US2003096752A1PendingUtilityA1

Aprotinin variants having improved properties

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Priority: Jul 25, 1996Filed: Sep 23, 2002Published: May 22, 2003
Est. expiryJul 25, 2016(expired)· nominal 20-yr term from priority
A61P 43/00A61P 7/04A61P 29/00C07K 14/8117A61P 17/00A61K 38/00C07K 14/8114A61K 38/16C07K 14/81
46
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Claims

Abstract

The present invention relates to aprotinin variants having improved enzyme-inhibitory, immunological and pharmacokinetic properties and their preparation.

Claims

exact text as granted — not AI-modified
1 . Aprotinin variants having a net charge of +3 to −3 at pH 7 and with the amino acids Arg15 or Arg15-Ala17 in the binding region.  
     
     
         2 . Aprotinin variants according to  claim 1  for the inhibition of serine proteases.  
     
     
         3 . Aprotinin variants according to  claim 1  having a modified N-terminal sequence.  
     
     
         4 . Aprotinin variants according to  claim 1  having an N-terminal extension or contraction or having deleted amino acids in the N-terminus.  
     
     
         5 . Aprotinin variants from the group consisting of DesPro2-Ser10-Arg15-Ala17-Asp24-Thr26-Glu31-Asn41-Glu53-aprotinin, DesPro2-Ser10-Arg15-Asp24-Thr26-Glu31-Asn41-Glu53-aprotinin, DesPro2-Ser10-Arg15-Ser17-Asp24-Thr26-Glu31-Asn41-Glu53-aprotinin, DesPro2-Ser10-Arg15-Ala17-Thr26-Glu31-Asn41-Glu53-aprotinin, DesPro2-Ser10-Arg15-Ala17-Asp24-Thr26-Asn41-Glu53-aprotinin, Ser10-Arg15-Ala17-Asp24-Thr26-Glu31-Asn41-Glu53-aprotinin, Ser10-Arg15-Asp24-Thr26-Glu31-Asn41-Glu53-aprotinin, Ser10-Arg15-Ser17-Asp24-Thr26-Glu31-Asn41-Glu53-aprotinin, Ser10-Arg15-Ala17-Thr26-Glu31-Asn41-Glu53-aprotinin and Ser10-Arg15-Ala17-Asp24-Thr26-Asn41-Glu53-aprotinin.  
     
     
         6 . Medicaments comprising one or more of the aprotinin variants according to  claim 1.

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