# US 10,307,416 B2 · Oligomer-opioid agonist conjugates

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- Number: US 10,307,416 B2
- Document ID: US10307416B2
- Status: Granted
- Kind: B2
- Application number: 15/247,472
- Filed: 2016-08-25
- Published: 2016-12-29
- Granted: 2019-06-04
- Earliest claimed: 2007-03-12
- Assignees: Nektar Therapeutics
- Applicants: Nektar Therapeuitcs
- Inventors: Jennifer Riggs-Sauthier; Bo-Liang Deng; Timothy A. Riley
- Web page: https://patentgrep.com/patent/US10307416B2

## CPC

- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 31/402: 1-aryl substituted, e.g. piretanide
- A61K 31/4025: not condensed and containing further heterocyclic rings, e.g. cromakalim
- A61K 31/439: the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46)
- A61K 31/4468: having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61P 25/00: Drugs for disorders of the nervous system
- C07D 489/02: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.

## Claims

### Claim 1

A compound of the following structure:
wherein n is an integer from 3 to 20.

### Claim 2 (depends on 1)

A composition comprising a compound of claim 1 and a pharmaceutically acceptable excipient.

### Claim 3 (depends on 2)

A composition of claim 2 present in a dosage form suitable for administration.

### Claim 4 (depends on 1)

A method of treating pain comprising administering a compound of claim 1 to a patient in need thereof.

### Claim 5 (depends on 1)

The compound of claim 1 wherein n is 3, 4, 5, 6, 7, 8, or 9.

### Claim 6 (depends on 1)

The compound of claim 1 wherein n is 3.

### Claim 7 (depends on 1)

The compound of claim 1 wherein n is 4.

### Claim 8 (depends on 1)

The compound of claim 1 wherein n is 5.

### Claim 9 (depends on 1)

The compound of claim 1 wherein n is 6.

### Claim 10 (depends on 1)

The compound of claim 1 wherein n is 7.

### Claim 11 (depends on 1)

The compound of claim 1 wherein n is 8.

### Claim 12 (depends on 1)

The compound of claim 1 wherein n is 9.