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US 2014/0005419 A1Published application
Method for Preparing a Polymer Conjugate
AssigneeNektar Therapeutics
InventorWen Zhang
Life of this patent
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Abstract
Provided herein is a straightforward and efficient method for covalently attaching a polyethylene glycol polymer to a taxane. The method involves, among other things, a step of reacting a taxame with a polyethylene glycol polymer comprising a functional group reactive with a functional group within said taxane in the presence of a coupling reagent and DPTS. The result of the reacting step is the formation of a polyethylene glycol-taxane conjugate.
Claims12
A method for covalently attaching a polyethylene glycol polymer to an active agent, said method comprising the step of:
- reacting a small molecule active agent having a molecular weight of less than about 800 Daltons and having a single hydroxyl group with a linear polyethylene glycol having a single functional group reactive with a hydroxyl group in the presence of a coupling reagent and 4-(dimethylamino)-pyridinium-p-toluenesulfonate (DPTS), under conditions effective to promote reaction between the single hydroxyl group of the small molecule active agent and the single functional group of the linear polyethylene glycol to thereby form a polyethylene glycol-small molecule active agent conjugate.
Dependencies are inferred from the claim text.