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US 6,605,299 B2Granted
Releasable linkage and compositions containing same
AssigneeAlza Corporation
InventorSamuel Zalipsky
Life of this patent
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Abstract
A compound comprised of a hydrophilic polymer covalently yet reversibly linked to a amine-containing ligand through a dithiobenzyl linkage is described.
Claims44
A polypeptide composition having the general structure:
- wherein
- R1 is a hydrophilic polymer comprising a linkage for attachment to the dithiobenzyl moiety;
- R2 is selected from the group consisting of H, alkyl, and aryl;
- R3 is selected from the group consisting of O(C═O), S(C═O), and O(C═S);
- R5 is selected from the group consisting of H, alkyl and aryl;
- where orientation of CH2—R3 is selected from the ortho position and the para position;
- and n is at least 1;
- and
- a pharmaceutically-acceptable carrier.
6 more elements
A polypeptide composition, comprising:
- a polypeptide conjugated to at least one a hydrophilic polymer chain to form a modified polypeptide having the general structure:
- wherein
- R1 is the hydrophilic polymer comprising a linkage for attachment to the dithiobenzyl moiety;
- R2 is selected from the group consisting of H, alkyl, and aryl;
- R3 is selected from the group consisting of O(C═O), S(C═O), and O(C═S);
- R4 is the polypeptide;
- R5 is selected from the group consisting of H, alkyl and aryl;
- where orientation of CH2—R3 is selected from the ortho position and the para position;
- and n is at least 1;
- and
- a pharmaceutically-acceptable carrier.
8 more elements
An improvement in a polypeptide modified with a hydrophilic polymer, comprising
- conjugating the polymer to the polypeptide to form a polymer-peptide conjugate having the general structural formula:
- wherein R1 is the hydrophilic polymer comprising a linkage for attachment to the dithiobenzyl moiety;
- R2 is selected from the group consisting of H, alkyl and aryl;
- R3 is selected from the group consisting of O(C═O), S(C═O), and O(C═S);
- R4 is the polypeptide;
- and R5 is selected from the group consisting of H, alkyl and aryl;
- where orientation of CH2—R3 is selected from the ortho position and the para position;
- and n is at least 1.
5 more elements
A method for improving the blood circulation lifetime of a polypeptide, comprising
- preparing a polymer-polypeptide conjugate having the general structure:
- wherein R1 is the hydrophilic polymer comprising a linkage for attachment to the dithiobenzyl moiety;
- R2 is selected from the group consisting of H, alkyl and aryl;
- R3 is selected from the group consisting of O(C═O), S(C═O), and O(C═S);
- R4 is the polypeptide;
- and R5 is selected from the group consisting of H, alkyl and aryl;
- where orientation of CH2—R3 is selected from the ortho position and the para position;
- and n is at least 1.
5 more elements
Dependencies are inferred from the claim text.