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公开(公告)号：US20120053295A1
公开(公告)日：2012-03-01
申请号：US13147319
申请日：2010-02-15
申请人： Kazunori Kataoka , Shourong Wu , Takehiko Ishii , HyunJin Kim , Kanjiro Miyata , Nobuhiro Nishiyama
发明人： Kazunori Kataoka , Shourong Wu , Takehiko Ishii , HyunJin Kim , Kanjiro Miyata , Nobuhiro Nishiyama
CPC分类号： A61K48/0041 , A61K9/5192 , A61K31/7088 , A61K47/6455 , C07K14/001 , C07K14/003 , C08G69/08 , C08G69/10 , C08G69/48 , C12N15/111 , C12N2310/3181 , C12N2310/3513 , C12N2320/32
摘要： The present invention provides an efficient delivery system for a nucleic acid, more specifically, a cationic poly(amino acid) that has a side chain having a plurality of different amine functional groups in a moiety including a cationic group and that has a hydrophobic group introduced into part of the side chain, and a polyion complex (PIC) of the poly(amino acid) and an oligo- or polynucleotide.
摘要翻译： 本发明提供了一种用于核酸的有效递送系统，更具体地说，一种阳离子聚（氨基酸），该阳离子聚（氨基酸）在包括阳离子基团的部分中具有多个不同胺官能团的侧链，并且具有引入疏水基团 成为侧链的一部分，以及聚（氨基酸）的聚离子复合物（PIC）和寡核苷酸或多核苷酸。
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公开(公告)号：US08546487B2
公开(公告)日：2013-10-01
申请号：US13147319
申请日：2010-02-15
申请人： Kazunori Kataoka , Shourong Wu , Takehiko Ishii , HyunJin Kim , Kanjiro Miyata , Nobuhiro Nishiyama
发明人： Kazunori Kataoka , Shourong Wu , Takehiko Ishii , HyunJin Kim , Kanjiro Miyata , Nobuhiro Nishiyama
IPC分类号： A61K47/48 , C08F283/04 , A01N25/26
CPC分类号： A61K48/0041 , A61K9/5192 , A61K31/7088 , A61K47/6455 , C07K14/001 , C07K14/003 , C08G69/08 , C08G69/10 , C08G69/48 , C12N15/111 , C12N2310/3181 , C12N2310/3513 , C12N2320/32
摘要： The present invention provides an efficient delivery system for a nucleic acid, more specifically, a cationic poly(amino acid) that has a side chain having a plurality of different amine functional groups in a moiety including a cationic group and that has a hydrophobic group introduced into part of the side chain, and a polyion complex (PIC) of the poly(amino acid) and an oligo- or polynucleotide.
摘要翻译： 本发明提供了一种用于核酸的有效递送系统，更具体地说，一种阳离子聚（氨基酸），该阳离子聚（氨基酸）在包括阳离子基团的部分中具有多个不同胺官能团的侧链，并且具有引入疏水基团 成为侧链的一部分，以及聚（氨基酸）的聚离子复合物（PIC）和寡核苷酸或多核苷酸。
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3.发明授权Copolymer including uncharged hydrophilic block and cationic polyamino acid block having hydrophobic group in part of side chains, and use thereof 有权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
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。
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公开(公告)号：US20110060123A1
公开(公告)日：2011-03-10
申请号：US12990386
申请日：2009-04-30
申请人： Kazunori Kataoka , Yan Lee , Nobuhiro Nishiyama , Kanjiro Miyata , Makoto Oba , Shigehiro Hiki , Mai Sanjo , HyunJin Kim
发明人： Kazunori Kataoka , Yan Lee , Nobuhiro Nishiyama , Kanjiro Miyata , Makoto Oba , Shigehiro Hiki , Mai Sanjo , HyunJin Kim
IPC分类号： C07K14/00
CPC分类号： C08G69/48 , A61K31/7084 , A61K31/785 , A61K48/0041 , C08G69/10 , C08G69/40 , C12N15/111 , C12N15/88 , C12N2310/14 , C12N2320/32
摘要： Disclosed is a polymer composite (polyplex) that contains nucleic acid, a cationic polymer, and an anionic polymer. The anionic polymer covers the surface of the composite comprising the cationic polymer and nucleic acid, has a negative charge at neutral pH, and can change so as to have a positive charge at mildly acidic pH.
摘要翻译： 公开了含有核酸，阳离子聚合物和阴离子聚合物的聚合物复合物（polyplex）。 阴离子聚合物覆盖包含阳离子聚合物和核酸的复合物的表面，在中性pH下具有负电荷，并且可以改变以在弱酸性pH下具有正电荷。
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5.发明申请公开(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
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。
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公开(公告)号：US08906503B2
公开(公告)日：2014-12-09
申请号：US13320314
申请日：2010-05-13
IPC分类号： B32B5/16 , B32B9/00 , B32B15/02 , B32B17/02 , B32B19/00 , B32B21/02 , B32B23/02 , B32B27/02 , C08G69/10 , A61K47/48 , A61K9/51 , C08G69/40 , C08L77/06 , A61K31/713 , C08J3/12 , C08L71/02 , C08L77/04 , C12N15/87 , C08G69/48 , A61K9/19
CPC分类号： A61K9/19 , A61K9/5123 , A61K9/5146 , A61K9/5192 , A61K31/713 , A61K47/62 , A61K47/6929 , A61K47/6935 , C08G69/10 , C08G69/40 , C08G69/48 , C08J3/12 , C08J2371/02 , C08L71/02 , C08L77/04 , C08L77/06 , C12N15/87 , Y10S977/788 , Y10S977/84 , Y10T428/2982 , C08L2666/20 , C08L2666/22
摘要： Fine particles of crystalline polyol are provided having a cationic polymer fixed on the crystal surfaces. These fine particles can stably carry an anionically charged compound on their surfaces.
摘要翻译： 提供结晶多元醇的细颗粒，其具有固定在晶体表面上的阳离子聚合物。 这些细颗粒可以在其表面上稳定地携带带阴离子的化合物。
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公开(公告)号：US20120064346A1
公开(公告)日：2012-03-15
申请号：US13320314
申请日：2010-05-13
CPC分类号： A61K9/19 , A61K9/5123 , A61K9/5146 , A61K9/5192 , A61K31/713 , A61K47/62 , A61K47/6929 , A61K47/6935 , C08G69/10 , C08G69/40 , C08G69/48 , C08J3/12 , C08J2371/02 , C08L71/02 , C08L77/04 , C08L77/06 , C12N15/87 , Y10S977/788 , Y10S977/84 , Y10T428/2982 , C08L2666/20 , C08L2666/22
摘要： Fine particles of crystalline polyol are provided having a cationic polymer fixed on the crystal surfaces. These fine particles can stably carry an anionically charged compound on their surfaces.
摘要翻译： 提供结晶多元醇的细颗粒，其具有固定在晶体表面上的阳离子聚合物。 这些细颗粒可以在其表面上稳定地携带带阴离子的化合物。
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8.发明授权Anionic polymer, polyion complex and ternary polymer composite using anionic polymer, and pharmaceutical composition 有权阴离子聚合物，聚离子络合物和三元聚合物复合材料使用阴离子聚合物，以及药物组成公开(公告)号：US08450282B2
公开(公告)日：2013-05-28
申请号：US13386554
申请日：2010-07-23
申请人： Kazunori Kataoka , Atsushi Ishii , Hiroyasu Takemoto , Masataka Nakanishi , Nobuhiro Nishiyama , Kanjiro Miyata
发明人： Kazunori Kataoka , Atsushi Ishii , Hiroyasu Takemoto , Masataka Nakanishi , Nobuhiro Nishiyama , Kanjiro Miyata
IPC分类号： A61K38/00 , C07K14/72 , C07K14/705
CPC分类号： C08L79/02 , C08G69/10 , C08G73/0206 , C08G73/028 , C08L77/04
摘要： There are provided an anionic polymer, a polyion complex, and a ternary polymer composite, each of which is stable in a biological environment and is capable of realizing small RNA delivery without causing any undesired immune response. An anionic polymer according to an embodiment of the invention includes: a main chain which includes repeating units having carboxyl groups; and a side chain which is linked with part of the carboxyl groups in the main chain and is represented by the following formula: -A-B—X where: A represents a residue having one or more aminoethyl bonds; B represents an in vivo cleavable bond; and X represents a small RNA. A polyion complex according to an embodiment of the invention includes the anionic polymer as described above and a cationic polymer. A ternary polymer composite according to an embodiment of the invention includes the polyion complex as described above and a charge conversional polymer.
摘要翻译： 提供阴离子聚合物，聚离子络合物和三元聚合物复合材料，其中每一种在生物环境中都是稳定的并且能够实现小的RNA递送而不引起任何不期望的免疫应答。 根据本发明实施方案的阴离子聚合物包括：主链，其包含具有羧基的重复单元; 和与主链中部分羧基连接并由下式表示的侧链：-A-B-X其中：A表示具有一个或多个氨基乙基的残基; B代表体内可剪切键; X表示小RNA。 根据本发明实施方案的聚离子络合物包括如上所述的阴离子聚合物和阳离子聚合物。 根据本发明实施方案的三元聚合物复合物包括如上所述的聚离子络合物和电荷转移聚合物。
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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
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。
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10.发明授权公开(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。
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