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US 8,252,275 B2Granted
Conjugates having a degradable linkage and polymeric reagents useful in preparing such conjugates
AssigneeNektar Therapeutics
InventorsMichael D. Bentley, Sean Culbertson, Samuel P. McManus
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Abstract
The present invention provides conjugates having a degradable linkage and polymeric reagents useful in preparing such conjugates. The conjugates as well as the polymeric reagents used to form the conjugates include at least one of each the following: an aromatic moiety comprising an ionizable hydrogen atom, a spacer moiety, and a water-soluble polymer. Methods of making polymeric reagents and conjugates, as well as methods for administering conjugates and compositions, are also provided.
Claims30
A polymeric reagent of the following formula:
- wherein:
- POLY1 is a first water-soluble polymer selected from the group consisting of poly(alkylene glycol), poly(olefinic alcohol), poly(vinylpyrrolidone), poly(hydroxyalkylmethacrylamide), poly(hydroxyalkylmethacrylate), poly(saccharides), poly(α-hydroxy acid), poly(vinyl alcohol), polyphosphazene, polyoxazoline, and poly(N-acrylmorpholine);
- POLY2 is a second water-soluble polymer selected from the group consisting of poly(alkylene glycol), poly(olefinic alcohol), poly(vinylpyrrolidone), poly(hydroxyalkylmethacrylamide), poly(hydroxyalkylmethacrylate), poly(saccharides), poly(α-hydroxy acid), poly(vinyl alcohol), polyphosphazene, polyoxazoline, and poly(N-acrylmorpholine);
- X1 is a first spacer moiety;
- X2 is a second spacer moiety;
- Hα is an ionizable hydrogen atom;
- R1 is H or an organic radical;
- R2 is H or an organic radical;
- and
- (FG) is a functional group capable of reacting with an amino group of an active agent to form a degradable linkage.
7 more elements
A conjugate of the following formula:
- wherein:
- POLY1 is a first water-soluble polymer;
- POLY2 is a second water-soluble polymer;
- X1 is a first spacer moiety;
- X2 is a second spacer moiety;
- Hα is an ionizable hydrogen atom;
- R1 is H or an organic radical;
- R2 is H or an organic radical;
- and
- Y1 is O or S;
- Y2 is O or S;
- and
- D is a residue of a biologically active agent.
10 more elements
Dependencies are inferred from the claim text.