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公开(公告)号:US09808480B2
公开(公告)日:2017-11-07
申请号:US14395745
申请日:2013-04-30
发明人: Kazunori Kataoka , Kanjiro Miyata , Nobuhiro Nishiyama , Kensuke Osada , Sumiyo Watanabe , Shigeto Fukushima , Hiroyuki Chaya , Hiroyasu Takemoto , Yasuki Kato
IPC分类号: C12N15/11 , A61K31/713 , A61K9/00 , A61K47/48
CPC分类号: A61K31/713 , A61K9/0019 , A61K47/60 , A61K47/64 , A61K47/645 , A61K47/6455 , A61K48/00
摘要: A unit structure-type pharmaceutical composition includes at least one nucleic acid, such as siRNA, electrostatically bound to at least one block copolymer having a cationic polyamino acid segment and a hydrophilic polymer chain segment. The negative charge(s) of the nucleic acid are counterbalanced, at least substantially, by the positive charge(s) of the cationic polyamino acid segment such that the pharmaceutical composition is electrically neutral or nearly electrically neutral. Further, the nucleic acid is covered with the hydrophilic polymer chain segment(s). The at least one block copolymer thereby improves the blood retention capability of the nucleic acid(s).
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公开(公告)号:US11020418B2
公开(公告)日:2021-06-01
申请号:US15725703
申请日:2017-10-05
发明人: Kazunori Kataoka , Kanjiro Miyata , Nobuhiro Nishiyama , Kensuke Osada , Sumiyo Watanabe , Shigeto Fukushima , Hiroyuki Chaya , Hiroyasu Takemoto , Yasuki Kato
摘要: A unit structure-type pharmaceutical composition includes a single nucleic acid, such as an antisense nucleic acid, electrostatically bound to a single block copolymer having a cationic polyamino acid segment and a hydrophilic polymer chain segment. The negative charges of the nucleic acid are counterbalanced, at least substantially, by the positive charges of the cationic polyamino acid segment such that the pharmaceutical composition is electrically neutral or nearly electrically neutral. Further, the nucleic acid is covered with the hydrophilic polymer chain segment. The block copolymer thereby improves the blood retention capability of the nucleic acids.
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公开(公告)号:US20150080454A1
公开(公告)日:2015-03-19
申请号:US14395745
申请日:2013-04-30
发明人: Kazunori Kataoka , Kanjiro Miyata , Nobuhiro Nishiyama , Kensuke Osada , Sumiyo Watanabe , Shigeto Fukushima , Hiroyuki Chaya , Hiroyasu Takemoto , Yasuki Kato
IPC分类号: A61K31/713 , A61K47/48
CPC分类号: A61K31/713 , A61K9/0019 , A61K47/60 , A61K47/64 , A61K47/645 , A61K47/6455 , A61K48/00
摘要: A unit structure-type pharmaceutical composition includes at least one nucleic acid, such as siRNA, electrostatically bound to at least one block copolymer having a cationic polyamino acid segment and a hydrophilic polymer chain segment. The negative charge(s) of the nucleic acid are counterbalanced, at least substantially, by the positive charge(s) of the cationic polyamino acid segment such that the pharmaceutical composition is electrically neutral or nearly electrically neutral. Further, the nucleic acid is covered with the hydrophilic polymer chain segment(s). The at least one block copolymer thereby improves the blood retention capability of the nucleic acid(s).
摘要翻译: 单体结构型药物组合物包含至少一种与至少一个具有阳离子聚氨基酸链段和亲水性聚合物链链段的嵌段共聚物静电结合的核酸,如siRNA。 核酸的负电荷至少基本上通过阳离子聚氨基酸片段的正电荷平衡,使得药物组合物是电中性的或接近电中性的。 此外,核酸被亲水性聚合物链段覆盖。 所述至少一种嵌段共聚物因此提高了核酸的血液保持能力。
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公开(公告)号:US10220026B2
公开(公告)日:2019-03-05
申请号:US15503370
申请日:2015-08-11
发明人: Hiroaki Kinoh , Kazunori Kataoka , Horacio Cabral , Yutaka Miura , Shigeto Fukushima , Nobuhiro Nishiyama , Tsukasa Chida
IPC分类号: A61K31/4402 , A61K31/4545 , A61K31/475 , A61K31/553 , A61K31/704 , A61K31/4375 , A61K47/48 , A61K9/00 , A61K45/06 , A61K47/60 , A61K47/59 , A61K47/69
摘要: The problem addressed by the present invention is to develop a pharmaceutical having therapeutic efficacy against epirubicin-resistant tumors. The present invention provides a micelle having an anti-cancer agent disposed inside the core of the micelle formed by an epirubicin-conjugated copolymer.
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公开(公告)号:US11324835B2
公开(公告)日:2022-05-10
申请号:US16642993
申请日:2018-08-30
发明人: Kazunori Kataoka , Kanjiro Miyata , Shigeto Fukushima , Kotaro Hayashi , Sumiyo Watanabe , HyunJin Kim , Kazuko Toh
IPC分类号: A61K47/64 , A61K47/34 , A61K9/10 , C12N15/113 , A61K48/00
摘要: A unit-type polyion complex for use in delivering nucleic acid to a target site in a patient includes one or more molecules of a block copolymer having a poly(ethylene glycol) segment and a cationic poly(amino acid) segment and one or more molecules of a nucleic acid. A total quantity of positive charges derived from side chains of the cationic poly(amino acid) segment of the block copolymer in the unit-type polyion complex is not offset by a total quantity of negative charges derived from the nucleic acid. Furthermore, the nucleic acid has a strand length of 10-50 bases, the molecular weight of the poly(ethylene glycol) segment is 40×103 or more, and the block copolymer has a binding constant (Ka) for the nucleic acid of 3.0×105 or more.
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公开(公告)号:US20170258922A1
公开(公告)日:2017-09-14
申请号:US15503370
申请日:2015-08-11
发明人: Hiroaki Kinoh , Kazunori Kataoka , Horacio Cabral , Yutaka Miura , Shigeto Fukushima , Nobuhiro Nishiyama , Tsukasa Chida
IPC分类号: A61K9/127 , A61K31/553 , A61K31/4545 , A61K31/475 , A61K31/704 , A61K31/4402 , A61K47/48 , C08L77/04
CPC分类号: A61K31/4402 , A61K9/0019 , A61K31/4375 , A61K31/4545 , A61K31/475 , A61K31/553 , A61K31/704 , A61K45/06 , A61K47/59 , A61K47/60 , A61K47/6907 , A61K2300/00
摘要: The problem addressed by the present invention is to develop a pharmaceutical having therapeutic efficacy against epirubicin-resistant tumors. The present invention provides a micelle having an anti-cancer agent disposed inside the core of the micelle formed by an epirubicin-conjugated copolymer.
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