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    SWITCHING-TYPE FLUORESCENT NANOPARTICLE PROBE, AND FLUORESCENT MOLECULAR IMAGING METHOD USING SAME
    2.
    发明公开
    SWITCHING-TYPE FLUORESCENT NANOPARTICLE PROBE, AND FLUORESCENT MOLECULAR IMAGING METHOD USING SAME 审中-公开
    与荧光纳米粒子和可逆的探针法用于说明荧光分子

    公开(公告)号：EP2682131A1

    公开(公告)日：2014-01-08

    申请号：EP12751966.8

    申请日：2012-03-01

    申请人： Kyoto University ,  Shimadzu Corporation

    发明人： SAJI, Hideo ,  KIMURA, Shunsaku ,  ONO, Masahiro ,  TEMMA, Takashi ,  HARA, Isao ,  OZEKI, Eiichi

    IPC分类号： A61K49/00

    CPC分类号： A61K49/0054 ,  A61K49/0032 ,  A61K49/0034 ,  A61K49/0069 ,  A61K49/0093

    摘要： [Abstract] [Problem] To provide a novel fluorescent nanoparticle imaging probe having a switching function (a function to quench a fluorescent dye in a blood component and emit fluorescence in a tumor or an inflamed site to be imaged).
    [Solution] A fluorescent nanoparticle probe comprising: a molecular assembly composed of an amphiphilic block polymer having a hydrophilic block chain and a hydrophobic block chain; and a fluorescent dye encapsulated in the assembly, wherein (a) the hydrophilic block chain comprises, as an essential hydrophilic structural unit, a unit selected from a sarcosine unit and an alkylene oxide unit, (b) the hydrophobic block chain comprises, as an essential hydrophobic structural unit, a unit selected from the group consisting of an amino acid unit and a hydroxylic acid unit, and (c) the fluorescent dye is a polylactic acid-bound cyanine compound comprising: a fluorescent group represented by the formula (I):[Chemical

    and a polylactic acid group having 5 to 50 lactic acid units, and two or more molecules of the fluorescent dye are encapsulated in the single molecular assembly. [Selected Figure] Fig.1

    摘要翻译： [摘要] [问题]提供一种具有切换功能（以淬灭在血液成分的荧光染料和在肿瘤或炎症部位要被成像发出荧光的函数）的新型荧光纳米颗粒成像探针。 [解决方法]一种荧光纳米颗粒探针，包括：具有亲水性嵌段链和疏水性嵌段链的两亲性嵌段聚合物组成的分子组件; 和封装在组件上的荧光染料，worin（a）所述亲水性嵌段链包含，作为基本亲水性结构单元，从一个肌氨酸单元选择的单元和烯化氧单元，（B）疏水性嵌段链包含，如在 基本疏水性结构单元，选自一种氨基酸单元和羟基羧酸单元，和（c）的荧光染料为聚乳酸结合的花青化合物，包含的选择的单元：由式（I）表示的荧光基团 ：[化学和具有5至50乳酸单元，和荧光染料的两个或多个分子的聚乳酸组被封装在单个分子组装。 [选定图]图1

    MOLECULAR ASSEMBLY USING BRANCHED AMPHIPHILIC BLOCK POLYMER, AND DRUG TRANSPORTATION SYSTEM
    5.
    发明公开
    MOLECULAR ASSEMBLY USING BRANCHED AMPHIPHILIC BLOCK POLYMER, AND DRUG TRANSPORTATION SYSTEM 审中-公开
    TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM TEM

    公开(公告)号：EP2893924A1

    公开(公告)日：2015-07-15

    申请号：EP13836159.7

    申请日：2013-09-03

    申请人： Shimadzu Corporation ,  Kyoto University

    发明人： HARA, Isao ,  OZEKI, Eiichi ,  KIMURA, Shunsaku ,  MAKINO, Akira

    IPC分类号： A61K9/51 ,  A61K9/10 ,  A61K47/34 ,  A61K49/00

    摘要： The present invention provides a molecular assembly whose retention time in a target site is adjusted depending on the kind or purpose of a labeling agent or drug encapsulated therein, and a molecular assembly that can suppress the ABC phenomenon and that can be administered more than once within a short span. A molecular assembly comprising: a branched-type amphiphilic block polymer A comprising a branched hydrophilic block comprising sarcosine and a hydrophobic block comprising a polylactic acid chain; and a functional substance F comprising a functional site and a polylactic acid chain, wherein the polylactic acid chain constituting the hydrophobic block of the amphiphilic block polymer A comprises L-lactic acid units, and the polylactic acid chain contained in the functional substance F comprises D-lactic acid units, or the Polylactic acid chain constituting the hydrophobic block of the amphiphilic block polymer A comprises D-lactic acid units, and the polylactic acid chain contained in the functional substance F comprises L-lactic acid units.

    摘要翻译： 本发明提供一种分子组合物，其在靶位点的保留时间取决于包封在其中的标记试剂或药物的种类或目的，以及可以抑制ABC现象并且可以多次施用的分子组装 短跨度 一种分子组合物，其包含：支链型两亲嵌段聚合物A，其包含含有肌氨酸的支链亲水嵌段和包含聚乳酸链的疏水嵌段; 和包含功能部位和聚乳酸链的功能性物质F，其中构成所述两亲性嵌段聚合物A的疏水性嵌段的聚乳酸链包含L-乳酸单元，所述功能性物质F中所含的聚乳酸链包含D 或者构成两亲性嵌段聚合物A的疏水嵌段的聚乳酸链包含D-乳酸单元，功能性物质F中所含的聚乳酸链包含L-乳酸单元。

    NOVEL MOLECULAR ASSEMBLY, MOLECULAR PROBE FOR MOLECULAR IMAGING AND MOLECULAR PROBE FOR DRUG DELIVERY SYSTEM USING THE SAME, AND MOLECULAR IMAGING SYSTEM AND DRUG DELIVERY SYSTEM
    9.
    发明公开
    NOVEL MOLECULAR ASSEMBLY, MOLECULAR PROBE FOR MOLECULAR IMAGING AND MOLECULAR PROBE FOR DRUG DELIVERY SYSTEM USING THE SAME, AND MOLECULAR IMAGING SYSTEM AND DRUG DELIVERY SYSTEM 有权
    新的分子排列，分子探针用于药物递送系统，有序，分子成像系统和药物递送系统的分子成像和分子探针

    公开(公告)号：EP2305214A1

    公开(公告)日：2011-04-06

    申请号：EP09758388.4

    申请日：2009-06-04

    申请人： Shimadzu Corporation ,  Kyoto University

    发明人： HARA, Isao ,  YAMAHARA, Ryo ,  OZEKI, Eiichi ,  TAKEUCHI, Eri ,  KIMURA, Shunsaku ,  KONDOH, Shinae ,  MAKINO, Akira ,  YAMAMOTO, Fumihiko

    IPC分类号： A61K9/10 ,  A61K9/127 ,  A61K9/19 ,  A61K47/34 ,  A61K47/42 ,  A61K47/48 ,  A61K49/00 ,  A61K51/00 ,  A61P35/00

    CPC分类号： A61K51/06 ,  A61K9/5153 ,  A61K49/0032 ,  A61K49/0034 ,  A61K49/0054 ,  A61K49/0082 ,  A61K51/1234

    摘要： The present invention provides a molecular assembly which is less likely to accumulate in tissue other than cancer tissue, is highly safe for a living body, and can be prepared by a simple and safe method and whose particle size can be easily controlled. The present invention provides a molecular imaging system and a molecular probe useful for the system, and a drug delivery system and a molecular probe useful for the system. The present invention provides a method for preparing molecular assembly, by which the particle size of molecular assembly having a signal group or a drug can be arbitrarily controlled in order to allow the molecular assembly to effectively accumulate in cancer tissue by utilizing EPR effect. A molecular assembly comprising: an amphiphilic block polymer A comprising a hydrophilic block chain and a hydrophobic block chain having 10 or more lactic acid units; a hydrophobic polymer A2 having at least 10 or more lactic acid units; and/or a labeled polymer B comprising at least 10 or more lactic acid units and a labeling group.

    摘要翻译： 本发明提供了一种分子组装所有这些不太可能在比癌组织的其它组织积累，为生物体高度安全的，并且可以通过简单和安全的方法和其颗粒尺寸可以容易地控制来制备。 本发明提供了一种分子成像系统和分子探针的系统是有用的，药物递送系统和分子探针的系统是有用的。本发明提供了用于制备分子组件的方法，通过该分子组装的粒径 具有信号基或药物可以以允许所述分子集合体通过利用EPR效果在癌组织中有效累积任意控制。 的分子组件，包括：两亲性嵌段聚合物A包含亲水性嵌段链和具有10个或更多的乳酸单元的疏水性嵌段链; 具有至少10个或更多的乳酸单元的疏水性聚合物A2; 和/或标记的聚合物B，其包含至少10个或更多的乳酸单元和标记基团。