Long lasting synthetic glucagon like peptide (GLP-1)

• US 20060058235A1
• Filed: 08/30/2005
• Published: 03/16/2006
• Est. Priority Date: 05/17/1999
• Status: Active Grant

• Current Assignee: ConjuChem LLC (Colabor Group, Inc.)
• Original Assignee: ConjuChem, Inc. (Colabor Group, Inc.)
• Inventors: Bridon, Dominique P., Ezrin, Alan M., Leblanc, Anouk, L'Archeveque, Benoit, Holmes, Darren L., St. Pierre, Serge
• Granted Patent: US 8,084,414 B2
• Time in Patent Office: Days
• US Class Current: 435/5
• CPC Class Codes: A61K 38/00 Medicinal preparations containing peptides peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00
• CPC Class Codes: A61K 47/643 Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: C07K 14/005 from viruses
• CPC Class Codes: C07K 14/57563 Vasoactive intestinal peptide [VIP]; Related peptides
• CPC Class Codes: C07K 14/605 Glucagons
• CPC Class Codes: C12N 2740/16122 New viral proteins or individual genes, new structural or functional aspects of known viral proteins or genes

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

1-19. -19. (canceled)

20. A method for treating diabetes in a patient, comprising administering to the patient an effective amount of a modified insulinotropic peptide comprising exendin-4 (1-39)-Lys⁴⁰ (a-MPA)-NH₂.

22. The method of claim 20, wherein said modified insulinotropic peptide is covalently bonded to a blood component.

23. The method of claim 22, wherein said blood component is serum albumin.

26. The method of claim 20, wherein said modified insulinotropic peptide is in association with a physiologically acceptable medium.

28. The method of claim 22, wherein said modified insulinotropic peptide is in association with a physiologically acceptable medium.

29. The method of claim 23, wherein said modified insulinotropic peptide is in association with a physiologically acceptable medium.

44. The method of claim 20 wherein said modified insulinotropic peptide is cavalently bonded to albumin.

46. The method of claim 44 wherein said albumin is purified from blood.

21. A method for treating diabetes in a patient, comprising administering to the patient an effective amount of a modified insulinotropic peptide comprising exendin-4 (1-39)-Lys⁴⁰ (ε

-AEEA-MPA)-NH₂,

24. The method of claim 21, wherein said modified insulinotropic peptide is covalently bonded to a blood component.

25. The method of claim 24, wherein said blood component is serum albumin.

27. The method of claim 21, wherein said modified insulinotropic peptide is in association with a physiologically acceptable medium.

30. The method of claim 24, wherein said modified insulinotropic peptide is in association with a physiologically acceptable medium.

31. The method of claim 25, wherein said modified insulintropic peptide is in association with a physiologically acceptable medium.

45. The method of claim 21 wherein said modified insulinotropic peptide is covalently bonded to albumin

47. The method of claim 45 wherein said albumin is purified from blood.

32. A method for enhancing the expression of insulin in a patient, comprising administering to the patient an effective amount of a modified insulinotropic peptide comprising exendin-4 (1-39).Lys⁴⁰ (ε

-MPA)-NH₂.

34. The method of claim 32, wherein said modified insulinotropic peptide is covalently bonded to a blood component.

35. The method of claim 34, wherein said blood component is serum albumin.

38. The method of claim 32, wherein said modified insulinotropic peptide is in association with a physiologically acceptable medium.

40. The method of claim 34, wherein said modified insulinotropic peptide is in association with a physiologically acceptable medium.

41. The method of claim 35, wherein said modified insulinotropic peptide is in association with a physiologically acceptable medium.

48. The method of claim 32 wherein said modified insulinotropic peptide is covalently bonded to albumin.

50. The method of claim 48 wherein said albumin is purified from blood.

33. A method for enhancing the expression of insulin in a patient, comprising administering to the patient an effective amount of a modified insulinotropic peptide comprising exendin-4 (1-39Lys⁴⁰ (ε

-AEEA-MPA)-NH₂.

36. The method of claim 33, wherein said modified insulinotropic peptide is covalently bonded to a blood component.

37. The method of claim 36, wherein said blood component is serum albumin.

39. The method of claim 33, wherein said modified insulinotropic peptide is in association with a physiologically acceptable medium.

42. The method of claim 36, wherein said modified insulinotropic peptide is in association with a physiologically acceptable medium.

43. The method of claim 37, wherein said modified insulinotropic peptide is in association with a physiologically acceptable medium.

49. The method of claim 33 wherein said modified insulinotropic peptide is covalenly bonded to albumin.

51. The method of claim 49 wherein said albumin is purified from blood.