USRE45313EExpiredUtilityPatentIndex 81

Exendin variant peptides

Assignee: ZEALAND PHARMA ASPriority: Jul 12, 1999Filed: Jul 17, 2013Granted: Dec 30, 2014

Est. expiryJul 12, 2019(expired)· nominal 20-yr term from priority

Inventors:LARSEN BJARNE DUE MIKKELSEN JENS DAMSGAARD NEVE SØREN

A61P 3/10A61K 47/62C07K 14/605A61K 38/00C07K 14/57563A61K 38/26A61P 3/04

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Claims

Abstract

The present invention relates to novel peptide conjugates which have increased stability and are useful in the treatment of excess levels of blood glucose.

Claims

exact text as granted — not AI-modified

What is claimed is: 
     
       1. A peptide consisting of any one of the following sequences:
 a) H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-(Lys) 6 -NH 2  (des-Pro 36 -exendin-4(1-39)-Lys 6 -NH 2 ) (SEQ ID NO:93),   b) H-Lys 6 -His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-(Lys) 6 -NH 2  (H-Lys 6 -des Pro 36 exendin-4(1-39)-Lys 6 -NH 2 ) (SEQ ID NO: 149),   c) H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-NH 2  (H-des Pro 36 ,Pro 37 ,Pro 38 exendin-4 (1-39)-NH 2 ) (SEQ ID NO: 132),   d) H-Lys-Lys-Lys-Lys-Lys-Lys-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-NH 2  (H-(Lys) 6 -des Pro 36 ,Pro 37 ,Pro 38 exendin-4(1-39)-NH 2 ), (SEQ ID NO: 134),   e) H-Asn-Glu-Glu-Glu-Glu-Glu-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-NH 2  (H-Asn-(Glu) 5 -des Pro 36 ,Pro 37 , Pro 38 exendin-4(1-39)-NH 2 ) (SEQ ID NO: 137),   f) H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-(Lys) 6 -NH 2  (des Pro 36 , Pro 37 ,Pro 38 exendin-4 (1-39)-(Lys) 6 -NH 2 ) (SEQ ID NO: 133),   g) H-(Lys) 6 -His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-(Lys) 6 -NH 2  (H-(Lys) 6 -des Pro 36 ,Pro 37 , Pro 38 exendin-4(1-39)-(Lys) 6 -NH 2 ) (SEQ ID NO: 135),   h) H-Asp-Glu-Glu-Glu-Glu-Glu-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-(Lys) 6 -NH 2  (H-Asn-(Glu) 5 -des Pro 36 ,Pro 37 ,Pro 38 exendin-4(1-39)-(Lys) 6 -NH 2 ) (SEQ ID NO: 136);   or a pharmaceutically acceptable salt thereof.   
     
     
       2. A composition comprising the peptide of  claim 1  and a physiologically acceptable carrier. 
     
     
       3. A peptide consisting of the sequence H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-(Lys) 6 -NH 2  (des-Pro 36 -exendin-4(1-39)-Lys 6 -NH 2 ) (SEQ ID NO:93), or a pharmaceutically acceptable salt thereof. 
     
     
       4. A composition comprising the peptide of claim 3 and a physiologically acceptable carrier.

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