US2004127398A1PendingUtilityA1

Long lasting synthetic glucagon like peptide (GLP-1)

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Assignee: CONJUCHEM INCPriority: May 17, 1999Filed: Nov 25, 2003Published: Jul 1, 2004
Est. expiryMay 17, 2019(expired)· nominal 20-yr term from priority
Inventors:Dominique P. BridonBenoit L'ArchevequeAlan M. EzrinDarren L. HolmesAnouk LeblancSerge St. Pierre
A61P 3/10C07K 14/605A61K 38/00C07K 14/57563A61K 47/643C12N 2740/16122A61P 1/00C07K 14/005
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Claims

Abstract

Modified insulinotropic peptides are disclosed. The modified insulinotropic peptides are capable of forming a peptidase stabilized insulinotropic peptide. The modified insulinotropic peptides are capable of forming covalent bonds with one or more blood components to form a conjugate. The conjugates may be formed in vivo or ex vivo. The modified peptides are administered to treat humans with diabetes and other related diseases.

Claims

exact text as granted — not AI-modified
We claim:  
     
         1 . A modified insulinotropic peptide or derivative thereof comprising a reactive group which reacts with amino groups, hydroxyl groups or thiol groups on blood components to form a stable covalent bond.  
     
     
         2 . The peptide of  claim 1  wherein said reactive group is selected from the group consisting of succinimidyl and maleimido groups.  
     
     
         3 . A peptide according to  claim 2 , wherein the derivative is reactive with a thiol group on a blood protein.  
     
     
         4 . A peptide according to  claim 1  wherein the peptide is selected from the group consisting of SEQ ID NO:2 SEQ ID NO:3, SEQ ID NO:11, SEQ ID NO:13, SEQ ID NO:14 and SEQ ID NO:15.  
     
     
         5 . A peptide according to  claim 1  wherein the peptide is selected from the group consisting of SEQ ID:16, SEQ ID NO:17, SEQ ID NO:18, SEQ ID NO:19, SEQ ID NO:20, SEQ ID NO:21 and SEQ ID NO:22.  
     
     
         6 . A composition comprising a derivative of insulinotropic peptide or analog thereof, said derivative comprising a reactive group which reacts with amino groups, hydroxyl groups or thiol groups on blood components to form stable covalent bonds wherein said reactive group is selected from the group consisting of succinimidyl and maleimido groups for use in a method of treating diabetes in a human.  
     
     
         7 . The composition of  claim 6  wherein said derivative is reactive with blood components.  
     
     
         8 . The composition of  claim 6  wherein said peptide is selected from the group consisting of SEQ ID NO:2 SEQ ID NO:3, SEQ ID NO:11, SEQ ID NO:13, SEQ ID NO:14 and SEQ ID NO:15.  
     
     
         9 . The composition of  claim 6  wherein said peptide is selected from the group consisting of SEQ ID:16, SEQ ID NO:17, SEQ ID NO:18, SEQ ID NO:19, SEQ ID NO:20, SEQ ID NO:21 and SEQ ID NO:22.  
     
     
         10 . A derivative of an insulintropic peptide, said derivative comprising a maleimido group which reacts with a thiol group on human serum albumin to form a covalent bond.  
     
     
         11 . The derivative of  claim 9  wherein said peptide is selected from the group consisting of SEQ ID NO:2 SEQ ID NO:3, SEQ ID NO:11, SEQ ID NO:13, SEQ ID NO:14 and SEQ ID NO:15.  
     
     
         12 . The derivative of  claim 9  wherein said peptide is selected from the group consisting of SEQ ID:16, SEQ ID NO:17, SEQ ID NO:18, SEQ ID NO:19, SEQ ID NO:20, SEQ ID NO:21 and SEQ ID NO:22.  
     
     
         13 . A composition comprising a derivative of an insulinotropic peptide, said derivative comprising a maleimido group which reacts with a thiol group on human serum albumin to form a covalent bond for use in a method of treating diabetes in a human.  
     
     
         14 . The composition of  claim 13  wherein the peptide is selected from the group consisting of SEQ ID NO:2 SEQ ID NO:3, SEQ ID NO:11, SEQ ID NO:13, SEQ ID NO:14 and SEQ ID NO:15.  
     
     
         15 . The compositions of  claim 13  wherein the peptide is selected from the group consisting of SEQ ID:16, SEQ ID NO:17, SEQ ID NO:18, SEQ ID NO:19, SEQ ID NO:20, SEQ ID NO:21 and SEQ ID NO:22.  
     
     
         16 . Use of a composition for the manufacturer of a medicament extending the in vivo half-life of an insulinotropic peptide in a diabetes patient the composition comprising a derivative of an insulinotropic peptide or analog thereof, said derivative comprising a reactive group which reacts with amino groups, hydroxo gropus, or thiol groups on blood components to form stable covalent bonds, wherein the reactive group is selected from the group consisting of succinimidyl and maleimido groups.  
     
     
         17 . Use of a composition according to  claim 16 , wherein the derivative is reacted with blood proteins.  
     
     
         18 . Use of the composition of  claim 16  wherein said peptide is selected from the group consisting of SEQ ID NO:2 SEQ ID NO:3, SEQ ID NO:11, SEQ ID NO:13, SEQ ID NO:14 and SEQ ID NO:15.  
     
     
         19 . An insulinotropic peptide selected from the group consisting of GLP-1(1-36)-Lys 37 (ε-MPA)-NH 2 , GLP-1(1-36)-Lys 37 (ε-AEEA-AEEA-MPA)-NH 2 , GLP-1(7-36)-Lys 37  (ε-MPA)-NH 2 , GLP-1(7-36)-Lys 37  (ε-AEEA-AEEA-MPA)-NH 2 , D-Ala 2  GLP-1(7-36)-Lys 37 -(C-MPA)-NH 2 , D-Ala 2  GLP-1(7-36)-Lys 37  (ε-AEEA-AEEA-MPA)-NH 2 , exendin-4 (1-39)-Lys 40  (ε-MPA)-NH 2 , exendin-4(1-39)-Lys 40  (ε-AEEA-AEEA-MPA)-NH 2 , exendin-3(1-39)-Lys 40  (ε-MPA)-NH 2  and exendin-3(1-39)-Lys 40  (ε-AEEA-AEEA-MPA).

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