Novel insulin derivatives having a rapid onset of action

Details Novel insulin derivatives having a rapid onset of action Novel insulin derivatives having a rapid onset of action

C - Chemistry, Metallurgy

12

N

C12N 15/17 (2006.01) A61K 38/28 (2006.01) C07K 14/62 (2006.01) C12P 21/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2235443

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.

La présente invention concerne des dérivés de l'insuline qui, comparativement à l'insuline humaine, commencent à agir plus rapidement, ainsi qu'un mode de préparation et d'utilisation de ces dérivés, notamment dans des préparations pharmaceutiques pour le traitement du diabète sucré. La présente invention concerne en particulier des dérivés de l'insuline ou des sels physiologiquement tolérables de ces dérivés, dans lesquels l'asparagine (Asn) en position B3 de la chaîne B est remplacée par un résidu naturel d'acide aminé et dans lesquels au moins un résidu d'acide aminé en position B27, B28 ou B29 de la chaîne B est remplacé par un autre résidu naturel d'acide aminé, avec la possibilité que l'asparagine (Asn) en position 21 de la chaîne A soit remplacée par Asp, Gly, Ser, Thr ou Ala et que la phénylalanine (Phe) en position B1 de la chaîne B et le résidu d'acide aminé en position B30 de la chaîne B soient absents.

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