IP Library › Granted Patent US 11,266,742
Granted Patent B2
US 11,266,742 · App. 16/878,401 · Granted Mar 8, 2022

Conjugates having a degradable linkage and polymeric reagents useful in preparing such conjugates

Inventors: Michael D. Bentley (Huntsville, AL); Sean M. Culbertson (Gurley, AL); Samuel P. McManus (Huntsville, AL)
Assignee: Nektar Therapeutics
A61K47/60A61K38/26A61K38/28C07C235/68C07D207/46C07K14/575C08G61/02C08G65/338C08G65/3348C08G65/33396C08G65/48C08K5/13A61K31/765C08K2201/012
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 11,266,742
App. No.
16/878,401
Granted
Mar 8, 2022
Kind
B2
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.

Claims (15)

1. A conjugate having a structure:

wherein each m-PEG is a methoxy poly(ethylene glycol), and

Drug is a residue of a biologically active agent comprising an amino group.

2. The conjugate of claim 1 , wherein each methoxy poly(ethylene glycol) has a weight-average molecular weight in the range of from about 120 Daltons to about 6,000 Daltons.

3. The conjugate of claim 1 , wherein each methoxy poly(ethylene glycol) has a weight-average molecular weight in the range of from about 6,000 Daltons to about 100,000 Daltons.

4. A pharmaceutical composition comprising the conjugate of claim 1 and a pharmaceutically acceptable excipient.

5. The pharmaceutical composition of claim 4 , in lyophilized form.

6. The pharmaceutical composition of claim 4 , further comprising a liquid diluent.

7. The pharmaceutical composition of claim 6 , wherein the liquid diluent is selected from the group consisting of bacteriostatic water for injection, dextrose 5% in water, phosphate-buffered saline, Ringer's solution, saline solution, sterile water, deionized water, and combinations thereof.

8. The pharmaceutical composition of claim 4 , in unit dosage form.

9. The conjugate of claim 1 , wherein the biologically active agent is a small molecule.

10. The conjugate of claim 1 , wherein the biologically active agent is a polypeptide.

11. A polymeric reagent of a structure:

wherein each m-PEG is a methoxy poly(ethylene glycol), and

(FG) is a functional group capable of reacting with an amino group of a biologically active agent.