# US 9,750,734 B2 · Use of flecainide as an anti-connexin agent and method for potentiating the effects of a psychotropic drug

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- Number: US 9,750,734 B2
- Document ID: US9750734B2
- Status: Granted
- Kind: B2
- Application number: 14/907,221
- Filed: 2014-07-24
- Published: 2016-06-09
- Granted: 2017-09-05
- Earliest claimed: 2013-07-24
- Assignees: Commissariat A L'energie Atomique Et Aux Energies Alternatives
- Applicants: Commissariat A L'energie Atomique Et Aux Energies Alternatives
- Inventors: Franck Mouthon; Mathieu Charveriat
- Web page: https://patentgrep.com/patent/US9750734B2

## CPC

- A61K 31/4458: only substituted in position 2, e.g. methylphenidate
- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/12: Antidiarrhoeals
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- 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 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers
- A61P 13/12: of the kidneys
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 15/10: for impotence
- A61P 15/12: for climacteric disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- 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 25/06: Antimigraine agents
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/20: Hypnotics; Sedatives
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- A61P 25/26: Psychostimulants, e.g. nicotine, cocaine
- 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 27/16: Otologicals
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/04: Antibacterial agents
- A61P 31/12: Antivirals
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

## Abstract

The present invention relates to the use of flecainide as an anti-connexin agent. This anti-connexin agent is advantageously used to potentiate the therapeutic effect of various psychotropic drugs. More specifically, the invention provides a combination product containing flecainide and modafinil.

## Claims

### Claim 1

A therapeutic composition comprising flecainide and at least one psychotropic drug, wherein said at least one psychotropic drug is modafinil.

### Claim 2 (depends on 1)

A method for treating fatigue, somnolence, or sleepiness in an individual in need thereof comprising administration of the therapeutic composition according to claim 1 to said individual.

### Claim 3 (depends on 1)

A method for at least one of enhancing the memory of healthy subjects or maintaining said healthy subjects awake for long-lasting periods of time comprising administration of the therapeutic composition of claim 1 to said healthy subjects.

### Claim 4 (depends on 1)

A method for treating cataplexy in a narcoleptic patient comprising administration of the therapeutic composition according to claim 1 to said narcoleptic patient.

### Claim 5 (depends on 1)

The therapeutic composition of claim 1, wherein said flecainide is the R enantiomer of formula:

### Claim 6

A method for enhancing the memory of healthy subjects and/or for maintaining them awake for long-lasting periods of time comprising the administration to said healthy subjects of a) flecainide and b) modafinil, in which said compounds a) and b) are administered simultaneously, separately or in a staggered manner.

### Claim 7 (depends on 2)

The method of claim 2, wherein said flecainide is the R enantiomer of formula:

### Claim 8

A method for potentiating the effects of modafinil, comprising the administration of flecainide as an anti-connexin agent.

### Claim 9 (depends on 8)

The method of claim 8, wherein potentiating the effects of modafinil further comprises potentiating the promnesiant effect and/or the awakening effect of modafinil.

### Claim 10 (depends on 8)

The method of claim 8, wherein said flecainide is the R enantiomer of formula:

### Claim 11 (depends on 2)

The method of claim 2, wherein said flecainide in said therapeutic composition is the R enantiomer of formula:

### Claim 12 (depends on 3)

The method of claim 3, wherein said flecainide in said therapeutic composition is the R enantiomer of formula:

### Claim 13 (depends on 4)

The method of claim 4, wherein said flecainide in said therapeutic composition is the R enantiomer of formula:

### Claim 14 (depends on 6)

The method of claim 6, wherein said flecainide is the R enantiomer of formula:

### Claim 15 (depends on 8)

The method of claim 8, wherein potentiating the effects of modafinil further comprises increasing at least one of the efficacy, safety, or duration of the action of modafinil.

### Claim 16 (depends on 15)

The method of claim 15, wherein said flecainide is the R enantiomer of formula:

### Claim 17 (depends on 9)

The method of claim 9, wherein said flecainide is the R enantiomer of formula:

### Claim 18 (depends on 2)

The method of claim 2 wherein the individual is suffering from excessive daytime sleepiness (EDS), sleep disorders, insufficient sleep time, central sleep apnea, narcolepsy with cataplexy, narcolepsy without cataplexy, obstructive sleep apnea/hypopnea (SAHOS), idiopathic hypersomnia, Kleine-Levin syndrome, circadian rhythm disorders, shift work sleep disorder, jet-lag, disorders after sleep restriction or sleep deprivation, attention disorders, alertness disorders, insomnia, parasomnia, medical-induced somnolence, restless legs syndrome (RLS), Periodic Lim Movement Disorders (PLMD), attention deficit hyperactivity disorder (ADHD), post-traumatic stress disorder (PTSD), Parkinson disease, multiple sclerosis, stroke, neuromuscular disorders, structural brain disorders, respiratory disorders, chronic renal failure, liver failure, rheumatologic disorders, mood disorders, anxiety disorders, schizophrenia, tinnitus, depression, malaise, dementia, bipolar disorder, obesity, hyperphagia, manic episode, obsessive-compulsive disorder, senility, dependence or addiction, cancer, neurodegenerative disorders, menopause, traumatic brain injuries, viral infection or post-myelitis, or fibromyalgia.

### Claim 19 (depends on 18)

The method of claim 18, for treating cataplexy in narcoleptic patients.

### Claim 20 (depends on 19)

The method of claim 19, wherein said flecainide is the R enantiomer of formula:

### Claim 21 (depends on 2)

The method of claim 2 wherein the flecainide and modafinil are administered simultaneously, separately or in a staggered manner.

### Claim 22 (depends on 18)

The method of claim 18 wherein the flecainide and modafinil are administered simultaneously, separately or in a staggered manner.