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1.发明授权Block copolymer having phenylboronic acid group introduced therein, and use thereof 有权其中引入苯基硼酸基的嵌段共聚物及其用途公开(公告)号：US09114177B2
公开(公告)日：2015-08-25
申请号：US14358816
申请日：2012-11-19
申请人： THE UNIVERSITY OF TOKYO , NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY , NanoCarrier Co., Ltd.
IPC分类号： A61K31/713 , A61K47/48 , C08G81/00 , C08G69/40 , C08G69/42
CPC分类号： A61K47/48323 , A61K31/713 , A61K47/48215 , A61K47/60 , A61K47/6455 , C08G69/40 , C08G69/42 , C08G81/00 , C08G2650/28
摘要： A block copolymer includes a polyamino acid chain segment and a hydrophilic polymer chain segment. The polyamino acid chain segment includes at least one amino acid residue having a side chain that contains a cationic group and at least one amino acid residue having a side chain that contains a substituted phenylboronic acid group. In the substituted phenylboronic acid group, at least one hydrogen of the phenyl ring is substituted so that the phenylboronic acid group has a pKa of less than 8. Such a block copolymer serves as a carrier that simultaneously imparts stability to a biotechnology-based drug in blood and provides suitable drug-releasing properties of the drug at an affected area.
摘要翻译： 嵌段共聚物包括聚氨基酸链段和亲水性聚合物链段。 聚氨基酸链段包括至少一个具有含有阳离子基团的侧链的氨基酸残基和至少一个具有含有取代的苯基硼酸基团的侧链的氨基酸残基。 在取代的苯基硼酸基团中，苯基环的至少一个氢被取代，使得苯基硼酸基团的pKa小于8.这种嵌段共聚物用作同时赋予基于生物技术的药物稳定性的载体 并在受影响的区域提供药物的合适的药物释放性质。
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2.发明申请公开(公告)号：US20150051347A1
公开(公告)日：2015-02-19
申请号：US14358816
申请日：2012-11-19
申请人： THE UNIVERSITY OF TOKYO , NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY , NanoCarrier Co., Ltd.
IPC分类号： A61K47/48 , A61K31/713 , 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： A block copolymer includes a polyamino acid chain segment and a hydrophilic polymer chain segment. The polyamino acid chain segment includes at least one amino acid residue having a side chain that contains a cationic group and at least one amino acid residue having a side chain that contains a substituted phenylboronic acid group. In the substituted phenylboronic acid group, at least one hydrogen of the phenyl ring is substituted so that the phenylboronic acid group has a pKa of less than 8. Such a block copolymer serves as a carrier that simultaneously imparts stability to a biotechnology-based drug in blood and provides suitable drug-releasing properties of the drug at an affected area.
摘要翻译： 嵌段共聚物包括聚氨基酸链段和亲水性聚合物链段。 聚氨基酸链段包括至少一个具有含有阳离子基团的侧链的氨基酸残基和至少一个具有含有取代的苯基硼酸基团的侧链的氨基酸残基。 在取代的苯基硼酸基团中，苯基环的至少一个氢被取代，使得苯基硼酸基团的pKa小于8.这种嵌段共聚物用作同时赋予基于生物技术的药物稳定性的载体 并在受影响的区域提供药物的合适的药物释放性质。
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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：US09920133B2
公开(公告)日：2018-03-20
申请号：US15111875
申请日：2015-02-03
发明人： Yasuhiro Matsumura , Masahiro Yasunaga , Yoshikatsu Koga , Yoshiyuki Yamamoto , Ryuta Sato , Ryo Tsumura , Kazunori Kataoka , Nobuhiro Nishiyama , Yutaka Miura , Shino Manabe , Yasuki Kato
IPC分类号： C07K16/36 , A61K47/48 , A61K39/395 , A61K39/00
CPC分类号： C07K16/36 , A61K39/3955 , A61K47/6813 , A61K47/6817 , A61K47/6849 , A61K2039/505 , C07K2317/24 , C07K2317/56 , C07K2317/565 , C07K2317/77 , C07K2317/92
摘要： Monoclonal antibodies against human and mouse tissue factor, and fragments thereof, are disclosed, as well as pharmaceutical compositions and compositions for drug delivery containing the same. Therapeutic methods using the same are also disclosed.
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6.发明申请公开(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：US20160058703A1
公开(公告)日：2016-03-03
申请号：US14930119
申请日：2015-11-02
发明人： Atsushi Ishii , Yasuki Kato
IPC分类号： A61K9/107 , A61K47/34 , A61K31/713 , A61K47/24
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。
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公开(公告)号：US09795563B2
公开(公告)日：2017-10-24
申请号：US14930119
申请日：2015-11-02
发明人： Atsushi Ishii , Yasuki Kato
IPC分类号： A61K9/107 , A61K31/7084 , A61K9/16 , A61K9/19 , A61K47/24 , A61K47/34 , A61K31/713
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.
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