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    • 7. 发明授权
    • Insulin derivatives having a rapid onset of action
    • 具有快速起效的胰岛素衍生物
    • US06221633B1
    • 2001-04-24
    • US09099307
    • 1998-06-18
    • Johann ErtlPaul HabermannKarl GeisenGerhard Seipke
    • Johann ErtlPaul HabermannKarl GeisenGerhard Seipke
    • C12N1517
    • C07K14/62A61K38/00C07K2319/00Y10S514/866
    • The present invention relates to insulin derivatives which in comparison to human insulin, have an accelerated onset of action, to a process for their preparation and to their use, in particular in pharmaceutical preparations for the treatment of diabetes mellitus. In particular, the present invention relates to insulin derivatives or physiologically tolerable salts thereof in which asparagine (Asn) in position B3 of the B chain is replaced by a naturally occurring basic amino acid residue and at least one amino acid residue in the positions B27, B28 or B29 of the B chain is replaced by another naturally occurring amino acid residue, it optionally being possible for asparagine (Asn) in position 21 of the A chain to be replaced by Asp, Gly, Ser, Thr or Ala and for phenylalanine (Phe) in position B1 of the B chain and the amino acid residue in position B30 of the B chain to be absent.
    • 本发明涉及与人胰岛素相比,加速起效的胰岛素衍生物,其制备方法及其用途,特别是用于治疗糖尿病的药物制剂中。 特别地,本发明涉及胰岛素衍生物或其生理上可耐受的盐,其中B链B3位的天冬酰胺(Asn)被天然存在的碱性氨基酸残基和B27位置的至少一个氨基酸残基所取代, B链的B28或B29被另一个天然存在的氨基酸残基替代,其任选可能是由A,A,D,Gly,Ser,Thr或Ala代替的A链的第21位的天冬酰胺(Asn)和苯丙氨酸 Phe)在B链的位置B1和B链的位置B30的氨基酸残基不存在。