N-maleimidyl polymer derivatives
AssigneeShearwater Corporation
InventorXiaoming Shen
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Abstract
The invention is directed to multi-functional N-maleimidyl polymer derivatives comprising a water soluble and non-peptidic polymer backbone having a terminal carbon, such as a poly(alkylene glycol), the terminal carbon of the polymer backbone being directly bonded to the nitrogen atom of a N-maleimidyl moiety without a linking group therebetween. The invention also provides two methods of preparing such linkerless N-maleimidyl polymer derivatives.
Claims36
A multi-functional N-maleimidyl polymer derivative comprising a water soluble and non-peptidic polymer backbone having an average molecular weight from about 800 Da to about 100,000 Da, the polymer backbone having a first terminus bonded to a first functional group and a second terminus having a terminal carbon, wherein said terminal carbon of said second terminus is directly bonded to a N-maleimidyl moiety having the structure:
- 12
- wherein L is the point of bonding to the terminal carbon of the second terminus of the polymer backbone.
A method of preparing a multi-functional N-maleimidyl polymer derivative, comprising:
- providing a water-soluble and non-peptidic polymer backbone having an average molecular weight from about 800 Da to about 100,000 Da, the polymer backbone having a first terminus bonded to a first functional group and a second terminus bonded to an amine group;
- reacting the polymer backbone with maleic anhydride to form an open ring intermediate;
- and
- heating the open ring intermediate in the presence of acetic anhydride and a salt of acetic acid to form a multi-functional N-maleimidyl polymer derivative product.
A method of preparing a N-maleimidyl polymer derivative, comprising
- providing a water-soluble and non-peptidic polymer backbone having an average molecular weight from about 800 Da to about 100,000 Da, the polymer backbone having a terminal amine group;
- and
- reacting the polymer backbone with an N-alkoxycarbonylmaleimide to form a N-maleimidyl polymer derivative product.
The method of claim 32, wherein the water-soluble and non-peptidic polymer backbone has the formula X-PEG-NH2, wherein PEG is poly(ethylene glycol) and X is a capping group.
Dependencies are inferred from the claim text.