公开(公告)号：EP2051977A2

公开(公告)日：2009-04-29

申请号：EP07813049.9

申请日：2007-07-18

申请人： Amgen Inc. ,  Biovitrum AB

发明人： FOTSCH, Christopher, H. ,  BARTBERGER, Michael, D. ,  HARALDSSON, Martin ,  ST. JEAN, David ,  JOHANSSON, Lars ,  NILSSON, Marianne ,  SUTIN, Lori

IPC分类号： C07D403/06

CPC分类号： C07D403/06 ,  C07D413/06 ,  C07D413/12

摘要： Compounds of formula I and IV are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:formula I and IV wherein the variables A-B, R, 1, r R> 2, m, and Q are described herein.

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：EP2694491A1

公开(公告)日：2014-02-12

申请号：EP12713839.4

申请日：2012-04-04

申请人： Amgen Inc.

发明人： BARTBERGER, Michael, D. ,  CROGHAN, Michael, D. ,  FOTSCH, Christopher, H. ,  NORMAN, Mark, H. ,  PENNINGTON, Lewis, D. ,  REICHELT, Andreas ,  ST. JEAN, David, J., Jr. ,  TEGLEY, Christopher, M.

IPC分类号： C07D321/10 ,  C07D333/58 ,  C07D407/12 ,  C07D407/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D513/04 ,  A61K31/357 ,  A61K31/381 ,  A61K31/422

CPC分类号： A61K31/506 ,  A61K31/155 ,  A61K31/357 ,  A61K31/381 ,  A61K31/422 ,  A61K31/427 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4709 ,  A61K45/06 ,  C07D321/10 ,  C07D333/58 ,  C07D405/14 ,  C07D407/12 ,  C07D407/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D513/04 ,  A61K2300/00

摘要： The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

公开(公告)号：EP1656355B1

公开(公告)日：2008-03-12

申请号：EP04820712.0

申请日：2004-06-21

申请人： AMGEN INC.

发明人： CHEN, Jian, J. ,  ASKEW, Ben, C. ,  BISWAS, Kaustav ,  CHAU, Jennifer, N. ,  D'AMICO, Derin, C. ,  HARRIED, Scott ,  NGUYEN, Thomas ,  QIAN, Wenyuan ,  ZHU, Jiawang ,  FOTSCH, Christopher, H. ,  HAN, Nianhe ,  LI, Aiwen ,  LIU, Qingyian ,  NISHIMURA, Nobuko ,  NOMAK, Rana ,  PETERKIN, Tanya ,  RIAHI, Babak ,  YANG, Kevin ,  YUAN, Chester, Chenguang

IPC分类号： A61K31/495 ,  C07D241/08 ,  C07D243/08 ,  C07D245/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D241/08 ,  C07D243/08 ,  C07D245/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14

摘要： Compounds (I) are effective for treatment of pain and diseases, such as inflammation 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 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：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：EP1603905A1

公开(公告)日：2005-12-14

申请号：EP04709532.8

申请日：2004-02-09

申请人： AMGEN INC.

发明人： DOHERTY, Elizabeth, M. ,  HAN, Nianhe ,  HUNGATE, Randall, W. ,  LIU, Qingyian ,  NORMAN, Mark, H. ,  XI, Ning ,  XU, Shimin ,  FOTSCH, Christopher, H.

IPC分类号： C07D417/04 ,  C07D417/12 ,  C07D403/04 ,  C07D277/20 ,  C07D233/66 ,  C07D263/34 ,  A61P29/00

CPC分类号： C07D233/90 ,  C07D263/34 ,  C07D277/56 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

公开(公告)号：EP1416933B8

公开(公告)日：2008-08-27

申请号：EP02750299.6

申请日：2002-07-25

申请人： Amgen Inc.

发明人： FOTSCH, Christopher, H. ,  CROGHAN, Michael ,  DOHERTY, Elizabeth, M. ,  KELLY, Michael, G. ,  NORMAN, Mark, H. ,  SMITH,Duncan, M. ,  TAMAYO, Nuria ,  XI, Ning ,  XU, Shimin

IPC分类号： A61K31/445 ,  C07D211/28 ,  C07K5/078 ,  A61P3/04 ,  C07D401/12 ,  C07D211/34 ,  C07D401/14

CPC分类号： C07K5/06191 ,  A61K38/00 ,  C07D211/28 ,  C07D211/34 ,  C07D401/12 ,  C07D401/14 ,  C07K5/06139

公开(公告)号：EP1656355A2

公开(公告)日：2006-05-17

申请号：EP04820712.0

申请日：2004-06-21

申请人： AMGEN INC.

发明人： CHEN, Jian, J. ,  ASKEW, Ben, C. ,  BISWAS, Kaustav ,  CHAU, Jennifer, N. ,  D'AMICIO, Derin, C. ,  HARRIED, Scott ,  NGUYEN, Thomas ,  QIAN, Wenyuan ,  ZHU, Jiawang ,  FOTSCH, Christopher, H. ,  HAN, Nianhe ,  LI, Aiwen ,  LIU, Qingyian ,  NISHIMURA, Nobuko ,  NOMAK, Rana ,  PETERKIN, Tanya ,  RIAHI, Babak ,  YANG, Kevin ,  YUAN, Chester, Chenguang

IPC分类号： C07D241/00

CPC分类号： C07D241/08 ,  C07D243/08 ,  C07D245/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14

摘要： Compounds (I) are effective for treatment of pain and diseases, such as inflammation 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 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.