公开(公告)号：WO2005009978A1

公开(公告)日：2005-02-03

申请号：PCT/US2004/023233

申请日：2004-07-15

Applicant: AMGEN INC. ,  BUCHANAN, John, L. ,  ELBAUM, Daniel ,  MARTIN, Matthew, W. ,  MCGOWAN, David, C. ,  NOVAK, Perry, M. ,  NUNES, Joseph, J.

Inventor： BUCHANAN, John, L. ,  ELBAUM, Daniel ,  MARTIN, Matthew, W. ,  MCGOWAN, David, C. ,  NOVAK, Perry, M. ,  NUNES, Joseph, J.

IPC: C07D239/48

CPC classification number: C04B35/632 ,  C07D213/75 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention relates to pyrimidine or pyridine carbamate compounds having the general Formula (1) and pharmaceutically acceptable salts or derivatives thereof. Also included are methods of treatment of various diseases and conditions, including inflammation, inhibition of T cell activation and proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, the methods comprising administering a therapeutically-effective amount a compound of Formula I, or a salt or derivative form thereof, as described above.

Abstract translation: 本发明涉及具有通式（1）的嘧啶或吡啶氨基甲酸酯化合物及其药学上可接受的盐或衍生物。 还包括治疗各种疾病和病症的方法，包括炎症，T细胞活化和增殖的抑制，关节炎，器官移植，缺血或再灌注损伤，心肌梗死，中风，多发性硬化，炎性肠病，克罗恩病，狼疮， 超敏反应，1型糖尿病，牛皮癣，皮炎，桥本甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进，艾迪生病，自身免疫性疾病，肾小球性肾炎，过敏性疾病，哮喘，干草病，湿疹，癌症，结肠癌，胸腺瘤，仅举几例 哺乳动物，所述方法包括给予治疗有效量的如上所述的式I化合物或其盐或衍生物形式。

公开(公告)号：WO2005070891A2

公开(公告)日：2005-08-04

申请号：PCT/US2005/002326

申请日：2005-01-24

Applicant: AMGEN INC

Inventor： POTASHMAN, Michele ,  KIM, Tae-seong ,  BELLON, Steven ,  BOOKER, Shon ,  CHENG, Yuan ,  KIM, Joseph, L. ,  TASKER, Andrew ,  XI, Ning ,  XU, Shimin ,  HARMANGE, Jean-Christophe ,  BORG, George ,  WEISS, Matthew ,  HODOUS, Brian, L. ,  GRACEFFA, Russell ,  BUCKNER, Willian, H. ,  MASSE, Craig, E. ,  CHOQUETTE, Deborah ,  MARTIN, Matthew, W. ,  GERMAIN, Julie ,  DIPIETRO, Lucian, V. ,  CHAFFEE, Stuart, C. ,  NUNES, Joseph, J. ,  BUCHANAN, John, L. ,  HABGOOD, Gregory, J. ,  MCGOWAN, David, C. ,  WHITTINGTON, Douglas, A.

IPC: C07D215/00

CPC classification number: C07D213/64 ,  C07D213/81 ,  C07D215/233 ,  C07D215/38 ,  C07D215/48 ,  C07D215/54 ,  C07D237/34 ,  C07D239/34 ,  C07D239/47 ,  C07D239/84 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutically compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗涉及癌症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在这些方法中有用的中间体。

公开(公告)号：WO2002083653A1

公开(公告)日：2002-10-24

申请号：PCT/US2002/011480

申请日：2002-04-11

Applicant: AMGEN INC.

Inventor： BUCHANAN, John, L. ,  KIM, Joseph, L. ,  NOVAK, Perry, M. ,  NUNES, Joseph, J. ,  PATEL, Vinod, F.

IPC: C07D251/18

CPC classification number: C07D401/12 ,  C07D251/18 ,  C07D401/14 ,  C07D403/12

Abstract: The invention encompasses compounds of formula I, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer and polycystic kidney disease.

Abstract translation: 本发明包括式I化合物，其类似物，前药和药学上可接受的盐，药物组合物，用于预防和治疗癌症和多囊肾病的用途和方法。

公开(公告)号：WO2006130160A2

公开(公告)日：2006-12-07

申请号：PCT/US2005/025725

申请日：2005-07-19

Applicant: AMGEN INC. ,  NUNES, Joseph, J. ,  MARTIN, Matthew, W. ,  WHITE, Ryan ,  MCGOWAN, David ,  BEMIS, Jean, E. ,  KAYSER, Frank ,  FU, Jiasheng ,  LIU, Jinqian ,  JIAO, XianYun

Inventor： NUNES, Joseph, J. ,  MARTIN, Matthew, W. ,  WHITE, Ryan ,  MCGOWAN, David ,  BEMIS, Jean, E. ,  KAYSER, Frank ,  FU, Jiasheng ,  LIU, Jinqian ,  JIAO, XianYun

CPC classification number: C07D491/04 ,  C07D491/14

Abstract: The present invention relates to furanopyridine compounds having the general Formula I (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of modulating Lck and ACK-1 enzymes and of treating various related diseases and conditions, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, comprising administering to the mammal a therapeutically effective amount a compound of Formula I, as described above, and methods of manufacturing medicaments comprising the compound of Formula I.

Abstract translation: 本发明涉及具有通式I（I）的呋喃并吡啶化合物及其立体异构体，互变异构体，溶剂合物，药学上可接受的盐和衍生物及其前药。 本发明还包括药物组合物，其包含式I化合物，调节Lck和ACK-1酶的方法以及治疗各种相关疾病和病症，包括炎症，T细胞活化抑制，增殖，关节炎，器官移植，缺血或再灌注 损伤，心肌梗塞，中风，多发性硬化，炎性肠病，克罗恩病，狼疮，超敏反应，1型糖尿病，牛皮癣，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，艾迪生病，自身免疫性疾病，肾小球肾炎，过敏性疾病，哮喘 ，干草组织，湿疹，癌症，结肠癌，胸腺瘤，仅举几个例子，在哺乳动物中，包括向哺乳动物施用治疗有效量的如上所述的式I化合物和制备包含以下化合物的药物的方法： 一级方程式