公开(公告)号：WO2011103196A1

公开(公告)日：2011-08-25

申请号：PCT/US2011/025092

申请日：2011-02-16

Applicant: AMGEN INC. ,  BREGMAN, Howard ,  BUCHANAN, John, L. ,  CHAKKA, Nagasree ,  DIMAURO, Erin, F. ,  DU, Bingfan ,  NGUYEN, Hanh, Nho ,  ZHENG, Xiao, Mei

Inventor： BREGMAN, Howard ,  BUCHANAN, John, L. ,  CHAKKA, Nagasree ,  DIMAURO, Erin, F. ,  DU, Bingfan ,  NGUYEN, Hanh, Nho ,  ZHENG, Xiao, Mei

IPC: C07D213/74 ,  C07D239/48 ,  C07D251/48 ,  C07D401/04 ,  C07D403/04 ,  C07D471/10 ,  A61K31/53 ,  A61K31/505 ,  A61K31/4427 ,  A61K31/506 ,  A61P29/00

CPC classification number: C07D471/10 ,  C07D213/74 ,  C07D239/48 ,  C07D251/48 ,  C07D401/04 ,  C07D403/04

Abstract: The present invention provides compounds that are inhibitors of voltage-gated sodium channels (Nav), in particular Nav 1.7, and are therefore useful for the treatment of diseases treatable by inhibition of these channels, in particular, chronic pain disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract translation: 本发明提供了作为电压门控钠通道（Nav），特别是Nav 1.7的抑制剂的化合物，因此可用于治疗通过抑制这些通道，特别是慢性疼痛障碍可治疗的疾病。 还提供含有这些化合物的药物组合物和制备这些化合物的方法。

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：WO2013134079A1

公开(公告)日：2013-09-12

申请号：PCT/US2013/028751

申请日：2013-03-01

Applicant: AMGEN INC.

Inventor： BREGMAN, Howard ,  BUCHANAN, John, L. ,  CHAKKA, Nagasree ,  DIMAURO, Erin ,  GUNAYDIN, Hakan ,  GUZMAN PEREZ, Angel ,  HUA, Zihao ,  HUANG, Hongbing ,  HUANG, Xin ,  MARTIN, Matthew, W. ,  PATEL, Vinod

IPC: C07D413/14 ,  C07D413/08 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07D263/34 ,  C07D519/00 ,  A61K31/4166 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D263/34 ,  C07D413/08 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D519/00

Abstract: Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.

Abstract translation: 式（I）和式（II）的化合物是阻聚酶的有用抑制剂。 式（I）和式（II）的化合物具有以下结构：其中在此提供变量的定义。

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：WO2003018022A1

公开(公告)日：2003-03-06

申请号：PCT/US2002/026926

申请日：2002-08-22

Applicant: AMGEN INC.

Inventor： BUCHANAN, John, L. ,  CHAFFEE, Stuart ,  HARMANGE, Jean-Christophe ,  NOVAK, Perry, M. ,  ZHU, Xiaotian

IPC: A61K31/506

CPC classification number: C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of Formula (I) are claimed, wherein R 1 is a heteroaryl ring containing at least one oxygen of sulfur heteroatom and R 2 is as defined in the claims. These compounds are useful in the treatment of cancer.

Abstract translation: 要求的式（I）化合物，其中R 1是含有至少一个硫杂原子氧的杂芳基环，R 2如权利要求中所定义。 这些化合物可用于治疗癌症。

公开(公告)号：WO2003018021A1

公开(公告)日：2003-03-06

申请号：PCT/US2002/026870

申请日：2002-08-22

Applicant: AMGEN INC.

Inventor： HARMANGE, Jean-Christophe ,  BOOKER, Shon ,  BUCHANAN, John, L. ,  CHAFFEE, Stuart ,  NOVAK, Perry, M. ,  VAN DER PLAS, Simon ,  ZHU, Xiaotian

IPC: A61K31/506

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

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

Abstract translation: 本发明包括其化合物，类似物，前药及其药学上可接受的盐，药物组合物，用途和预防和治疗癌症的方法。

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。