# US 2014/0155412 A1 · Oligomer-diarylpiperazine conjugates

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2014/0155412 A1
- Document ID: US20140155412A1
- Status: Published application
- Kind: A1
- Application number: 14/175,410
- Filed: 2014-02-07
- Published: 2014-06-05
- Earliest claimed: 2008-01-25
- Assignees: Nektar Therapeutics
- Applicants: Nektar Therapeutics
- Inventors: Zhongxu Ren; Jennifer Riggs-Sauthier
- Web page: https://patentgrep.com/patent/US20140155412A1

## CPC

- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/12: Antidiarrhoeals
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/00: Drugs for disorders of the urinary system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/24: Antidepressants
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 25/30: for treating abuse or dependence
- A61P 25/32: Alcohol-abuse
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- C07D 241/04: having no double bonds between ring members or between ring members and non-ring members
- 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 relates to (among other things) oligomer-diarylpiperazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated diarylpiperazine compounds.

## Claims

### Claim 1

A method of treatment comprising administering a therapeutically effective amount of a compound to a subject in need of opioid receptor agonism, wherein the compound has a structure selected from the group consisting of
wherein, in each structure, R3 is either H or CH3, R5 is either H or CH3, X is a spacer moiety, and POLY is a water-soluble, non-peptidic oligomer.

### Claim 2 (depends on 1)

The method of claim 1, wherein the water-soluble, non-peptidic oligomer is a poly(alkylene oxide).

### Claim 3 (depends on 2)

The method of claim 2, wherein the poly(alkylene oxide) is a poly(ethylene oxide).

### Claim 4 (depends on 1)

The method of claim 1, wherein the water-soluble, non-peptidic oligomer has between 1 and 30 monomers.

### Claim 5 (depends on 4)

The method of claim 4, wherein the water-soluble, non-peptidic oligomer has between 1 and 10 monomers.

### Claim 6 (depends on 2)

The method of claim 2, wherein the poly(alkylene oxide) includes an alkoxy or hydroxy end-capping moiety.

### Claim 7 (depends on 1)

The method of claim 1, wherein the water-soluble, non-peptidic oligomer is covalently attached via a stable linkage.

### Claim 8 (depends on 1)

The method of claim 1, wherein the water-soluble, non-peptidic oligomer is covalently attached via a degradable linkage.

### Claim 9 (depends on 1)

The method of claim 1, wherein X is an oxygen.

### Claim 10 (depends on 1)

The method of claim 1, wherein X is an ester.

### Claim 11 (depends on 1)

The method of claim 1, wherein the opioid receptor is a delta opioid receptor.