Insulin derivatives
    3.
    发明授权
    Insulin derivatives 有权
    胰岛素衍生物

    公开(公告)号:US08476228B2

    公开(公告)日:2013-07-02

    申请号:US13273659

    申请日:2011-10-14

    IPC分类号: A61K38/28 C07K14/62

    CPC分类号: A61K38/28 C07K14/62

    摘要: The present invention relates to insulin derivatives having a side chain attached either to the α-amino group of the N-terminal amino acid residue of the B chain or to the ε-amino group of a Lys residue present in the B chain of the parent insulin via an amide bond which side chain comprises at least one aromatic group; at least one free carboxylic acid group or a group which is negatively charged at neutral pH, a fatty acid moiety with 4 to 22 carbon atoms in the carbon chain; and possible linkers which link the individual components in the side chain together via amide bonds.

    摘要翻译: 本发明涉及具有侧链连接到B链的N末端氨基酸残基的α-氨基或母体B链中存在的Lys残基的ε-氨基的胰岛素衍生物 胰岛素通过酰胺键,该侧链包含至少一个芳族基团; 至少一个游离羧酸基团或在中性pH下带负电荷的基团,碳链中具有4-22个碳原子的脂肪酸部分; 以及通过酰胺键将侧链中各个组分连接在一起的可能接头。

    PEGylated, extended insulins
    7.
    发明授权
    PEGylated, extended insulins 失效
    聚乙二醇化,延长胰岛素

    公开(公告)号:US08710001B2

    公开(公告)日:2014-04-29

    申请号:US13224538

    申请日:2011-09-02

    IPC分类号: A61K38/28

    CPC分类号: A61K38/28 A61K47/60

    摘要: PEGylated, extended insulins are insulins which, compared with human insulin, has one or more extensions extended from the A1, B1, A21 and/or B30 position(s), said extension(s) consist(s) of amino acid residue(s) and wherein a PEG moiety, via a linker, is attached to one or more of the amino acid residues in the extension(s). PEG is polyethyleneglycol. Such PEGylated, extended insulins have higher bioavailability and a longer time-action profile than regular insulin and are in particular suited for pulmonary administration and can, conveniently, be used to treat diabetes.

    摘要翻译: 聚乙二醇化的延长胰岛素是胰岛素,其与人胰岛素相比具有从A1,B1,A21和/或B30位置延伸的一个或多个延伸,所述延伸部分包含氨基酸残基(s) ),并且其中通过接头的PEG部分连接到延伸中的一个或多个氨基酸残基。 PEG是聚乙二醇。 这种聚乙二醇化的延长的胰岛素具有比常规胰岛素更高的生物利用度和更长的时间作用特征,并且特别适合于肺部给药,并且可以方便地用于治疗糖尿病。

    Pegylated, Extended Insulins
    8.
    发明申请
    Pegylated, Extended Insulins 审中-公开
    聚乙二醇化,延长胰岛素

    公开(公告)号:US20090306337A1

    公开(公告)日:2009-12-10

    申请号:US12375678

    申请日:2007-07-16

    IPC分类号: C07K14/62

    CPC分类号: A61K38/28 A61K47/60

    摘要: PEGylated, extended insulins are insulins which, compared with human insulin, has one or more extensions extended from the A1, B1, A21 and/or B30 position(s), said extension(s) consist(s) of amino acid residue(s) and wherein a PEG moiety, via a linker, is attached to one or more of the amino acid residues in the extension(s). PEG is polyethyleneglycol. Such PEGylated, extended insulins have higher bioavailability and a longer time-action profile than regulär insulin and are in particular suited for pulmonary administration and can, conveniently, be used to treat diabetes.

    摘要翻译: 聚乙二醇化的延长胰岛素是胰岛素,其与人胰岛素相比具有从A1,B1,A21和/或B30位置延伸的一个或多个延伸,所述延伸部分包含氨基酸残基(s) ),并且其中通过接头的PEG部分连接到延伸中的一个或多个氨基酸残基。 PEG是聚乙二醇。 这种聚乙二醇化的延长胰岛素具有比调节胰岛素更高的生物利用度和更长的时间作用特征,并且特别适合于肺部给药,并且可以方便地用于治疗糖尿病。

    PEGYLATED, EXTENDED INSULINS
    9.
    发明申请
    PEGYLATED, EXTENDED INSULINS 失效
    PEGYLATED,EXTENDED INSULINS

    公开(公告)号:US20110319591A1

    公开(公告)日:2011-12-29

    申请号:US13224538

    申请日:2011-09-02

    IPC分类号: C07K14/62

    CPC分类号: A61K38/28 A61K47/60

    摘要: PEGylated, extended insulins are insulins which, compared with human insulin, has one or more extensions extended from the A1, B1, A21 and/or B30 position(s), said extension(s) consist(s) of amino acid residue(s) and wherein a PEG moiety, via a linker, is attached to one or more of the amino acid residues in the extension(s). PEG is polyethyleneglycol. Such PEGylated, extended insulins have higher bioavailability and a longer time-action profile than regular insulin and are in particular suited for pulmonary administration and can, conveniently, be used to treat diabetes.

    摘要翻译: 聚乙二醇化的延长胰岛素是胰岛素,其与人胰岛素相比具有从A1,B1,A21和/或B30位置延伸的一个或多个延伸,所述延伸部分包含氨基酸残基(s) ),并且其中通过接头的PEG部分连接到延伸中的一个或多个氨基酸残基。 PEG是聚乙二醇。 这种聚乙二醇化的延长的胰岛素具有比常规胰岛素更高的生物利用度和更长的时间作用特征,并且特别适合于肺部给药,并且可以方便地用于治疗糖尿病。