Glucagon/GLP-1 receptor co-agonists

• US 9,156,902 B2
• Filed: 06/12/2012
• Issued: 10/13/2015
• Est. Priority Date: 06/22/2011
• Status: Expired due to Fees

• Current Assignee: Indiana University Research & Technology Corporation (Indiana University)
• Original Assignee: Indiana University Research & Technology Corporation (Indiana University)
• Inventors: DiMarchi, Richard D., Smiley, David L.
• Primary Examiner(s): Chandra, Gyan
• Application Number:
  US13/494,484
• Publication Number:
  US 20120329708A1
• Time in Patent Office: 1,218 Days
• Field of Search: 514/7.2
• US Class Current: 1/1
• 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 38/26 Glucagons
• CPC Class Codes: A61K 39/3955 against proteinaceous materials, e.g. enzymes, hormones, lymphokines
• CPC Class Codes: A61K 47/60 the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
• CPC Class Codes: A61K 49/00 Preparations for testing in vivo
• CPC Class Codes: A61P 1/16 for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/14 for treating abnormal movements, e.g. chorea, dyskinesia
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 3/08 for glucose homeostasis pancreatic hormones A61P5/48
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07K 14/605 Glucagons
• CPC Class Codes: C07K 16/283 against Fc-receptors, e.g. CD16, CD32, CD64 CD23 C07K16/2851
• CPC Class Codes: C07K 2319/00 : Fusion polypeptide
• CPC Class Codes: C07K 2319/30 : Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto
• CPC Class Codes: C07K 2319/33 : fusions for targeting to specific cell types, e.g. tissue specific targeting, targeting of a bacterial subspecies
• CPC Class Codes: G01N 2333/605 : Glucagons
• CPC Class Codes: G01N 2800/042 : Disorders of carbohydrate metabolism, e.g. diabetes, glucose metabolism
• CPC Class Codes: G01N 2800/085 : Liver diseases, e.g. portal hypertension, fibrosis, cirrhosis, bilirubin
• CPC Class Codes: G01N 2800/2821 : Alzheimer
• CPC Class Codes: G01N 2800/2835 : Movement disorders, e.g. Parkinson, Huntington, Tourette
• CPC Class Codes: G01N 33/74 : involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors

Abstract

Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.

Claims

1. A peptide comprising the amino acid sequence of SEQ ID NO:

17, or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising the peptide of claim 1, or a pharmaceutically acceptable salt thereof;

and a pharmaceutically acceptable carrier.

3. The pharmaceutical composition of claim 2, additionally comprising an anti-diabetic or anti-obesity agent.

4. A method of treating a disease or medical condition in a patient in need thereof, wherein the disease or medical condition is selected from the group consisting of:

metabolic syndrome, diabetes, obesity, and liver steatosis, comprising administering to the patient the pharmaceutical composition of claim 3 in an amount effective to treat the disease or medical condition.

5. The method of claim 4, wherein the disease or medical condition is type II diabetes.

6. A method of treating a disease or medical condition in a patient in need thereof, wherein the disease or medical condition is selected from the group consisting of:

metabolic syndrome, diabetes, obesity, and liver steatosis, comprising administering to the patient the pharmaceutical composition of claim 2 in an amount effective to treat the disease or medical condition.

7. The method of claim 6, wherein the disease or medical condition is type II diabetes.

8. A peptide comprising the amino acid sequence of SEQ ID NO:

17.

9. A pharmaceutical composition comprising the peptide of claim 8;

and a pharmaceutically acceptable carrier.

10. The pharmaceutical composition of claim 9, additionally comprising an anti-diabetic or anti-obesity agent.

11. A method of treating a disease or medical condition in a patient in need thereof, wherein the disease or medical condition is selected from the group consisting of:

metabolic syndrome, diabetes, obesity, and liver steatosis, comprising administering to the patient the pharmaceutical composition of claim 10 in an amount effective to treat the disease or medical condition.

12. The method of claim 11, wherein the disease or medical condition is type II diabetes.

13. A method of treating a disease or medical condition in a patient in need thereof, wherein the disease or medical condition is selected from the group consisting of:

metabolic syndrome, diabetes, obesity, and liver steatosis, comprising administering to the patient the pharmaceutical composition of claim 9 in an amount effective to treat the disease or medical condition.

14. The method of claim 13, wherein the disease or medical condition is type II diabetes.

15. A peptide consisting of the amino acid sequence of SEQ ID NO:

17 or a pharmaceutically acceptable salt thereof.

16. A pharmaceutical composition comprising the peptide of claim 15, or a pharmaceutically acceptable salt thereof;

and a pharmaceutically acceptable carrier.

17. The pharmaceutical composition of claim 16, additionally comprising an anti-diabetic or anti-obesity agent.

18. A method of treating a disease or medical condition in a patient in need thereof, wherein the disease or medical condition is selected from the group consisting of:

metabolic syndrome, diabetes, obesity, and liver steatosis, comprising administering to the patient the pharmaceutical composition of claim 17 in an amount effective to treat the disease or medical condition.

19. A method of treating a disease or medical condition in a patient in need thereof, wherein the disease or medical condition is selected from the group consisting of:

metabolic syndrome, diabetes, obesity, and liver steatosis, comprising administering to the patient the pharmaceutical composition of claim 16 in an amount effective to treat the disease or medical condition.

20. The method of claim 19, wherein the disease or medical condition is type II diabetes.

21. The method of claim 18, wherein the disease or medical condition is type II diabetes.

22. A peptide consisting of the amino acid sequence of SEQ ID NO:

17.

23. A pharmaceutical composition comprising the peptide of claim 22;

and a pharmaceutically acceptable carrier.

24. The pharmaceutical composition of claim 23, additionally comprising an anti-diabetic or anti-obesity agent.

25. A method of treating a disease or medical condition in a patient in need thereof, wherein the disease or medical condition is selected from the group consisting of:

metabolic syndrome, diabetes, obesity, and liver steatosis, comprising administering to the patient the pharmaceutical composition of claim 24 in an amount effective to treat the disease or medical condition.

26. The method of claim 25, wherein the disease or medical condition is type II diabetes.

27. A method of treating a disease or medical condition in a patient in need thereof, wherein the disease or medical condition is selected from the group consisting of:

metabolic syndrome, diabetes, obesity, and liver steatosis, comprising administering to the patient the pharmaceutical composition of claim 23 in an amount effective to treat the disease or medical condition.

28. The method of claim 27, wherein the disease or medical condition is type II diabetes.