公开(公告)号：EP2306994B1

公开(公告)日：2013-08-14

申请号：EP09767088.9

申请日：2009-06-18

申请人： Amgen Inc.

发明人： CEE, Victor, J. ,  FROHN, Michael, J. ,  NEIRA, Susana, C. ,  LANMAN, Brian, Alan ,  REED, Anthony, B. ,  SHAM, Kelvin, K., C.

IPC分类号： C07D513/04 ,  A61K31/4365 ,  A61P37/00

CPC分类号： C07D513/04 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/48

公开(公告)号：EP2306994A1

公开(公告)日：2011-04-13

申请号：EP09767088.9

申请日：2009-06-18

申请人： Amgen, Inc

发明人： CEE, Victor, J. ,  FROHN, Michael, J. ,  NIERA, Susana, C. ,  LANMAN, Brian, Alan ,  REED, Anthony, B. ,  SHAM, Kelvin, K., C.

IPC分类号： A61K31/00

CPC分类号： C07D513/04 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/48

摘要： The present invention relates to compounds of Formula (I), that have activity as S1P receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.

摘要翻译： 本发明涉及式（I）化合物，其具有作为S1P受体调节剂的活性，更具体地涉及具体为S1P1受体激动剂的化合物。 本发明还涉及这些化合物用于治疗与不适当的S1P1受体活性相关的疾病如自身免疫性疾病的用途。

公开(公告)号：EP4257152A3

公开(公告)日：2023-12-06

申请号：EP23171158.1

申请日：2015-06-10

申请人： Amgen Inc.

发明人： HOLDER, Jerry Ryan ,  SWAMINATH, Gayathri ,  FROHN, Michael, J. ,  LANMAN, Brian Alan ,  REED, Anthony B. ,  MIRANDA, Leslie P. ,  ALLEN, John Gordon ,  PICKRELL, Alexander J. ,  SIEGMUND, Aaron C. ,  PENNINGTON, Lewis D ,  YANG, Bryant

IPC分类号： C07K14/47 ,  A61K47/54 ,  A61K47/60 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  C07K19/00 ,  A61K38/00

摘要： The invention provides modified apelin polypeptides having increased stability, circulating half-life, and/or potency relative to the native apelin-13 polypeptide. Compositions comprising the modified apelin polypeptides and methods of using the polypeptides for treating cardiac disorders, such as heart failure, are also disclosed.

公开(公告)号：EP1765825A1

公开(公告)日：2007-03-28

申请号：EP05762492.6

申请日：2005-06-24

申请人： AMGEN INC.

发明人： ANDERSON, Denise, Lyn ,  FROHN, Michael, J. ,  HONG, Fang-Tsao ,  LIU, Longin ,  LOPEZ, Patricia

IPC分类号： C07D487/04 ,  C07D471/04 ,  A61K31/4196 ,  A61K31/4188

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The present invention relates to triazolopyrimidines, imidazolopyrimidines and derivatives thereof of Formula (I), and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shack syndrome, fever, myalgias due to HIV-l, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.

公开(公告)号：EP4257152A2

公开(公告)日：2023-10-11

申请号：EP23171158.1

申请日：2015-06-10

申请人： Amgen Inc.

发明人： HOLDER, Jerry Ryan ,  SWAMINATH, Gayathri ,  FROHN, Michael, J. ,  LANMAN, Brian Alan ,  REED, Anthony B. ,  MIRANDA, Leslie P. ,  ALLEN, John Gordon ,  PICKRELL, Alexander J. ,  SIEGMUND, Aaron C. ,  PENNINGTON, Lewis D ,  YANG, Bryant

IPC分类号： A61K47/60

摘要： The invention provides modified apelin polypeptides having increased stability, circulating half-life, and/or potency relative to the native apelin-13 polypeptide. Compositions comprising the modified apelin polypeptides and methods of using the polypeptides for treating cardiac disorders, such as heart failure, are also disclosed.

公开(公告)号：EP1794135A1

公开(公告)日：2007-06-13

申请号：EP05802134.6

申请日：2005-09-27

申请人： Amgen Inc.

发明人： ANDERSEN, Denise, Lyn ,  CHANG, Catherine, H. ,  FALSEY, James, R. ,  FROHN, Michael, J. ,  HONG, Fang-Tsao ,  LIAO, Hongyu ,  LIU, Longbin ,  LOPEZ, Patricia ,  RETZ, Daniel, Martin ,  RISHTON, Gilbert, M. ,  RZASA, Robert, M. ,  SIEGMUND, Aaron, C. ,  TADESSE, Seifu ,  TAMAYO, Nuria ,  TEGLEY, Christopher, M.

IPC分类号： C07D239/48 ,  A61K31/506 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

CPC分类号： C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

摘要： The present invention relates to pyridines, pyrimidines and derivatives thereof, (I) or a pharmaceutically acceptable salts thereof, wherein X1 is N or CR3; X2 is N or CR4; or -X1=X2- is -C(=O)-N(Ra)- or -N(Ra)-C(=O)-; X3 is N or CR4; X4 is N or CR4; X5 is N or CR6; X6 is N or CR6; wherein only 1, 2 or 3 of X1, X2, X3 and X4 are N; R1 is a saturated partially saturated or unsaturated 5-, 6- or 7-membered, ring containing 0, 1, 2 or 3 atoms selected from N, O and S, wherein the ring is substituted by 0, 1, 2 or 3 substituents. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.

公开(公告)号：EP1716150A2

公开(公告)日：2006-11-02

申请号：EP05711810.1

申请日：2005-01-21

申请人： AMGEN INC.

发明人： FROHN, Michael, J. ,  HONG, Fang-Tsao ,  LIU, Longbin ,  LOPEZ, Patricia ,  SIEGMUND, Aaron, C. ,  TADESSE, Seifu ,  TAMAYO, Nuria

IPC分类号： C07D487/04 ,  A61K31/506 ,  A61K31/513

CPC分类号： C07D487/04 ,  C07D471/04

摘要： The present invention relates to pyrimidinones and pyridones and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.

公开(公告)号：EP2964644B1

公开(公告)日：2018-12-26

申请号：EP14717004.7

申请日：2014-03-06

申请人： AMGEN, INC.

发明人： MINATTI, Ana Elena ,  LOW, Jonathan, D. ,  ALLEN, Jennifer, R. ,  AMEGADZIE, Albert ,  BROWN, James ,  FROHN, Michael, J. ,  GUZMAN-PEREZ, Angel ,  HARRINGTON, Paul, E. ,  LOPEZ, Patricia ,  MA, Vu Van ,  NISHIMURA, Nobuko ,  QIAN, Wenyuan ,  RUMFELT, Shannon ,  RZASA, Robert, M. ,  SHAM, Kelvin ,  SMITH, Adrian, L. ,  WHITE, Ryan ,  XUE, Qiufen

IPC分类号： C07D413/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D265/12 ,  C07D491/048 ,  A61P25/00 ,  A61K31/536

CPC分类号： C07D413/12 ,  C07D265/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048

摘要： The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

公开(公告)号：EP2964644A1

公开(公告)日：2016-01-13

申请号：EP14717004.7

申请日：2014-03-06

申请人： Amgen Inc.

发明人： MINATTI, Ana Elena ,  LOW, Jonathan, D. ,  ALLEN, Jennifer, R. ,  AMEGADZIE, Albert ,  BROWN, James ,  FROHN, Michael, J. ,  GUZMAN-PEREZ, Angel ,  HARRINGTON, Paul, E. ,  LOPEZ, Patricia ,  MA, Vu Van ,  NISHIMURA, Nobuko ,  QIAN, Wenyuan ,  RUMFELT, Shannon ,  RZASA, Robert, M. ,  SHAM, Kelvin ,  SMITH, Adrian, L. ,  WHITE, Ryan ,  XUE, Qiufen

IPC分类号： C07D413/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D265/12 ,  C07D491/048 ,  A61P25/00 ,  A61K31/536

CPC分类号： C07D413/12 ,  C07D265/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048

摘要： The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

摘要翻译： 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 所述化合物具有通式I：其中式I中的每个R a，R b，R 1，R 2，R 3和R 7各自独立地定义的变量A4，A5，A6，A8在本文中定义。 本发明还提供包含该化合物的药物组合物，以及由BACE的生物活性产生的化合物和组合物用于治疗与A-β斑块形成和沉积相关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。

公开(公告)号：EP1716150B1

公开(公告)日：2008-04-23

申请号：EP05711810.1

申请日：2005-01-21

申请人： AMGEN INC.

发明人： FROHN, Michael, J. ,  HONG, Fang-Tsao ,  LIU, Longbin ,  LOPEZ, Patricia ,  SIEGMUND, Aaron, C. ,  TADESSE, Seifu ,  TAMAYO, Nuria

IPC分类号： C07D487/04 ,  A61K31/506 ,  A61K31/513

CPC分类号： C07D487/04 ,  C07D471/04

摘要： The present invention relates to pyrimidinones and pyridones and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.