Maleamic acid polymer derivatives and their bioconjugates
AssigneeNektar Therapeutics AL, Corporation
InventorsAntoni Kozlowski, Remy F. Gross III, Samuel P. McManus
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Abstract
The present invention is directed to maleamic acid derivatives of water soluble polymers, to chemically stable water-soluble polymer succinamic acid-active agent conjugates, and to methods for reproducibly preparing, characterizing and using such polymer reagents and their conjugates.
Claims65
A method for preparing a polymer conjugate, said method comprising:
- (a) providing a water-soluble polymer comprising a maleimide group,
- (b) reacting said polymer with an active agent comprising a nucleophile under conditions effective to couple said agent to said water soluble polymer via a Michael-type addition reaction to form a polymer-succinimide-linked active agent conjugate, and
- (c) treating the conjugate from (b) under conditions effective to force open said succinimide ring to thereby form a polymer-conjugate composition comprising a polymer-succinamic acid-conjugate.
A composition comprising a water-soluble polymer covalently attached to a maleamic acid group, optionally via an interposing linker.
A composition comprising at least about 50% by weight of a water-soluble polymer covalently attached to a maleamic acid group, optionally via an interposing linker.
A chemically stable composition comprising:
- 30
- wherein:
- POLY is a water-soluble polymer segment,
- L is an optional linker, and
- “Nu-Active agent” represents an active agent comprising a nucleophile, “Nu”.
A protein derivatized with a water-soluble polymer, wherein the polymer is coupled to the protein via succinimide groups covalently attached to either cysteine sulfyhydryl groups or lysine amino groups, and substantially all of the succinimide groups are present in a ring-opened form.
Dependencies are inferred from the claim text.