10 ,  C07D493/10 ,  C07D495/10 ,  A61P25/28 ,  A61K31/438

CPC分类号： C07D491/107 ,  C07D221/06 ,  C07D311/96 ,  C07D471/10 ,  C07D491/10 ,  C07D493/10 ,  C07D495/10

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 R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z 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 (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.

公开(公告)号：EP1638954A1

公开(公告)日：2006-03-29

申请号：EP04758050.1

申请日：2004-03-22

申请人： AMGEN INC.

发明人： DIPIETRO, Lucian V. ,  HARMANGE, Jean-Christophe ,  ASKEW, JR., Benny C. ,  ELBAUM, Daniel ,  GERMAIN, Julie ,  HABGOOD, Gregory J. ,  KIM, Joseph L. ,  PATEL, Vinod F. ,  POTASHMAN, Michele ,  VAN DER PLAS, Simon

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/4184 ,  A61P35/00

CPC分类号： C07D401/12 ,  C07D235/30 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

摘要： The invention relates to compounds of the formulae (I) to (III) wherein the substituents are as defined in the specification. These compounds have kinase inhibitory activity, such as VEGFR/KDR inhibitory activity. Accordingly, the compounds of the formulae (I) to (III) would be useful in the prevention and treatment of angiogenesis related disorders, ophthalmological conditions, proliferative diseases, inflammatory diseases, and other pathological conditions as described in the specification.

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：EP2673279A1

公开(公告)日：2013-12-18

申请号：EP12705212.4

申请日：2012-02-06

申请人： Amgen Inc.

发明人： DINEEN, Thomas ,  WEISS, Matthew ,  PATEL, Vinod F. ,  ZHENG, Xiao Mei ,  WHITE, Ryan

IPC分类号： C07D498/10 ,  C07D498/20 ,  C07D513/10 ,  A61K31/553 ,  A61K31/554 ,  A61P25/16 ,  A61P25/28

CPC分类号： C07D498/20 ,  C07D498/10 ,  C07D513/10

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 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 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 Formulas (II) and sub-formula embodiments of Formula (I) and (II), intermediates and processes and methods useful for the preparation of compounds of Formulas (I)-(II).

公开(公告)号：EP1836174B2

公开(公告)日：2019-10-02

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

公开(公告)号：EP1984353B1

公开(公告)日：2015-12-30

申请号：EP07716912.6

申请日：2007-01-22

申请人： Amgen, Inc

发明人： CEE, Victor J. ,  DEAK, Holly L. ,  DU, Bingfan ,  GEUNS-MEYER, Stephanie D. ,  HODOUS, Brian L. ,  NGUYEN, Hanh Nho ,  OLIVIERI, Philip R. ,  PATEL, Vinod F. ,  ROMERO, Karina ,  SCHENKEL, Laurie

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D497/04 ,  A61K31/502 ,  A61P35/00

CPC分类号： C07D401/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D497/04