Protein-polymer conjugates

• US 8,273,343 B2
• Filed: 07/31/2009
• Issued: 09/25/2012
• Est. Priority Date: 07/31/2008
• Status: Active Grant

• Current Assignee: PharmaEssentia Corporation
• Original Assignee: PharmaEssentia Corporation
• Inventors: Lin, Ko-Chung
• Primary Examiner(s): Landsman, Robert
• Assistant Examiner(s): Hissong, Bruce D
• Application Number:
  US12/533,147
• Publication Number:
  US 20100029907A1
• Time in Patent Office: 1,152 Days
• Field of Search: None
• US Class Current: 424/85.6
• CPC Class Codes: A61K 38/1816 Erythropoietin [EPO]
• CPC Class Codes: A61K 38/215 IFN-beta
• CPC Class Codes: A61K 38/27 Growth hormone [GH], i.e. somatotropin
• 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: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 31/14 for RNA viruses
• CPC Class Codes: A61P 31/20 for DNA viruses
• CPC Class Codes: A61P 37/02 Immunomodulators
• CPC Class Codes: A61P 7/06 Antianaemics

Abstract

This invention relates to a conjugate of a polymer moiety and an interferon-β moiety, an erythropoietin moiety, or a growth hormone moiety.

Claims

1. A peptide-polymer conjugate of the following formula:

2. The conjugate of claim 1, wherein P is interferon-β

.

3. The conjugate of claim 2, wherein P is rINF-β

Ser₁₇.

4. The conjugate of claim 2, wherein P is modified interferon-β

containing 1-4 additional amino acid residues at the N-terminus.

5. The conjugate of claim 1, wherein P is erythropoietin.

6. The conjugate of claim 1, wherein each of A₁ and A₂ is a polyethylene glycol having a molecular weight of 2-100 kD.

7. The conjugate of claim 6, wherein each of A₁ and A₂ is a polyethylene glycol having a molecular weight of 10-30 kD.

8. The conjugate of claim 7, wherein each of G₁ and G₂ is

9. The conjugate of claim 8, wherein m is 4, n is 2, and each of R₁, R₂, R₃, R₄, and R₅ is H.

10. The conjugate of claim 9, wherein P is interferon-β

.

11. The conjugate of claim 10, wherein P is rINF-β

Ser₁₇.

12. The conjugate of claim 10, wherein P is modified interferon-β

containing 1-4 additional amino acid residues at the N-terminus.

13. The conjugate of claim 9, wherein P is erythropoietin.

14. The conjugate of claim 9, wherein P is growth hormone.

15. The conjugate of claim 1, wherein P is growth hormone.

16. The conjugate of claim 1, wherein the conjugate is

17. The conjugate of claim 1, wherein the conjugate is

18. The conjugate of claim 1, wherein the conjugate is