公开(公告)号：EP2682131A4

公开(公告)日：2014-09-17

申请号：EP12751966

申请日：2012-03-01

申请人： UNIV KYOTO ,  SHIMADZU CORP

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

公开(公告)号：EP2609935A4

公开(公告)日：2015-05-06

申请号：EP11819780

申请日：2011-08-08

申请人： SHIMADZU CORP ,  UNIV KYOTO

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.

摘要翻译： 本发明提供了具有开关功能（以猝灭的纳米颗粒制备过程中的荧光染料，和在成像期间发出荧光的函数）的新型荧光纳米颗粒成像探针。 一种开关荧光纳米颗粒探针，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; 和包封在分子组装荧光染料，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）疏水性嵌段链包含作为 到必要的疏水性结构单元，选自一种氨基酸单元和羟基羧酸单元，和（c）中选择的单元中的荧光染料是由式（I）表示的花青化合物：和的两个或多个分子 荧光染料被封装在单个分子组装。

公开(公告)号：EP2893924A4

公开(公告)日：2016-04-20

申请号：EP13836159

申请日：2013-09-03

申请人： SHIMADZU CORP ,  UNIV KYOTO

发明人： HARA ISAO ,  OZEKI EIICHI ,  KIMURA SHUNSAKU ,  MAKINO AKIRA

IPC分类号： A61K49/00 ,  A61K9/10 ,  A61K9/51 ,  A61K47/48

CPC分类号： A61K49/0054 ,  A61K9/5153 ,  A61K47/50 ,  A61K47/51 ,  A61K47/593 ,  A61K49/0034 ,  A61K49/0089 ,  A61K49/12 ,  A61K49/124 ,  A61K51/0404 ,  A61K51/06

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.

公开(公告)号：EP2745850A4

公开(公告)日：2015-04-29

申请号：EP12832548

申请日：2012-09-12

申请人： SHIMADZU CORP ,  UNIV KYOTO

发明人： TAKEUCHI ERI ,  HARA ISAO ,  YAMAHARA RYO ,  OZEKI EIICHI ,  KIMURA SHUNSAKU ,  KURIHARA KENSUKE

IPC分类号： A61K51/00 ,  A61B1/00 ,  A61B5/055 ,  A61B6/03 ,  A61B8/08 ,  A61K31/765 ,  A61N5/10 ,  A61P35/00 ,  G01T1/161

CPC分类号： A61K51/1244 ,  A61B5/055 ,  A61B5/061 ,  A61B5/0813 ,  A61B6/037 ,  A61B6/12 ,  A61B6/4258 ,  A61B6/485 ,  A61B6/508 ,  A61B8/085 ,  A61B18/0218 ,  A61B18/1477 ,  A61B18/1815 ,  A61B2018/0293 ,  A61B2018/1869 ,  A61K49/0054 ,  A61K49/0086 ,  A61K51/06 ,  A61K51/12 ,  A61K51/1237 ,  A61K2123/00 ,  A61N5/10 ,  A61N2005/1011 ,  A61N2005/1021 ,  A61N2005/1052 ,  A61N2005/1098

摘要： The present invention provides a therapeutic system that is widely applicable to general solid cancers, can achieve both a reduction in side effects of cancer therapy and suppression of cancer recurrence and metastasis, and requires no expensive drug such as an antibody; and a nanoparticle for internal radiation therapy. A system for internal radiation therapy of a vascular lesion site comprising: a device comprising a means for acquiring image data showing a position of a vascular lesion site, and a means for positioning a needle, which should be punctured into the vascular lesion site, at the vascular lesion site based on the image data; and a nanoparticle comprising an amphiphilic block polymer comprising a hydrophilic block having a sarcosine unit and a hydrophobic block having a lactic acid unit, and a substance labeled with a ²-ray emitting nuclide. The nanoparticle for internal radiation therapy.

公开(公告)号：EP2305214A4

公开(公告)日：2013-07-10

申请号：EP09758388

申请日：2009-06-04

申请人： SHIMADZU CORP

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.