公开(公告)号：EP2077998A1

公开(公告)日：2009-07-15

申请号：EP07837737.1

申请日：2007-09-04

申请人： Amgen Inc. ,  Tasker, Andrew ,  Zhang, Dawei

发明人： TASKER, Andrew ,  ZHANG, Dawei ,  PETTUS, Liping, H. ,  RZASA, Robert, M. ,  SHAM, Kelvin, K.C. ,  XU, Shimin ,  CHAKRABARTI, Partha, Pratim

IPC分类号： C07D237/30 ,  C07D237/34 ,  C07D403/12 ,  C07D413/12 ,  C07D417/10 ,  C07D471/04 ,  A61K31/501 ,  A61P29/00

CPC分类号： C07D403/12 ,  C07D237/30 ,  C07D237/34 ,  C07D403/10 ,  C07D413/12 ,  C07D417/10 ,  C07D471/04

摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

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：EP1467721A2

公开(公告)日：2004-10-20

申请号：EP02723086.1

申请日：2002-01-11

申请人： Amgen Inc.

发明人： CHEN, Guoqing ,  ADAMS, Jeffrey ,  BEMIS, Jean ,  CROGHAN, Michael ,  DIPIETRO, Lucian ,  DOMINGUEZ, Celia ,  ELBAUM, Daniel ,  GERMAIN, Julie ,  HUANG, Qi ,  KIM, Joseph, L. ,  OUYANG, Xiaohu ,  PATEL, Vinod, F. ,  SMITH, Leon, M. ,  TASKER, Andrew ,  XI, Ning ,  XU, Shimin ,  YUAN, Chester, Chenguang ,  KIM, Tae-Seong

IPC分类号： A61K31/00 ,  A61P19/02 ,  A61P35/00 ,  C07D231/56 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04

CPC分类号： C07D401/14 ,  A61K31/00 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  Y02A50/401

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：EP1836174B1

公开(公告)日：2013-02-27

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

CPC分类号： C07D215/38 ,  C07C205/37 ,  C07D215/12 ,  C07D217/12 ,  C07D217/22 ,  C07D217/26 ,  C07D239/26 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A 1 , A 2 , A 3 , B, R 1 , R 2 , R 3 and R 4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

公开(公告)号：EP1509518B1

公开(公告)日：2012-02-08

申请号：EP03736701.8

申请日：2003-05-23

申请人： Amgen, Inc.

发明人： KELLY, Michael, G. ,  XU, Shimin ,  XI, Ning ,  TOWNSEND, Robert ,  SEMIN, David, J. ,  GHIRON, Chiara ,  COUTLER, Thomas

IPC分类号： C07D413/04 ,  C07D491/04 ,  C07D471/04 ,  C07D403/04 ,  C07D401/04 ,  C07D249/18 ,  C07D235/08 ,  C07D209/86 ,  C07D209/80 ,  C07D209/12 ,  C07D209/10 ,  C07D209/08

CPC分类号： C07D235/06 ,  C07D209/08 ,  C07D209/10 ,  C07D209/12 ,  C07D209/86 ,  C07D209/88 ,  C07D249/04 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D471/04 ,  C07D491/04

摘要： The compounds of the invention are represented by the following general structure (I) or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. 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：EP2152706A1

公开(公告)日：2010-02-17

申请号：EP08743342.1

申请日：2008-04-24

申请人： Amgen Inc.

发明人： PETTUS, Liping H. ,  TASKER, Andrew ,  XU, Shimin ,  WURZ, Ryan

IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/437 ,  A61K31/4985

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have general Formula (I) wherein A1, A2, B, R1, R2, R4, R5, R6 and Z are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula (I).

公开(公告)号：EP1711495A2

公开(公告)日：2006-10-18

申请号：EP05711976.0

申请日：2005-01-24

申请人： AMGEN INC.

发明人： HARMANGE, Jean-Christophe ,  BOOKER, Shon ,  BAUER, David ,  KIM, Tae-Seong ,  CHENG, Yuan ,  XU, Shimin ,  XI, Ning ,  KIM, Joseph, L. ,  TASKER, Andrew

IPC分类号： C07D417/00 ,  C07D401/12 ,  A61K31/47

CPC分类号： C07D495/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF 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：EP1551811A1

公开(公告)日：2005-07-13

申请号：EP03809075.9

申请日：2003-10-16

申请人： Amgen Inc.

发明人： BALAN, Chenera ,  BO, Yunxin ,  DOMINGUEZ, Celia ,  FOTSCH, Christopher, H. ,  GORE, Vijay, K. ,  MA, Vu Van ,  NORMAN, Mark, H. ,  OGNYANOV, Vassil, I. ,  QIAN, Yi-xin ,  WANG, Xianghong ,  XI, Ning ,  XU, Shimin

IPC分类号： C07D235/30 ,  C07D401/12 ,  C07D401/14 ,  C07D401/04 ,  C07D403/12 ,  C07D417/14 ,  C07D471/04 ,  C07D417/12 ,  C07D403/14 ,  C07D409/14 ,  C07D405/14 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496

CPC分类号： C07D401/04 ,  C07D235/30 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Compounds of formula (I) are useful in the treatment of vanilloid-receptor-meditated diseases, such as inflammatory or neuropathic pain and diseases involving sensory nerve function such as asthma, rheumatoid arthritis, osteoarthritis, inflammatory bowel disorders, urinary incontinence, migraine and psoriasis.

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：EP1509518A1

公开(公告)日：2005-03-02

申请号：EP03736701.8

申请日：2003-05-23

申请人： Amgen, Inc.

发明人： KELLY, Michael, G. ,  XU, Shimin ,  XI, Ning ,  TOWNSEND, Robert ,  SEMIN, David, J. ,  GHIRON, Chiara ,  COUTLER, Thomas

IPC分类号： C07D413/04 ,  C07D491/04 ,  C07D471/04 ,  C07D403/04 ,  C07D401/04 ,  C07D249/18 ,  C07D235/08 ,  C07D209/86 ,  C07D209/80 ,  C07D209/12 ,  C07D209/10 ,  C07D209/08

CPC分类号： C07D235/06 ,  C07D209/08 ,  C07D209/10 ,  C07D209/12 ,  C07D209/86 ,  C07D209/88 ,  C07D249/04 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D471/04 ,  C07D491/04

摘要： The compounds of the invention are represented by the following general structure (I) or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.