公开(公告)号：EP2609935B1

公开(公告)日：2018-10-10

申请号：EP11819780.5

申请日：2011-08-08

申请人： Shimadzu Corporation ,  Kyoto University

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

IPC分类号： A61K49/00 ,  A61K9/51 ,  A61K47/34 ,  A61K47/42

CPC分类号： A61K49/0089 ,  A61K49/0032 ,  A61K49/0093 ,  Y10S977/773 ,  Y10S977/927

摘要： The present invention provides a novel fluorescent nanoparticle imaging probe having a switching function (a function to quench a fluorescent dye during nanoparticle preparation, and emit fluorescence during imaging). A switching 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 molecular 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 cyanine compound represented by the formula (I): and two or more molecules of the fluorescent dye are encapsulated in the single molecular assembly.

公开(公告)号：EP2609935A1

公开(公告)日：2013-07-03

申请号：EP11819780.5

申请日：2011-08-08

申请人： Shimadzu Corporation ,  Kyoto University

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

IPC分类号： A61K49/00 ,  A61K9/51 ,  A61K47/34 ,  A61K47/42

CPC分类号： A61K49/0089 ,  A61K49/0032 ,  A61K49/0093 ,  Y10S977/773 ,  Y10S977/927

摘要： The present invention provides a novel fluorescent nanoparticle imaging probe having a switching function (a function to quench a fluorescent dye during nanoparticle preparation, and emit fluorescence during imaging). A switching 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 molecular 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 cyanine compound represented by the formula (I):

and two or more molecules of the fluorescent dye are encapsulated in the single molecular assembly.

公开(公告)号：EP2682131B1

公开(公告)日：2020-05-13

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 ,  A61K47/50 ,  A61K41/00

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