# US 9,040,658 B2 · Thiol-selective water-soluble polymer derivatives

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- Number: US 9,040,658 B2
- Document ID: US9040658B2
- Status: Granted
- Kind: B2
- Application number: 14/229,547
- Filed: 2014-03-28
- Published: 2014-11-06
- Granted: 2015-05-26
- Earliest claimed: 2003-01-06
- Assignees: Nektar Therapeutics
- Applicants: Nektar Therapeutics
- Inventors: Antoni Kozlowski; Remy F. Gross, III; Samuel P. McManus
- Web page: https://patentgrep.com/patent/US9040658B2

## CPC

- C08G 65/00: Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61K 47/62: the modifying agent being a protein, peptide or polyamino acid
- C07C 319/06: from sulfides, hydropolysulfides or polysulfides
- C07C 323/41: Y being a hydrogen or an acyclic carbon atom
- C08G 65/2636: {the other compounds containing sulfur}
- C08G 65/329: with organic compounds
- C08G 65/334: containing sulfur
- C08L 2203/02: for biomedical use
- C08G: MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C08L: COMPOSITIONS OF MACROMOLECULAR COMPOUNDS (compositions based on polymerisable monomers C08F, C08G; artificial filaments or fibres D01F; textile treating compositions D06)

## Abstract

The present invention provides water-soluble, polymer derivatives having a thiol-selective terminus suitable for selective coupling to thiol groups, such as those contained in the cysteine residues of proteins, as well as methods for preparing the water-soluble, polymer derivatives having a thiol-selective terminus.

## Claims

### Claim 1

A polymer having the following structure:
POLY-L0,1-X—Y—S—S—Y—X-L0,1-POLY
wherein:
POLY is an end-capped polyalkylene oxide;
L is an optional linker;
X is selected from the group consisting of amide, carbamate, carbonate ester, ether and thioester;
Y is selected from the group consisting of alkylene, substituted alkylene, cycloalkylene, substituted cycloalkylene, aryl, and substituted aryl, comprising from about 2 to about 10 carbon atoms; and
S is a sulfur atom.

### Claim 2 (depends on 1)

The polymer of claim 1, wherein L1 is a linker selected from the group consisting of C1-C10 alkyl and C1-C10 substituted alkyl.

### Claim 3 (depends on 1)

The polymer of claim 1, wherein L1 is a linker selected from the group consisting of (CH2)1, 2, 3, 4 and 5.

### Claim 4 (depends on 1)

The polymer of claim 1, wherein L is —CH2—.

### Claim 5 (depends on 1)

The polymer of claim 1, wherein POLY is a polyethylene glycol having the structure H3CO—(CH2CH2O)nCH2CH2— wherein n ranges from 10 to about 4,000.

### Claim 6 (depends on 1)

The polymer of claim 1, wherein L is absent (L0).