公开(公告)号：EP1358184B1

公开(公告)日：2007-05-02

申请号：EP02717325.1

申请日：2002-01-11

申请人： AMGEN INC.

发明人： CHEN, Guoqing ,  ADAMS, Jeffrey ,  BEMIS, Jean ,  BOOKER, Shon ,  CAI, Guolin ,  CROGHAN, Michael ,  DIPIETRO, Lucian ,  DOMINGUEZ, Celia ,  ELBAUM, Daniel ,  GERMAIN, Julie ,  GEUNS-MEYER, Stephanie ,  HANDLEY, Michael ,  HUANG, Qi ,  KIM, Joseph, L. ,  KIM, Tae-Seong ,  KISELYOV, Alexander ,  OUYANG, Xiaohu ,  PATEL, Vinod, F. ,  SMITH, Leon, M. ,  STEC, Markian ,  TASKER, Andrew ,  XI, Ning ,  XU, Shimin ,  YUAN, Chester Chenguang

IPC分类号： C07D401/14

CPC分类号： C07D213/82 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/00 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives 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：EP1358184A1

公开(公告)日：2003-11-05

申请号：EP02717325.1

申请日：2002-01-11

申请人： Amgen Inc.

发明人： CHEN, Guoqing ,  ADAMS, Jeffrey ,  BEMIS, Jean ,  BOOKER, Shon ,  CAI, Guolin ,  CROGHAN, Michael ,  DIPIETRO, Lucian ,  DOMINGUEZ, Celia ,  ELBAUM, Daniel ,  GERMAIN, Julie ,  GEUNS-MEYER, Stephanie ,  HANDLEY, Michael ,  HUANG, Qi ,  KIM, Joseph, L. ,  KIM, Tae-Seong ,  KISELYOV, Alexander ,  OUYANG, Xiaohu ,  PATEL, Vinod, F. ,  SMITH, Leon, M. ,  STEC, Markian ,  TASKER, Andrew ,  XI, Ning ,  XU, Shimin ,  YUAN, Chester Chenguang

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

CPC分类号： C07D213/82 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/00 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives 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：EP1981884B1

公开(公告)日：2012-06-13

申请号：EP07718125.3

申请日：2007-01-11

申请人： Amgen, Inc

发明人： ZENG, Qingping ,  ALLEN, John G. ,  BOURBEAU, Matthew P. ,  DOMINGUEZ, Celia ,  FOTSCH, Christopher H. ,  HAN, Nianhe ,  HONG, Fang-Tsao ,  HUANG, Xin ,  LEE, Matthew R. ,  LI, Aiwen ,  LIU, Qingyian ,  RIDER, James T. ,  TADESSE, Seifu ,  TASKER, Andrew S. ,  VISWANADHAN, Vellarkad N. ,  WANG, Xianghong ,  WEILER, Kurt E. ,  WOHLHIETER, George E. ,  YAO, Guomin ,  YUAN, Chester Chenguang

IPC分类号： C07D417/04

CPC分类号： C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

摘要： The invention relates to thiazole compounds of Formula (I) and Formula (II) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

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：EP2387570A1

公开(公告)日：2011-11-23

申请号：EP10700466.5

申请日：2010-01-13

申请人： Amgen, Inc

发明人： ZENG, Qingping ,  YUAN, Chester Chenguang ,  YAO, Guomin ,  WANG, Xianghong ,  TADESSE, Seifu ,  ST. JEAN, JR., David J. ,  REICHELT, Andreas ,  LIU, Qingyian ,  HONG, Fang-Tsao ,  HAN, Nianhe ,  FOTSCH, Christopher H. ,  DAVIS, Carl D. ,  BOURBEAU, Matthew P. ,  ASHTON, Kate S. ,  ALLEN, John G.

IPC分类号： C07D409/04 ,  A61K31/427 ,  A61K31/4709

CPC分类号： C07D417/14 ,  C07D417/04

摘要： The invention relates to thiazole compounds of Formula (I) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

摘要翻译： 本发明涉及式（I）的噻唑化合物及其组合物，其用于治疗由蛋白激酶B（PKB）介导的疾病，其中变量具有本文提供的定义。 本发明还涉及这种噻唑化合物及其组合物在治疗与异常细胞生长，癌症，炎症和代谢紊乱有关的疾病状态中的治疗用途。

公开(公告)号：EP2231602A1

公开(公告)日：2010-09-29

申请号：EP08859465.0

申请日：2008-12-12

申请人： Amgen, Inc

发明人： HITCHCOCK, Stephen ,  CHEN, Jian J. ,  NCUBE, Mqhele ,  NIXEY, Thomas ,  AMEGADZIE, Albert ,  KUNZ, Roxanne ,  QIAN, Wenyuan ,  CHEN, Ning ,  TEGLEY, Christopher M. ,  DEMORIN, Frenel ,  YUAN, Chester Chenguang ,  LIU, Qingyian ,  ZHU, Jiawang ,  PETERKIN, Tanya ,  ADAMS, Jeffrey A. ,  HU, Essa ,  CHAVEZ, JR., Frank

IPC分类号： C07D213/40 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/12 ,  A61K31/00 ,  A61P25/28

CPC分类号： C07D213/40 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/12

摘要： The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

摘要翻译： 本发明提供了为γ分泌酶调节剂的化合物，因此可用于治疗通过调节γ分泌酶例如阿尔茨海默氏病可治疗的疾病。 还提供了含有这些化合物的药物组合物以及制备这些化合物的方法。

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：EP2820014A1

公开(公告)日：2015-01-07

申请号：EP13709033.8

申请日：2013-02-28

申请人： Amgen Inc.

发明人： ALLEN, Jennifer R. ,  AMEGADZIE, Albert ,  ANDREWS, Kristin L. ,  BROWN, James ,  CHEN, Jian J. ,  CHEN, Ning ,  HARRINGTON, Essa Hu ,  LIU, Qingyian ,  NGUYEN, Thomas T. ,  PICKRELL, Alexander J. ,  QIAN, Wenyuan ,  RUMFELT, Shannon ,  RZASA, Robert M. ,  YUAN, Chester Chenguang ,  ZHONG, Wenge

IPC分类号： C07D417/12 ,  C07D471/04 ,  C07D473/00 ,  C07D473/30 ,  C07D473/34 ,  C07D473/40 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  A61K31/437 ,  A61P25/18

CPC分类号： C07D487/04 ,  C07D417/12 ,  C07D471/04 ,  C07D473/00 ,  C07D473/30 ,  C07D473/34 ,  C07D473/40 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

摘要： Heterobicyclic compounds of Formula (I): (I); or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.

公开(公告)号：EP2167504A2

公开(公告)日：2010-03-31

申请号：EP08780217.9

申请日：2008-07-16

申请人： Amgen, Inc

发明人： ALLEN, John, G. ,  BOURBEAU, Matthew, P. ,  DOMINGUEZ, Celia ,  FOTSCH, Christopher, H. ,  HAN, Nianhe ,  HONG, Fang-tsao ,  HUANG, Xin ,  LEE, Matthew, R. ,  LIU, Qingyian ,  REICHELT, Andreas ,  TADESSE, Seifu ,  WANG, Xianghong ,  YAO, Guomin ,  YUAN, Chester Chenguang ,  ZENG, Qingping

IPC分类号： C07D471/02 ,  C07D285/135 ,  C07D285/125 ,  A61K31/433 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D285/135 ,  C07D417/04 ,  C07D417/14 ,  C07D495/04

摘要： The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

摘要翻译： 本发明涉及式I和式II的噻唑化合物及其组合物，其用于治疗由蛋白激酶B（PKB）介导的疾病，其中变量具有本文提供的定义。 本发明还涉及这种噻唑化合物及其组合物在治疗与异常细胞生长，癌症，炎症和代谢紊乱有关的疾病状态中的治疗用途。

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.