# US 8,772,308 B2 · Non-peptidyl, potent, and selective mu opioid receptor antagonists

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- Number: US 8,772,308 B2
- Document ID: US8772308B2
- Status: Granted
- Kind: B2
- Application number: 13/144,788
- Filed: 2010-01-15
- Published: 2011-12-15
- Granted: 2014-07-08
- Earliest claimed: 2009-01-16
- Assignees: Virginia Commonwealth University
- Applicants: Yan Zhang; Dana E. Selley; William Dewey
- Inventors: Yan Zhang; Dana E. Selley; William Dewey
- Web page: https://patentgrep.com/patent/US8772308B2

## CPC

- C07D 405/12: linked by a chain containing hetero atoms as chain links
- A61P 25/32: Alcohol-abuse
- A61P 25/36: Opioid-abuse
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D 491/10: Spiro-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Selective, non-peptide antagonists of the mu opioid receptor (MOR) and methods of their use are provided. The antagonists may be used, for example, to identify MOR agonists in competitive binding assays, and to treat conditions related to addiction in which MOR is involved, e.g. heroin, prescription drug and alcohol addiction.

## Claims

### Claim 1

A selective, non-peptide MOR antagonist represented by formula
where
Z is selected from the group consisting of an aliphatic moiety, NH, CO, (NHCO)n where n=1-5, (CONH)n where n=1-5, (NHCO)(CH2)n(NHCO), where n=1-5, (NHCO)(CH2)n where n=1-5, (CH2)n(NHCO), where n=1-5, and O, and
R is selected from the group consisting of

### Claim 2 (depends on 1)

The selective, non-peptide MOR antagonist of claim 1, wherein said non-peptide MOR antagonist is represented by formula

### Claim 3 (depends on 1)

The selective, non-peptide MOR antagonist of claim 1, wherein said non-peptide MOR antagonist is represented by formula

### Claim 4

A method of testing whether or not a candidate compound is a MOR agonist, comprising the step of
conducting competitive inhibition tests between said candidate compound and a MOR antagonist represented by formula
where
Z is selected from the group consisting of an aliphatic moiety, NH, CO, (NHCO)n where n=1-5, (CONH)n where n=1-5, (NHCO)(CH2)n(NHCO), where n=1-5, (NHCO)(CH2)n where n=1-5, (CH2)n(NHCO), where n=1-5, and O, and
R is selected from the group consisting of

### Claim 5

A method of treating symptoms of opiate addiction in a patient in need thereof, comprising
administering to said patient a MOR antagonist represented by formula
where
Z is selected from the group consisting of an aliphatic moiety, NH, CO, (NHCO)n where n=1-5, (CONH)n where n=1-5, (NHCO)(CH2)n(NHCO), where n=1-5, (NHCO)(CH2)n where n=1-5, (CH2)n(NHCO), where n=1-5, and O, and
R is selected from the group consisting of