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。

公开(公告)号：US08318205B2

公开(公告)日：2012-11-27

申请号：US12656307

申请日：2010-01-25

申请人： Kazunori Kataoka ,  Naoki Kanayama ,  Keiji Itaka ,  Shigeto Fukushima ,  Atsushi Harada

发明人： Kazunori Kataoka ,  Naoki Kanayama ,  Keiji Itaka ,  Shigeto Fukushima ,  Atsushi Harada

IPC分类号： A61K9/14

CPC分类号： C08G69/10 ,  A61K9/1075 ,  A61K47/645 ,  A61K47/6907 ,  C08G69/48 ,  C08G81/00 ,  C12N15/87

摘要： The invention provides block copolymers formed of poly(ethylene glycol) segments and poly(amino acid derivative) segments having side chains of at least one kind of specific amine residue. The invention also provides polyion complexes of such copolymers with polynucleotides and the like. These block copolymers are useful as carriers for in vivo delivery of active substances such as DNA.

摘要翻译： 本发明提供由聚（乙二醇）链段和具有至少一种特定胺残基的侧链的聚（氨基酸衍生物）链段形成的嵌段共聚物。 本发明还提供了这种共聚物与多核苷酸等的聚离子配合物。 这些嵌段共聚物可用作体内递送活性物质如DNA的载体。

公开(公告)号：US20100137512A1

公开(公告)日：2010-06-03

申请号：US12656307

申请日：2010-01-25

申请人： Kazunori Kataoka ,  Naoki Kanayama ,  Keiji Itaka ,  Shigeto Fukushima ,  Atsushi Harada

发明人： Kazunori Kataoka ,  Naoki Kanayama ,  Keiji Itaka ,  Shigeto Fukushima ,  Atsushi Harada

IPC分类号： A61K47/48

CPC分类号： C08G69/10 ,  A61K9/1075 ,  A61K47/645 ,  A61K47/6907 ,  C08G69/48 ,  C08G81/00 ,  C12N15/87

摘要： The invention provides block copolymers formed of poly(ethylene glycol) segments and poly(amino acid derivative) segments having side chains of at least one kind of specific amine residue. The invention also provides polyion complexes of such copolymers with polynucleotides and the like. These block copolymers are useful as carriers for in vivo delivery of active substances such as DNA.

摘要翻译： 本发明提供由聚（乙二醇）链段和具有至少一种特定胺残基的侧链的聚（氨基酸衍生物）链段形成的嵌段共聚物。 本发明还提供了这种共聚物与多核苷酸等的聚离子配合物。 这些嵌段共聚物可用作体内递送活性物质如DNA的载体。

公开(公告)号：US07780957B2

公开(公告)日：2010-08-24

申请号：US10556058

申请日：2004-05-07

申请人： Kazunori Kataoka ,  Naoki Kanayama ,  Keiji Itaka ,  Shigeto Fukushima ,  Atsushi Harada

发明人： Kazunori Kataoka ,  Naoki Kanayama ,  Keiji Itaka ,  Shigeto Fukushima ,  Atsushi Harada

IPC分类号： A61K31/74 ,  A61K9/14

CPC分类号： C08G69/10 ,  A61K9/1075 ,  A61K47/645 ,  A61K47/6907 ,  C08G69/48 ,  C08G81/00 ,  C12N15/87

摘要： The invention provides block copolymers formed of poly(ethylene glycol) segments and poly(amino acid derivative) segments having side chains of at least one kind of specific amine residue. The invention also provides polyion complexes of such copolymers with polynucleotides and the like. These block copolymers are useful as carriers for in vivo delivery of active substances such as DNA.

公开(公告)号：US07829657B2

公开(公告)日：2010-11-09

申请号：US11884146

申请日：2006-02-08

申请人： Kazunori Kataoka ,  Keiji Itaka ,  Nobuhiro Nishiyama ,  Shigeto Fukushima ,  Woo-Dong Jang ,  Kanjiro Miyata ,  Masataka Nakanishi ,  Shunsaku Asano ,  Naoki Kanayama

发明人： Kazunori Kataoka ,  Keiji Itaka ,  Nobuhiro Nishiyama ,  Shigeto Fukushima ,  Woo-Dong Jang ,  Kanjiro Miyata ,  Masataka Nakanishi ,  Shunsaku Asano ,  Naoki Kanayama

IPC分类号： C08G69/08

CPC分类号： A61K48/0041 ,  A61K47/60 ,  A61K47/6455 ,  C08G18/0814 ,  C08G63/6854 ,  C08G69/10 ,  C08G73/028 ,  C08G73/0293 ,  C12N15/88

摘要： Disclosed is a composition for the delivery of nucleic acid to target cells or tissues, which comprises a polycationically charged polymer as a carrier of nucleic acid. The polycationically charged polymer is a polymer which may comprise a charged polymer segment having a main chain based on poly(amino acid), polysaccharide, polyester, polyether, polyurethane or vinyl polymer and having, as a side chain, a group of formula —NH—(CH2)a—(NH(CH2)2)e—NH2 (wherein a and e independently denote an integer of 1 to 5) which is connected to the main chain either directly or via a linker. The disclosed composition has low toxicity, and has a high efficiency in introducing nucleic acid into cells.

摘要翻译： 公开了用于将核酸递送至靶细胞或组织的组合物，其包含作为核酸载体的聚阳离子带电聚合物。 聚阳离子带电聚合物是聚合物，其可以包含具有基于聚（氨基酸），多糖，聚酯，聚醚，聚氨酯或乙烯基聚合物的主链的带电聚合物链段，并且具有作为侧链的式-NH基团 - （CH 2）a - （NH（CH 2）2）e-NH 2（其中a和e独立地表示1至5的整数），其直接或通过连接体与主链连接。 所公开的组合物具有低毒性，并且在将核酸引入细胞中具有高效率。

公开(公告)号：US20090081458A1

公开(公告)日：2009-03-26

申请号：US11919744

申请日：2006-04-28

申请人： Kazunori Kataoka ,  Aya Koide ,  Kensuke Osada ,  Yuichi Yamasaki ,  Shigeto Fukushima ,  Joon-Sik Park

发明人： Kazunori Kataoka ,  Aya Koide ,  Kensuke Osada ,  Yuichi Yamasaki ,  Shigeto Fukushima ,  Joon-Sik Park

IPC分类号： B32B27/08

CPC分类号： A61K9/1273 ,  C08G73/028 ,  Y10T428/2982

摘要： The present invention discloses a vesicle which is excellent in structure stability and environmental responsiveness and also can be produced by a simple operation. More particularly, the present invention discloses a vesicle comprising a membrane formed of a first block copolymer containing a non-chargeable hydrophilic segment and a chargeable segment, and a second block copolymer containing a non-chargeable hydrophilic segment and a chargeable segment having an electric charge which is opposite to that of the chargeable segment of the first block copolymer.

摘要翻译： 本发明公开了一种结构稳定性和环境响应性优异的囊泡，也可以通过简单的操作来制造。 更具体地，本发明公开了一种囊泡，其包含由含有不可充电的亲水性片段和可带电部分的第一嵌段共聚物形成的膜，以及含有不可充电亲水片段的第二嵌段共聚物和具有电荷的带电部分 其与第一嵌段共聚物的可带电段的相反。

公开(公告)号：US20140017328A1

公开(公告)日：2014-01-16

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

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。

公开(公告)号：US08304497B2

公开(公告)日：2012-11-06

申请号：US11919744

申请日：2006-04-28

申请人： Kazunori Kataoka ,  Aya Koide ,  Kensuke Osada ,  Yuichi Yamasaki ,  Shigeto Fukushima ,  Joon-Sik Park

发明人： Kazunori Kataoka ,  Aya Koide ,  Kensuke Osada ,  Yuichi Yamasaki ,  Shigeto Fukushima ,  Joon-Sik Park

IPC分类号： A61K47/30 ,  C08L77/04

CPC分类号： A61K9/1273 ,  C08G73/028 ,  Y10T428/2982

摘要： The present invention discloses a vesicle which is excellent in structure stability and environmental responsiveness and also can be produced by a simple operation. More particularly, the present invention discloses a vesicle comprising a membrane formed of a first block copolymer containing a non-chargeable hydrophilic segment and a chargeable segment, and a second block copolymer containing a non-chargeable hydrophilic segment and a chargeable segment having an electric charge which is opposite to that of the chargeable segment of the first block copolymer.

摘要翻译： 本发明公开了一种结构稳定性和环境响应性优异的囊泡，也可以通过简单的操作来制造。 更具体地，本发明公开了一种囊泡，其包含由含有不可充电的亲水性片段和可带电部分的第一嵌段共聚物形成的膜，以及含有不可充电亲水片段的第二嵌段共聚物和具有电荷的带电部分 其与第一嵌段共聚物的可带电段的相反。

公开(公告)号：US20070059271A1

公开(公告)日：2007-03-15

申请号：US10556058

申请日：2004-05-07

申请人： Kazunori Kataoka ,  Naoki Kanayama ,  Keiji Itaka ,  Shigeto Fukushima ,  Atsushi Harada

发明人： Kazunori Kataoka ,  Naoki Kanayama ,  Keiji Itaka ,  Shigeto Fukushima ,  Atsushi Harada

IPC分类号： A61K31/787 ,  C08L71/02

CPC分类号： C08G69/10 ,  A61K9/1075 ,  A61K47/645 ,  A61K47/6907 ,  C08G69/48 ,  C08G81/00 ,  C12N15/87

摘要： The invention provides block copolymers formed of poly(ethylene glycol) segments and poly(amino acid derivative) segments having side chains of at least one kind of specific amine residue. The invention also provides polyion complexes of such copolymers with polynucleotides and the like. These block copolymers are useful as carriers for in vivo delivery of active substances such as DNA.

摘要翻译： 本发明提供由聚（乙二醇）链段和具有至少一种特定胺残基的侧链的聚（氨基酸衍生物）链段形成的嵌段共聚物。 本发明还提供了这种共聚物与多核苷酸等的聚离子配合物。 这些嵌段共聚物可用作体内递送活性物质如DNA的载体。

公开(公告)号：US6080396A

公开(公告)日：2000-06-27

申请号：US836965

申请日：1997-08-18

申请人： Masayuki Yokoyama ,  Kazunori Kataoka ,  Teruo Okano ,  Yasuhisa Sakurai ,  Shigeto Fukushima ,  Ryuji Uehara ,  Tomoko Akutsu ,  Kazuya Okamoto ,  Hiroko Mashiba ,  Megumi Machida ,  Kazuhisa Shimizu

发明人： Masayuki Yokoyama ,  Kazunori Kataoka ,  Teruo Okano ,  Yasuhisa Sakurai ,  Shigeto Fukushima ,  Ryuji Uehara ,  Tomoko Akutsu ,  Kazuya Okamoto ,  Hiroko Mashiba ,  Megumi Machida ,  Kazuhisa Shimizu

IPC分类号： A61K9/107 ,  A61K9/51 ,  A61K9/127 ,  A61K31/70 ,  C07M17/08

CPC分类号： A61K9/1075

摘要： A dimer, trimer or tetramer of an anthracycline compound which can be obtained by directly, chemically bonding anthracycline compounds having anticancer activities to each other by an alkali treatment. A high molecular block copolymer-drug complex pharmaceutical preparation in which the high molecular block copolymer having a hydrophilic polymer segment and a hydrophobic polymer segment forms a micelle having the hydrophilic segment as its outer shell and contains in its hydrophobic inner core a dimer, trimer or tetramer of anthracycline compound alone or together with other drugs. A high molecular block copolymer-drug complex pharmaceutical preparation in which the high molecular block copolymer having a hydrophilic polymer segment and a hydrophobic polymer segment forms a micelle having the hydrophilic segment as its outer shell and contains in its hydrophobic inner core an anthracycline anticancer agent, wherein, when the pharmaceutical preparation is intravenously administered to a CDF1 mouse, the amount of the anthracycline anticancer agent in 1 ml of the mouse blood plasma after 1 hour of its administration becomes 10 (% of dose/ml) or more, provided that the amount of anthracycline anticancer agent in the administered preparation is defined as 100. The aforementioned pharmaceutical preparations have high drug effects and low toxicities.

摘要翻译： PCT No.PCT / JP96 / 02789第 371日期：1997年8月18日 102（e）日期1997年8月18日PCT提交1996年9月26日PCT公布。 公开号WO97 / 12895 日期1997年04月10日可以通过碱处理直接化学键合具有抗癌活性的蒽环类化合物而获得的蒽环类化合物的二聚体，三聚体或四聚体。 一种高分子嵌段共聚物 - 药物复合药物制剂，其中具有亲水性聚合物链段和疏水性聚合物链段的高分子嵌段共聚物形成具有亲水链段作为其外壳的胶束，并且在其疏水内核中含有二聚体，三聚体或 蒽环类化合物的四聚体单独或与其他药物一起。 一种高分子嵌段共聚物 - 药物复合药物制剂，其中具有亲水性聚合物链段和疏水性聚合物链段的高分子嵌段共聚物形成具有亲水链段作为其外壳并在其疏水内核中含有蒽环类抗癌剂的胶束， 其中，当向CDF1小鼠静脉内施用药物制剂时，在施用1小时后1ml小鼠血浆中的蒽环类抗癌剂的量为10（％/剂量）以上，条件是 给药制剂中蒽环类抗癌剂的量定义为100.上述药物制剂具有高药物作用和低毒性。