Nova Patents
CA2592006C

Conjugates of insulin-like growth factor-1 (igf-1) and poly(ethylene glycol)

Abstract

A conjugate consisting of an insulin-like growth factor-1 (IGF-I) variant and one or two poly(ethylene glycol) group(s), characterized in that said IGF-I variant has an amino acid alteration at up to three amino acid positions 27, 37, 65, 68 of the wild-type IGF-I amino acid sequence so that one or two of said amino acids is/are lysine and amino acid 27 is a polar aminio acid but not lysine, is conjugated via the primary amino group(s) of said lysine(s) and said poly(ethylene glycol) group(s) have an overall molecular weight of from 20 to 100 kDa is disclosed. This conjugate is useful for the treatment of neurodegenerative disorders like Alzheimer's Disease.

CA2592006C, drawing sheet 1
Sheet 1 of 12

Term

No projected expiry on record.

  1. Priority
  2. Filed
  3. Granted
  4. Today

10 claims: 5 independent, 5 dependent

  1. 1
    CA 02592006 2014-02-26 -39CLAIMS:1. A conjugate consisting of an insulin-like growth factor-1 (IGF-I) variant and polyethylene glycol (PEG), wherein said IGF-I variant has amino acid alterations at amino acid positions 27 and 65 of the wild-type IGF-I amino acid sequence (SEQ ID NO:1), wherein said IGF-I variant is R27, R37, R65, K68 (RRRK), and said PEG is conjugated to said IGF-I variant via a primary amino group of the lysine.
  2. 2
    A conjugate consisting of an insulin-like growth factor-1 (IGF-I) variant and polyethylene glycol (PEG), wherein said IGF-I variant has amino acid alterations at amino acid positions 27 and 65 of the wild-type IGF-I amino acid sequence (SEQ ID NO:1), wherein said IGF-I variant is R27, R37, R65, K68 (RRRK), and said PEG is conjugated to said IGF-I variant via a primary amino group of the lysine;and wherein up to three amino acids at the N-terminus of the IGF-I variant are truncated.
  3. 3
    A conjugate consisting of an insulin-like growth factor-1 (IGF-I) variant and polyethylene glycol (PEG) at two locations, wherein:a) said IGF-I variant has amino acid alterations at amino acid positions 27 and 65 of the wild-type IGF-I amino acid sequence (SEQ ID NO:1), wherein said IGF-I variant is R27, R37, R65, K68 (RRRK), or b) said IGF-I variant has amino acid alterations at amino acid positions 27 and 65 of the wild-type IGF-I amino acid sequence (SEQ ID NO:1), and wherein said IGF-I variant is R27, R37, R65, K68 (RRRK), and wherein up to three amino acids at the N-terminus of the IGF-I variant are truncated;and wherein said IGF-I variant is PEGylated at the N-terminal amino acid and at a primary amino group of the lysine.
  4. 6
    7. A composition comprising the conjugate of any one of claims 1 to 5 and a pharmaceutically acceptable carrier.
  5. 7
    8. A pharmaceutical composition comprising the conjugate of any one of claims 1 to 5 and a pharmaceutically acceptable carrier, for use in treatment of Alzheimer's Disease.
Independent claims5