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1. 发明申请

WO2012129338A1 AZOLE COMPOUNDS AS PIM INHIBITORS 审中-公开
标题翻译： AZOLE化合物作为PIM抑制剂
公开(公告)号：WO2012129338A1
公开(公告)日：2012-09-27
申请号：PCT/US2012/029997
申请日：2012-03-21
申请人： AMGEN INC. , WANG, Hui-Ling , CEE, Victor, C. , HERBERICH, Bradley, J. , JACKSON, Claire, L., M. , LANMAN, Brian, Alan , NIXEY, Thomas , PETTUS, Liping, H. , REED, Anthony, B. , WU, Bin , WURZ, Ryan , TASKER, Andrew
发明人： WANG, Hui-Ling , CEE, Victor, C. , 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.
摘要翻译：本发明涉及式I和Ia的双环化合物及其盐。在一些实施方案中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。在另外的实施方案中，本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病，优选癌症中的用途。

2. 发明申请

WO2006094187A3 PHTHALAZINE, AZA- AND DIAZA-PHTHALAZINE COMPOUNDS AND METHODS OF USE 审中-公开
公开(公告)号：WO2006094187A3
公开(公告)日：2006-09-08
申请号：PCT/US2006/007583
申请日：2006-03-03
申请人： AMGEN INC
发明人： TASKER, Andrew , ZHANG, Dawei , CAO, Guo-Qiang , CHAKRABARTI, Partha, Pratim , FALSEY, James, Richard , HERBERICH, Bradley, J. , HUNGATE, Randall, W. , PETTUS, Liping, H. , REED, Anthony , RZASA, Robert, M. , SHAM, Kelvin, K.C. , THAMAN, Maya, C. , XU, Shimin
IPC分类号： C07D237/32 , C07D237/34 , C07D237/30 , C07D413/12 , C07D417/12 , C07D498/04 , C07D487/04 , C07D417/04 , C07D491/10 , C07D409/04 , C07D401/04 , C07D403/04 , A61K31/502 , A61P29/00
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 A 1 , A 2 , B, R 1 , R 2 , R 3 and R 4 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. The compounds have effect on the levels of TNF-X and various Interleukins.

3. 发明授权

EP2086973B1 IMIDAZO- AND TRIAZOLO-PYRIDINE COMPOUNDS AND METHODS OF USE THEROF 有权
标题翻译：咪唑和TRIAZOLOPYRIDINVERBINDUNGEN和申请流程。
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).

4. 发明公开

EP2424859A1 INHIBITORS OF PI3 KINASE AND / OR MTOR 有权
标题翻译： PI3激酶和/或mTOR的抑制剂
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.

5. 发明申请

WO2010126895A1 INHIBITORS OF PI3 KINASE AND / OR MTOR 审中-公开
标题翻译： PI3激酶和/或MTOR的抑制剂
公开(公告)号：WO2010126895A1
公开(公告)日：2010-11-04
申请号：PCT/US2010/032593
申请日：2010-04-27
申请人： AMGEN INC. , 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
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.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐; 使用该化合物治疗疾病或病症如癌症的方法; 和含有这些化合物的药物组合物，其中变量如本文所定义。

6. 发明申请

WO2008045393A2 IMIDAZO- AND TRIAZOLO-PYRIDINE COMPOUNDS AND METHODS OF USE THEROF 审中-公开
标题翻译：咪唑并 - 三唑并吡啶化合物及其使用方法
公开(公告)号：WO2008045393A2
公开(公告)日：2008-04-17
申请号：PCT/US2007/021505
申请日：2007-10-05
申请人： AMGEN INC. , ZHANG, Dawei , TASKER, Andrew , SHAM, Kelvin, K.C. , CHAKRABARTI, Partha, Pratim , FALSEY, Richard, James , HERBERICH, Bradley, J. , PETTUS, Liping, H. , RZASA, Robert, M.
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.
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, R 1 , R 2 , R 3 and R 4 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).
摘要翻译：本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。化合物具有通式（I），其中A，B，R 1，R 2，R 3和R 4， / SUP>。本发明还包括包含一种或多种式（I）化合物的药物组合物，这些化合物和组合物用于治疗P38地图激酶介导的疾病（包括类风湿性关节炎，牛皮癣和其他炎症疾病）的用途，以及可用于式（I）化合物的制备。

7. 发明申请

WO2005070934A1 SUBSTITUTED DIAZABICYCLOHEPTANES AND THEIR USE AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：替代双联蛋白及其作为蛋白激酶抑制剂的用途
公开(公告)号：WO2005070934A1
公开(公告)日：2005-08-04
申请号：PCT/US2005/000993
申请日：2005-01-12
申请人： AMGEN INC. , CAO, Guo-Qiang , CHEN, Jian, J. , DOMINGUEZ, Celia , REED, Anthony , SHAM, Kelvin, K., C. , THAMAN, Maya, C. , ZHANG, Dawei , HERBERICH, Bradley, J.
发明人： CAO, Guo-Qiang , CHEN, Jian, J. , DOMINGUEZ, Celia , REED, Anthony , SHAM, Kelvin, K., C. , THAMAN, Maya, C. , ZHANG, Dawei , HERBERICH, Bradley, J.
IPC分类号： C07D487/08
CPC分类号： C07D487/06 , C07D213/56 , C07D239/95 , C07D401/04 , C07D401/14 , C07D417/14
摘要： The present invention relates to therapeutic diazobicyclo pyridines and their use in the treatment of arthritis, rheumatoid arthritis, psoriatic arthritis or osteoarthritis, organ transplant, acute transplant or heterograft and homograft rejection, ischemic and reperfusion injury, transplantation tolerance induction, multiple sclerosis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, lupus, graft vs. host diseases, T -cell mediated hypersensitivity diseases, contact hypersensitivity, delayed-type hypersensitivity, gluten-sensitive enteropathy, Type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism,Graves' Disease, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, autoimmune diseases, glomerulonephritis, serum sickness, uticaria, respiratory allergies, asthma, hayfever, allergic rhinitis, skin allergies, scleracielma, mycosis fungoides, acute inflammatory responses, acute respiratory distress syndrome, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, Type II diabetes and cancers where PKC theta or other PKC-family kinases are activated, overexpressed or facilitate tumor growth or survival of tumor cells, T cell leukemia, thymoma, T and B cell lymphoma, colon carcinoma, breast carcinoma and lung carcinoma or provides resistance to chemotherapeutic drugs.
摘要翻译：本发明涉及治疗性重氮二环吡啶及其在治疗关节炎，类风湿性关节炎，银屑病关节炎或骨关节炎，器官移植，急性移植或异种移植和同种异体移植排斥，缺血和再灌注损伤，移植耐受诱导，多发性硬化，炎性肠中的用途疾病，溃疡性结肠炎，克罗恩病，狼疮，移植物抗宿主病，T细胞介导的超敏反应性疾病，接触性超敏反应，延迟型超敏反应，麸质敏感性肠病，1型糖尿病，牛皮癣，接触性皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进症，格雷夫斯病，艾迪生病，自身免疫性多腺病，自身免疫性脱发，恶性贫血，白癜风，自身免疫性低位虚型，吉兰巴利综合征，自身免疫性疾病，肾小球肾炎，血清病，uticaria，呼吸系统过敏，哮喘，过敏性鼻炎，皮肤过敏 s，scleracielma，蕈样真菌病，急性炎症反应，急性呼吸窘迫综合征，皮肌炎，斑秃，慢性光化性皮炎，湿疹，贝切特病，脓疱疮，疱疹性坏疽，Sezary综合征，特应性皮炎，全身性硬化症，morphea，II型糖尿病和其中PKCθ或其他PKC家族激酶被激活，过度表达或促进肿瘤细胞，T细胞白血病，胸腺瘤，T细胞和B细胞淋巴瘤，结肠癌，乳腺癌和肺癌的肿瘤生长或存活的癌症，或提供对化学治疗的抗性药物。

8. 发明授权

EP2424859B1 INHIBITORS OF PI3 KINASE AND / OR MTOR 有权
标题翻译： PI3激酶和/或mTOR的抑制剂
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

9. 发明公开

EP2688886A1 AZOLE COMPOUNDS AS PIM INHIBITORS 审中-公开
标题翻译：吡咯化合物ALS抑制剂PIM
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.

10. 发明公开

EP2086973A2 IMIDAZO- AND TRIAZOLO-PYRIDINE COMPOUNDS AND METHODS OF USE THEROF 有权
标题翻译：咪唑和TRIAZOLOPYRIDINVERBINDUNGEN和申请流程。
公开(公告)号：EP2086973A2
公开(公告)日：2009-08-12
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).

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