Sterically hindered poly(ethylene glycol) alkanoic acids and derivatives thereof
AssigneeShearwater Corporation
InventorsMichael David Bentley, Xuan Zhao, Xiaoming Shen, Lihong Guo
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Abstract
The invention provides a sterically hindered polymer that comprises a water-soluble and non-peptidic polymer backbone having at least one terminus covalently bonded to an alkanoic acid or alkanoic acid derivative, wherein the carbon adjacent to the carbonyl group of the acid or acid derivative group has an alkyl or aryl group pendent thereto. The steric effects of the alkyl or aryl group allow greater control of the hydrolytic stability of polymer derivatives. The polymer backbone may be poly(ethylene glycol).
Claims31
A sterically hindered polymer, comprising a water-soluble and non-peptidic polymer backbone having at least one terminus, said terminus being covalently bonded to the structure
- 9
- wherein:
- L is the point of bonding to the terminus of the polymer backbone;
- Q is O or S;
- m is 0 to about 20;
- Z is selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl;
- and
- X is a leaving group.
A biologically active polymer conjugate, comprising a water-soluble and non-peptidic polymer backbone having at least one terminus, said terminus being covalently bonded to the structure
- 13
- wherein:
- L is the point of bonding to the terminus of the polymer backbone;
- Q is O or S;
- m is 0 to about 20;
- Z is selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl;
- W is a linker;
- and
- D is a biologically active agent.
A method of preparing a biologically active polymer conjugate, comprising:
- providing a water-soluble and non-peptidic polymer comprising a polymer backbone having at least one terminus, said terminus being covalently bonded to the structure
- 14
- wherein:
- L is the point of bonding to the terminus of the polymer backbone;
- Q is O or S;
- m is 0 to about 20;
- Z is selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl;
- and
- X is a leaving group;
- reacting the polymer with a biologically active agent to form a biologically active polymer conjugate having at least one terminus covalently bonded to the following structure
- 15
- wherein:
- L is the point of bonding to the terminus of the polymer backbone;
- Q is O or S;
- m is 0 to about 20;
- Z is selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl;
- W is a linker;
- and
- D is a biologically active agent.
Dependencies are inferred from the claim text.