公开(公告)号：EP1817294A1

公开(公告)日：2007-08-15

申请号：EP05771399.2

申请日：2005-07-15

申请人： Amgen Inc.

发明人： ASKEW, JR., Benny C. ,  AYA, Toshihiro ,  BISWAS, Kaustav ,  CAI, Guolin ,  CHEN, Jian Jeffrey ,  HAN, Nianhe ,  LIU, Qingyian ,  NGUYEN, Thomas ,  NISHIMURA, Nobuko ,  NOMAK, Rana, Bogazi University ,  PETERKIN, Tanya ,  QIAN, Wenyuan ,  YANG, Kevin ,  YUAN, Chester Chenguang ,  ZHU, Jiawang ,  D'AMICO, Derin C. ,  HUMAN, Jason Brooks ,  HUANG, QI

IPC分类号： C07D241/08 ,  C07D405/12 ,  C07D405/14 ,  C07D403/12 ,  C07D401/12 ,  C07D409/12 ,  C07D243/08 ,  A61K31/496 ,  A61P29/00

CPC分类号： C07D221/10 ,  C07D221/08 ,  C07D239/74 ,  C07D241/08 ,  C07D243/08 ,  C07D249/08 ,  C07D295/135 ,  C07D311/96 ,  C07D335/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D491/04

摘要： Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds of formula (I) and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, 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：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：EP1848463A2

公开(公告)日：2007-10-31

申请号：EP06733881.4

申请日：2006-01-24

申请人： Amgen Inc.

发明人： D'AMICO, Derin C. ,  ASKEW, JR., Benny C.

IPC分类号： A61K47/48

CPC分类号： C07K1/1077 ,  A61K38/043 ,  A61K47/60 ,  C07D513/04

摘要： The present invention relates to a novel chemical process that provides novel vehicle derivatives that are exceptional 1,2- or 1,3-aminothiol specific reagents for conjugation to unprotected targeted compounds (e.g., polypeptides, peptides, or organic compounds) having or modified to have a 1,2- or 1,3 aminothiol group. The invention further relates to the methods of using novel water-soluble polymer derivatives and conjugates thereof.

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：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.