公开(公告)号：EP2585611A2

公开(公告)日：2013-05-01

申请号：EP11790116.5

申请日：2011-06-03

申请人： The Texas A&M University System ,  The Board of Trustees of the Leland Stanford Junior University

发明人： CIRILLO, Jeffrey, D. ,  SACHETTINI, James, C. ,  RAO, Jianghong ,  XIE, Hexin

IPC分类号： C12Q1/34 ,  C12Q1/04 ,  G01N33/52 ,  G01N33/15 ,  C12R1/32

CPC分类号： A61K49/0013 ,  A61K49/0021 ,  A61K49/0028 ,  A61K49/0032 ,  A61K49/0041 ,  A61K49/0052 ,  C12Q1/04 ,  C12Q1/34 ,  G01N2333/986

摘要： Provided herein are imaging methods for detecting, diagnosing and imaging pathogenic bacteria or a pathophysiological condition associated therewith using fluorogenic substrates for bacterial enzymes. Fluorescent, luminescent or colorimetric signals emitted by substrates or enzyme products in the presence of the bacteria are compared to controls to detect and locate the pathogenic bacteria. Provided is a method for screening therapeutic agents to treat the pathophysiological conditions by measuring a signal emitted from the fluorogenic substrates or products in the presence and absence of the potential therapeutic agent. In addition, a diagnostic method for detecting a mycobacterial infection in a subject by contacting biological samples with a fluorogenic substrate and imaging for signals emitted from a mycobacterial beta-lactamase product. Provided are fluorogenic substrates CC1, CC2, CHPQ, CR2, CNIR1, CNIR2, CNIR3, CNIR4, CNIR5, CNIR5-QSY22, CNIR7, CNIR9, CNIR10, CNIR-TAT, CDC-1, CDC-2, CDC-3, CDC-4, CDC-5, XHX2-81, XHX2-91, XHX3-26, or XHX3-32 or a derivative thereof.

公开(公告)号：EP3094623A1

公开(公告)日：2016-11-23

申请号：EP15737920.7

申请日：2015-01-15

申请人： The Board of Trustees of the Leland Stanford Junior University

发明人： RAO, Jianghong ,  SHI, Haibin

IPC分类号： C07D221/00 ,  C07D501/14 ,  C07D498/00

CPC分类号： C07D501/00 ,  C12Q1/34 ,  C12Q1/66 ,  G01N2333/986

摘要： The present invention discloses a probe useful for the selective detection of metallo-beta-lactamases, in particular carbapenemases, thereby distinguishing those species of bacteria that are carbapenem-resistant from bacterial strains that are sensitive. Cephalospori based probes that have the 6,7 R,R configuration are susceptible to cleavage by beta-lactamases but cannot distinguish between cleavage by metallo-beta-lactamases and other beta-lactamases. By modifying a side group of the cephalosporin, selectivity can be introduced allowing the probes to distinguish between various types of metallo-beta-lactamases,

公开(公告)号：EP3027217A1

公开(公告)日：2016-06-08

申请号：EP14742552.4

申请日：2014-07-25

申请人： University of Bradford ,  The Board of Trustees of the Leland Stanford Junior University

发明人： LOADMAN, Paul ,  FALCONER, Robert ,  GILL, Jason ,  RAO, Jianghong ,  DALDRUP-LINK, Heike E.

IPC分类号： A61K47/48 ,  A61K49/18

CPC分类号： A61K49/1866 ,  A61K31/165 ,  A61K47/60 ,  A61K47/65 ,  A61K47/6927 ,  A61K47/6929 ,  A61K49/085 ,  A61K49/186

摘要： The present inventors have harnessed the targeting of nanoparticles to tumour sites, combined with the tumour site specific elevated MMP-14 activity within one conjugate to simultaneously deliver a vascular disrupting agent (VDA) and a MRI contrast agent to a tumour site. The MMP activatable conjugate of the present invention provides both therapeutic and diagnostic functions - and is referred to as a "theranostic". The theranostic conjugate of the present invention achieves the benefits of tumour site specificity, VDA delivery and MRI contrast agent delivery in a single theranostic conjugate. Consequently, the present invention provides a cancer "theranostic" which improves therapeutic efficacy whilst simultaneously reducing dose-limiting systemic toxicities and provides a tool for rapidly and non-invasively identifying tumour location, monitoring drug delivery and pharmacodynamics.

公开(公告)号：EP2318834A2

公开(公告)日：2011-05-11

申请号：EP09805273.1

申请日：2009-08-06

申请人： The Texas A&M University System ,  The Board of Trustees of The Leland Stanford Junior University

发明人： CIRILLO, Jeffrey, D. ,  RAO, Jianghong

IPC分类号： G01N33/52 ,  C12Q1/25 ,  G01N33/569

CPC分类号： C12Q1/04 ,  A61K49/0013 ,  C12Q1/34 ,  G01N2333/986

摘要： Provided herein are imaging methods for detecting, diagnosing and imaging pathogenic bacteria or a pathophysiological condition associated therewith using fluorescent, luminescent or colorimetric detection agents, e.g., fluorogenic substrates for bacterial enzymes, caged luciferins and fluorescent proteins, luciferases and enzymes expressed by recombinant bacteria. Signals emitted by the fluorescent, luminescent or colorimetric detection agents in the presence of the bacteria are compared to controls to detect and locate the pathogenic bacteria. Also provided is a method for screening therapeutic agents to treat the pathophysiological conditions by measuring fluorescence or luminescence emitted from the detection agents in the presence and absence of the potential therapeutic agent. In addition, a method for detecting a pathogenic bacteria via PET or SPECT imaging using a positron-emitting or gamma-emitting substrate for a beta-lactamase or other enzyme or protein of the pathogenic bacteria. Further provided are the fluorogenic substrates CNIR-7 or CNIR7-TAT or the radiolabeled substrates.

公开(公告)号：EP3102583A1

公开(公告)日：2016-12-14

申请号：EP15746117.9

申请日：2015-02-03

申请人： The Texas A&M University System ,  The Board of Trustees of the Leland Stanford Junior University

发明人： RAO, Jianghong ,  XIE, Hexin ,  CHENG, Yunfeng ,  CIRILLO, Jeffrey, D.

IPC分类号： C07D501/60

CPC分类号： C09B11/24 ,  C07D501/52 ,  C07D501/62 ,  C09B57/02 ,  C12Q1/04 ,  C12Q1/18 ,  C12Q1/34 ,  G01N2333/30 ,  G01N2333/986 ,  G01N2800/12 ,  G01N2800/52

摘要： β-Lactamase substrates and methods for using the substrates to detect β-lactamase and to diagnose tuberculosis.

摘要翻译： β-内酰胺酶底物和使用该基板，以检测β-内酰胺酶和诊断结核病的方法。