EP0539167A2
Expired / Lapsed
EP
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Peg imidates and protein derivatives thereof
Assignee: Ortho Pharmaceutical Corp
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Filing: 1992-10-20
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Granted: —
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Expires: 2012-10-20
Abstract
Abstract The present invention provides methods and compounds for modifying proteins, peptides and organic compounds with free amino group(s) with an imidate derivative of PEG or related water-soluble organic polymers. Novel imidate derivatives of PEG and other water-soluble polymers are provided for. The water-soluble polymer modifying reagents of the subject invention included imidates of polyethylene glycol, polypropylene glycol, polyoxyethylated polyol, heparin, heparin fragments, dextran, polysaccharides, polyamino acids, polyvinyl alcohol, and other water-soluble organic polymers also is included. An advantage of PEG-imidates is that on reaction with the amino groups of proteins the resulting derivative still preserves the positive charge and displaces the positive charge away from the water-soluble polymer backbone. Also provided for are polypeptides of interest derivatized by water-soluble polymer imidates.
Inventors
- 👤 David E. Wright
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-01 12:55
CPC Classifications
C; C08; C08G; C08G63/00; C08G63/91; C08G65/00; C08G65/02; C08G65/32; C08G65/329; C08G65/333; C08G65/33303; C08G65/33306; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/59; A61K47/60; A61P; A61P43/00
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
13 words
A compound according to the formula (I) wherein P is a water-soluble polymer.
Claim 2
Dependent Claim
19 words
A compound according to the formula (II) wherein P is a water-soluble polymer, and m is 1 to 20.
Claim 3
Dependent Claim
60 words
The compound of Claim 1 or Claim 2, wherein said polymer P is a polyethylene glycol homopolymer, a polypropylene glycol homopolymer, a copolymer of ethylene glycol with propylene glycol, wherein said homopolymer or said copolymer is unsubstituted or substituted at one end with an alkyl group, a polyoxyethylated polyol, a polyvinyl alcohol, a polysaccharide, a polyvinyl ethyl ether, or α,β-poly[(2-hydroxyethyl)-DL-aspartamide].
Claim 4
Dependent Claim
12 words
The compound of Claim 3, wherein said water-soluble polymer is polyethylene glycol.
Claim 5
Independent Claim
34 words
A method a covalently joining at least one water-soluble polymer to a polypeptide, said method comprising the step of reacting a compound according to any one of Claims 1 to 4 with a polypeptide.
Claim 6
Dependent Claim
26 words
The method of Claim 5, wherein said polypeptide is a hormone, a lymphokine, a cytokine, a growth factor, an enzyme, a vaccine antigen, or an antibody.
Claim 7
Dependent Claim
41 words
The method of Claim 6, wherein said polypeptide is an antibody, and said method further comprises the step of combining said antibody with a compound capable of specifically binding to a binding site on said antibody, prior to said reacting step.
Claim 8
Dependent Claim
33 words
The method of Claim 6, wherein said polypeptide is an enzyme, and said method further comprises the step of mixing said polypeptide with a substrate for said enzyme, prior to said reacting step.
Claim 9
Dependent Claim
14 words
A polypeptide modified by the method of any one of Claims 5 to 8.
Claim 10
Dependent Claim
13 words
A composition comprising the polypeptide of Claim 9, and a pharmaceutically acceptable carrier.
Claim 11
Dependent Claim
52 words
A compound of the formula (III) wherein n is 1 to x, x being one larger than the number of lysine residues in Z, P is a water-soluble polymer, and Z is a polypeptide, wherein Z is covalently joined to the non-polypeptide portion of said compound through a lysine residue in Z.
Claim 12
Dependent Claim
57 words
A compound of the formula (IV) wherein m is 1 to 20, n is 1 to x, x being one larger than the number of lysine residues in Z, P is a water-soluble polymer, and Z is a polypeptide, wherein Z is covalently joined to the non-polypeptide portion of said compound through a lysine residue in Z.
Claim 13
Dependent Claim
58 words
The compound of Claim 11 or Claim 12, wherein said polymer is a polyethylene glycol homopolymer, a polypropylene glycol homopolymer, a copolymer of ethylene glycol with propylene glycol, wherein said homopolymer or copolymer is unsubstituted or substituted at one end with an alkyl group, a polyoxyethylated polyol, a polyvinyl alcohol, a polysaccharide, a polyvinyl ethyl ether, or α,β-poly[(2-hydroxyethyl)-DL-aspartamide].
Claim 14
Dependent Claim
31 words
The compound of any one of Claima 11 to 13, wherein said polypeptide is a hormone, a lymphokine, a cytokine, a growth factor, an enzyme, a vaccine antigen, or an antibody.
Claim 15
Dependent Claim
11 words
The compound of Claim 14, wherein said polypeptide is an antibody.
Claim 16
Dependent Claim
10 words
The compound of Claim 14, wherein said polypeptide is erythropoietin.
Claim 17
Dependent Claim
18 words
A composition comprising the compound of any one of Claims 11 to 16, and a pharmaceutically acceptable carrier.
Claim 18
Dependent Claim
21 words
A compound according to the formula (V) (V) P-NH-(CH₂) n -CN wherein P is a water-soluble polymer and n = 1-20.
Claim 19
Dependent Claim
55 words
The compound of Claim 18, wherein said polymer is a polyethylene glycol homopolymer, a polypropylene glycol homopolymer, a copolymer of ethylene glycol with propylene glycol, wherein said homopolymer or copolymer is unsubstituted or substituted at one end with an alkyl group, a polyoxyethylated polyol, a polyvinyl alcohol, a polysaccharide, a polyvinyl ethyl ether, or α,β-poly[(2-hydroxyethyl)-DL-aspartamide].
Claim 20
Dependent Claim
12 words
The compound of Claim 19, wherein said water-soluble polymer is polyethylene glycol.
Claim 21
Dependent Claim
64 words
An erythropoietin molecule modified by at least one tresyl water-soluble polymer ester, wherein said water soluble polymer is a polyethylene glycol homopolymer, a polypropylene glycol homopolymer, a copolymer of ethylene glycol with propylene glycol, wherein said homopolymer or copolymer is unsubstituted or substituted at one end with an alkyl group, a polyoxyethylated polyol, a polyvinyl alcohol, a polysaccharide, a polyvinyl ethyl ether, or α,β-poly[2-hydroxyethyl)-DL-aspartamide].
Claim 22
Dependent Claim
64 words
An erythropoietin molecule modified by at least one succinimide water-soluble polymer ester, wherein said water soluble polymer is a polyethylene glycol homopolymer, a polypropylene glycol homopolymer, a copolymer of ethylene glycol with propylene glycol, wherein said homopolymer or copolymer is unsubstituted or substituted at one end with an alkyl group, a polyoxyethylated polyol, a polyvinyl alcohol, a polysaccharide, a polyvinyl ethyl ether, or α,β-poly[(2-hydroxyethyl)-DL-aspartamide].
Claim 23
Dependent Claim
16 words
The erythropoietin molecule of Claim 21 or Claim 22, wherein said water-soluble polymer is polyethylene glycol.
References Cited (Backward Citations)
No citation records indexed.
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