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1. 发明授权

EP3141243B1 PHARMACEUTICAL COMPOSITION 有权转让
公开(公告)号：EP3141243B1
公开(公告)日：2020-07-08
申请号：EP15789186.2
申请日：2015-05-08
申请人： The University of Tokyo
发明人： KATAOKA, Kazunori , ISHII, Takehiko , NAITO, Mitsuru , YOSHINAGA, Naoto , ENDO, Taisuke
IPC分类号： A61K31/80 , A61K9/107 , A61K31/7105 , A61K31/711 , A61K47/34 , A61K48/00

2. 发明授权

EP3037107B1 POLYMER NANOPARTICLE COMPOSITE AND COMPOSITION FOR MRI IMAGING INCLUDING SAME 有权
公开(公告)号：EP3037107B1
公开(公告)日：2019-10-09
申请号：EP14837292.3
申请日：2014-08-22
申请人： The University of Tokyo
发明人： KATAOKA, Kazunori , NISHIYAMA, Nobuhiro , CABRAL, Horacio , MI, Peng , KISHIMURA, Akihiro , MIURA, Yutaka , AOKI, Ichio , KOKURYO, Daisuke , SAGA, Tsuneo
IPC分类号： A61K49/18 , A61K49/12

3. 发明授权

EP2462938B1 ANIONIC POLYMER, POLYION COMPLEX AND TERNARY POLYMER COMPOSITE USING ANIONIC POLYMER, AND PHARMACEUTICAL COMPOSITION 有权
公开(公告)号：EP2462938B1
公开(公告)日：2018-08-29
申请号：EP10802334.2
申请日：2010-07-23
申请人： The University of Tokyo
发明人： KATAOKA, Kazunori , ISHII, Atsushi , TAKEMOTO, Hiroyasu , NAKANISHI, Masataka , NISHIYAMA, Nobuhiro , MIYATA, Kanjiro
IPC分类号： A61K31/74 , C08G69/12 , C12N15/09
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: amain 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: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ-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.

4. 发明公开

EP3141243A1 PHARMACEUTICAL COMPOSITION 有权转让
标题翻译：药物组合物
公开(公告)号：EP3141243A1
公开(公告)日：2017-03-15
申请号：EP15789186.2
申请日：2015-05-08
申请人： The University of Tokyo
发明人： KATAOKA, Kazunori , ISHII, Takehiko , NAITO, Mitsuru , YOSHINAGA, Naoto , ENDO, Taisuke
IPC分类号： A61K9/107 , A61K31/7105 , A61K31/711 , A61K47/34 , A61K48/00
摘要： Provided is a carrier that can achieve both the stability of a biological drug in blood and its release in a target cell. A pharmaceutical composition of the present invention includes: a polymer unit α having a hydrophilic polymer chain segment and a cationic polymer chain segment; a polymer unit β having a hydrophilic polymer chain segment and a cationic polymer chain segment; and a drug. The polymer unit α and the polymer unit β form a micelle by being radially arranged so that the cationic polymer chain segments are directed inward and the hydrophilic polymer chain segments are directed outward, the micelle encapsulating the drug. The cationic polymer chain segment of the polymer unit α has a phenylboronic acid group in a side chain, and the cationic polymer chain segment of the polymer unit β has a phenylboronic acid binding site in a side chain, and the phenylboronic acid group and the phenylboronic acid binding site form a cross-linked structure that is disintegrable under an acidic environment or in the presence of a substance capable of competitive binding.
摘要翻译：提供了一种能够实现血液中生物药物的稳定性和其在靶细胞中的释放的载体。本发明的药物组合物包括：具有亲水聚合物链段和阳离子聚合物链段的聚合物单元α; 具有亲水性聚合物链段和阳离子聚合物链段的聚合物单元β; 和一种药物。聚合物单元α和聚合物单元β通过径向排列形成胶束，使得阳离子聚合物链段向内定向并且亲水聚合物链段向外定向，胶束包封药物。聚合物单元α的阳离子聚合物链段在侧链中具有苯基硼酸基团，并且聚合物单元β的阳离子聚合物链段在侧链中具有苯基硼酸结合位点，并且苯基硼酸基团和苯基硼酸基团酸结合位点形成在酸性环境下或在能够竞争性结合的物质存在下可崩解的交联结构。

5. 发明公开

EP3037107A1 POLYMER NANOPARTICLE COMPOSITE AND COMPOSITION FOR MRI IMAGING INCLUDING SAME 有权
标题翻译：聚合物纳米颗粒复合物和组合物用于MRI成像为了
公开(公告)号：EP3037107A1
公开(公告)日：2016-06-29
申请号：EP14837292.3
申请日：2014-08-22
申请人： The University of Tokyo
发明人： KATAOKA, Kazunori , NISHIYAMA, Nobuhiro , CABRAL, Horacio , MI, Peng , KISHIMURA, Akihiro , MIURA, Yutaka , AOKI, Ichio , KOKURYO, Daisuke , SAGA, Tsuneo
IPC分类号： A61K49/00
CPC分类号： A61K49/1872 , A61K9/14 , A61K9/143 , A61K49/128 , A61K49/1818 , A61K49/1824 , A61K49/1851 , A61K49/1866 , C08K3/32
摘要： The present invention provides a safe polymer nanoparticle composite with few side effects, and an MRI contrast agent incorporating said polymer nanoparticle composite. The polymer nanoparticle composite is capable of specifically accumulating on a tumor tissue to selectively extract the tissue, exhibiting high contrast even when used in small amounts, and enabling imaging over prolonged periods of time. This polymer nanoparticle composite is characterized by containing a block copolymer that includes a non-charged hydrophilic polymer chain segment and an anionic polymer chain segment, and MnCaP.

6. 发明公开

EP2272897A1 COPOLYMER INCLUDING UNCHARGED HYDROPHILIC BLOCK AND CATIONIC POLYAMINO ACID BLOCK HAVING LATERAL CHAIN TO WHICH HYDROPHOBIC RADICAL IS PARTIALLY INTRODUCED, AND USE OF COPOLYMER 有权
标题翻译：无负载亲水性嵌段和阳离子POLYAMINOSÄUREBLOCK与部分地插入疏水基团A侧链和共聚物的用途共聚物
公开(公告)号：EP2272897A1
公开(公告)日：2011-01-12
申请号：EP09720268.3
申请日：2009-03-06
申请人： The University of Tokyo
发明人： KATAOKA, Kazunori , NISHIYAMA, Nobuhiro , ISHII, Atsushi , KATO, Yasuki , MIYATA, Kanjiiro , KIM, Hyunjin , TAKEMOTO, Hiroyasu
IPC分类号： C08G81/00 , C08L87/00 , C08L89/00
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：本发明涉及一种嵌段共聚物含有不带电荷的亲水性聚合物链嵌段以及阳离子性聚氨基酸链嵌段的，worin亲水性聚合物链嵌段共价结合到聚氨基酸链嵌段的主链的一端，并且所述疏水性基团共价结合到不小于10％的侧链和氨基酸在聚氨基酸链嵌段的重复单元不大于70％。该嵌段共聚物形成的siRNA，小分子核酸稳定的聚集体，在生理条件下。

8. 发明授权

EP2272897B1 COPOLYMER INCLUDING UNCHARGED HYDROPHILIC BLOCK AND CATIONIC POLYAMINO ACID BLOCK HAVING LATERAL CHAIN TO WHICH HYDROPHOBIC RADICAL IS PARTIALLY INTRODUCED, AND USE OF COPOLYMER 有权
标题翻译：无负载亲水性嵌段和阳离子POLYAMINOSÄUREBLOCK与部分地插入疏水基团A侧链和共聚物的用途共聚物
公开(公告)号：EP2272897B1
公开(公告)日：2016-12-28
申请号：EP09720268.3
申请日：2009-03-06
申请人： The University of Tokyo
发明人： KATAOKA, Kazunori , NISHIYAMA, Nobuhiro , ISHII, Atsushi , KATO, Yasuki , MIYATA, Kanjiiro , KIM, Hyunjin , TAKEMOTO, Hiroyasu
IPC分类号： C08G81/00 , C08L87/00 , C08L89/00 , C08G69/10
CPC分类号： C08G69/10 , C08G81/00 , Y10T428/2982

9. 发明授权

EP2415871B1 POLYION COMPLEX OF DOUBLE-STRANDED RIBONUCLEIC ACID 有权
标题翻译：从双链核糖核酸聚离子
公开(公告)号：EP2415871B1
公开(公告)日：2015-04-22
申请号：EP10758784.2
申请日：2010-03-31
申请人： The University of Tokyo
发明人： HORI, Yuichi , KATAOKA, Kazunori , FUJITA, Toshiro , SHIMIZU, Hideki , KANAME, Shinya , MATSUMOTO, Satoru , NISHIYAMA, Nobuhiro , MIYATA, Kanjiro , OBA, Makoto
IPC分类号： C12N15/113 , A61K31/713 , A61K47/34 , A61K48/00 , C12N15/09
CPC分类号： C12N15/87 , C12N15/111 , C12N2320/32 , Y10T428/2982

10. 发明公开

EP2842546A1 UNIT STRUCTURE-TYPE PHARMACEUTICAL COMPOSITION FOR NUCLEIC ACID DELIVERY 审中-实审转让
标题翻译：药剂师ZUSAMMENSETZUNG MIT EINHEITENSTRUKTUR ZURNUKLEINSÄUREFREISETZUNG
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。

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