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    Compound modified with glycerol derivative
    1.
    发明申请
    Compound modified with glycerol derivative 失效
    用甘油衍生物修饰的化合物

    公开(公告)号：US20060280784A1

    公开(公告)日：2006-12-14

    申请号：US10570623

    申请日：2004-09-03

    申请人： Hisao Nemoto ,  Masahiro Yamauchi ,  Hiroko Kusano ,  Yasuki Kato ,  Motoo Yamasaki ,  Toshiyuki Suzawa

    发明人： Hisao Nemoto ,  Masahiro Yamauchi ,  Hiroko Kusano ,  Yasuki Kato ,  Motoo Yamasaki ,  Toshiyuki Suzawa

    IPC分类号： A61K9/127 ,  A61K31/685 ,  C07F9/02

    CPC分类号： C07D207/452 ,  A61K47/00 ,  A61K47/54 ,  A61K47/6911 ,  B82Y5/00 ,  C07C323/60 ,  C07F9/10 ,  C07K5/0202

    摘要： Objects of the present invention are to provide a compound which is useful as a surface modifier for producing a drug carrier or the like, or a salt thereof; a fine particle comprising the same; and the like. The present invention provides a compound in which a substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, is modified with a glycerol derivative represented by the following formula (1): wherein R represents a residue comprising a reactive group for the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance or for a spacer capable of binding the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, to R-X, or a group capable of being transformed into the reactive group; n represents an integer of 3 or more; and X represents a residue capable of having the following structure by n in number: directly or via the spacer, or a salt thereof; a fine particle comprising the same; and the like.

    摘要翻译： 本发明的目的是提供一种可用作生产药物载体等的表面改性剂或其盐的化合物; 包含该颗粒的细颗粒; 等等。 本发明提供一种化合物，其中选自由两亲物质和疏水性物质组成的组中的被改性物质用下式（1）表示的甘油衍生物进行改性：其中R表示残基 包括选自两亲物质和疏水性物质的待修饰物质的反应性基团或能够与被修饰物质结合的间隔基，其选自两亲物质 和疏水性物质，至RX或能够转化为反应性基团的基团; n表示3以上的整数， X表示可以直接或经由间隔基或其盐具有n数的以下结构的残基： 包含该颗粒的细颗粒; 等等。

    COMPOUND MODIFIED WITH GLYCEROL DERIVATIVE
    2.
    发明申请
    COMPOUND MODIFIED WITH GLYCEROL DERIVATIVE 审中-公开
    用甘油衍生物修饰的化合物

    公开(公告)号：US20100172967A1

    公开(公告)日：2010-07-08

    申请号：US12708714

    申请日：2010-02-19

    申请人： Hisao Nemoto ,  Masahiro Yamauchi ,  Hiroko Kusano ,  Yasuki Kato ,  Motoo Yamasaki ,  Toshiyuki Suzawa

    发明人： Hisao Nemoto ,  Masahiro Yamauchi ,  Hiroko Kusano ,  Yasuki Kato ,  Motoo Yamasaki ,  Toshiyuki Suzawa

    IPC分类号： A61K9/127 ,  C07C237/06 ,  C07F9/06 ,  C07F9/02 ,  C07K2/00 ,  A61K9/107

    CPC分类号： C07D207/452 ,  A61K47/00 ,  A61K47/54 ,  A61K47/6911 ,  B82Y5/00 ,  C07C323/60 ,  C07F9/10 ,  C07K5/0202

    摘要： Objects of the present invention are to provide a compound which is useful as a surface modifier for producing a drug carrier or the like, or a salt thereof; a fine particle comprising the same; and the like. The present invention provides a compound in which a substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, is modified with a glycerol derivative represented by the following formula (1): wherein R represents a residue comprising a reactive group for the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance or for a spacer capable of binding the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, to R—X, or a group capable of being transformed into the reactive group; n represents an integer of 3 or more; and X represents a residue capable of having the following structure by n in number: directly or via the spacer, or a salt thereof; a fine particle comprising the same; and the like.

    摘要翻译： 本发明的目的是提供一种可用作生产药物载体等的表面改性剂或其盐的化合物; 包含该颗粒的细颗粒; 等等。 本发明提供一种化合物，其中选自由两亲物质和疏水性物质组成的组中的被改性物质用下式（1）表示的甘油衍生物进行改性：其中R表示残基 包括选自两亲物质和疏水性物质的待修饰物质的反应性基团或能够与被修饰物质结合的间隔基，其选自两亲物质 和疏水性物质，R-X或能够转化为反应性基团的基团; n表示3以上的整数， X表示可以直接或经由间隔基或其盐具有n数的以下结构的残基： 包含该颗粒的细颗粒; 等等。

    Compound modified with glycerol derivative
    3.
    发明授权
    Compound modified with glycerol derivative 失效
    用甘油衍生物修饰的化合物

    公开(公告)号：US07696359B2

    公开(公告)日：2010-04-13

    申请号：US10570623

    申请日：2004-09-03

    申请人： Hisao Nemoto ,  Masahiro Yamauchi ,  Hiroko Kusano ,  Yasuki Kato ,  Motoo Yamasaki ,  Toshiyuki Suzawa

    发明人： Hisao Nemoto ,  Masahiro Yamauchi ,  Hiroko Kusano ,  Yasuki Kato ,  Motoo Yamasaki ,  Toshiyuki Suzawa

    IPC分类号： C07D207/46 ,  C07F9/09

    CPC分类号： C07D207/452 ,  A61K47/00 ,  A61K47/54 ,  A61K47/6911 ,  B82Y5/00 ,  C07C323/60 ,  C07F9/10 ,  C07K5/0202

    摘要： Objects of the present invention are to provide a compound which is useful as a surface modifier for producing a drug carrier or the like, or a salt thereof; a fine particle comprising the same; and the like. The present invention provides a compound in which a substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, is modified with a glycerol derivative represented by the following formula (1): wherein R represents a residue comprising a reactive group for the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance or for a spacer capable of binding the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, to R-X, or a group capable of being transformed into the reactive group; n represents an integer of 3 or more; and X represents a residue capable of having the following structure by n in number: directly or via the spacer, or a salt thereof; a fine particle comprising the same; and the like.

    摘要翻译： 本发明的目的是提供一种可用作生产药物载体等的表面改性剂或其盐的化合物; 包含该颗粒的细颗粒; 等等。 本发明提供一种化合物，其中选自由两亲物质和疏水性物质组成的组中的被改性物质用下式（1）表示的甘油衍生物进行改性：其中R表示残基 包括选自两亲物质和疏水性物质的待修饰物质的反应性基团或能够与被修饰物质结合的间隔基，其选自两亲物质 和疏水性物质，至RX或能够转化为反应性基团的基团; n表示3以上的整数， X表示可以直接或经由间隔基或其盐具有n数的以下结构的残基： 包含该颗粒的细颗粒; 等等。

    Medicinal preparations
    7.
    发明授权
    Medicinal preparations 失效
    药用制剂

    公开(公告)号：US07067618B1

    公开(公告)日：2006-06-27

    申请号：US09869049

    申请日：1999-12-24

    申请人： Yasuki Kato ,  Hiroko Kusano ,  Yuji Kawaguchi ,  Kunio Ito

    发明人： Yasuki Kato ,  Hiroko Kusano ,  Yuji Kawaguchi ,  Kunio Ito

    IPC分类号： C07K38/28 ,  C07K17/04 ,  C07K17/08 ,  A61K38/00 ,  A61K38/14

    CPC分类号： A61K47/62 ,  A61K47/54 ,  A61K47/549

    摘要： The present invention provides a pharmaceutical preparation comprising a compound which can be obtained by reacting a compound having a free amino group with a sugar having the reducing power. The preparation is capable of improving the in vivo durability of various compounds and releasing the compounds in response to changes in pH, and thus is useful for causing the compounds to act specifically on target parts.

    摘要翻译： 本发明提供一种药物制剂，其包含可通过具有游离氨基的化合物与具有还原力的糖反应而获得的化合物。 该制剂能够改善各种化合物的体内耐久性并响应于pH变化释放化合物，因此可用于使化合物特异性地作用于目标部位。

    Complex Particles and Coated Complex Particles
    8.
    发明申请
    Complex Particles and Coated Complex Particles 审中-公开
    复合颗粒和涂层复合颗粒

    公开(公告)号：US20090010999A1

    公开(公告)日：2009-01-08

    申请号：US10591827

    申请日：2005-03-10

    申请人： Masahiro Yamauchi ,  Yasuki Kato

    发明人： Masahiro Yamauchi ,  Yasuki Kato

    IPC分类号： A61K9/127 ,  A61K9/14 ,  A61K31/711 ,  A61K31/7105 ,  A61K31/7088

    CPC分类号： A61K9/1272 ,  A61K9/1271 ,  A61K31/7088 ,  A61K31/713

    摘要： The present invention provides, for example, a method of inhibiting aggregation of complex particles in which a drug is adhered to lead particles, characterized by containing a lipid derivative or a fatty acid derivative of one or more substance(s) selected from sugars, peptides, nucleic acids and water-soluble polymers or a surfactant in the lead particles. Further, it provides, for example, a method of producing the complex particles in which a nucleic acid as a drug or a drug is adhered to lead particles, comprising the step of dispersing or dissolving the nucleic acid as a drug or the drug and an adhesion-competitive agent so as to be contained in a liquid in which the lead particles containing a lipid derivative or a fatty acid derivative of one or more substance(s) selected from sugars, peptides, nucleic acids and water-soluble polymers or a surfactant are dispersed, thereby allowing the nucleic acid as a drug or the drug and the adhesion-competitive agent adhered to the lead particles.

    摘要翻译： 本发明提供了例如抑制药物粘附于铅粒子的复合粒子聚集的方法，其特征在于，含有选自糖，肽的一种或多种物质的脂质衍生物或脂肪酸衍生物 ，核酸和水溶性聚合物或铅颗粒中的表面活性剂。 此外，例如提供了将作为药物或药物的核酸与铅粒子附着的复合粒子的制造方法，其包括将核酸作为药物或药物分散或溶解的工序，以及 粘附竞争剂，以便包含在其中含有选自糖，肽，核酸和水溶性聚合物的一种或多种物质的脂质衍生物或脂肪酸衍生物的铅颗粒的液体中，或表面活性剂 从而允许作为药物或药物的核酸和附着于铅颗粒的粘附竞争性试剂。

    Composition for Suppressing Expression of Target Gene
    10.
    发明申请
    Composition for Suppressing Expression of Target Gene 审中-公开
    抑制靶基因表达的组成

    公开(公告)号：US20090011003A1

    公开(公告)日：2009-01-08

    申请号：US11883168

    申请日：2005-10-24

    申请人： Masahiro Yamauchi ,  Tsuneaki Tottori ,  Atsushi Ishihara ,  Nobuhiro Yagi ,  Yasuki Kato

    发明人： Masahiro Yamauchi ,  Tsuneaki Tottori ,  Atsushi Ishihara ,  Nobuhiro Yagi ,  Yasuki Kato

    IPC分类号： A61K9/127 ,  A61K31/7105 ,  A61K48/00

    CPC分类号： C12N15/1135 ,  A61K9/127 ,  A61K31/7105 ,  C12N2310/14

    摘要： The present invention has its object to provide a composition for suppressing the expression of a target gene and the like, and provides a composition, comprising an RNA-encapsulated liposome which comprises complex particles comprising as constituent components a lead particle and an RNA comprising a sequence consisting of 15 to 30 contiguous nucleotides of a target gene mRNA and a sequence complementary to the sequence, and a lipid membrane for coating the complex particles, wherein constituent components of the lipid membrane can be solved in a polar organic solvent, and wherein the polar organic solvent can be contained in a liquid at such a concentration that the constituent components of the lipid membrane are dispersible and the complex particles are dispersible, and the like.

    摘要翻译： 本发明的目的是提供抑制靶基因表达等的组合物，提供包含RNA包封的脂质体的组合物，其包含作为铅粒子的构成成分的复合粒子和包含序列的RNA 由靶基因mRNA的15〜30个连续核苷酸和与该序列互补的序列构成，以及用于涂布复合粒子的脂质膜，其中脂质膜的构成成分可以在极性有机溶剂中溶解，其中极性 有机溶剂可以以使得脂质膜的组成成分可分散并且复合颗粒可分散的浓度包含在液体中。