# US 11,439,603 B2 · Compositions for ameliorating, preventing or treating somnipathy including phloroglucinol as active ingredient and compositions for suppressing intolerance to or alleviating side effects of agonist at benzodiazepine binding site of GABA-A receptor including phloroglucinol as active ingredient

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- Number: US 11,439,603 B2
- Document ID: US11439603B2
- Status: Granted
- Kind: B2
- Application number: 16/612,089
- Filed: 2018-05-10
- Published: 2020-04-16
- Granted: 2022-09-13
- Earliest claimed: 2017-05-11
- Assignees: Korea Food Research Institute
- Applicants: Korea Food Research Institute
- Inventors: Sueng Mok Cho; Min Young Um; Min Seok Yoon; Hye Jin Yang; Jae Kwang Lee; Jong Hoon Jung
- Web page: https://patentgrep.com/patent/US11439603B2

## CPC

- A61K 31/05: Phenols {(cannabinoids A61K31/658)}
- A23L 33/10: using additives (addition of substantially indigestible substances A23L33/21)
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/0056: {Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/145: {with organic compounds}
- A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin}
- A61K 9/4858: {Organic compounds}
- A61K 31/047: having two or more hydroxy groups, e.g. sorbitol
- A61K 31/437: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/5025: ortho- or peri-condensed with heterocyclic ring systems
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61P 25/20: Hypnotics; Sedatives
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- A23V 2200/31: having an effect on comfort perception and well-being
- 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)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION

## Abstract

The present invention relates to a pharmaceutical composition and a health functional food composition, which include phloroglucinol active ingredient, for preventing, treating, or ameliorating somnipathy and suppressing intolerance to, alleviating, or ameliorating side effects of an agonist at the benzodiazepine binding site of the GABA-A receptor. The pharmaceutical composition and the food composition rapidly and reliably induce and maintain sleep, prevent repeated awakenings, unalter physiological sleep architecture, are particularly devoid of residual sedative effects, which could impair daytime functioning and cognitive performance, and neither cause side effects nor intolerance to a conventional agonist at the benzodiazepine binding site of the GABA-A receptor despite long-term administration. The pharmaceutical composition uses a reduced amount of the agonist, which may increase the amount of sleep but degrade the quality of sleep to cause various side effects, to alleviate side effects of the agonist or suppress tolerance to the agonist resulting from long-term administration.

## Claims

### Claim 1

A method for suppressing intolerance to or alleviating side effects of an agonist at the benzodiazepine binding site of the GABA-A receptor, comprising administrating a pharmaceutical composition comprising phloroglucinol as an active ingredient to a patient who has intolerance to or suffers from side effects of the agonist;
wherein the agonist is previously-administered or co-administered with the composition; and
wherein the agonist is administered at an amount of 2 to 10 mg on a daily basis.

### Claim 2

A method for treating somnipathy, comprising administering a pharmaceutical composition comprising phloroglucinol and an agonist at the benzodiazepine binding site of the GABA-A receptor as active ingredients to a patient who has intolerance to or suffers from side effects of an agonist at the benzodiazepine binding site of the GABA-A receptor.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the intolerance to the agonist is a reduced therapeutic effect on somnipathy resulting from long-term administration of the agonist.

### Claim 4 (depends on 1)

The method according to claim 1, wherein the side effect of the agonist is one or more selected from the group of EEG delta power suppression and residual sedation.

### Claim 5 (depends on 1)

The method according to claim 1, wherein the agonist is a non-benzodiazepine drug selected from the group of zolpidem, zopiclone, zaleplon, trazodone, and combinations thereof.