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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。

    Soluble, stable insulin-containing formulations with a protamine salt
    6.
    发明授权
    Soluble, stable insulin-containing formulations with a protamine salt 有权
    可溶性，稳定的含有鱼精蛋白盐的含胰岛素的制剂

    公开(公告)号：US08263551B2

    公开(公告)日：2012-09-11

    申请号：US11791064

    申请日：2005-11-21

    申请人： Helle Birk Olsen ,  Niels Christian Kaarsholm ,  Per Balschmidt

    发明人： Helle Birk Olsen ,  Niels Christian Kaarsholm ,  Per Balschmidt

    IPC分类号： A61K38/17 ,  A61K38/28

    CPC分类号： A61K38/28 ,  A61K9/0019 ,  A61K47/42

    摘要： The present invention relates to pharmaceutical formulations comprising insulin, an insulin analog, an insulin derivative, or a combination of any of the foregoing, and a salt of protamine, to methods of preparing such formulations, and to uses of such formulations in the treatment of diseases and conditions for which use of the insulin peptide(s) contained in such formulations is indicated. The present invention further relates to methods for increasing the stability and/or solubility of insulin in insulin-containing formulations at a pH less than 7.0 by adding a salt of protamine to the insulin-containing formulations.

    摘要翻译： 本发明涉及包含胰岛素，胰岛素类似物，胰岛素衍生物，或前述任何一种的组合和鱼精蛋白盐的药物制剂，以及制备这些制剂的方法，以及这些制剂在治疗中的用途 指示使用这些制剂中所含的胰岛素肽的疾病和病症。 本发明还涉及通过向含有胰岛素的制剂中加入鱼精蛋白盐来增加胰岛素在含胰岛素制剂中的pH小于7.0的稳定性和/或溶解度的方法。

    Soluble, Stable Insulin-Containing Formulations with a Protamine Salt
    8.
    发明申请
    Soluble, Stable Insulin-Containing Formulations with a Protamine Salt 有权
    可溶性，稳定的含有鱼精蛋白盐的含胰岛素的制剂

    公开(公告)号：US20110046049A1

    公开(公告)日：2011-02-24

    申请号：US11791064

    申请日：2005-11-21

    申请人： Helle Birk Olsen ,  Niels Christian Kaarsholm ,  Per Balschmidt

    发明人： Helle Birk Olsen ,  Niels Christian Kaarsholm ,  Per Balschmidt

    IPC分类号： A61K38/28 ,  A61P3/10

    CPC分类号： A61K38/28 ,  A61K9/0019 ,  A61K47/42

    摘要： The present invention relates to pharmaceutical formulations comprising insulin, an insulin analog, an insulin derivative, or a combination of any of the foregoing, and a salt of protamine, to methods of preparing such formulations, and to uses of such formulations in the treatment of diseases and conditions for which use of the insulin peptide(s) contained in such formulations is indicated. The present invention further relates to methods for increasing the stability and/or solubility of insulin in insulin-containing formulations at a pH less than 7.0 by adding a salt of protamine to the insulin-containing formulations.

    摘要翻译： 本发明涉及包含胰岛素，胰岛素类似物，胰岛素衍生物，或前述任何一种的组合和鱼精蛋白盐的药物制剂，以及制备这些制剂的方法，以及这些制剂在治疗中的用途 指示使用这些制剂中所含的胰岛素肽的疾病和病症。 本发明还涉及通过向含有胰岛素的制剂中加入鱼精蛋白盐来增加胰岛素在含胰岛素制剂中的pH小于7.0的稳定性和/或溶解度的方法。