公开(公告)号：WO2013086229A1

公开(公告)日：2013-06-13

申请号：PCT/US2012/068297

申请日：2012-12-06

Applicant: AMGEN INC.

Inventor： BOEZIO, Christiane ,  BREGMAN, Howard ,  COATS, James, R. ,  DIMAURO, Erin, F. ,  DINEEN, Thomas ,  DU, Bingfan ,  GRACEFFA, Russell ,  KREIMAN, Charles ,  LA, Daniel ,  MARX, Isaac, E. ,  CHAKKA, Nagasree ,  NGUYEN, Hanh Nho ,  PETERSON, Emily, Anne ,  WEISS, Matthew ,  COPELAND, Katrina, W. ,  DEAK, Holly, L. ,  BOEZIO, Alessandro

IPC: C07D239/42 ,  C07D277/52 ,  C07D285/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  A61K31/427

CPC classification number: C07D498/04 ,  C07D239/42 ,  C07D277/52 ,  C07D285/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. (The Formula I should be inserted here.) The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.

Abstract translation: 本发明提供式I化合物或其药学上可接受的盐，其是电压门控钠通道的抑制剂，特别是Nav 1.7。 （此处应插入式I）。该化合物可用于治疗通过抑制钠通道（如疼痛障碍）治疗的疾病。 还提供含有本发明化合物的药物组合物。

公开(公告)号：WO2010022055A2

公开(公告)日：2010-02-25

申请号：PCT/US2009/054169

申请日：2009-08-18

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

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

CPC classification number: C07D401/12 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04

Abstract: The present invention provides compounds that are inhibitors of voltage-gated sodium channel (Nav), in particular Nav 1.7 and are therefore useful for the treatment of diseases 5 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）的抑制剂，特别是Nav 1.7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：WO2008124083A3

公开(公告)日：2008-10-16

申请号：PCT/US2008/004432

申请日：2008-04-03

Applicant: AMGEN INC. ,  CEE, Victor, J. ,  DEAK, Holly, L. ,  GEUNS-MEYER, Stephanie, D. ,  DU, Bingfan ,  HODOUS, Brian, L. ,  MARTIN, Mathew, W. ,  NGUYEN, Hanh, Nho ,  OLIVIERI, Philip, R. ,  PANTER, Kathleen ,  ROMERO, Karina ,  SCHENKEL, Laurie ,  WHITE, Ryan

Inventor： CEE, Victor, J. ,  DEAK, Holly, L. ,  GEUNS-MEYER, Stephanie, D. ,  DU, Bingfan ,  HODOUS, Brian, L. ,  MARTIN, Mathew, W. ,  NGUYEN, Hanh, Nho ,  OLIVIERI, Philip, R. ,  PANTER, Kathleen ,  ROMERO, Karina ,  SCHENKEL, Laurie ,  WHITE, Ryan

IPC: C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/04 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  C07D495/04 ,  A61K31/502 ,  A61P35/00

Abstract: The present invention relates to chemical compounds having a general formula (I), wherein A 1-8 , D , , L 1 , L 2 , R 1 , R 6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.

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：WO2007087276A1

公开(公告)日：2007-08-02

申请号：PCT/US2007/001714

申请日：2007-01-22

Applicant: AMGEN INC. ,  CEE, Victor J. ,  DEAK, Holly L. ,  DU, Bingfan ,  GEUNS-MEYER, Stephanie D. ,  HODOUS, Brian L. ,  NGUYEN, Hanh Nho ,  OLIVIERI, Philip R. ,  PATEL, Vinod F. ,  ROMERO, Karina ,  SCHENKEL, Laurie

Inventor： CEE, Victor J. ,  DEAK, Holly L. ,  DU, Bingfan ,  GEUNS-MEYER, Stephanie D. ,  HODOUS, Brian L. ,  NGUYEN, Hanh Nho ,  OLIVIERI, Philip R. ,  PATEL, Vinod F. ,  ROMERO, Karina ,  SCHENKEL, Laurie

IPC: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D497/04 ,  A61K31/502 ,  A61P35/00

CPC classification number: C07D401/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D497/04

Abstract: The present invention relates to chemical compounds having a general formula (I) wherein A 1 , A 2 , C 1 , C 2 , D, L 1 , L 2 , Z and R 1-8 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.

Abstract translation: 本发明涉及具有通式（I）的化合物，其中A 1，A 2，C 1，C 2 D，L 1，L 2，Z和R 1-8均在本文中定义，合成中间体是 能够调节各种蛋白激酶受体酶，从而影响与这些激酶的活性相关的各种疾病状态和状况。 例如，化合物能够调节Aurora激酶，从而影响细胞周期和细胞增殖的过程，以治疗癌症和与癌症有关的疾病。 本发明还包括药物组合物，包括该化合物，以及治疗与Aurora激酶活性有关的疾病状态的方法。