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    Segmented chelating polymers as imaging and therapeutic agents
    5.
    发明授权
    Segmented chelating polymers as imaging and therapeutic agents 失效
    分段螯合聚合物作为成像和治疗剂

    公开(公告)号：US5730968A

    公开(公告)日：1998-03-24

    申请号：US221714

    申请日：1994-03-31

    申请人： Dennis E. Butterfield ,  Dennis K. Fujii ,  David L. Ladd ,  Robert A. Snow ,  Julia S. Tan ,  John L. Toner

    发明人： Dennis E. Butterfield ,  Dennis K. Fujii ,  David L. Ladd ,  Robert A. Snow ,  Julia S. Tan ,  John L. Toner

    IPC分类号： A61K47/48 ,  A61K51/00 ,  C08G65/32 ,  C08G65/329 ,  A61K31/77 ,  A61K49/00 ,  C08G65/48

    CPC分类号： C08G65/329 ,  Y10S530/815 ,  Y10S530/816

    摘要： A composition suitable for use in diagnostic imaging or as a cell killing agent comprising a chelating residue linked via an amide linkage to a poly(alkylene oxide) moiety, said composition having a molecular weight of at least 4,500; ##STR1## wherein: Z is a chelating residue; Q is a divalent poly(alkylene oxidylene) moiety having a carbon terminus at R and at L; L represents an amide linkage; E.sup.(b) is one or more counterions each having a charge of b; b is an integer from 1, 2 and 3; n is an integer selected from the group 1, 2, 3 and 4; w is zero or an integer from 1 to 5; M.sup.(+a) is a cation, having a charge of +a; a is an integer from 1 to 4; r is 0 or an integer from 1 to 3, provided that when r is 2-3, each M.sup.(+a) can be the same or different cation; d is the total charge on the chelating residue and is an integer from 0 to 10; d+.SIGMA.(b.multidot.w)+.SIGMA.(a.multidot.r)=O; and R is a capping moiety chosen from the group consisting of hydrogen, hydroxyl, C.sub.1 -C.sub.4 alkyl, aryl containing 6 to 24 carbon atoms, C.sub.2 -C.sub.5 alkanoyloxyl and C.sub.1 -C.sub.4 alkoxy, or R is an immunoreactive group or cytotoxic drug linked to Q by a chemical bond or a linking group.

    摘要翻译： 适用于诊断成像或细胞杀伤剂的组合物，其包含通过酰胺键与聚（环氧烷）部分连接的螯合残基，所述组合物的分子量至少为4,500; 其中：Z是螯合残基; Q是在R和L具有碳末端的二价聚（亚烷基亚氧烷基）部分; L表示酰胺键; E（b）是一个或多个各自具有b的电荷的抗衡离子; b是1,2和3的整数; n是选自1,2,3,4组的整数; w为0或1〜5的整数; M（+ a）为阳离子，电荷为+ a; a是从1到4的整数; r为0或1〜3的整数，条件是当r为2-3时，每个M（+ a）可以是相同或不同的阳离子; d是螯合残基上的总电荷，为0至10的整数; d + SIGMA（bxw）+ SIGMA（axr）= O; 并且R是选自氢，羟基，C 1 -C 4烷基，含有6至24个碳原子的芳基，C 2 -C 5烷酰氧基和C 1 -C 4烷氧基的封端部分，或R是免疫反应性基团或与 Q通过化学键或连接基团。

    MR imaging compositions and methods
    7.
    发明授权
    MR imaging compositions and methods 失效
    MR成像组合物和方法

    公开(公告)号：US5817292A

    公开(公告)日：1998-10-06

    申请号：US960746

    申请日：1992-10-14

    申请人： Robert A. Snow ,  David L. Ladd ,  John L. Toner

    发明人： Robert A. Snow ,  David L. Ladd ,  John L. Toner

    IPC分类号： A61K49/06 ,  A61K49/12 ,  A61K49/00

    CPC分类号： A61K49/128

    摘要： This invention provides compositions useful in MR imaging comprising a polymer comprising units comprising the residue of a chelating agent linked to a poly(alkylene oxide) moiety, the polymer having a paramagetic metal ion associated therewith.

    摘要翻译： 本发明提供了可用于MR成像的组合物，其包含包含与聚（环氧烷）部分连接的螯合剂残基的单元的聚合物，所述聚合物具有与其相关的参与性金属离子。

    Segmented chelating polymers as imaging and therapeutic agents
    8.
    发明授权
    Segmented chelating polymers as imaging and therapeutic agents 失效
    分段螯合聚合物作为成像和治疗剂

    公开(公告)号：US6017522A

    公开(公告)日：2000-01-25

    申请号：US845421

    申请日：1997-04-25

    申请人： Dennis E. Butterfield ,  Dennis K. Fujii ,  David L. Ladd ,  Robert A. Snow ,  Julia S. Tan ,  John L. Toner

    发明人： Dennis E. Butterfield ,  Dennis K. Fujii ,  David L. Ladd ,  Robert A. Snow ,  Julia S. Tan ,  John L. Toner

    IPC分类号： A61K47/48 ,  A61K51/00 ,  C08G65/32 ,  C08G65/329 ,  A61K31/77 ,  A61K49/00 ,  C08G65/48

    CPC分类号： C08G65/329 ,  Y10S530/815 ,  Y10S530/816

    摘要： A composition suitable for use in diagnostic imaging or as a cell killing agent comprising a chelating residue linked via an amide linkage to a poly(alkylene oxide) moiety, said compisition having a molecular weight of at least 4,500; ##STR1## wherein: Z is a chelating residue;Q is a divalent poly(alkylene oxidylene) moiety having a carbon terminus at R and at L;L represents an amide linkage;E.sup.(b) is one or more counterions each having a charge of b;b is an integer from 1, 2 and 3;n is an integer selected from the group 1, 2, 3 and 4;w is zero or an integer from 1 to 5;M.sup.(+a) is a cation, having a charge of +a;a is an integer from 1 to 4;r is 0 or an integer from 1 to 3, provided that when r is 2-3, each M.sup.(+a) can be the same or different cation;d is the total charge on the chelating residue and is an integer from 0 to 10;d+.SIGMA.(b.multidot.w)+.SIGMA.(a.multidot.r)=O; andR is a capping moiety chosen from the group consisting of hydrogen, hydroxyl, C.sub.1 -C.sub.4 alkyl, aryl containing 6 to 24 carbon atoms, C.sub.2 -C.sub.5 alkanoyloxyl and C.sub.1 -C.sub.4 alkoxy, or R is an immunoreactive group or cytotoxic drug linked to Q by a chemical bond or a linking group.

    摘要翻译： 适合用于诊断成像的组合物或作为细胞杀伤剂的组合物，其包含通过酰胺键与聚（环氧烷）部分连接的螯合残基，所述制剂具有至少4,500的分子量; 其中：Z是螯合残基; Q是在R和L具有碳末端的二价聚（亚烷基亚氧烷基）部分; L表示酰胺键; E（b）是一个或多个各自具有b的电荷的抗衡离子; b是1,2和3的整数; n是选自1,2,3,4组的整数; w为0或1〜5的整数; M（+ a）为阳离子，电荷为+ a; a是从1到4的整数; r为0或1〜3的整数，条件是当r为2-3时，每个M（+ a）可以是相同或不同的阳离子; d是螯合残基上的总电荷，为0至10的整数; d + SIGMA（bxw）+ SIGMA（axr）= O; 并且R是选自氢，羟基，C 1 -C 4烷基，含有6至24个碳原子的芳基，C 2 -C 5烷酰氧基和C 1 -C 4烷氧基的封端部分，或R是免疫反应性基团或与 Q通过化学键或连接基团。

    Vinyl sulfone coupling of polyoxyalkylenes to proteins
    9.
    发明授权
    Vinyl sulfone coupling of polyoxyalkylenes to proteins 失效
    乙烯基砜偶联的聚氧化烯与蛋白质

    公开(公告)号：US5414135A

    公开(公告)日：1995-05-09

    申请号：US153553

    申请日：1993-11-16

    申请人： Robert A. Snow ,  David L. Ladd

    发明人： Robert A. Snow ,  David L. Ladd

    IPC分类号： C07C317/18 ,  C07K1/107 ,  C07K14/54 ,  C12N9/02 ,  C12N9/08 ,  C12N9/56 ,  C07C315/04 ,  C07C317/04

    CPC分类号： C12N9/0089 ,  C07C317/18 ,  C07K1/1077 ,  C07K14/5406 ,  C12N9/0065 ,  C12N9/54

    摘要： A new class of polyalkylene oxide vinyl sulfone reagents is described. Also described are a method by which these reagents can be prepared as well as a method for using them in hydrated media for the modification of proteins. The novel polymer-to-protein conjugates made by reacting these reagents with proteins have advantages over similar conjugates prepared with prior art reagents in that they are more stable against hydrolysis and retain the positive charge carrying capacity at amine sites at which the modifying reagents are attached.

    摘要翻译： 描述了一类新的聚环氧烷乙烯基砜试剂。 还描述了可以制备这些试剂的方法以及在水合培养基中用于蛋白质修饰的方法。 通过使这些试剂与蛋白质反应制备的新型聚合物 - 蛋​​白质缀合物具有优于使用现有技术试剂制备的相似共轭物的优点，因为它们对水解更稳定并且在修饰试剂连接的胺位置保留正电荷携带能力 。