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1. 发明公开

EP3150195A4 AGENT FOR EXTERNAL USE ON SKIN AND AGENT FOR REDUCING SKIN IRRITATION 有权
公开(公告)号：EP3150195A4
公开(公告)日：2018-01-10
申请号：EP15795860
申请日：2015-05-21
申请人： SHIMADZU CORP
发明人： SUZUKI KENICHI , NAKAGAWA HARUKI , YAMAKITA YOSHIHIRO , OZEKI EIICHI , KAWABE TAKASHI , MATSUTANI ERI
IPC分类号： A61K9/107 , A61K9/50 , A61K31/47 , A61K47/34 , A61P3/06
CPC分类号： A61K47/34 , A61K9/0014 , A61K9/107 , A61K9/1075 , A61K9/50 , A61K31/13 , A61K31/325 , A61K31/47 , C08G63/912 , C08G2230/00
摘要： Provided is a skin external preparation including a drug and nanometer-size molecular assemblies. The molecular assemblies contain an amphiphilic block copolymer having a hydrophilic block chain including a sarcosine-derived structural unit and a hydrophobic block chain including a hydroxy acid-derived structural unit. The skin external preparation according to the present invention may reduce skin irritation caused by the drug, be very safe, and have excellent pharmacological effects, even when a drug that is generally difficult to be transdermally administered due to its strong skin irritation is contained therein.

2. 发明公开

EP3127943A4 PROCESS FOR PRODUCING NANOPARTICLES 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG VON NANOPARTIKELN
公开(公告)号：EP3127943A4
公开(公告)日：2017-09-27
申请号：EP15773129
申请日：2015-03-25
申请人： SHIMADZU CORP
发明人： KAWABE TAKASHI , OZEKI EIICHI
IPC分类号： C08J3/14 , A61K9/14 , A61K47/30 , A61K49/00 , B01J19/00 , B82Y5/00 , B82Y40/00
CPC分类号： A61K9/5192 , A61K9/5153 , A61K49/126 , A61K49/1824 , A61K51/06 , A61K51/1262 , B01J19/0093 , B01J2219/00783 , B01J2219/00873 , B01J2219/00889 , B01J2219/00894 , B01J2219/00903 , B01J2219/00954 , B01J2219/00961 , B01J2219/0097 , B01J2219/00986 , B82Y5/00 , B82Y40/00 , C08G69/44 , C08J3/07 , C08J3/12 , C08J2353/00 , C08J2377/12
摘要： Provided is a method for producing a nanoparticle having a uniform particle diameter. A method for producing a nanoparticle comprising an amphiphilic block polymer, the method comprising: with use of a nanoparticle production device that includes: a polymer solution supply channel Cp; an aqueous liquid supply channel Cw1, Cw2; a junction J of the channels; a nanoparticle formation channel Cn; and a nanoparticle-containing liquid outlet On, supplying a solution of a polymer and an aqueous liquid to the junction J; forming a nanoparticle while bringing a laminar flow of the polymer solution and a laminar flow of the aqueous liquid into contact with each other; obtaining a liquid containing the formed nanoparticle from the nanoparticle-containing liquid outlet; and controlling a particle diameter of the nanoparticle by measuring a statistic of the particle diameter of the formed nanoparticle in real time, and by controlling at least one of an amount of the polymer solution supplied to the junction and an amount of the aqueous liquid supplied to the junction such that the statistic becomes a desired value.
摘要翻译：提供一种粒径均匀的纳米粒子的制造方法。一种用于生产包含两亲嵌段聚合物的纳米粒子的方法，所述方法包括：使用纳米粒子生产装置，所述纳米粒子生产装置包括：聚合物溶液供应通道Cp; 含水液体供应通道Cw1，Cw2; 通道的J点; 纳米颗粒形成通道Cn; 和含纳米粒子的液体出口1n，将聚合物和含水液体的溶液供应到接合部J; 在使聚合物溶液的层流与含水液体的层流彼此接触的同时形成纳米粒子; 从含纳米粒子的液体出口获得含有所形成的纳米粒子的液体; 以及通过实时测量所形成的纳米粒子的粒径统计值并且通过控制供应到所述接合处的所述聚合物溶液的量和供应到所述纳米粒子的所述水性液体的量中的至少一个来控制所述纳米粒子的粒径，该联合使得统计成为期望值。

3. 发明公开

EP2682131A4 SWITCHING-TYPE FLUORESCENT NANOPARTICLE PROBE, AND FLUORESCENT MOLECULAR IMAGING METHOD USING SAME 审中-公开
标题翻译：具有荧光纳米粒子的可切换探针及其插图荧光分子的方法
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

4. 发明公开

EP2609935A4 SWITCHING FLUORESCENT NANOPARTICLE PROBE AND FLUORESCENT PARTICLE IMAGING METHOD USING SAME 审中-公开
标题翻译：切换为说明荧光纳米颗粒荧光纳米粒子探针和方法THAT
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。

5. 发明公开

EP2893924A4 MOLECULAR ASSEMBLY USING BRANCHED AMPHIPHILIC BLOCK POLYMER, AND DRUG TRANSPORTATION SYSTEM 有权
标题翻译：分子排列与支链双亲嵌段共聚物和主动运输系统
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.

6. 发明公开

EP2745850A4 NANO-PARTICLES FOR INTERNAL RADIATION THERAPY OF INVOLVED AREA, AND THERAPY SYSTEM 失效
标题翻译：内部放射治疗设备纳米疫区和
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.

7. 发明公开

EP2725053A4 BRANCHED AMPHIPATHIC BLOCK POLYMER AND MOLECULAR AGGREGATE AND DRUG DELIVERY SYSTEM USING SAME 有权
标题翻译：两亲性支化嵌段聚合物分子聚集体和药监系统为了
公开(公告)号：EP2725053A4
公开(公告)日：2014-10-29
申请号：EP12802877
申请日：2012-06-22
申请人： SHIMADZU CORP , UNIV KYOTO
发明人： OZEKI EIICHI , KIMURA SHUNSAKU , MAKINO AKIRA
IPC分类号： C08G81/00 , A61K9/10 , A61K9/51 , A61K47/34 , A61K49/00 , A61K51/06 , B82Y5/00 , C08G83/00 , C08L67/04
CPC分类号： A61K49/0054 , A61K9/1075 , A61K9/5153 , A61K47/34 , A61K47/641 , A61K49/0002 , A61K49/0034 , A61K49/0082 , A61K49/124 , B82Y40/00 , C08G69/44 , C08G83/005 , C08G83/008 , C08L101/005 , Y10S424/16 , Y10T428/2982

8. 发明公开

EP2305214A4 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
标题翻译：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：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.

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