公开(公告)号：WO2010096314A1

公开(公告)日：2010-08-26

申请号：PCT/US2010/023764

申请日：2010-02-10

Applicant: AMGEN INC. ,  BOEZIO, Alessandro ,  CHENG, Alan, C. ,  COATS, James, R. ,  COPELAND, Katrina, W. ,  GRACEFFA, Russell ,  HARMANGE, Jean-Christophe ,  HUANG, Hongbing ,  LA, Daniel ,  OLIVIERI, Philip, R. ,  PETERSON, Emily, A. ,  SCHENKEL, Laurie

Inventor： BOEZIO, Alessandro ,  CHENG, Alan, C. ,  COATS, James, R. ,  COPELAND, Katrina, W. ,  GRACEFFA, Russell ,  HARMANGE, Jean-Christophe ,  HUANG, Hongbing ,  LA, Daniel ,  OLIVIERI, Philip, R. ,  PETERSON, Emily, A. ,  SCHENKEL, Laurie

IPC: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/53 ,  A61K31/506 ,  A61K31/5355 ,  A61P35/00

CPC classification number: C07D403/14 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention provides compounds that are kinase inhibitors, specifically PIK kinase inhibitors, more specifically, mTOR inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PIK kinase inhibitors, more specifically, mTOR such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract translation: 本发明提供了化合物，其是激酶抑制剂，特别是PIK激酶抑制剂，更具体地，mTOR抑制剂，因此可用于治疗通过抑制激酶可治疗的疾病，特别是PIK激酶抑制剂，更具体地，mTOR如癌症。 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：WO2015051043A1

公开(公告)日：2015-04-09

申请号：PCT/US2014/058699

申请日：2014-10-01

Applicant: AMGEN INC.

Inventor： BREGMAN, Howard ,  CHAKKA, Nagasree ,  DIMAURO, Erin F. ,  GAO, Hua ,  GUNAYDIN, Hakan ,  HUANG, Hongbing ,  OLIVIERI, Philip ,  SCHENKEL, Laurie ,  WEISS, Matthew

IPC: C07D213/64 ,  A61K31/4418 ,  A61P25/04

CPC classification number: C07D417/12 ,  C07D213/26 ,  C07D213/64 ,  C07D213/643 ,  C07D213/70 ,  C07D401/04 ,  C07D405/12

Abstract: The present invention provides compounds of Formula (Ia), and pharmaceutically acceptable salts thereof. The compounds are useful as inhibitors of voltage-gated sodium channels, in particular Nav 1.7. (Ia); as described in the specification. 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, as well as intermediates and processes useful for making the compounds.

Abstract translation: 本发明提供式（Ia）化合物及其药学上可接受的盐。 该化合物可用作电压门控钠通道的抑制剂，特别是Nav 1.7。 式（Ia）; 如说明书中所述。 该化合物可用于治疗可通过抑制钠通道（例如疼痛障碍）治疗的疾病。 还提供了含有本发明化合物的药物组合物，以及可用于制备化合物的中间体和方法。

公开(公告)号：WO2010132598A1

公开(公告)日：2010-11-18

申请号：PCT/US2010/034596

申请日：2010-05-12

Applicant: AMGEN INC. ,  BODE, Christiane ,  BOEZIO, Alessandro ,  CHENG, Alan, C. ,  CHOQUETTE, Deborah ,  COATS, James, R. ,  COPELAND, Katrina, W. ,  HUANG, Hongbing ,  LA, Daniel ,  LEWIS, Richard ,  LIAO, Hongyu ,  POTASHMAN, Michele ,  STELLWAGEN, John ,  YI, Shuyan ,  NORMAN, Mark ,  STEC, Markian ,  PETERSON, Emily, A. ,  GRACEFFA, Russell

Inventor： BODE, Christiane ,  BOEZIO, Alessandro ,  CHENG, Alan, C. ,  CHOQUETTE, Deborah ,  COATS, James, R. ,  COPELAND, Katrina, W. ,  HUANG, Hongbing ,  LA, Daniel ,  LEWIS, Richard ,  LIAO, Hongyu ,  POTASHMAN, Michele ,  STELLWAGEN, John ,  YI, Shuyan ,  NORMAN, Mark ,  STEC, Markian ,  PETERSON, Emily, A. ,  GRACEFFA, Russell

IPC: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/506 ,  A61K31/437 ,  A61K31/52 ,  A61K31/53 ,  A61P35/00

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3Kα kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3Kα, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract translation: 本发明提供了PIKK抑制剂，更具体地，mTOR和/或PI3Ka激酶抑制剂的化合物，因此可用于治疗通过抑制激酶可以治疗的疾病，特别是PI3激酶，更具体地，mTOR和/或PI3Kα，例如 癌症。 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：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：WO2010030954A1

公开(公告)日：2010-03-18

申请号：PCT/US2009/056748

申请日：2009-09-11

Applicant: AMGEN INC. ,  WHITE, Ryan ,  AMEGADZIE, Albert ,  BRYAN, Marian C. ,  CHEN, Jian J. ,  CHENG, Alan C. ,  DINEEN, Thomas ,  EPSTEIN, Oleg ,  GORE, Vijay Keshav ,  HUA, Zihao ,  HUMAN, Jason B. ,  HUANG, Hongbing ,  KREIMAN, Charles ,  LA, Daniel ,  LIU, Qingyian ,  MA, Vu Van ,  MARX, Isaac ,  PATEL, Vinod F. ,  QIAN, Wenyuan ,  WEISS, Matthew ,  YUAN, Chester C.

Inventor： WHITE, Ryan ,  AMEGADZIE, Albert ,  BRYAN, Marian C. ,  CHEN, Jian J. ,  CHENG, Alan C. ,  DINEEN, Thomas ,  EPSTEIN, Oleg ,  GORE, Vijay Keshav ,  HUA, Zihao ,  HUMAN, Jason B. ,  HUANG, Hongbing ,  KREIMAN, Charles ,  LA, Daniel ,  LIU, Qingyian ,  MA, Vu Van ,  MARX, Isaac ,  PATEL, Vinod F. ,  QIAN, Wenyuan ,  WEISS, Matthew ,  YUAN, Chester C.

IPC: C07D498/10 ,  C07D513/10 ,  A61K31/424 ,  A61K31/429 ,  A61P25/28

CPC classification number: C07D498/10 ,  C07D513/10

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , T 1 , T 2 , W, X, Y and Z of Formula (I) are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula (I).

Abstract translation: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式（I）; 其中本文定义式（I）的A1，A2，A3，A4，A5，A6，T1，T2，W，X，Y和Z。 本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的疾病和病症的用途。 这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式I的其它实施方案，可用于制备式（I）化合物的中间体和方法。