# US 10,441,579 B2 · 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compounds

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- Number: US 10,441,579 B2
- Document ID: US10441579B2
- Status: Granted
- Kind: B2
- Application number: 16/239,265
- Filed: 2019-01-03
- Published: 2019-05-09
- Granted: 2019-10-15
- Earliest claimed: 2008-11-14
- Assignees: Theravance Biopharma R&D IP, LLC
- Applicants: Theravance Biopharma R&D IP, LLC
- Inventors: Lori Jean Patterson; Eric L. Stangeland
- Web page: https://patentgrep.com/patent/US10441579B2

## CPC

- A61K 31/4465: only substituted in position 4
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/02: Nutrients, e.g. vitamins, minerals
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/02: Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
- A61P 11/06: Antiasthmatics
- A61P 13/00: Drugs for disorders of the urinary system
- A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers
- A61P 13/10: of the bladder
- A61P 15/10: for impotence
- A61P 15/12: for climacteric disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/22: Anxiolytics
- 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 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 211/22: by oxygen atoms
- C07D 211/32: by oxygen atoms
- 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 compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

## Claims

### Claim 1

A pharmaceutical composition comprising:
(a) a compound of the formula:
or a pharmaceutically acceptable salt thereof; and
(b) a pharmaceutically acceptable carrier selected from starch, microcrystalline cellulose, lactose, sucrose, glucose, mannitol, silicic acid and mixtures thereof.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1, wherein the pharmaceutically acceptable carrier is microcrystalline cellulose.

### Claim 3 (depends on 1)

The pharmaceutical composition of claim 1, wherein the pharmaceutically acceptable carrier is lactose.

### Claim 4 (depends on 1)

The pharmaceutical composition of claim 1, wherein the pharmaceutical composition further comprises a lubricant selected from talc, calcium stearate, magnesium stearate, solid polyethylene glycol, sodium lauryl sulfate and mixtures thereof.

### Claim 5 (depends on 4)

The pharmaceutical composition of claim 4, wherein the lubricant is magnesium stearate.

### Claim 6 (depends on 1)

The pharmaceutical composition of claim 1, wherein the pharmaceutical composition contains about 1 milligram to about 20 milligrams of the compound or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 1)

The pharmaceutical composition of claim 1, wherein the pharmaceutical composition contains about 1 milligram to about 15 milligrams of the compound or a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 1)

The pharmaceutical composition of claim 1 wherein the pharmaceutical composition contains about 1 milligram to about 10 milligrams of the compound or a pharmaceutically acceptable salt thereof.

### Claim 9 (depends on 1, 2, 3, 4, 5, 6, 7, 8)

The pharmaceutical composition of any one of claims 1-8, wherein the compound is a hydrochloride salt.