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

Applicant: AMGEN INC

Inventor： 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: 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

Abstract: 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.

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

Applicant: 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

Inventor： 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: C07D311/96 ,  C07C235/82 ,  C07D213/56 ,  C07D213/61 ,  C07D307/94 ,  C07C237/24 ,  C07D221/20 ,  C07D215/48 ,  C07C59/88 ,  C07D217/02 ,  A61K31/352 ,  A61P9/10

Abstract: 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.

公开(公告)号：WO2006039718A3

公开(公告)日：2006-04-13

申请号：PCT/US2005/035873

申请日：2005-10-03

Applicant: AMGEN INC

Inventor： PATEL, Vinod F. ,  KIM, Joseph L. ,  GEUNS-MEYER, Stephanie D. ,  CHAFFEE, Stuart C. ,  CEE, Victor J. ,  HODOUS, Brian L. ,  BELLON, Steven ,  HARMANGE, Jean-christophe ,  OLIVIERI, Philip R. ,  THAMAN, Maya C. ,  DIMAURO, Erin F. ,  BUCHANAN, John L. ,  MCGOWAN, David C. ,  ALBRECHT, Brian K. ,  DEAK, Holly L. ,  BEMIS, Jean E. ,  WHITE, Ryan ,  MARTIN, Matthew W. ,  HABGOOD, Gregory J. ,  TEMPEST, Paul A. ,  MASSE, Craig E. ,  BUCKNER, William H. ,  HERBERICH, Bradley J. ,  GRACEFFA, Russell ,  ZHANG, Dawei ,  XU, Shimin ,  SHAM, Kelvin ,  RZASA, Robert M. ,  FALSEY, James Richard ,  CHAKRABARTI, Partha P. ,  CAO, Guo-qiang ,  TOMLINSON, Susan Ann ,  PETTUS, Liping H. ,  SMITH, Adrian Leonard ,  PARAS, Nick A. ,  LIU, Gang ,  DEMORIN, Frenel F. ,  TASKER, Andrew ,  REED, Anthony

IPC: C07D239/84 ,  C07D239/95 ,  C07D401/12 ,  C07D409/04 ,  C07D405/12 ,  C07D409/14 ,  C07D405/04 ,  C07D403/10 ,  C07D401/04 ,  C07D471/04 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D409/12 ,  C07D215/12

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I, wherein A1, A2, A3, B, R1, R2, R3 and R4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

公开(公告)号：WO2008076425A1

公开(公告)日：2008-06-26

申请号：PCT/US2007/025799

申请日：2007-12-17

Applicant: AMGEN INC. ,  ALLEN, Jennifer, R. ,  BISWAS, Kaustav ,  CAO, Guo-Qiang ,  GOLDEN, Jennifer, E. ,  MERCEDE, Stephanie ,  PETERKIN, Tanya ,  REED, Anthony ,  TEGLEY, Christopher, M.

Inventor： ALLEN, Jennifer, R. ,  BISWAS, Kaustav ,  CAO, Guo-Qiang ,  GOLDEN, Jennifer, E. ,  MERCEDE, Stephanie ,  PETERKIN, Tanya ,  REED, Anthony ,  TEGLEY, Christopher, M.

IPC: C07D487/04

CPC classification number: C07D471/04

Abstract: Compounds of Formula (I) are useful as inhibitors of HIF prolyl hydroxylases where the definitions of the variables are provided herein.

Abstract translation: 式（I）的化合物可用作HIF脯氨酰羟化酶的抑制剂，其中本文提供变量的定义。

公开(公告)号：WO2006044823A2

公开(公告)日：2006-04-27

申请号：PCT/US2005/037299

申请日：2005-10-17

Applicant: AMGEN INC. ,  CHAFFEE, Stuart C. ,  ALBRECHT, Brian K. ,  HODOUS, Brian L. ,  MARTIN, Matthew W. ,  MCGOWAN, David C. ,  DIMAURO, Erin F. ,  REDDY, Gade ,  CEE, Victor J. ,  OLIVIERI, Philip R. ,  REED, Anthony ,  ROMERO, Karina

Inventor： CHAFFEE, Stuart C. ,  ALBRECHT, Brian K. ,  HODOUS, Brian L. ,  MARTIN, Matthew W. ,  MCGOWAN, David C. ,  DIMAURO, Erin F. ,  REDDY, Gade ,  CEE, Victor J. ,  OLIVIERI, Philip R. ,  REED, Anthony ,  ROMERO, Karina

IPC: C07D239/42 ,  A61K31/505 ,  A61P35/00

CPC classification number: C07D213/74 ,  C07D213/81 ,  C07D215/14 ,  C07D239/42 ,  C07D241/42 ,  C07D401/06 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/06 ,  C07D409/06 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I: wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 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，癌症和相关病症的化合物。 化合物具有通式I：其中A1，A2，A3，A4，R1和R2如本文所定义。 因此，本发明还包括含有本发明化合物的药物组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

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

Applicant: AMGEN INC. ,  CAO, Guo-Qiang ,  CHEN, Jian, J. ,  DOMINGUEZ, Celia ,  REED, Anthony ,  SHAM, Kelvin, K., C. ,  THAMAN, Maya, C. ,  ZHANG, Dawei ,  HERBERICH, Bradley, J.

Inventor： CAO, Guo-Qiang ,  CHEN, Jian, J. ,  DOMINGUEZ, Celia ,  REED, Anthony ,  SHAM, Kelvin, K., C. ,  THAMAN, Maya, C. ,  ZHANG, Dawei ,  HERBERICH, Bradley, J.

IPC: C07D487/08

CPC classification number: C07D487/06 ,  C07D213/56 ,  C07D239/95 ,  C07D401/04 ,  C07D401/14 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。