发明名称 |
Insulin analogues containing <i>penta</i>-fluoro-Phenylalanine at position B24 |
摘要 |
An insulin analog comprises a B-chain polypeptide incorporating a halogenated phenylalanine at position B24, B25 or B26. The halogenated phenylalanine may be ortho-monofluoro-phenylalanine, ortho-monobromo-phenylalanine, ortho-monochloro-phenylalanine, or para-monochloro-phenylalanine or penta-fluoro-Phenylalanine at position B24 alone or in combination with an acidic substitution (Aspartic Acid or Glutamic Acid) at position B10. The analog may be of a mammalian insulin, such as human insulin. A nucleic acid encodes such an insulin analog. The halogenated insulin analogs retain significant activity. A method of treating a patient comprises administering a physiologically effective amount of the insulin analog or a physiologically acceptable salt thereof to a patient. Halogen substitution-based stabilization of insulin may enhance the treatment of diabetes mellitus in regions of the developing world lacking refrigeration. |
申请公布号 |
US9200053(B2) |
申请公布日期 |
2015.12.01 |
申请号 |
US201314046620 |
申请日期 |
2013.10.04 |
申请人 |
Case Western Reserve University |
发明人 |
Weiss Michael |
分类号 |
A61K38/28;C07K14/62;A61K38/00 |
主分类号 |
A61K38/28 |
代理机构 |
Hahn Loeser & Parks LLP |
代理人 |
Hahn Loeser & Parks LLP |
主权项 |
1. An insulin analogue comprising an insulin B-chain polypeptide modified by penta-fluoro-Phenylalanine at position B24. |
地址 |
Cleveland OH US |