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    Polymer conjugate of bioactive substance having hydroxy group
    1.
    发明授权
    Polymer conjugate of bioactive substance having hydroxy group 有权
    具有羟基的生物活性物质的聚合物缀合物

    公开(公告)号：US08808749B2

    公开(公告)日：2014-08-19

    申请号：US13319175

    申请日：2010-05-12

    申请人： Masayuki Kitagawa ,  Chieko Seno ,  Keiko Ebara ,  Kazutoshi Takashio

    发明人： Masayuki Kitagawa ,  Chieko Seno ,  Keiko Ebara ,  Kazutoshi Takashio

    IPC分类号： A61K9/14 ,  A61K31/365 ,  A61K31/19 ,  A61K31/195 ,  A61K31/337 ,  C08G69/10 ,  A61K47/48 ,  A61K31/167 ,  C08G69/48 ,  A61K31/573 ,  A61K31/7068 ,  A61K31/704 ,  A61K31/52 ,  C08G69/40 ,  A61K31/4745 ,  A61K31/7052

    CPC分类号： C08G69/10 ,  A61K31/167 ,  A61K31/19 ,  A61K31/195 ,  A61K31/337 ,  A61K31/365 ,  A61K31/4745 ,  A61K31/52 ,  A61K31/573 ,  A61K31/704 ,  A61K31/7052 ,  A61K31/7068 ,  A61K47/60 ,  A61K47/645 ,  C08G69/40 ,  C08G69/48

    摘要： A polymer conjugate of a physiologically active substance, which enables drug release independent of a biological enzyme and can be expected to have a high therapeutic effect, is demanded.Provided is a polymer conjugate of a physiologically active substance, comprising a block copolymer of a polyethylene glycol moiety and a polymer having two or more carboxy groups, in which a substituent represented by general formula (I) or general formula (II) is linked to at least one of the side-chain carboxy groups of the block copolymer via an amide bond [in the formula, R8 and R9 each independently are hydrogen atom or (C1-C6)alkyl which may have a substituent, R10 is hydrogen atom, (C1-C40)alkyl which may have a substituent, (C1-C40) aralkyl group which may have a substituent, an aromatic group which may have a substituent, an amino acid residue having a protected carboxy group, or a sugar residue which may have a substituent, CX—CY represents CH—CH or C═C (double bond), and A represents a residue obtained by removing, from a physiologically active substance having one or more hydroxy groups, one of the one or more hydroxy groups].

    摘要翻译： 需要生物活性物质的聚合物缀合物，其使药物释放与生物酶无关并且可以预期具有高治疗效果。 提供了一种生理活性物质的聚合物缀合物，其包含聚乙二醇部分和具有两个或更多个羧基的聚合物的嵌段共聚物，其中由通式（I）或通式（II）表示的取代基与 嵌段共聚物中的至少一个侧链羧基通过酰胺键[在式中，R8和R9各自独立地为氢原子或可具有取代基的（C1-C6）烷基，R10为氢原子（ 可以具有取代基的C 1 -C 40的烷基，可以具有取代基的（C 1〜C 40）芳烷基，可以具有取代基的芳香族基，具有被保护的羧基的氨基酸残基， 取代基，CX-CY表示CH-CH或C = C（双键），A表示通过从具有一个或多个羟基的生理活性物质除去一个或多个羟基之一而获得的残基]。

    High-molecular weight derivative of nucleic acid antimetabolite
    2.
    发明授权
    High-molecular weight derivative of nucleic acid antimetabolite 有权
    核酸抗代谢物的高分子量衍生物

    公开(公告)号：US08334364B2

    公开(公告)日：2012-12-18

    申请号：US12312009

    申请日：2007-11-01

    申请人： Keiichiro Yamamoto ,  Kazutoshi Takashio

    发明人： Keiichiro Yamamoto ,  Kazutoshi Takashio

    IPC分类号： C07K5/093 ,  C07K5/113 ,  C07K7/06 ,  C07K7/08 ,  C07H19/06 ,  C07H19/10 ,  C07H19/067 ,  C07H19/073 ,  C07H19/09 ,  C07H19/167 ,  C07H19/173 ,  C07H19/19 ,  C07H19/20

    CPC分类号： A61K31/787 ,  A61K47/60 ,  A61K47/645 ,  C08G69/10 ,  C08G69/40 ,  C08G69/48

    摘要： [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a high therapeutic effect at a low dose.[Means For Solving Problems] Disclosed is a high molecular weight derivative of a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the carboxyl group in the side chain is bound to a hydroxyl group in the nucleoside derivative via an ester bond. Also disclosed is a method for producing the high molecular weight derivative.

    摘要翻译： [问题]需要可以在低剂量下显示高治疗效果的核酸抗代谢物的衍生物。 解决问题的手段公开了核酸抗代谢物的高分子量衍生物，其特征在于包含高分子量化合物，其包含聚乙二醇部分和在侧链具有羧基的聚合物部分和核苷衍生物 其可以作为核酸抗代谢物，其中侧链中的羧基通过酯键与核苷衍生物中的羟基结合。 还公开了高分子量衍生物的制造方法。

    Polymer Conjugate Of Bioactive Substance Having Hydroxy Group
    3.
    发明申请
    Polymer Conjugate Of Bioactive Substance Having Hydroxy Group 有权
    具有羟基的生物活性物质的共轭物

    公开(公告)号：US20120116051A1

    公开(公告)日：2012-05-10

    申请号：US13319175

    申请日：2010-05-12

    申请人： Masayuki Kitagawa ,  Chieko Seno ,  Keiko Ebara ,  Kazutoshi Takashio

    发明人： Masayuki Kitagawa ,  Chieko Seno ,  Keiko Ebara ,  Kazutoshi Takashio

    IPC分类号： C08H1/00 ,  A61P9/10 ,  A61P17/14 ,  A61P29/00 ,  A61P35/00

    CPC分类号： C08G69/10 ,  A61K31/167 ,  A61K31/19 ,  A61K31/195 ,  A61K31/337 ,  A61K31/365 ,  A61K31/4745 ,  A61K31/52 ,  A61K31/573 ,  A61K31/704 ,  A61K31/7052 ,  A61K31/7068 ,  A61K47/60 ,  A61K47/645 ,  C08G69/40 ,  C08G69/48

    摘要： A polymer conjugate of a physiologically active substance, which enables drug release independent of a biological enzyme and can be expected to have a high therapeutic effect, is demanded.Provided is a polymer conjugate of a physiologically active substance, comprising a block copolymer of a polyethylene glycol moiety and a polymer having two or more carboxy groups, in which a substituent represented by general formula (I) or general formula (II) is linked to at least one of the side-chain carboxy groups of the block copolymer via an amide bond [in the formula, R8 and R9 each independently are hydrogen atom or (C1-C6)alkyl which may have a substituent, R10 is hydrogen atom, (C1-C40)alkyl which may have a substituent, (C1-C40) aralkyl group which may have a substituent, an aromatic group which may have a substituent, an amino acid residue having a protected carboxy group, or a sugar residue which may have a substituent, CX—CY represents CH—CH or C═C (double bond), and A represents a residue obtained by removing, from a physiologically active substance having one or more hydroxy groups, one of the one or more hydroxy groups].

    摘要翻译： 需要生物活性物质的聚合物缀合物，其使药物释放与生物酶无关并且可以预期具有高治疗效果。 提供了一种生理活性物质的聚合物缀合物，其包含聚乙二醇部分和具有两个或更多个羧基的聚合物的嵌段共聚物，其中由通式（I）或通式（II）表示的取代基与 嵌段共聚物中的至少一个侧链羧基通过酰胺键[在式中，R8和R9各自独立地为氢原子或可具有取代基的（C1-C6）烷基，R10为氢原子（ 可以具有取代基的C 1 -C 40的烷基，可以具有取代基的（C 1〜C 40）芳烷基，可以具有取代基的芳香族基，具有被保护的羧基的氨基酸残基， 取代基，CX-CY表示CH-CH或C = C（双键），A表示通过从具有一个或多个羟基的生理活性物质除去一个或多个羟基之一而获得的残基]。

    HIGH MOLECULAR WEIGHT DERIVATIVE OF NUCLEIC ACID ANTIMETABOLITE
    5.
    发明申请
    HIGH MOLECULAR WEIGHT DERIVATIVE OF NUCLEIC ACID ANTIMETABOLITE 有权
    高分子量重量的核酸抗微生物剂

    公开(公告)号：US20100029849A1

    公开(公告)日：2010-02-04

    申请号：US12312157

    申请日：2007-11-06

    申请人： Keiichiro Yamamoto ,  Kazutoshi Takashio

    发明人： Keiichiro Yamamoto ,  Kazutoshi Takashio

    IPC分类号： C08F287/00

    CPC分类号： A61K31/787 ,  A61K47/60 ,  A61K47/645 ,  C08G69/42 ,  C08G69/48 ,  C08G73/028

    摘要： [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a higher therapeutic effect at a lower dose.[Means for Solving Problems] Disclosed is a high molecular weight derivative a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the nucleoside derivative is bound to the carboxyl group in the side chain of the high molecular weight compound via a highly hydrophobic linker.

    摘要翻译： [问题]需要核酸抗代谢物的衍生物，其可以在较低剂量下显示更高的治疗效果。 解决问题的手段公开了一种核酸抗代谢产物的高分子量衍生物，其特征在于包含包含聚乙二醇部分和侧链中具有羧基的聚合物部分的高分子量化合物和核苷衍生物， 可以作为核酸抗代谢物，其中核苷衍生物通过高度疏水的接头与高分子量化合物的侧链中的羧基结合。

    High-Molecular Weight Conjugate of Combretastatins
    6.
    发明申请
    High-Molecular Weight Conjugate of Combretastatins 审中-公开
    组合蛋白的高分子量缀合物

    公开(公告)号：US20100004403A1

    公开(公告)日：2010-01-07

    申请号：US12309061

    申请日：2007-07-13

    申请人： Masayuki Kitagawa ,  Keizou Ishikawa ,  Akira Masuda ,  Kazutoshi Takashio

    发明人： Masayuki Kitagawa ,  Keizou Ishikawa ,  Akira Masuda ,  Kazutoshi Takashio

    IPC分类号： C08L71/02

    CPC分类号： C08G73/1092 ,  A61K47/60 ,  A61K47/645

    摘要： A novel derivative of combretastatins which has water solubility and is capable of releasing the drug independent of biological enzymes likely to cause individual differences and whose effective therapeutic effect can be expected has been demanded. A high-molecular weight conjugate of combretastatins, characterized by having a structure in which a hydroxyl group of a combretastatin is linked via an ester bond to a carboxylic acid group of the polymer moiety in a block copolymer of a polyethylene glycol moiety with the polymer moiety having two or more carboxylic acid groups such as polyaspartic acid or polyglutamic acid is provided.

    摘要翻译： 已经要求具有水溶性并且能够释放药物的新型衍生物，其独立于可能导致个体差异的生物酶，并且可以预期其有效的治疗效果。 考布斯他汀的高分子量缀合物，其特征在于具有以下结构：考布他汀的羟基通过酯键与聚乙烯部分与聚合物部分的嵌段共聚物中的聚合物部分的羧酸基团连接 提供具有两个或更多个羧酸基团，例如聚天冬氨酸或聚谷氨酸。

    HIGH-MOLECULAR WEIGHT DERIVATIVE OF NUCLEIC ACID ANTIMETABOLITE
    9.
    发明申请
    HIGH-MOLECULAR WEIGHT DERIVATIVE OF NUCLEIC ACID ANTIMETABOLITE 有权
    高分子重量衍生物的核酸抗微生物剂

    公开(公告)号：US20090281300A1

    公开(公告)日：2009-11-12

    申请号：US12312009

    申请日：2007-11-01

    申请人： Keiichiro Yamamoto ,  Kazutoshi Takashio

    发明人： Keiichiro Yamamoto ,  Kazutoshi Takashio

    IPC分类号： C07H19/06

    CPC分类号： A61K31/787 ,  A61K47/60 ,  A61K47/645 ,  C08G69/10 ,  C08G69/40 ,  C08G69/48

    摘要： [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a high therapeutic effect at a low dose.[Means For Solving Problems] Disclosed is a high molecular weight derivative of a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the carboxyl group in the side chain is bound to a hydroxyl group in the nucleoside derivative via an ester bond. Also disclosed is a method for producing the high molecular weight derivative.

    摘要翻译： [问题]需要可以在低剂量下显示高治疗效果的核酸抗代谢物的衍生物。 解决问题的手段公开了核酸抗代谢物的高分子量衍生物，其特征在于包含高分子量化合物，其包含聚乙二醇部分和在侧链具有羧基的聚合物部分和核苷衍生物 其可以作为核酸抗代谢物，其中侧链中的羧基通过酯键与核苷衍生物中的羟基结合。 还公开了高分子量衍生物的制造方法。