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1. 发明申请

WO2008076427A3 NAPHTHALENONE COMPOUNDS EXHIBITING PROLYL HYDROXYLASE INHIBITORY ACTIVITY, COMPOSITIONS, AND USES THEREOF 审中-公开
公开(公告)号：WO2008076427A3
公开(公告)日：2008-06-26
申请号：PCT/US2007/025819
申请日：2007-12-17
申请人： AMGEN INC. , ALLEN, Jennifer, R. , BISWAS, Kaustav , BRYAN, Marian, C. , BURLI, Roland , CAO, Guo-Qiang , FROHN, Michael, J. , GOLDEN, Jennifer, E. , MERCEDE, Stephanie , NEIRA, Susana , PETERKIN, Tanya , PICKRELL, Alexander, J. , REED, Anthony , TEGLEY, Christopher, M. , WANG, Xiang
发明人： ALLEN, Jennifer, R. , BISWAS, Kaustav , BRYAN, Marian, C. , BURLI, Roland , CAO, Guo-Qiang , FROHN, Michael, J. , GOLDEN, Jennifer, E. , MERCEDE, Stephanie , NEIRA, Susana , PETERKIN, Tanya , PICKRELL, Alexander, J. , REED, Anthony , TEGLEY, Christopher, M. , WANG, Xiang
IPC分类号： C07D311/96 , C07C235/82 , C07D213/56 , C07D213/61 , C07D307/94 , C07C237/24 , C07D221/20 , C07D215/48 , C07C59/88 , C07D217/02 , A61K31/352 , A61P9/10
摘要： Compounds of Formula (I) and Formula (II) are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula(I) and Formula (II) have the following structures, where the definitions of the variables are provided herein.

2. 发明申请

WO2017024180A1 VINYL FLUORIDE CYCLOPROPYL FUSED THIAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 审中-公开
标题翻译：作为β-分泌酶抑制剂的乙烯基氟化物环丙二烯化的噻嗪-2-胺化合物及其使用方法
公开(公告)号：WO2017024180A1
公开(公告)日：2017-02-09
申请号：PCT/US2016/045650
申请日：2016-08-04
申请人： AMGEN INC.
发明人： ALLEN, Jennifer, R. , AMEGADZIE, Albert , BOURBEAU, Matthew, P. , BROWN, James, A. , CHEN, Ning , FROHN, Michael, J. , LIU, Longbin , LIU, Qingyian , PETTUS, Liping, H. , QIAN, Wenyuan , REEVES, Corey, M. , SIEGMUND, Aaron, C.
IPC分类号： A61K31/5415 , A61P25/28 , C07D417/10 , C07D417/14 , C07D471/04 , C07D491/056 , C07D279/08
CPC分类号： C07D417/10 , C07D279/08 , C07D417/14 , C07D471/04 , C07D491/056
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 A 4 , A 5 , A 6 , A 7 , and each of R a , R b , R 1 , R 2 , R 3 , R 8 R 9 and R 10 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 Aβ 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.
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。化合物具有通式I：其中式I中的变量A4，A5，A6，A7以及式I的R a，R b，R 1，R 2，R 3，R 8 R 9和R 10各自独立地定义。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Aβ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。

3. 发明申请

WO2009154775A1 S1P1 RECEPTOR AGONISTS AND USE THEREOF 审中-公开
标题翻译： S1P1受体激动剂及其用途
公开(公告)号：WO2009154775A1
公开(公告)日：2009-12-23
申请号：PCT/US2009/003666
申请日：2009-06-18
申请人： AMGEN INC. , CEE, Victor, J. , FROHN, Michael, J. , NIERA, Susana, C. , LANMAN, Brian, Alan , REED, Anthony, B. , SHAM, Kelvin, K., C.
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：本发明涉及具有作为S1P受体调节剂的活性的式（I）化合物，更具体地涉及作为S1P1受体激动剂的具体化合物。本发明还涉及使用这些化合物来治疗与不适当的S1P1受体活性相关的疾病，例如自身免疫性疾病。

4. 发明申请

WO2006004702A1 CONDENSED TRIAZOLES AND INDAZOLES USEFUL IN TREATING CITOKINES MEDIATED DISEASES AND OTHER DISEASES 审中-公开
标题翻译：浓缩的三唑和吲哚有用的治疗介质性疾病和其他疾病
公开(公告)号：WO2006004702A1
公开(公告)日：2006-01-12
申请号：PCT/US2005/022835
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
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.
摘要翻译：本发明涉及式（I）的三唑并嘧啶，咪唑并嘧啶及其衍生物及其药学上可接受的盐。还包括治疗炎症，类风湿性关节炎，佩吉特病，骨质疏松症，多发性骨髓瘤，葡萄膜炎，急性或慢性骨髓性白血病，胰腺β细胞破坏，骨关节炎，类风湿性脊椎炎，痛风性关节炎，炎性肠病，成人呼吸窘迫综合征（ARDS），牛皮癣，克罗恩病，过敏性鼻炎，溃疡性结肠炎，过敏反应，接触性皮炎，哮喘，肌肉退化，恶病质，赖特综合征，I型糖尿病，II型糖尿病，骨吸收疾病，移植物抗宿主反应，阿尔茨海默病，中风，心肌梗死，缺血再灌注损伤，动脉粥样硬化，脑外伤，多发性硬化，脑疟疾，败血症，脓毒性休克，毒性综合症，发热，HIV-1，HIV-3，巨细胞病毒（CMV）），流感病毒，腺病毒，哺乳动物中的疱疹病毒或带状疱疹感染，包括给予有效量的如上所述的化合物。

5. 发明申请

WO2014138484A1 PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 审中-公开
标题翻译：作为β-分泌酶抑制剂的全氟化环丙氯联-1,3-氧化物-2-胺化合物及其使用方法
公开(公告)号：WO2014138484A1
公开(公告)日：2014-09-12
申请号：PCT/US2014/021412
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： PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE ABSTRACT OF THE DISCLOSURE 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: {INSERT STRUCTURE HERE} 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：作为β-分泌酶抑制剂的全氟化环丙氯联-1,3-氧化物-2-胺化合物及其使用方法本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。该化合物具有通式I：其中式I中的各个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的定义如下。本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/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。

6. 发明申请

WO2006037117A1 SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：取代的杂环化合物及其使用方法
公开(公告)号：WO2006037117A1
公开(公告)日：2006-04-06
申请号：PCT/US2005/035134
申请日：2005-09-27
申请人： AMGEN INC.
发明人： ANDERSEN, Denise, Lyn , CHANG, Catherine, M. , 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 X 1 is N or CR 3 ; X 2 is N or CR 4 ; or -X 1 =X 2 - is -C(=O)-N(R a )- or -N(R a )-C(=O)-; X 3 is N or CR 4 ; X 4 is N or CR 4 ; X 5 is N or CR 6 ; X 6 is N or CR 6 ; wherein only 1, 2 or 3 of X 1 , X 2 , X 3 and X 4 are N; R 1 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.
摘要翻译：本发明涉及吡啶，嘧啶及其衍生物，（I）或其药学上可接受的盐，其中X 1是N或CR 3; X 2是N或CR 4; 或-X 1 = X 2 - 是-C（= O）-N（R a） - 或-N（R 0） >一） - C（= O） - ; X 3是N或CR 4; X 4是N或CR 4; X 5是N或CR 6; X 6是N或CR 6; 其中X 1，X 2，X 3和X 4中仅有1,2或3是N; R 1是饱和的部分饱和或不饱和的含有0,1,2或3个选自N，O和S的原子的5-，6-或7-元环，其中环被 0,1,2或3个取代基。还包括治疗炎症，类风湿性关节炎，佩吉特病，骨质疏松症，多发性骨髓瘤，葡萄膜炎，急性或慢性骨髓性白血病，胰腺β细胞破坏，骨关节炎，类风湿性脊椎炎，痛风性关节炎，炎性肠病，成人呼吸窘迫综合征（ARDS），牛皮癣，克罗恩病，过敏性鼻炎，溃疡性结肠炎，过敏反应，接触性皮炎，哮喘，肌肉退化，恶病质，赖特综合征，I型糖尿病，II型糖尿病，骨吸收疾病，移植物抗宿主反应，阿尔茨海默病，中风，心肌梗塞，缺血再灌注损伤，动脉粥样硬化，脑外伤，多发性硬化，脑疟疾，败血症，败血性休克，中毒性休克综合征，发热，HIV-1，HIV-2，HIV-3，巨细胞病毒），流感病毒，腺病毒，哺乳动物中的疱疹病毒或带状疱疹感染，包括给予有效量的如上所述的化合物。

7. 发明申请

WO2005070932A3 SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
公开(公告)号：WO2005070932A3
公开(公告)日：2005-08-04
申请号：PCT/US2005/002013
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
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.

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