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    • 1. 发明申请
    • METHODS AND REAGENTS FOR PREPARING MULTIFUNCTIONAL PROBES
    • 制备多功能探针的方法和试剂
    • WO2010009246A3
    • 2010-05-06
    • PCT/US2009050714
    • 2009-07-15
    • GEN HOSPITAL CORPJOSEPHSON LEEGARANGER ELISABETH
    • JOSEPHSON LEEGARANGER ELISABETH
    • G01N33/50G01N33/53G01N33/68
    • C07K17/02G01N33/531G01N33/532
    • Multifunctional probes are synthesized in a single step using peptide scaffold-based multifunctional single-attachment-point reagents. To obtain multifunctional probes using the methods of the invention, a substrate (e.g., a nanoparticle, polymer, antibody, protein, low molecular weight compound, drug, etc.) is reacted with a multifunctional single-attachment-point (MSAP) reagent. The MSAP reagents can include three components: (i) a peptide scaffold, (ii) a single chemically reactive group on the peptide scaffold for reaction of the MSAP with a substrate having a complementary reactive group, and (iii) multiple functional groups on the peptide scaffold. The peptide scaffold can include any number of residues; however, for ease of synthesis and reproducibility in clinical trials, it is preferred to limit the residues in the peptide to 20 or less. The reagent can be prepared to yield a predetermined stoichiometric ratio of the functional groups on the scaffold such that the probe has a fixed stoichiometric ratio of the functional groups.
    • 使用基于肽基脚手架的多功能单附着点试剂,可以一步合成多功能探针。 为了使用本发明的方法获得多功能探针,将底物(例如纳米颗粒,聚合物,抗体,蛋白质,低分子量化合物,药物等)与多功能单附着点(MSAP)试剂反应。 MSAP试剂可以包括三种组分:(i)肽支架,(ii)肽支架上的单个化学反应基团,用于MSAP与具有互补反应基团的底物反应,和(iii)多肽上的多个官能团 肽支架。 肽骨架可以包括任何数量的残基; 然而,为了便于临床试验中的合成和再现性,优选将肽中的残基限制在20或更少。 可以制备试剂以产生预定的化学计量比的支架上的官能团,使得探针具有固定的官能团的化学计量比。
    • 5. 发明申请
    • DETECTING IONS AND MEASURING ION CONCENTRATIONS
    • 检测离子和测量离子浓度
    • WO2009026251A1
    • 2009-02-26
    • PCT/US2008/073515
    • 2008-08-18
    • THE GENERAL HOSPITAL CORPORATIONJOSEPHSON, LeeTAKTAK, Sonia
    • JOSEPHSON, LeeTAKTAK, Sonia
    • A61K9/16
    • A61K49/1863A61K49/085A61K49/1833G01N33/84
    • The present inventions include methods and compositions for detecting the presence of ions and measuring the level or concentration of ions in a sample by nuclear magnetic resonance (NMR) using magnetic particles. In particular, the inventions include the preparation and use of magnetic particles having synthetic ion chelators covalently bound to their surfaces. In the presence of target ions, the surface-modified magnetic particles form clusters, which can be monitored by NMR relaxation measurements. The relaxation times can then be used to detect specific ions and determine their concentration. The described methods, compositions, and devices are useful for a variety of applications including biomedical applications in diagnostics and imaging.
    • 本发明包括用于通过使用磁性颗粒的核磁共振(NMR)检测离子的存在和测量样品中离子的水平或浓度的方法和组合物。 特别地,本发明包括制备和使用具有共价结合到其表面上的合成离子螯合剂的磁性颗粒。 在存在目标离子的情况下,表面改性的磁性颗粒形成簇,这可以通过NMR弛豫测量来监测。 然后松弛时间可用于检测特定离子并确定其浓度。 所描述的方法,组合物和装置对于包括诊断和成像中的生物医学应用的各种应用是有用的。
    • 9. 发明申请
    • METHODS AND REAGENTS FOR PREPARING MULTIFUNCTIONAL PROBES
    • 制备多功能探针的方法和试剂
    • WO2010009246A2
    • 2010-01-21
    • PCT/US2009/050714
    • 2009-07-15
    • THE GENERAL HOSPITAL CORPORATIONJOSEPHSON, LeeGARANGER, Elisabeth
    • JOSEPHSON, LeeGARANGER, Elisabeth
    • G01N33/50G01N33/53G01N33/68
    • C07K17/02G01N33/531G01N33/532
    • Multifunctional probes are synthesized in a single step using peptide scaffold-based multifunctional single-attachment-point reagents. To obtain multifunctional probes using the methods of the invention, a substrate (e.g., a nanoparticle, polymer, antibody, protein, low molecular weight compound, drug, etc.) is reacted with a multifunctional single-attachment-point (MSAP) reagent. The MSAP reagents can include three components: (i) a peptide scaffold, (ii) a single chemically reactive group on the peptide scaffold for reaction of the MSAP with a substrate having a complementary reactive group, and (iii) multiple functional groups on the peptide scaffold. The peptide scaffold can include any number of residues; however, for ease of synthesis and reproducibility in clinical trials, it is preferred to limit the residues in the peptide to 20 or less. The reagent can be prepared to yield a predetermined stoichiometric ratio of the functional groups on the scaffold such that the probe has a fixed stoichiometric ratio of the functional groups.
    • 多功能探针使用基于肽支架的多功能单连接点试剂在一个步骤中合成。 为了使用本发明的方法获得多功能探针,将底物(例如纳米颗粒,聚合物,抗体,蛋白质,低分子化合物,药物等)与多功能单连接点(MSAP)试剂反应。 MSAP试剂可以包括三个组分:(i)肽支架,(ii)肽支架上的单个化学反应性基团,用于使MSAP与具有互补反应性基团的底物反应,和(iii)多个官能团 肽支架。 肽支架可以包括任何数量的残基; 然而,为了便于在临床试验中的合成和再现性,优选将肽中的残基限制在20以下。 可以制备试剂以产生支架上官能团的预定化学计量比,使得探针具有官能团的固定化学计量比。