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1. 发明申请

WO2003044021A2 SUBSTITUTED INDOLIZINE-LIKE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：取代的吲哚类化合物和使用方法
公开(公告)号：WO2003044021A2
公开(公告)日：2003-05-30
申请号：PCT/US2002/036699
申请日：2002-11-16
申请人： AMGEN INC. , CAI, Guolin , CHAU, Jennifer, N. , DOMINGUEZ, Celia , RISHTON, Gilbert, M. , LU, Yuelie
发明人： CAI, Guolin , CHAU, Jennifer, N. , DOMINGUEZ, Celia , RISHTON, Gilbert, M. , LU, Yuelie
IPC分类号： C07D487/04
CPC分类号： C07D401/04 , C07D471/04 , C07D487/04
摘要： Selected novel substituted indolizine-like compounds are effective for treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：所选择的新型取代的中氮茚样化合物对于治疗疾病如TNF-α，IL-1β，IL-6和/或IL-8介导的疾病以及其他疾病，例如癌症，疼痛和糖尿病。本发明包括新化合物，类似物，前药和药学上可接受的盐，用于治疗涉及炎症，癌症，疼痛，糖尿病等的疾病和其它疾病或病症的药物组合物和方法。本发明还涉及制备这些化合物的方法以及用于这些方法的中间体。

2. 发明申请

WO2003044021A3 SUBSTITUTED INDOLIZINE-LIKE COMPOUNDS AND METHODS OF USE 审中-公开
公开(公告)号：WO2003044021A3
公开(公告)日：2003-05-30
申请号：PCT/US2002/036699
申请日：2002-11-16
申请人： AMGEN INC. , CAI, Guolin , CHAU, Jennifer, N. , DOMINGUEZ, Celia , RISHTON, Gilbert, M. , LU, Yuelie
发明人： CAI, Guolin , CHAU, Jennifer, N. , DOMINGUEZ, Celia , RISHTON, Gilbert, M. , LU, Yuelie
IPC分类号： C07D487/04
摘要： Selected novel substituted indolizine-like compounds are effective for treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

3. 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。

4. 发明公开

EP1794135A1 SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：取代的杂环化合物及使用方法
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.

5. 发明公开

EP1448564A2 SUBSTITUTED INDOLIZINE-LIKE COMPOUNDS AND METHODS OF USE 有权
标题翻译：取代氮茚化合物及其用途
公开(公告)号：EP1448564A2
公开(公告)日：2004-08-25
申请号：EP02789671.1
申请日：2002-11-16
申请人： Amgen Inc.
发明人： CAI, Guolin , CHAU, Jennifer, N. , DOMINGUEZ, Celia , RISHTON, Gilbert, M. , LU, Yuelie
IPC分类号： C07D487/04 , C07D519/00 , C07D471/04 , A61P35/00
CPC分类号： C07D401/04 , C07D471/04 , C07D487/04
摘要： Selected novel substituted indolizine-like compounds are effective for treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

6. 发明授权

EP1448564B1 SUBSTITUTED INDOLIZINE-LIKE COMPOUNDS AND METHODS OF USE 有权
标题翻译：取代氮茚化合物及其用途
公开(公告)号：EP1448564B1
公开(公告)日：2006-04-19
申请号：EP02789671.1
申请日：2002-11-16
申请人： AMGEN INC.
发明人： CAI, Guolin , CHAU, Jennifer, N. , DOMINGUEZ, Celia , RISHTON, Gilbert, M. , LU, Yuelie
IPC分类号： C07D487/04 , C07D519/00 , C07D471/04 , A61K31/519 , A61K31/551 , A61P35/00
CPC分类号： C07D401/04 , C07D471/04 , C07D487/04
摘要： Selected novel substituted indolizine-like compounds are effective for treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

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