Polymer derivatives having particular atom arrangements
AssigneeNektar Therapeutics
InventorsJ. Milton Harris, Antoni Kozlowski, Samuel P. McManus, Michael D. Bentley, Stephen A. Charles
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Abstract
Polymeric reagents are provided comprising a moiety of atoms arranged in a specific order, wherein the moiety is positioned between a water-soluble polymer and a reactive group. The polymeric reagents are useful for, among other things, forming polymer-active agent conjugates. Related methods, compositions, preparations, and so forth are also provided.
Claims33
A polymeric reagent comprising a
- moiety positioned between a water-soluble polymer and a reactive group, wherein:
- (i) the nitrogen atom in the
- moiety is proximal to the water-soluble polymer;
- (ii) the carbonyl carbon atom of the
- moiety is proximal to the reactive group;
- and (iii) R1 is H or an organic radical.
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A method of preparing a polymeric reagent comprising the steps of
- (i) providing a precursor molecule optionally comprised of a protected reactive group and one or more hydroxyl groups;
- (ii) activating at least one of the one or more hydroxyl groups of the precursor molecule for reaction with an amino group to form an activated precursor molecule;
- (iii) contacting under covalent coupling conditions at least one of the one or more activated hydroxyl groups with a water-soluble polymer having an amino group, thereby forming a polymer comprised of the water-soluble polymer portion and the protected reactive group;
- and
- (iv) deprotecting the protected reactive group, when present, thereby forming the polymeric reagent.
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A conjugate comprising a water-soluble polymer, a
- moiety, and a pharmacologically active agent, wherein:
- (i) the water-soluble polymer is linked to the nitrogen atom of the
- moiety through either a direct covalent bond or through a first spacer moiety;
- (ii) the pharmacologically active agent is linked to the carbonyl carbon atom of the
- moiety through either a direct covalent bond or a second spacer moiety;
- and (iii) R1 is H or an organic radical.
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Dependencies are inferred from the claim text.