# US 11,306,117 B2 · Whitening composition containing novel quercetin-based compound

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- Number: US 11,306,117 B2
- Document ID: US11306117B2
- Status: Granted
- Kind: B2
- Application number: 16/622,017
- Filed: 2018-06-11
- Published: 2020-05-07
- Granted: 2022-04-19
- Earliest claimed: 2017-06-12
- Assignees: Amorepacific Corporation
- Applicants: Amorepacific Corporation
- Inventors: Yong-Deog Hong; Jeong-Kee Kim
- Web page: https://patentgrep.com/patent/US11306117B2

## CPC

- C07H 17/04: Heterocyclic radicals containing only oxygen as ring hetero atoms
- A23L 2/52: Adding ingredients (adding preservatives A23B70/10)
- A23L 33/105: Plant extracts, their artificial duplicates or their derivatives
- A61K 8/602: {Glycosides, e.g. rutin}
- A61K 8/9789: Magnoliopsida [dicotyledons]
- 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 31/7048: having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin {, digitoxin or digoxin}
- A61K 36/82: Theaceae (Tea family), e.g. camellia
- A61Q 19/02: for chemically bleaching or whitening the skin
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- A61K 2236/33: involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K 2236/331: using water, e.g. cold water, infusion, tea, steam distillation or decoction
- A61K 2236/333: using mixed solvents, e.g. 70% EtOH
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- 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)
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY 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 specification relates to a whitening composition containing a novel quercetin-based compound isolated from post-fermented tea, an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof, wherein the whitening composition can be widely utilized in fields associated with skin whitening and skin care.

## Claims

### Claim 1

A method for skin whitening comprising administering a compound of following formula 1, an optical isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, or an extract of post-fermented tea comprising the same to a subject in need thereof:
wherein in formula 1, R1 is C15H9O7, R2 is H or C6H11O5, and R3 is C9H7O2.

### Claim 2 (depends on 1)

The method according to claim 1, wherein R1 is represented by following formula 2:

### Claim 3 (depends on 1)

The method according to claim 1, wherein R2 is represented by following formula 3:

### Claim 4 (depends on 1)

The method according to claim 1, wherein R3 is represented by following formula 4:

### Claim 5 (depends on 1)

The method according to claim 1, wherein the compound is Quercetin3-O-[3-O″-(E)-p-coumaroyl][β-D-glucopyranosyl-(1→3)-O-α-L-rhamnopyranosyl-(1→6)-O-β-D-glucopyranoside].

### Claim 6 (depends on 1)

The method according to claim 1, wherein the compound is quercetin3-O-[3-O″-(E)-p-Cumaroyl][α-L-Rhamnopyranosyl-(1→6)-O-β-D-Glucopyranoside].

### Claim 7 (depends on 1)

The skin whitening composition according to claim 1, wherein the compound of the formula 1, the optical isomer thereof, the pharmaceutically acceptable salt thereof, the hydrate thereof, the solvate thereof, or the extract of post-fermented tea comprising the same inhibits one or more of tyrosinase activity and melanogenesis.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the compound of the formula 1, the optical isomer thereof, the pharmaceutically acceptable salt thereof, the hydrate thereof, the solvate thereof, or the extract of post-fermented tea comprising the same improves or treats one or more selected from the group consisting of freckle, ephelides, lentigo, birthmark, Melanoma, pigmentation caused by ultraviolet rays, pigmentation caused by drugs, pigmentation after inflammation, and pigmentation occurring in dermatitis.

### Claim 9 (depends on 1)

The method according to claim 1, wherein:
the compound of the formula 1, the optical isomer thereof, the pharmaceutically acceptable salt thereof, the hydrate thereof, or the solvate thereof is administered in a form of a composition, and
the amount of the compound of formula 1, the optical isomer thereof, the pharmaceutically acceptable salt thereof, the hydrate thereof, or the solvate thereof in the composition is 0.00001 wt. % to 10 wt. %, relative to the total weight of the composition.

### Claim 10 (depends on 1)

The method according to claim 1, wherein:
the extract of post-fermented tea is administered in a form of a composition, and
the amount of the extract of post-fermented tea in the composition is 0.1 wt. % to 90 wt. %, relative to the total weight of the composition.

### Claim 11 (depends on 1)

The method according to claim 1, wherein the extract comprises the compound of formula 1, the optical isomer thereof, the pharmaceutically acceptable salt thereof, the hydrate thereof, or the solvate thereof in the amount of 0.00001 wt. % to 20 wt. %, relative to the total weight of the extract.

### Claim 12 (depends on 1)

The method according to claim 1, wherein the dosage of the compound of formula 1, the optical isomer thereof, the pharmaceutically acceptable salt thereof, the hydrate thereof, or the solvate thereof is 0.00001 mg/kg/day to 100 mg/kg/day.

### Claim 13 (depends on 1)

The method according to claim 1, wherein:
the compound of formula 1, the optical isomer thereof, the pharmaceutically acceptable salt thereof, the hydrate thereof, the solvate thereof, or the extract of post-fermented tea comprising the same is administered in form of a composition, and
the composition is a food composition, a cosmetic composition, or a pharmaceutical composition.