Polymeric reagents comprising a terminal vinylic group and conjugates formed therefrom
View Patent ↗The present invention provides conjugates having a degradable linkage and polymeric reagents useful in preparing such conjugates. Methods of making polymeric reagents and conjugates, as well as methods for administering conjugates and compositions, are also provided.
1. A purified polymeric reagent in solid form, the polymeric reagent having the structure:
wherein:
POLY 1 is a poly(alkylene oxide);
POLY 2 is a poly(alkylene oxide);
X 1 is a first spacer moiety of atoms;
X 2 is a second spacer moiety of atoms;
R 1 is H or an organic radical; and
R 2 is H or an organic radical.
2. The purified polymeric reagent of claim 1 , wherein POLY 1 and POLY 2 are the same.
3. The purified polymeric reagent of claim 1 , wherein each poly(alkylene oxide) is terminally capped with an end-capping moiety selected from the group consisting hydroxy, alkoxy, substituted alkoxy, alkenoxy, substituted alkenoxy, alkynoxy, substituted alkynoxy, aryloxy and substituted aryloxy.
4. The purified polymeric reagent of claim 3 , wherein each poly(alkylene oxide) is terminally capped with methoxy.
5. The purified polymeric reagent of claim 1 , wherein each poly(alkylene oxide) has a weight-average molecular weight in the range of from about 120 Daltons to about 6,000 Daltons.
6. The purified polymeric reagent of claim 1 , wherein each poly(alkylene oxide) has a weight-average molecular weight in the range of from about 6,000 Daltons to about 100,000 Daltons.
7. The purified polymeric reagent of claim 6 , wherein each poly(alkylene oxide glycol) has a weight-average molecular weight in the range of from about 10,000 Daltons to about 85,000 Daltons.
8. The purified polymeric reagent of claim 7 , wherein each poly(alkylene oxide) has a weight-average molecular weight in the range of from about 20,000 Daltons to about 85,000 Daltons.
9. The purified polymeric reagent of claim 1 , wherein each poly(alkylene oxide) is linear.
10. The purified polymeric reagent of claim 1 , wherein each of the first spacer moiety and second spacer moiety is selected from the group consisting of —NH—C(O)—CH 2 —, —NH—C(O)—CH 2 —O—, —CH 2 —C(O)—NH—, and O—CH 2 —C(O)—NH—.