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    Rapid Acting Insulin Analogues
    1.
    发明申请
    Rapid Acting Insulin Analogues 有权
    快速作用胰岛素类似物

    公开(公告)号：US20110021423A1

    公开(公告)日：2011-01-27

    申请号：US12673226

    申请日：2008-08-12

    申请人： Helle Birk Olsen ,  Thomas Børglum Kjeldsen ,  Per Balschmidt ,  Tine Glendorf ,  Svend Havelund

    发明人： Helle Birk Olsen ,  Thomas Børglum Kjeldsen ,  Per Balschmidt ,  Tine Glendorf ,  Svend Havelund

    IPC分类号： A61K38/28 ,  C07K14/62 ,  A61P3/10

    CPC分类号： C07K14/62 ,  A61K38/00

    摘要： The invention is related to fast acting insulin analogues which can form soluble mix-tures (pre-mixed or self-mixed) with long acting insulin analogues. The fast action is achieved through monomerizing substitutions/deletions in the C-terminus of the B-chain of human insulin and the mixability with long acting insulin analogues is achieved through a substitution of the Zn-binding His in position B10 of human insulin with a Gln amino acid residue. In one embodiment the invention is related to fast acting insulin analogues in which at least one of the natural amino acid residues in position B22-B30 in the human B-chain has been substituted with another amino acid residue having the effect of promoting formation of the monomeric form of insulin, the His amino acid residue in position 10 in the B-chain is substituted with a Gln and wherein further one or more of the amino acid residues in position B22-B30 optionally have been deleted.

    摘要翻译： 本发明涉及可与长效胰岛素类似物形成可溶性混合物（预混合或自混合）的快速作用胰岛素类似物。 快速作用通过在人胰岛素的B链的C末端进行单体取代/缺失实现，并且通过用人胰岛素B10位置上的Zn结合His取代长效胰岛素类似物的混合性来实现 Gln氨基酸残基。 在一个实施方案中，本发明涉及快速作用的胰岛素类似物，其中人B链中位置B22-B30中的至少一个天然氨基酸残基已经被另一个氨基酸残基取代，其具有促进形成 单体形式的胰岛素，B链中10位的His氨基酸残基被Gln取代，并且其中位置B22-B30中的一个或多个氨基酸残基任选地被缺失。

    Rapid acting insulin analogues
    2.
    发明授权
    Rapid acting insulin analogues 有权
    快速作用胰岛素类似物

    公开(公告)号：US08575096B2

    公开(公告)日：2013-11-05

    申请号：US12673226

    申请日：2008-08-12

    申请人： Helle Birk Olsen ,  Thomas Børglum Kjeldsen ,  Per Balschmidt ,  Tine Glendorf ,  Svend Havelund

    发明人： Helle Birk Olsen ,  Thomas Børglum Kjeldsen ,  Per Balschmidt ,  Tine Glendorf ,  Svend Havelund

    IPC分类号： C07K14/62

    CPC分类号： C07K14/62 ,  A61K38/00

    摘要： The invention is related to fast acting insulin analogues which can form soluble mix-tures (pre-mixed or self-mixed) with long acting insulin analogues. The fast action is achieved through monomerizing substitutions/deletions in the C-terminus of the B-chain of human insulin and the mixability with long acting insulin analogues is achieved through a substitution of the Zn-binding His in position B10 of human insulin with a Gln amino acid residue. In one embodiment the invention is related to fast acting insulin analogues in which at least one of the natural amino acid residues in position B22-B30 in the human B-chain has been substituted with another amino acid residue having the effect of promoting formation of the monomeric form of insulin, the His amino acid residue in position 10 in the B-chain is substituted with a Gln and wherein further one or more of the amino acid residues in position B22-B30 optionally have been deleted.

    摘要翻译： 本发明涉及可与长效胰岛素类似物形成可溶性混合物（预混合或自混合）的快速作用胰岛素类似物。 快速作用通过在人胰岛素的B链的C末端进行单体取代/缺失实现，并且通过用人胰岛素B10位置上的Zn结合His取代长效胰岛素类似物的混合性来实现 Gln氨基酸残基。 在一个实施方案中，本发明涉及快速作用的胰岛素类似物，其中人B链中位置B22-B30中的至少一个天然氨基酸残基已经被另一个氨基酸残基取代，其具有促进形成 单体形式的胰岛素，B链中10位的His氨基酸残基被Gln取代，并且其中位置B22-B30中的一个或多个氨基酸残基任选地被缺失。

    PEGYLATED, EXTENDED INSULINS
    10.
    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

    申请人： Peter Madsen ,  Thomas Børglum Kjeldsen ,  Tina Møller Tagmose ,  Palle Jackobsen

    发明人： Peter Madsen ,  Thomas Børglum Kjeldsen ,  Tina Møller Tagmose ,  Palle Jackobsen

    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。