公开(公告)号：EP2842546A1

公开(公告)日：2015-03-04

申请号：EP13782198.9

申请日：2013-04-30

申请人： The University of Tokyo ,  NanoCarrier Co., Ltd.

发明人： KATAOKA, Kazunori ,  MIYATA, Kanjiro ,  NISHIYAMA, Nobuhiro ,  OSADA, Kensuke ,  WATANABE, Sumiyo ,  FUKUSHIMA, Shigeto ,  CHAYA, Hiroyuki ,  TAKEMOTO, Hiroyasu ,  KATO, Yasuki

IPC分类号： A61K9/107 ,  A61K31/7088 ,  A61K47/34 ,  C12N15/09

CPC分类号： A61K31/713 ,  A61K9/0019 ,  A61K47/60 ,  A61K47/64 ,  A61K47/645 ,  A61K47/6455 ,  A61K48/00

摘要： According to the present invention, it is possible to improve the blood retention capability by a carrier for delivering a nucleic acid such as siRNA. A unit structure-type pharmaceutical composition of the present invention contains a block copolymer having a cationic polyamino acid segment and a hydrophilic polymer chain segment and a nucleic acid; the composition is electrically neutral by counterbalancing negative charge (s) of the nucleic acid with positive charge(s) of the cationic polyamino acid segment, and the nucleic acid is covered with the hydrophilic polymer chain segment.

摘要翻译： 根据本发明，可以提高用于输送siRNA等核酸的载体的保血能力。 本发明的单体结构型药物组合物含有具有阳离子性聚氨基酸链段和亲水性高分子链链段和核酸的嵌段共聚物， 该组合物通过用阳离子聚氨基酸片段的正电荷平衡核酸的负电荷而电中性，并且核酸被亲水性聚合物链段覆盖。

公开(公告)号：EP2305275B1

公开(公告)日：2013-07-10

申请号：EP09769989.6

申请日：2009-05-27

申请人： NanoCarrier Co., Ltd. ,  The University of Tokyo

发明人： KATAOKA, Kazunori ,  NISHIYAMA, Nobuhiro ,  TSUCHIYA, Chieko ,  HAYASHI, Tatsuyuki

IPC分类号： C08G69/10 ,  C08G69/40 ,  A61K9/00 ,  A61K47/48 ,  A61K9/107

CPC分类号： A61K47/488 ,  A61K9/0019 ,  A61K9/1075 ,  A61K47/60 ,  A61K47/6907 ,  C08G69/10 ,  C08G69/40 ,  C08G73/0233 ,  C08K5/0091

公开(公告)号：EP2397487A1

公开(公告)日：2011-12-21

申请号：EP11740552.2

申请日：2011-02-23

申请人： NanoCarrier Co., Ltd. ,  The University of Tokyo

发明人： KATO, Yasuki ,  ISHII, Atsushi ,  SHIBATA, Naoya ,  HAYASHI, Tatsuyuki ,  KATAOKA, Kazunori ,  MIYATA, Kanjiro ,  NISHIYAMA, Nobuhiro

IPC分类号： C07K4/00 ,  A61K31/7105 ,  A61K31/713 ,  A61K47/42 ,  A61K47/48 ,  A61K48/00 ,  C08G69/48

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： 本发明提供了适合于能够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。 阳离子聚氨基酸包括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。

公开(公告)号：EP1398635B1

公开(公告)日：2009-02-25

申请号：EP02730783.4

申请日：2002-05-30

申请人： Mitsubishi Kagaku Iatron, Inc. ,  NanoCarrier Co., Ltd.

发明人： KATAOKA, Kazunori ,  NAGASAKI, Yukio ,  SHIBATA, Naoya ,  HOSHINO, Nobuhiro MITSUBISHI KAGAKU IATRON, INC.

IPC分类号： G01N33/533 ,  G01N33/545

CPC分类号： G01N33/585 ,  Y10S525/902 ,  Y10T428/2998

公开(公告)号：EP2781536A1

公开(公告)日：2014-09-24

申请号：EP12850688.8

申请日：2012-11-19

申请人： The University of Tokyo ,  National University Corporation Tokyo Medical and Dental University ,  NanoCarrier Co., Ltd.

发明人： KATAOKA, Kazunori ,  ISHII, Takehiko ,  NAITO, Mitsuru ,  MATSUMOTO, Akira ,  KATO, Yasuki

IPC分类号： C08G81/00

CPC分类号： A61K47/48323 ,  A61K31/713 ,  A61K47/48215 ,  A61K47/60 ,  A61K47/6455 ,  C08G69/40 ,  C08G69/42 ,  C08G81/00 ,  C08G2650/28

摘要： The present invention provides a block copolymer as a carrier that simultaneously achieves stability of a biotechnology-based drug in blood and drug-releasing property of the drug at an affected area. The block copolymer of the present invention is a block copolymer, including: a polyamino acid chain segment; and a hydrophilic polymer chain segment, wherein the polyamino acid chain segment includes an amino acid residue having a cationic group in a side chain and an amino acid residue having a substituted phenylboronic acid group in a side chain, the substituted phenylboronic acid group having a phenyl ring in which at least one hydrogen atom is substituted to have a pKa around a physiological pH.

摘要翻译： 本发明提供了一种作为载体的嵌段共聚物，其同时使得生物技术型药物在血液中的稳定性和药物在患处的药物释放性质。 本发明的嵌段共聚物是嵌段共聚物，包括：聚氨基酸链段; 和亲水性聚合物链段，其中所述聚氨基酸链段包含在侧链具有阳离子基团的氨基酸残基和在侧链中具有取代的苯基硼酸基团的氨基酸残基，所述取代的苯基硼酸基团具有苯基 其中至少一个氢原子被取代以在生理pH附近具有pKa。

公开(公告)号：EP2666482A1

公开(公告)日：2013-11-27

申请号：EP12733905.9

申请日：2012-01-16

申请人： The University of Tokyo ,  NanoCarrier Co., Ltd.

发明人： KATAOKA, Kazunori ,  CHRISTIE, Ronald James ,  NISHIYAMA, Nobuhiro ,  MIYATA, Kanjiro ,  FUKUSHIMA, Shigeto ,  MATSUMOTO, Yu ,  NOMOTO, Takahiro ,  KATO, Yasuki

IPC分类号： A61K47/34 ,  A61K9/10 ,  A61K31/7088 ,  A61K48/00 ,  C07K14/00 ,  C12N15/113

CPC分类号： A61K9/5031 ,  A61K9/107 ,  A61K31/711 ,  A61K31/713 ,  A61K38/193 ,  A61K47/60 ,  A61K47/6455

摘要： The present invention provides a block copolymer applicable as a drug carrier capable of forming a stable complex with a nucleic acid and releasing the nucleic acid in cells. The block copolymer is represented by the following formula (1) or (2)


where: R 1 and R 2 each independently represent a hydrogen atom or a linear or branched alkyl group having 1 to 12 carbon atoms which may have a substituent; A represents a hydrophilic polymer chain; L 1 and L 3 each represent a linking group; B represents a cation-containing group; R 3 represents a side chain of any appropriate amino acid; z represents an integer of 5 to 500; x represents an integer of 40% or more of z; y represents an integer and may represent 0; z-x-y represents an integer and may represent 0; p represents an integer of 1 to 10; and q represents an integer of 1 to 10.

摘要翻译： 本发明提供了可用作能够与核酸形成稳定的复合物并在细胞中释放核酸的药物载体的嵌段共聚物。 嵌段共聚物由下式（1）或（2）表示，其中：R 1和R 2各自独立地表示氢原子或可具有取代基的碳原子数1〜12的直链或支链烷基; A表示亲水性聚合物链; L 1和L 3各自表示连接基团; B表示含阳离子基团; R 3表示任何合适的氨基酸的侧链; z表示5〜500的整数， x表示z的40％以上的整数。 y表示整数，可以表示0; z-x-y表示整数，可以表示0; p表示1〜10的整数， q表示1〜10的整数。

公开(公告)号：EP1167418B1

公开(公告)日：2004-10-20

申请号：EP99918308.0

申请日：1999-05-06

申请人： NanoCarrier Co., Ltd.

发明人： KATAOKA, Kazunori ,  KATO, Masao ,  NAGASAKI, Yukio ,  HAYASHIDA, Takahisa ,  IIJIMA, Michihiro ,  OKANO, Teruo

IPC分类号： C08G65/32 ,  C08G63/66 ,  C08G65/26 ,  C08G63/685 ,  C08L71/02

CPC分类号： C08G65/2639 ,  C08G63/664 ,  C08G63/6852 ,  C08G65/2618 ,  C08L71/02 ,  C08L2666/18

公开(公告)号：EP2397487B1

公开(公告)日：2013-12-25

申请号：EP11740552.2

申请日：2011-02-23

申请人： NanoCarrier Co., Ltd. ,  The University of Tokyo

发明人： KATO, Yasuki ,  ISHII, Atsushi ,  SHIBATA, Naoya ,  HAYASHI, Tatsuyuki ,  KATAOKA, Kazunori ,  MIYATA, Kanjiro ,  NISHIYAMA, Nobuhiro

IPC分类号： C07K4/00 ,  A61K31/7105 ,  A61K31/713 ,  A61K47/42 ,  A61K47/48 ,  A61K48/00 ,  C08G69/48 ,  C08F212/00 ,  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.

公开(公告)号：EP2305275A1

公开(公告)日：2011-04-06

申请号：EP09769989.6

申请日：2009-05-27

申请人： NanoCarrier Co., Ltd. ,  The University of Tokyo

发明人： KATAOKA, Kazunori ,  NISHIYAMA, Nobuhiro ,  TSUCHIYA, Chieko ,  HAYASHI, Tatsuyuki

IPC分类号： A61K33/24 ,  A61K9/08 ,  A61K47/10 ,  A61K47/34 ,  A61K47/48 ,  A61P35/00 ,  C08G69/40 ,  C08G81/00

CPC分类号： A61K47/488 ,  A61K9/0019 ,  A61K9/1075 ,  A61K47/60 ,  A61K47/6907 ,  C08G69/10 ,  C08G69/40 ,  C08G73/0233 ,  C08K5/0091

摘要： A liquid composition containing a polymer micelle and having a pH values of 3.0 to 7.0 is provided. The micelle is constituted of a coordination compound having a block copolymer of polyethylene glycol and polyglutamic acid and cisplatin that is coordinate-bonded to the block copolymer.

摘要翻译： 提供含有聚合物胶束并具有3.0至7.0的pH值的液体组合物。 胶束由具有聚乙二醇和聚谷氨酸的嵌段共聚物的配位化合物和与嵌段共聚物配位键合的顺铂构成。

公开(公告)号：EP1582539B1

公开(公告)日：2007-05-30

申请号：EP03782830.8

申请日：2003-12-19

申请人： NanoCarrier Co., Ltd.

发明人： SHIBATA, Naoya ,  NAGASAKI, Yukio ,  KATAOKA, Kazunori

IPC分类号： C08F290/02 ,  C08F2/44 ,  G01N33/545 ,  A61K49/00 ,  A61K49/04 ,  C08F290/06

CPC分类号： C08F290/06 ,  A61K49/0414 ,  C08F2/44 ,  C08F290/00 ,  C08F290/02 ,  C08F290/062

摘要： It is intended to provide a method of effectively incorporating an inorganic fluorescent substance or an inorganic contrast medium into latex polymer particles to be used in a diagnostic test or the like and fluorescent substance-containing latex polymer particles thus produced which show reduced non-specific adsorption of protein, etc. Latex polymer particles are produced by subjecting a latex-forming monomer, a macromer containing at least a hydrophilic polymer segment and a fluorescent substance or an inorganic contrast medium, which simultaneously coexist together in an aqueous medium, to polymerization.