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：EP2334673A1

公开(公告)日：2011-06-22

申请号：EP09791961.7

申请日：2009-08-26

申请人： Amgen Inc. ,  Pettus, Liping H. ,  Tasker, Andrew

发明人： PETTUS, Liping, H. ,  TASKER, Andrew ,  WU, Bin

IPC分类号： C07D471/04 ,  A61K31/444 ,  A61P29/00

CPC分类号： 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 R
1 , R
2 , R
3 , R
4 , R
5 , W and X 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：EP1725529A1

公开(公告)日：2006-11-29

申请号：EP05711838.2

申请日：2005-01-21

申请人： AMGEN INC.

发明人： HULME, Christopher ,  NCUBE, Mqhele, Vellah ,  NORMAN, Mark, H. ,  OGNYANOV, Vassil, I. ,  PETTUS, Liping, H. ,  ZHU, Jiawang

IPC分类号： C07D209/08 ,  C07D319/20 ,  C07D277/82 ,  C07D235/06 ,  C07D215/38 ,  C07D417/12 ,  C07D407/12 ,  C07D405/12 ,  A61K31/428 ,  A61K31/4709 ,  A61K31/36 ,  A61K31/4184 ,  A61K31/404 ,  A61P29/00

CPC分类号： C07D495/04 ,  C07D209/08 ,  C07D215/38 ,  C07D235/06 ,  C07D277/82 ,  C07D319/18 ,  C07D319/20 ,  C07D405/12 ,  C07D407/12 ,  C07D417/12

摘要： bis-Bicyclic amides and derivatives thereof 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：EP2086973B1

公开(公告)日：2012-01-25

申请号：EP07839356.8

申请日：2007-10-05

申请人： Amgen Inc.,

发明人： ZHANG, Dawei ,  TASKER, Andrew ,  SHAM, Kelvin, K.C. ,  CHAKRABARTI, Partha, Pratim ,  FALSEY, Richard, James ,  HERBERICH, Bradley, J. ,  PETTUS, Liping, H. ,  RZASA, Robert, M.

IPC分类号： C07D471/04

CPC分类号： 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 general Formula (I), wherein A, 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 P38 map 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：EP1737414A2

公开(公告)日：2007-01-03

申请号：EP05711834.1

申请日：2005-01-21

申请人： AMGEN INC.

发明人： NORMAN, Mark, H. ,  OGNYANOV, Vassil, I. ,  PETTUS, Liping, H.

IPC分类号： A61K6/00

CPC分类号： C07D401/12 ,  C07D213/26 ,  C07D277/82 ,  C07D319/18 ,  C07D405/12 ,  C07D409/12

摘要： N-Bicyclic amides and derivatives thereof 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：EP2424859A1

公开(公告)日：2012-03-07

申请号：EP10718364.2

申请日：2010-04-27

申请人： Amgen, Inc

发明人： ANDREWS, Kristin ,  BO, Yunxin, Y. ,  BOOKER, Shon ,  CEE, Victor, J. ,  D'ANGELO, Noel ,  HERBERICH, Bradley, J. ,  HONG, Fang-Tsao ,  JACKSON, Claire, L., M. ,  LANMAN, Brian, A. ,  LIAO, Hongyu ,  LIU, Longbin ,  NISHIMURA, Nobuko ,  NORMAN, Mark, H. ,  PETTUS, Liping, H. ,  REED, Anthony, B. ,  SMITH, Adrian, L. ,  TADESSE, Seifu ,  TAMAYO, Nuria, A. ,  WU, Bin ,  WURZ, Ryan ,  YANG, Kevin

IPC分类号： C07D401/14 ,  C07D473/00 ,  A61K31/52 ,  A61P35/00

CPC分类号： C07D473/00 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.

公开(公告)号：EP2077998B1

公开(公告)日：2011-03-09

申请号：EP07837737.1

申请日：2007-09-04

申请人： Amgen Inc.

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：EP1546116A1

公开(公告)日：2005-06-29

申请号：EP03785220.9

申请日：2003-08-08

申请人： Amgen Inc.

发明人： CHAKRABARTI, Partha, P ,  CHEN, Ning ,  DOHERTY, Elizabeth, M. ,  DOMINGUEZ, Celia ,  FALSEY, James, Richard ,  FOTSH, Christopher, H. ,  HULME, Christopher ,  KATON, Jodie ,  NIXEY, Thomas ,  NORMAN, Mark, H. ,  OGNYANOV, Vassil, I. ,  PETTUS, Liping, H. ,  RZASA, Robert, Michael ,  STEC, Markian ,  WANG, Hui-Ling ,  ZHU, Jiawang

IPC分类号： C07D239/34 ,  C07D239/38 ,  C07D417/12 ,  C07D401/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/501 ,  A61K31/506 ,  A61K31/505 ,  A61K31/4427 ,  A61K31/5377 ,  A61K31/551 ,  A61P29/00

CPC分类号： C07D231/40 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/56 ,  C07D233/38 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

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：EP2424859B1

公开(公告)日：2015-04-08

申请号：EP10718364.2

申请日：2010-04-27

申请人： Amgen, Inc

发明人： ANDREWS, Kristin ,  BO, Yunxin, Y. ,  BOOKER, Shon ,  CEE, Victor, J. ,  D'ANGELO, Noel ,  HERBERICH, Bradley, J. ,  HONG, Fang-Tsao ,  JACKSON, Claire, L., M. ,  LANMAN, Brian, A. ,  LIAO, Hongyu ,  LIU, Longbin ,  NISHIMURA, Nobuko ,  NORMAN, Mark, H. ,  PETTUS, Liping, H. ,  REED, Anthony, B. ,  SMITH, Adrian, L. ,  TADESSE, Seifu ,  TAMAYO, Nuria, A. ,  WU, Bin ,  WURZ, Ryan ,  YANG, Kevin

IPC分类号： C07D401/14 ,  C07D473/00 ,  A61K31/52 ,  A61P35/00

CPC分类号： C07D473/00 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

公开(公告)号：EP2688886A1

公开(公告)日：2014-01-29

申请号：EP12719496.7

申请日：2012-03-21

申请人： Amgen Inc.

发明人： WANG, Hui-Ling ,  CEE, Victor, J. ,  HERBERICH, Bradley, J. ,  JACKSON, Claire, L., M. ,  LANMAN, Brian, Alan ,  NIXEY, Thomas ,  PETTUS, Liping, H. ,  REED, Anthony, B. ,  WU, Bin ,  WURZ, Ryan ,  TASKER, Andrew

IPC分类号： C07D413/14 ,  C07D417/14 ,  C07D417/04 ,  C07D487/04 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/4745 ,  A61K31/433 ,  A61P35/00

CPC分类号： C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.