# US 10,766,864 B2 · Morphinan derivatives for the treatment of neuropathic pain

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- Number: US 10,766,864 B2
- Document ID: US10766864B2
- Status: Granted
- Kind: B2
- Application number: 15/569,726
- Filed: 2016-05-05
- Published: 2018-05-10
- Granted: 2020-09-08
- Earliest claimed: 2015-05-08
- Assignees: Nektar Therapeutics
- Applicants: Nektar Therapeutics
- Inventors: Neel K. Anand; Natalia Aurrecoechea; Lin Cheng; Bo-Liang Deng; Donogh John Roger O'Mahony; YongQi Mu; Erik Krogh-Jespersen
- Web page: https://patentgrep.com/patent/US10766864B2

## CPC

- C07D 221/28: Morphinans
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 407/04: directly linked by a ring-member-to-ring-member bond
- C07D 407/12: linked by a chain containing hetero atoms as chain links
- C07D 417/12: linked by a chain containing hetero atoms as chain links
- C07D 471/08: Bridged systems
- C07D 513/08: Bridged systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to compounds and their use as ligands for mu opioid receptors. Also included are methods for preparing the compounds and pharmaceutical compositions containing the compounds. In one or more embodiments of the invention, a compound according to Formula I is provided: and pharmaceutically acceptable salts thereof, wherein R1-R11 are as described herein.

## Claims

### Claim 1

A compound of Formula I:
wherein:
R1 is —N(R17)(R18);
R2, R3, R4, R5, R6, R7 R9, R19, and R11 are hydrogen;
R8 is —CH3;
R17 is a heteroaryl substituted with —X-POLY;
R18 is hydrogen;
X is a linker;
POLY is a poly(alkylene oxide); and
pharmaceutically acceptable salts thereof.

### Claim 2 (depends on 1)

The compound of claim 1, having a structure of Formula II,
wherein:
—X-POLY is —X—(CH2CH2O)n—R, where n is 1 to 30 and R is selected from hydrogen, lower alkyl, haloalkyl and carboxyl.

### Claim 3

A method for treating an individual in need of treatment for neuropathic pain, the method comprising the step of administering to the individual a compound having the following formula:
wherein:
R1 is —N(R17)(R18);
R2, R3, R4, R5, R6, R7, R9, R10, and R11 are hydrogen
R8 is —CH3;
R17 is a heteroaryl substituted with X-POLY;
R18 is hydrogen;
X is a linker;
POLY is a poly(alkylene oxide); and
pharmaceutically acceptable salts thereof.

### Claim 4 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1, and at least one pharmaceutically acceptable excipient.

### Claim 5

A composition of matter comprising a compound of 1, wherein the compound is present in a dosage form.

### Claim 6 (depends on 1)

The compound of claim 1, wherein a heteroatom of the heterocycle is selected from O, N, and S.

### Claim 7 (depends on 1)

The compound of claim 1, wherein the heterocycle is selected from an imidazole, a pyrimidine, a thiazole, and a pyridine.

### Claim 8 (depends on 1)

The compound of claim 1, wherein R17 is selected from