IP Library › Granted Patent US 11,446,385
Granted Patent B2
US 11,446,385 · App. 16/841,669 · Granted Sep 20, 2022

Polymer derivatives having particular atom arrangements

Inventors: J. Milton Harris (Huntsville, AL); Antoni Kozlowski (Huntsville, AL); Samuel P. McManus (Huntsville, AL); Michael D. Bentley (Huntsville, AL); Stephen A. Charles (Chagrin Falls, OH)
Assignee: Nektar Therapeutics
A61K47/60A61K31/357A61K31/4025A61K31/52A61K38/095A61K38/1816A61K38/193A61K38/212A61K38/215A61K38/24A61K38/27A61K38/37C08G65/329C08G65/33337C08G65/33344
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Quick Facts
Patent No.
US 11,446,385
App. No.
16/841,669
Granted
Sep 20, 2022
Kind
B2
Abstract

Polymeric reagents are provided comprising a moiety of atoms arranged in a specific order, wherein the moiety is positioned between a water-soluble polymer and a reactive group. The polymeric reagents are useful for, among other things, forming polymer-active agent conjugates. Related methods, compositions, preparations, and so forth are also provided.

Claims (26)

1. A water-soluble polymer conjugate having a structure:

wherein:

POLY 1 is a linear water-soluble polymer;

(a) is 0, 1, 2 or 3;

(b) is 0, 1, 2 or 3;

R 1 is H or an organic radical;

X 1 , when present, is a first spacer moiety;

X 2 , when present, is a second spacer moiety; and

Active Agent is a pharmacologically active agent selected from the group consisting of small molecules, peptides, polypeptides, and proteins.

2. The water-soluble polymer conjugate of claim 1 , wherein R 1 is H.

3. The water-soluble polymer conjugate of claim 1 , wherein the linear water-soluble polymer is selected from the group consisting of a poly(alkylene oxide), poly(vinyl pyrrolidone), poly(vinyl alcohol), polyoxazoline, poly(acryloylmorpholine), and poly(oxyethylated polyols).

4. The water-soluble polymer conjugate of claim 1 , wherein the water-soluble polymer is a poly(alkylene oxide).

5. The water-soluble polymer conjugate of claim 4 , wherein the poly(alkylene oxide) is a poly(ethylene glycol).

6. The water-soluble polymer conjugate of claim 5 , wherein the poly(ethylene glycol) is terminally capped with an end-capping moiety selected from the group consisting hydroxyl and alkoxy.

7. The water-soluble polymer conjugate of claim 6 , wherein the poly(ethylene glycol) has a molecular weight of from about 100 Daltons to about 100,000 Daltons.

8. The water-soluble polymer conjugate of claim 7 , wherein the poly(ethylene glycol) has a molecular weight of from about 1,000 Daltons to about 60,000 Daltons.

9. The water-soluble polymer conjugate of claim 7 , wherein the poly(ethylene glycol) has a nominal average molecular mass of from about 2,000 Daltons to about 50,000 Daltons.

10. The water-soluble polymer conjugate of claim 5 , wherein the poly(ethylene glycol) is terminally capped with methoxy.

11. The water-soluble polymer conjugate of claim 1 , wherein the water-soluble polymer is a homopolymer.

12. The water-soluble polymer conjugate of claim 1 , wherein the nitrogen atom of the

moiety is linked to the water-soluble polymer through a direct covalent bond.

13. The water-soluble polymer conjugate of claim 1 , wherein the nitrogen atom of the

moiety is linked to the water-soluble polymer through a first spacer moiety.

14. The water-soluble polymer conjugate of claim 1 , wherein (a) is 0 or 1; and (b) is 0 or 1.

15. The water-soluble polymer conjugate of claim 1 , wherein POLY 1 -(X 1 ) a —N(R 1 )˜ is selected from:

where (m) is 2 to 4,000.