公开(公告)号：EP1951696A2

公开(公告)日：2008-08-06

申请号：EP06844335.7

申请日：2006-11-13

申请人： Amgen Inc. ,  BIOVITRUM AB

发明人： HENRIKSSON, Martin ,  HOMAN, Evert ,  JOHANSSON, Lars ,  VALLGARDA, Jerk ,  WILLIAMS, Meredith ,  BERCOT, Eric, A. ,  FOTSCH, Christopher, H. ,  LI, Aiwen ,  CAI, Guolin ,  HUNGATE, Randall, W. ,  YUAN, Chester, Chenguang ,  TEGLEY, Christopher ,  ST. JEAN, David, J., Jr. ,  HAN, Nianhe ,  HUANG, Qi ,  LIU, Qingyian ,  BARTBEGER, Michael, D. ,  MONIZ, George, A. ,  FRIZZLE, Matthew, J. ,  MARSHALL, Teresa, L.

IPC分类号： C07D277/54 ,  C07D277/60 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  A61K31/426 ,  A61K31/427

CPC分类号： C07D277/54 ,  C07D277/60 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11- β-hydroxysteroid dehydrogenase type 1 enzyme.

公开(公告)号：EP1753736A2

公开(公告)日：2007-02-21

申请号：EP05756354.6

申请日：2005-05-24

申请人： Amgen Inc. ,  BIOVITRUM AB

发明人： HENRIKSSON, Martin ,  HOMAN, Evert ,  JOHANSSON, Lars ,  VALLGARDA, Jerk ,  WILLIAMS, Meredith ,  BERCOT, Eric ,  FOTSCH, Christopher, H. ,  LI, Aiwen ,  CAI, Guolin ,  HUNGATE, Randall, W. ,  YUAN, Chester, Chenguang ,  TEGLEY, Chirstopher ,  ST. JEAN, David ,  HAN, Nianhe ,  HUANG, Qi ,  LIU, Qingyian ,  BARTBERGER, Michael D. ,  MONIZ, George, A. ,  FRIZZLE, Matthew, J.

IPC分类号： C07D277/54 ,  C07D263/48 ,  A61K31/42 ,  A61K31/426 ,  A61P3/04 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  A61P19/10 ,  A61P31/12 ,  A61P29/00 ,  A61P25/28 ,  A61P25/24

CPC分类号： C07D417/06 ,  C07D263/34 ,  C07D263/48 ,  C07D275/03 ,  C07D277/42 ,  C07D277/54 ,  C07D277/60 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10 ,  C07F7/1856

摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): (I) (II), (III), or (IV), wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

公开(公告)号：EP1753736B1

公开(公告)日：2008-12-17

申请号：EP05756354.6

申请日：2005-05-24

申请人： Amgen Inc. ,  BIOVITRUM AB

发明人： HENRIKSSON, Martin ,  HOMAN, Evert ,  JOHANSSON, Lars ,  VALLGARDA, Jerk ,  WILLIAMS, Meredith ,  BERCOT, Eric ,  FOTSCH, Christopher, H. ,  LI, Aiwen ,  CAI, Guolin ,  HUNGATE, Randall, W. ,  YUAN, Chester, Chenguang ,  TEGLEY, Chirstopher ,  ST. JEAN, David ,  HAN, Nianhe ,  HUANG, Qi ,  LIU, Qingyian ,  BARTBERGER, Michael D. ,  MONIZ, George, A. ,  FRIZZLE, Matthew, J.

IPC分类号： C07D277/54 ,  C07D263/48 ,  A61K31/42 ,  A61K31/426 ,  A61P3/04 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  A61P19/10 ,  A61P31/12 ,  A61P29/00 ,  A61P25/28 ,  A61P25/24

CPC分类号： C07D417/06 ,  C07D263/34 ,  C07D263/48 ,  C07D275/03 ,  C07D277/42 ,  C07D277/54 ,  C07D277/60 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10 ,  C07F7/1856

摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): (I) (II), (III), or (IV), wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

公开(公告)号：EP1537084B1

公开(公告)日：2013-08-21

申请号：EP03764794.8

申请日：2003-07-15

申请人： AMGEN INC.

发明人： ASKEW JR, Benny C. ,  ADAMS, Jeffrey ,  BOOKER, Shon ,  CHEN, Guoqing ,  DIPIETRO, Lucian, V. ,  ELBAUM, Daniel ,  GERMAIN, Julie ,  GEUNS-MEYER, Stephanie, D. ,  HABGOOD, Gregory, J. ,  HANDLEY, Michael ,  HUANG, Qi ,  KIM, Tae-Seong ,  LI, Aiwen ,  NISHIMURA, Nobuko ,  NOMAK, Rana, Bogazici University ,  PATEL, Vinod, F. ,  RIAHI, Babak ,  KIM, Joseph, L. ,  XI, Ning ,  YUAN, Chester, Chenguang

IPC分类号： C07D213/82 ,  C07D401/12 ,  C07D417/12 ,  C07D471/04 ,  A61K31/44 ,  A61P19/00 ,  A61P35/00

CPC分类号： C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

公开(公告)号：EP1976836A2

公开(公告)日：2008-10-08

申请号：EP06848110.0

申请日：2006-12-22

申请人： Amgen Inc.

发明人： DE MORIN, Frenel, F. ,  CHEN, Jian J. ,  DOHERTY, Elizabeth M. ,  HITCHCOCK, Stephen ,  HUANG, Qi ,  KIM, Joseph, L. ,  LIU, Gang ,  NIXEY, Thomas ,  PARAS, Nick, A. ,  PETKUS, Jeffrey ,  RETZ, Daniel, M. ,  SMITH, Adrian, L. ,  TASKER, Andrew ,  ZHU, Jiawang

IPC分类号： C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D401/14 ,  C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have Formula (I) wherein R1 is Formula (II), (III) or (IV) and A1, A2, A3, A4, X, Z, Z', R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

公开(公告)号：EP1773817A1

公开(公告)日：2007-04-18

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：EP1562933A2

公开(公告)日：2005-08-17

申请号：EP03764755.9

申请日：2003-07-15

申请人： Amgen Inc.

发明人： PATEL, Vinod, F. ,  ASKEW JR, Benny, C. ,  BOOKER, Shon ,  CHEN, Guoqing ,  DIPIETRO, Lucian, V. ,  GERMAIN, Julie ,  HABGOOD, Gregory, J. ,  HUANG, Qi ,  KIM, Tae-Seong ,  LI, Aiwen ,  NISHIMURA, Nobuko ,  NOMAK, Rana ,  RIAHI, Babak ,  YUAN, Chester, Chenguang ,  ELBAUM, Daniel

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D417/14 ,  C07D405/14 ,  C07D407/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4433 ,  C07D413/14

CPC分类号： C07D471/04 ,  A61K31/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

摘要： Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis 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：EP1537084A1

公开(公告)日：2005-06-08

申请号：EP03764794.8

申请日：2003-07-15

申请人： Amgen Inc.

发明人： ASKEW JR, Benny C. ,  ADAMS, Jeffrey ,  BOOKER, Shon ,  CHEN, Guoqing ,  DIPIETRO, Lucian, V. ,  ELBAUM, Daniel ,  GERMAIN, Julie ,  GEUNS-MEYER, Stephanie, D. ,  HABGOOD, Gregory, J. ,  HANDLEY, Michael ,  HUANG, Qi ,  KIM, Tae-Seong ,  LI, Aiwen ,  NISHIMURA, Nobuko ,  NOMAK, Rana ,  PATEL, Vinod, F. ,  RIAHI, Babak ,  KIM, Joseph, L. ,  XI, Ning ,  YUAN, Chester, Chenguang

IPC分类号： C07D213/82 ,  C07D401/12 ,  C07D417/12 ,  C07D471/04 ,  A61K31/44 ,  A61P19/00 ,  A61P35/00

CPC分类号： C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： Selected amines of Formula XIII, which are effective for prophylaxis and treatment of diseases, such as angiogenesis 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.

摘要翻译： 选择的式ⅩⅢ胺有效预防和治疗疾病，如血管生成介导的疾病。 本发明包括新化合物，类似物，前药和药学上可接受的盐，用于预防和治疗涉及癌症等的疾病和其他疾病或病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及用于这些方法的中间体。

公开(公告)号：EP1976836B1

公开(公告)日：2012-08-22

申请号：EP06848110.0

申请日：2006-12-22

申请人： Amgen Inc.

发明人： DE MORIN, Frenel, F. ,  CHEN, Jian J. ,  DOHERTY, Elizabeth M. ,  HITCHCOCK, Stephen ,  HUANG, Qi ,  KIM, Joseph, L. ,  LIU, Gang ,  NIXEY, Thomas ,  PARAS, Nick, A. ,  PETKUS, Jeffrey ,  RETZ, Daniel, M. ,  SMITH, Adrian, L. ,  TASKER, Andrew ,  ZHU, Jiawang

IPC分类号： C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/435 ,  A61K31/495 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D413/04

CPC分类号： C07D401/14 ,  C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have Formula (I) wherein R1 is Formula (II), (III) or (IV) and A1, A2, A3, A4, X, Z, Z', R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

公开(公告)号：EP1519921A2

公开(公告)日：2005-04-06

申请号：EP03763451.6

申请日：2003-07-09

申请人： Amgen Inc.

发明人： HUANG, Qi ,  CHEN, Guoqing ,  LI, Aiwen ,  RIAHI, Babak ,  TASKER, Andrew ,  YANG, Kevin ,  YUAN, Chester, Chenguang

IPC分类号： C07D213/36

CPC分类号： C07D401/12 ,  C07D209/20 ,  C07D213/36 ,  C07D215/12 ,  C07D217/02 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D471/12 ,  C07D487/04

摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis 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.