公开(公告)号：WO2015057402A1

公开(公告)日：2015-04-23

申请号：PCT/US2014/058948

申请日：2014-10-03

Applicant: UNIVERSITY HEALTH NETWORK ,  BECKMAN COULTER, INC.

Inventor： SHANKEY, T. Vincent ,  GULNIK, Sergei ,  LOPEZ, Lidice L. ,  HEDLEY, David W. ,  CHOW, Sue

IPC: C12Q1/37

CPC classification number: G01N33/5041 ,  C07K14/47 ,  C07K16/18 ,  C12Q1/37 ,  G01N15/14 ,  G01N33/4915 ,  G01N33/5011 ,  G01N33/5047 ,  G01N33/53 ,  G01N33/582 ,  G01N2015/008 ,  G01N2015/1006 ,  G01N2015/149 ,  G01N2333/4704 ,  G01N2440/14

Abstract: Assays that can measure the effect of proteasome inhibitors on target cells in a biological sample are provided. The assays include detecting proteasome activity in a target cell comprising: a) contacting a biological sample comprising one of more target cells with an 1KB degradation agonist to activate the one or more target cells in the biological sample; b) contacting the activated biological sample with a first labeled binding agent that is capable of binding ΙκΒ; c) detecting a target cell in the biological sample of b); and d) determining an amount of the first labeled binding agent bound to the detected target cell, thereby detecting proteasome activity in the target cell.

Abstract translation: 提供了可以测量蛋白酶体抑制剂对生物样品中靶细胞的影响的测定。 所述测定法包括检测靶细胞中的蛋白酶体活性，包括：a）使包含更多靶细胞的生物样品与1KB降解激动剂接触以活化生物样品中的一种或多种靶细胞; b）使活化的生物样品与能够结合ΙκB的第一标记结合剂接触; c）检测b）生物样品中的靶细胞; 以及d）测定与所检测的靶细胞结合的第一标记结合剂的量，由此检测靶细胞中的蛋白酶体活性。

公开(公告)号：WO2015054781A1

公开(公告)日：2015-04-23

申请号：PCT/CA2014/050952

申请日：2014-10-03

Applicant: UNIVERSITY HEALTH NETWORK

Inventor： HEDLEY, David W. ,  LOHSE, Ines ,  MASON, Jacqueline M. ,  BRAY, Mark R.

IPC: A61K31/5377 ,  A61K31/416 ,  A61P35/00 ,  C07D413/14

CPC classification number: A61K31/5377 ,  A61K31/7068 ,  A61K33/24 ,  A61K45/06 ,  C07D403/08 ,  C07D413/14 ,  A61K2300/00

Abstract: The invention is related to a method of treating a subject with pancreatic cancer with administration of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明涉及通过施用结构式（I）表示的化合物或其药学上可接受的盐来治疗患有胰腺癌的受试者的方法。

公开(公告)号：EP3058086A1

公开(公告)日：2016-08-24

申请号：EP14790888.3

申请日：2014-10-03

Applicant: University Health Network ,  Beckman Coulter, Inc.

Inventor： SHANKEY, T. Vincent ,  GULNIK, Sergei ,  LOPEZ, Lidice L. ,  HEDLEY, David W. ,  CHOW, Sue

IPC: C12Q1/37

CPC classification number: G01N33/5041 ,  C07K14/47 ,  C07K16/18 ,  C12Q1/37 ,  G01N15/14 ,  G01N33/4915 ,  G01N33/5011 ,  G01N33/5047 ,  G01N33/53 ,  G01N33/582 ,  G01N2015/008 ,  G01N2015/1006 ,  G01N2015/149 ,  G01N2333/4704 ,  G01N2440/14

Abstract: Assays that can measure the effect of proteasome inhibitors on target cells in a biological sample are provided. The assays include evaluation of the effects of proteasome inhibitors on proteasome activity in cells in a biological sample.

Abstract translation: 提供了可以测量蛋白酶体抑制剂对生物样品中靶细胞的影响的测定。 测定包括蛋白酶体抑制剂对生物样品中细胞中蛋白酶体活性的影响的评估。

公开(公告)号：EP3058086B1

公开(公告)日：2018-04-25

申请号：EP14790888.3

申请日：2014-10-03

Applicant: University Health Network ,  Beckman Coulter, Inc.

Inventor： SHANKEY, T. Vincent ,  GULNIK, Sergei ,  LOPEZ, Lidice L. ,  HEDLEY, David W. ,  CHOW, Sue

IPC: C12Q1/37

CPC classification number: G01N33/5041 ,  C07K14/47 ,  C07K16/18 ,  C12Q1/37 ,  G01N15/14 ,  G01N33/4915 ,  G01N33/5011 ,  G01N33/5047 ,  G01N33/53 ,  G01N33/582 ,  G01N2015/008 ,  G01N2015/1006 ,  G01N2015/149 ,  G01N2333/4704 ,  G01N2440/14

Abstract: Assays that can measure the effect of proteasome inhibitors on target cells in a biological sample are provided. The assays include detecting proteasome activity in a target cell comprising: a) contacting a biological sample comprising one of more target cells with an 1KB degradation agonist to activate the one or more target cells in the biological sample; b) contacting the activated biological sample with a first labeled binding agent that is capable of binding ???; c) detecting a target cell in the biological sample of b); and d) determining an amount of the first labeled binding agent bound to the detected target cell, thereby detecting proteasome activity in the target cell.

公开(公告)号：EP3057593A1

公开(公告)日：2016-08-24

申请号：EP14853347.4

申请日：2014-10-03

Applicant: University Health Network

Inventor： HEDLEY, David W. ,  LOHSE, Ines ,  MASON, Jacqueline M. ,  BRAY, Mark R.

IPC: A61K31/5377 ,  A61K31/416 ,  A61P35/00 ,  C07D413/14

CPC classification number: A61K31/5377 ,  A61K31/7068 ,  A61K33/24 ,  A61K45/06 ,  C07D403/08 ,  C07D413/14 ,  A61K2300/00

Abstract: The invention is related to a method of treating a subject with pancreatic cancer with administration of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof.