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US 5,637,749 AGranted
Aryl imidate activated polyalkylene oxides
AssigneeEnzon, Inc.
InventorRichard B. Greenwald
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Abstract
Water-soluble aryl imidate activated polyalkylene oxides having improved hydrolytic stability and conjugates of the aryl imidate activated polyalkylene oxides with biologically active nucleophiles are disclosed. Methods of preparing the activated polyalkylene oxides and conjugates thereof are also disclosed.
Claims20
A polyalkylene oxide conjugate comprising:
- a nucleophile having biological activity;
- and
- at least one water-soluble polyalkylene oxide covalently bonded thereto by a hydrolyrically stable linkage formed by reacting said nucleophile with an aryl imidate activated polyalkylene oxide, having a structure represented by (I):
- ##STR5## wherein R is a water-soluble polyalkylene oxide;
- L is NHC(O) such that the carbonyl is attached to the phenyl ring;
- R.sub.1 is a moiety selected from the group consisting of alkyl, phenyl, phenyl alkyl, and cycloalkyl moieties;
- and
- X is a terminal moiety of said polyalkylene oxide selected from the group consisting of OH,C.sub.1-4 alkoxy moieties and aryl imidates corresponding to the structure:
- ##STR6## wherein L and R.sub.1 are defined as above.
6 more elements
A method of forming a biologically active conjugate of a biologically active nucleophile and one or more water-soluble polyalkylene oxides covalently bonded thereto, said method comprising the steps of:
- providing a biologically active nucleophile;
- contacting said nucleophile with one or more aryl imidate activated polyalkylene oxides, so that a biologically active conjugate of said biologically active nucleophile and said polyalkylene oxides is formed;
- and
- recovering said biologically active conjugate.
1 more element
Dependencies are inferred from the claim text.