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EP0400486A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Polyethylene glycol derivatives, modified peptides and production thereof

Assignee: Sumitomo Pharma Co Ltd
•
Filing: 1990-05-24
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Granted: —
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Expires: 2010-05-24
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Abstract

Abstract A polyethylene glycol derivative of the formula wherein R₁ and R₂ are the same or different and each represents a lower alkyl and m and n are same or different and each represents an optional positive integer which ren­ders the average molecular weight of the polyethylene glycol moiety about 1,000 to 12,000, a peptide modified by said polyethylene glycol derivative and a method for production thereof are described. The polyethylene glycol derivative (I) is capable of modifying the guanidino groups in peptides. The thereby modified peptides are extremely stable, are con­siderably delayed in biological clearance (i.e. the durability is extended) and exhibit their physiological activities effectively over the long period.

Inventors

  • 👤 Keiichi Ono
  • 👤 Yoshiyuki Kai
  • 👤 Yoshiharu Ikeda
  • 👤 Hiroo Maeda

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-23 16:31
CPC Classifications
C; C12; C12N; C12N9/00; C12N9/96; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/59; A61K47/60; C07; C07K; C07K1/00; C07K1/107; C07K1/1072; C07K1/1077; C08; C08G; C08G65/00; C08G65/02; C08G65/32; C08G65/329; C08G65/331; C08G65/3311; C08G65/3314; C08G65/3315; C08G65/3317; C08G65/334; C08G65/3344; C08G65/3346

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 52 words
A polyethylene glycol derivative of the formula wherein R₁ and R₂ are the same or different and each repre­sents a lower alkyl and m and n are same or different and each represents an optional positive integer which renders the average molecular weight of the polyethylene glycol moiety about 1,000 to 12,000.
Claim 2
Dependent Claim 52 words
A polyethylene glycol derivative of the formula wherein R₁ and R₂ are the same or different and each repre­sents a lower alkyl and m and n are same or different and each represents an optional positive integer which renders the average molecular weight of the polyethylene glycol moiety about 1,000 to 12,000.
Claim 3
Dependent Claim 33 words
A polyethylene glycol derivative as claimed in Claim 1 which is selected from a group consisting of 3,5-bis-­methoxypolyethylene glycol phenylglyoxal and 3-monomethoxy­polyethylene glycol (average molecular weight 2,000)-5-mono­methoxypolyethylene glycol (average molecular weight 4,500) phenylglyoxal.
Claim 4
Dependent Claim 23 words
A modified peptide in which the guanidino group in the peptide is modified by a polyethylene glycol derivative as claimed in Claim 1.
Claim 5
Dependent Claim 63 words
A modified peptide as claimed in Claim 3 selected from among a group consisting of superoxide dismutase modi­fied by 3,5-bis-methoxypolyethylene glycol phenylglyoxal, insulin-like growth factor-I modified by 3,5-bis-methoxy­ polyethylene glycol phenylglyoxal, insulin-like growth factor-­II modified by 3,5-bis-methoxypolyethylene glycol phenylglyoxal, calcitonin gene related peptide modified by 3,5-bis-methoxy­polyethylene glycol phenylglyoxal, elastase modified by 3,5-­bis-methoxypolyethylene glycol phenylglyoxal and superoxide dismutase modified by 3-monomethoxypolyethylene glycol-5-­monomethoxypolyethylene glycol phenylglyoxal.
Claim 6
Dependent Claim 25 words
A method for producing a modified peptide which comprises reacting a polyethylene glycol derivative as claimed in Claim 1 with a peptide having guanidino group.
Claim 7
Dependent Claim 42 words
A method for producing a modified peptide which comprises protecting the amino group(s) of a peptide having guanidino group and then reacting the amino-protected peptide with a polyethylene glycol derivative as claimed in Claim 1, followed by deprotection of the amino-protective group(s).

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