PEPTIDE-POLYMER CONJUGATES

• US 20110098451A1
• Filed: 12/29/2010
• Published: 04/28/2011
• Est. Priority Date: 07/31/2008
• Status: Abandoned Application

• Current Assignee: PharmaEssentia Corporation
• Original Assignee: PharmaEssentia Corporation
• Inventors: Lin, Ko-Chung
• Application Number:
  US12/981,183
• Publication Number:
  US 20110098451A1
• Time in Patent Office: Days
• US Class Current: 530/397
• 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 erythropoietin moiety.

Claims

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

2. The conjugate of claim 1, wherein P is an erythropoietin moiety in which 1-4 additional amino acid residues are attached to the N-terminus of a native erythropoietin.

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

4. The conjugate of claim 3, wherein each of A₁ and A₂ is a polyethylene glycol moiety having a molecular weight of 10-30 kD.

5. The conjugate of claim 4, wherein each of G₁ and G₂ is

6. The conjugate of claim 5, wherein m is 4, n is 2, and each of R₁, R₂, R₃, R₄, and R₅ is H.

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

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

9. The conjugate of claim 8, wherein G is

10. The conjugate of claim 9, wherein A is a polyethylene glycol moiety having a molecular weight of 10-40 kD.

11. The conjugate of claim 10, wherein A is a polyethylene glycol moiety having a molecular weight of 20-30 kD.

12. The conjugate of claim 8, wherein n is 1.