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1. 发明授权

US09278075B2 Particle composition and pharmaceutical composition using particle composition 有权
标题翻译：使用颗粒组成的颗粒组成和药物组成
公开(公告)号：US09278075B2
公开(公告)日：2016-03-08
申请号：US13979546
申请日：2012-01-16
申请人： Kazunori Kataoka , Ronald James Christie , Nobuhiro Nishiyama , Kanjiro Miyata , Shigeto Fukushima , Yu Matsumoto , Takahiro Nomoto , Yasuki Kato
发明人： Kazunori Kataoka , Ronald James Christie , Nobuhiro Nishiyama , Kanjiro Miyata , Shigeto Fukushima , Yu Matsumoto , Takahiro Nomoto , Yasuki Kato
IPC分类号： A61K9/50 , A61K38/19 , A61K31/713 , A61K31/711 , A61K9/107 , A61K47/48
CPC分类号： A61K9/5031 , A61K9/107 , A61K31/711 , A61K31/713 , A61K38/193 , A61K47/60 , A61K47/6455
摘要： A composition of matter for use in encapsulating a drug is expressed by formula (1) or formula (2): wherein R1 and R2 are each independently a hydrogen atom or a substituted or unsubstituted, linear or branched alkyl group having 1 to 12 carbon atoms; A is a hydrophilic polymer chain; L1 and L3 are each a linking group; B is a cation-containing group; R3 is a side chain of an amino acid; z is an integer of 5 to 500; x is an integer of 40% or more of z; y is 0 or a positive integer; z-x-y is 0 or a positive integer; p is an integer of 1 to 10; and q is an integer of 1 to 10.
摘要翻译：用于包封药物的物质组合物由式（1）或式（2）表示：其中R 1和R 2各自独立地为氢原子或具有1至12个碳原子的取代或未取代的直链或支链烷基 ; A是亲水性聚合物链; L1和L3各自是连接基团; B是含阳离子基团; R3是氨基酸的侧链; z为5〜500的整数。 x是z的40％以上的整数; y为0或正整数; z-x-y为0或正整数; p为1〜10的整数。 q为1〜10的整数。

2. 发明申请

US20140017328A1 PARTICLE COMPOSITION AND PHARMACEUTICAL COMPOSITION USING PARTICLE COMPOSITION 有权
标题翻译：颗粒组合物和使用颗粒组合物的药物组合物
公开(公告)号：US20140017328A1
公开(公告)日：2014-01-16
申请号：US13979546
申请日：2012-01-16
申请人： Kazunori Kataoka , Ronald James Christie , Nobuhiro Nishiyama , Kanjiro Miyata , Shigeto Fukushima , Yu Matsumoto , Takahiro Nomoto , Yasuki Kato
发明人： Kazunori Kataoka , Ronald James Christie , Nobuhiro Nishiyama , Kanjiro Miyata , Shigeto Fukushima , Yu Matsumoto , Takahiro Nomoto , Yasuki Kato
IPC分类号： A61K9/50 , A61K38/19 , A61K31/713
CPC分类号： A61K9/5031 , A61K9/107 , A61K31/711 , A61K31/713 , A61K38/193 , A61K47/60 , A61K47/6455
摘要： A composition of matter for use in encapsulating a drug is expressed by formula (1) or formula (2): wherein R1 and R2 are each independently a hydrogen atom or a substituted or unsubstituted, linear or branched alkyl group having 1 to 12 carbon atoms; A is a hydrophilic polymer chain; L1 and L3 are each a linking group; B is a cation-containing group; R3 is a side chain of an amino acid; z is an integer of 5 to 500; x is an integer of 40% or more of z; y is 0 or a positive integer; z-x-y is 0 or a positive integer; p is an integer of 1 to 10; and q is an integer of 1 to 10.
摘要翻译：用于包封药物的物质组合物由式（1）或式（2）表示：其中R 1和R 2各自独立地为氢原子或具有1至12个碳原子的取代或未取代的直链或支链烷基 ; A是亲水性聚合物链; L1和L3各自是连接基团; B是含阳离子基团; R3是氨基酸的侧链; z为5〜500的整数。 x是z的40％以上的整数; y为0或正整数; z-x-y为0或正整数; p为1〜10的整数。 q为1〜10的整数。

3. 发明授权

US08853167B2 Short-chain cationic polyamino acid and use thereof 有权
标题翻译：短链阳离子聚氨基酸及其用途
公开(公告)号：US08853167B2
公开(公告)日：2014-10-07
申请号：US13258663
申请日：2011-02-23
申请人： Yasuki Kato , Atsushi Ishii , Naoya Shibata , Tatsuyuki Hayashi , Kazunori Kataoka , Kanjiro Miyata , Nobuhiro Nishiyama
发明人： Yasuki Kato , Atsushi Ishii , Naoya Shibata , Tatsuyuki Hayashi , Kazunori Kataoka , Kanjiro Miyata , Nobuhiro Nishiyama
IPC分类号： A61K47/48 , C08G69/10 , C12N15/11
CPC分类号： C08G69/10 , A61K47/60 , A61K47/6455 , C12N15/111 , C12N2310/14 , C12N2320/32
摘要： The present invention provides a cationic polyamino acid suitable for a carrier that can form a stable complex with a nucleic acid under a physiological condition and release the nucleic acid in cells suitably. The cationic polyamino acid can associate with a nucleic acid and includes a cationic amino acid residue having a cationic group in a side chain and a hydrophobic amino acid residue having a hydrophobic group in a side chain. The cationic polyamino acid includes 1 to 20 units of the cationic amino acid residue and is represented by the following formula (1). The meaning of each symbol in the formula is as shown in the description.
摘要翻译：本发明提供一种适用于可在生理条件下与核酸形成稳定复合物的载体的阳离子聚氨基酸，并适当地释放细胞中的核酸。阳离子聚氨基酸可以与核酸结合，并且包括在侧链中具有阳离子基团的阳离子氨基酸残基和在侧链中具有疏水基团的疏水性氨基酸残基。阳离子聚氨基酸包含1〜20个单元的阳离子氨基酸残基，由下式（1）表示。公式中每个符号的含义如说明书所示。

4. 发明申请

US20110052917A1 COPOLYMER INCLUDING UNCHARGED HYDROPHILIC BLOCK AND CATIONIC POLYAMINO ACID BLOCK HAVING HYDROPHOBIC GROUP IN PART OF SIDE CHAINS, AND USE THEREOF 有权
标题翻译：共聚物包括在侧链部分的疏水性嵌段和阳离子聚氨酯嵌段，并使用它们
公开(公告)号：US20110052917A1
公开(公告)日：2011-03-03
申请号：US12922116
申请日：2009-03-06
申请人： Kazunori Kataoka , Nobuhiro Nishiyama , Atsushi Ishii , Yasuki Kato , Kanjiro Miyata , Hyunjin Kim , Hiroyasu Takemoto
发明人： Kazunori Kataoka , Nobuhiro Nishiyama , Atsushi Ishii , Yasuki Kato , Kanjiro Miyata , Hyunjin Kim , Hiroyasu Takemoto
IPC分类号： B32B27/00 , C08G69/48 , B82Y5/00
CPC分类号： C08G69/10 , C08G81/00 , Y10T428/2982
摘要： The present invention relates to a block copolymer containing an uncharged hydrophilic polymer chain block and a cationic polyamino acid chain block, wherein the hydrophilic polymer chain block is covalently bound to one end of the main chain of the polyamino acid chain block, and the hydrophobic group is covalently bound to the side chains of not less than 10% and not greater than 70% of amino acid repeating units in the polyamino acid chain block. This block copolymer forms a stable aggregate with siRNA, a small-molecule nucleic acid, under a physiological condition.
摘要翻译：本发明涉及含有不带电荷的亲水性聚合物链段和阳离子聚氨基酸链嵌段的嵌段共聚物，其中亲水性聚合物链嵌段共价键合到聚氨基酸链嵌段的主链的一端，疏水基与聚氨基酸链嵌段中氨基酸重复单元的侧链共价结合不少于10％且不大于70％。该嵌段共聚物在生理条件下与siRNA（小分子核酸）形成稳定的聚集体。

5. 发明授权

US08431545B2 Copolymer including uncharged hydrophilic block and cationic polyamino acid block having hydrophobic group in part of side chains, and use thereof 有权
标题翻译：包括不带电荷的亲水嵌段和在一部分侧链具有疏水基团的阳离子聚氨基酸嵌段的共聚物及其用途
公开(公告)号：US08431545B2
公开(公告)日：2013-04-30
申请号：US12922116
申请日：2009-03-06
申请人： Kazunori Kataoka , Nobuhiro Nishiyama , Atsushi Ishii , Yasuki Kato , Kanjiro Miyata , Hyunjin Kim , Hiroyasu Takemoto
发明人： Kazunori Kataoka , Nobuhiro Nishiyama , Atsushi Ishii , Yasuki Kato , Kanjiro Miyata , Hyunjin Kim , Hiroyasu Takemoto
IPC分类号： A61K48/00 , A61K38/00 , A61K47/00 , A61K9/127 , A61K9/14 , A61P35/00 , A01N25/00
CPC分类号： C08G69/10 , C08G81/00 , Y10T428/2982
摘要： The present invention relates to a block copolymer containing an uncharged hydrophilic polymer chain block and a cationic polyamino acid chain block, wherein the hydrophilic polymer chain block is covalently bound to one end of the main chain of the polyamino acid chain block, and the hydrophobic group is covalently bound to the side chains of not less than 10% and not greater than 70% of amino acid repeating units in the polyamino acid chain block. This block copolymer forms a stable aggregate with siRNA, a small-molecule nucleic acid, under a physiological condition.
摘要翻译：本发明涉及含有不带电荷的亲水性聚合物链段和阳离子聚氨基酸链嵌段的嵌段共聚物，其中亲水性聚合物链嵌段共价键合到聚氨基酸链嵌段的主链的一端，疏水基与聚氨基酸链嵌段中氨基酸重复单元的侧链共价结合不少于10％且不大于70％。该嵌段共聚物在生理条件下与siRNA（小分子核酸）形成稳定的聚集体。

6. 发明申请

US20120149649A1 SHORT-CHAIN CATIONIC POLYAMINO ACID AND USE THEREOF 有权
标题翻译：短链阳离子聚氨酯酸及其用途
公开(公告)号：US20120149649A1
公开(公告)日：2012-06-14
申请号：US13258663
申请日：2011-02-23
申请人： Yasuki Kato , Atsushi Ishii , Naoya Shibata , Tatsuyuki Hayashi , Kazunori Kataoka , Kanjiro Miyata , Nobuhiro Nishiyama
发明人： Yasuki Kato , Atsushi Ishii , Naoya Shibata , Tatsuyuki Hayashi , Kazunori Kataoka , Kanjiro Miyata , Nobuhiro Nishiyama
IPC分类号： A61K38/16 , C07K7/08 , A61P43/00 , A61K38/08 , A61K38/10 , C07K7/06 , C07K14/00
CPC分类号： C08G69/10 , A61K47/60 , A61K47/6455 , C12N15/111 , C12N2310/14 , C12N2320/32
摘要： The present invention provides a cationic polyamino acid suitable for a carrier that can form a stable complex with a nucleic acid under a physiological condition and release the nucleic acid in cells suitably. The cationic polyamino acid can associate with a nucleic acid and includes a cationic amino acid residue having a cationic group in a side chain and a hydrophobic amino acid residue having a hydrophobic group in a side chain. The cationic polyamino acid includes 1 to 20 units of the cationic amino acid residue and is represented by the following formula (1). The meaning of each symbol in the formula is as shown in the description.
摘要翻译：本发明提供一种适用于可在生理条件下与核酸形成稳定复合物的载体的阳离子聚氨基酸，并适当地释放细胞中的核酸。阳离子聚氨基酸可以与核酸结合，并且包括在侧链中具有阳离子基团的阳离子氨基酸残基和在侧链中具有疏水基团的疏水性氨基酸残基。阳离子聚氨基酸包含1〜20个单元的阳离子氨基酸残基，由下式（1）表示。公式中每个符号的含义如说明书所示。

7. 发明授权

US09198860B2 Particulate pharmaceutical composition 有权
标题翻译：颗粒状药物组成
公开(公告)号：US09198860B2
公开(公告)日：2015-12-01
申请号：US13122546
申请日：2011-02-14
申请人： Atsushi Ishii , Yasuki Kato
发明人： Atsushi Ishii , Yasuki Kato
IPC分类号： A61K9/14 , A61K31/7088 , A61K38/02 , A61K9/107 , A61K31/7084 , A61K9/16 , A61K9/19 , A61K47/24 , A61K47/34
CPC分类号： A61K9/1075 , A61K9/16 , A61K9/19 , A61K31/7084 , A61K31/713 , A61K47/24 , A61K47/34
摘要： The present invention provides a particulate pharmaceutical composition which has improved drug encapsulation stability and is suitable for a drug delivery system. The particulate pharmaceutical composition 1 contains: a plurality of block copolymer unit 2 arranged radially, each of which has a hydrophobic polymer-chain segment 2b, which is arranged radially inside, and a hydrophilic polymer-chain segment 2a, which is arranged radially outside; a drug 4, which includes a biomacromolecule; and a charged lipid 3, which has an electrical charge opposite to that of the drug 4; wherein the charged lipid 3 is being attracted to the hydrophobic polymer-chain segment 2b, and the drug 3 is positioned radially inside the hydrophobic polymer-chain segment 2b. The pharmaceutical composition 1 can effectively prevent the drug 4 from disengaging from the particle.
摘要翻译：本发明提供了具有改善的药物包封稳定性并且适合于药物递送系统的颗粒药物组合物。颗粒状药物组合物1包含：径向配置的多个嵌段共聚物单元2，其各自具有径向配置的疏水性聚合物链段2b和位于径向外侧的亲水性聚合物链段2a; 包括生物大分子的药物4; 和带电荷的脂质3，其具有与药物4的电荷相反的电荷; 其中带电脂质3被吸引到疏水聚合物链段2b，并且药物3位于疏水性聚合物链段2b的径向内侧。药物组合物1可以有效地防止药物4与粒子分离。

8. 发明授权

US07799860B2 Composition improved in the solubility or oral absorbability 有权
标题翻译：组合物的溶解度或口服吸收性提高
公开(公告)号：US07799860B2
公开(公告)日：2010-09-21
申请号：US11544320
申请日：2006-10-06
申请人： Jun Sugishita , Makoto Kigoshi , Setsuko Yano , Hideki Morita , Yasuki Kato
发明人： Jun Sugishita , Makoto Kigoshi , Setsuko Yano , Hideki Morita , Yasuki Kato
IPC分类号： B01D11/02
CPC分类号： A61K31/56 , A61K9/145 , A61K9/146 , A61K9/1617 , A61K9/1623 , A61K9/1652 , A61K9/1682 , A61K31/122 , A61K31/335 , A61K31/522
摘要： An object of the present invention is to provide a composition improved in the solubility or oral absorbability.The present invention provides a composition which comprises three components of a slightly water-soluble component, a surfactant and a hydrophilic polymer, and is obtainable by wet granulation in the presence of water.
摘要翻译：本发明的目的是提供改善溶解性或口服吸收性的组合物。本发明提供一种组合物，其包含微溶于水的组分，表面活性剂和亲水性聚合物的三种组分，并且可通过在水存在下通过湿法制粒获得。

9. 发明申请

US20080226704A1 Method of Producing Coated Fine Particles 审中-公开
标题翻译：生产涂层微粒的方法
公开(公告)号：US20080226704A1
公开(公告)日：2008-09-18
申请号：US10593723
申请日：2005-03-23
申请人： Makoto Kigoshi , Nobuhiro Yagi , Yasuki Kato
发明人： Makoto Kigoshi , Nobuhiro Yagi , Yasuki Kato
IPC分类号： A61K9/127 , B05D7/00 , B32B5/16 , A61K9/50
CPC分类号： B01J13/02 , Y10T428/2989
摘要： The present invention provides a method of producing coated fine particles in which core fine particles is coated with a coating layer, which comprises the steps of preparing a liquid (liquid A) containing a polar organic solvent in which core fine particles are dispersed and a component constituting a coating layer is dissolved; preparing a liquid (liquid B) which is miscible with the liquid A and does not contain a polar organic solvent or contains a polar organic solvent in a ratio lower than that in the liquid A; and letting the liquid A flow from at least one inlet of a device for producing coated fine particles equipped with an in-line mixing means having two or more inlets and one or more outlet(s) and letting the liquid B flow from at least one remaining inlet to mix the liquids thereby coating the core fine particles with the coating layer.
摘要翻译：本发明提供一种制备其中芯细颗粒涂覆有涂层的涂覆微粒的方法，该方法包括以下步骤：制备包含其中分散芯细颗粒的极性有机溶剂的液体（液体A）和组分构成涂层溶解; 制备与液体A混溶并且不含极性有机溶剂或含有比液体A中的比例低的极性有机溶剂的液体（液体B）; 并且使液体A从用于生产包含具有两个或更多个入口和一个或多个出口的直列混合装置的涂覆微粒的装置的至少一个入口流出并使液体B从至少一个流出剩余的入口混合液体，从而涂覆核心微粒与涂层。

10. 发明申请

US20080171090A1 Method Of Producing Coated Fine Particles 审中-公开
标题翻译：生产涂层微粒的方法
公开(公告)号：US20080171090A1
公开(公告)日：2008-07-17
申请号：US11883165
申请日：2006-01-27
申请人： Nobuhiro Yagi , Takuya Tokuda , Masashi Nakakura , Yasuki Kato
发明人： Nobuhiro Yagi , Takuya Tokuda , Masashi Nakakura , Yasuki Kato
IPC分类号： A61K9/14 , A61J3/00 , A61P35/00 , A61P29/00 , B32B1/00
CPC分类号： A61K9/5123 , A61K9/1075 , A61K9/5192 , A61K31/7088 , B01J13/04 , Y10T428/2991
摘要： An object of the present invention is to provide a method for easily producing coated fine particles in which core fine particles are coated with a coating layer component, etc. There are provided a method of producing coated fine particles comprising core fine particles coated with a coating layer component, comprising the steps of dispersing the core fine particles and the coating layer component(s) in a liquid and the process of coating the core fine particles with the coating layer component, wherein the liquid contains a polar organic solvent in which the coating layer component(s) is soluble, and the concentration of the polar organic solvent is such that the core fine particles is not dissolved and the coating layer component(s) can be in the dispersed state in the liquid, and the like.
摘要翻译：本发明的目的是提供一种容易地生产其中芯细颗粒涂覆有涂层组分等的涂覆微粒的方法。提供了一种制备涂覆微粒的方法，其包括涂覆有涂层的芯细颗粒包括以下步骤：将芯细颗粒和涂层组分分散在液体中，以及用芯层细颗粒涂覆涂层组分的方法，其中液体含有极性有机溶剂，其中涂层层组分是可溶的，并且极性有机溶剂的浓度使得芯细颗粒不溶解，并且涂层组分可以在液体中处于分散状态等。

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