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.
Claims49
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:
- wherein L is the point of bonding to the terminal carbon of the second terminus of the polymer backbone, said first functional group being different from said N-maleimidyl moiety bonded to the terminal carbon of said second terminus.
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, wherein a terminal carbon at the second terminus of the polymer backbone of the N-maleimidyl polymer derivative product is bonded to the nitrogen atom of an N-maleimidyl moiety and the first functional group is different from the N-maleimidyl moiety.
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.
A multi-functional branched N-maleimidyl polymer derivative comprising a central branched core moiety and a plurality of water soluble and non-peptidic polymer backbones attached to said central branched core moiety, each polymer backbone comprising a terminal carbon and having an average molecular weight from about 800 Da to about 100,000 Da, wherein said terminal carbon of each polymer backbone is directly bonded to a N-maleimidyl moiety having the structure:
- wherein L is the point of bonding to the terminal carbon of each polymer backbone.
Dependencies are inferred from the claim text.