# US 9,433,593 B1 · Composition for anti-inflammation containing 5-adamantan-1-yl-N-(2,4-dihydroxy-benzyl)-2,4-dimethoxy-benzamide

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- Number: US 9,433,593 B1
- Document ID: US9433593B1
- Status: Granted
- Kind: B1
- Application number: 15/085,628
- Filed: 2016-03-30
- Granted: 2016-09-06
- Earliest claimed: 2015-03-31
- Assignees: Amorepacific Corporation
- Applicants: Amorepacific Corporation
- Inventors: Yung Hyup Joo; Heung Soo Baek; Jeong Hwan Kim; Chang Geun Yi; Hyung Jun Lim; Hong-Ju Shin; Yongjin Kim; Jon Hwan Lee
- Web page: https://patentgrep.com/patent/US9433593B1

## CPC

- A61K 31/166: having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
- A23G 1/42: containing microorganisms or enzymes; containing paramedical or dietetical agents, e.g. vitamins (containing dairy products A23G1/46)
- A23G 3/36: characterised by the composition {containing organic or inorganic compounds}
- A23G 4/12: containing microorganisms or enzymes; containing paramedical or dietetical agents, e.g. vitamins (containing dairy products A23G4/16)
- A23G 9/36: containing microorganisms or enzymes; containing paramedical or dietetical agents, e.g. vitamins (characterised by the dairy products used A23G9/40)
- A23L 33/00: Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L 33/10: using additives (addition of substantially indigestible substances A23L33/21)
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin}
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- 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)
- A23G: COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION

## Abstract

5-Adamantan-1-yl-N-(2,4-dihydroxybenzyl)-2,4-dimethoxybenzamide disclosed in the present disclosure lacks toxicity and can exhibit superior anti-inflammatory effect. It exhibits superior anti-inflammatory effect, for example, by inhibiting the production of one or more of NO and PGE2, by inhibiting the activity of one or more of the transcription factors NF-κB and AP-1 or by inhibiting proinflammatory cytokines such as IL-1β.

## Claims

### Claim 1

A method for inhibiting one or more of the following activities in a subject suffering from inflammation:
(i) the production of one or more of NO and PGE2;
(ii) the expression of one or more of iNOS and COX-2;
(iii) the activity of one or more of the transcription factors NF-κB and AP-1;
(iv) the expression of the proinflammatory cytokine IL-1β,
wherein the method comprises administering an effective amount of 5-adamantan-1-yl-N-(2,4-dihydroxybenzyl)-2,4-dimethoxybenzamide of Chemical Formula 1, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof to a subject in need thereof:

### Claim 2 (depends on 1)

The method according to claim 1, wherein the 5-adamantan-1-yl-N-(2,4-dihydroxybenzyl)-2,4-dimethoxybenzamide of Chemical Formula 1, the pharmaceutically acceptable salt thereof, the hydrate thereof or the solvate thereof inhibits the production of one or more of NO and PGE2.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the 5-adamantan-1-yl-N-(2,4-dihydroxybenzyl)-2,4-dimethoxybenzamide of Chemical Formula 1, the pharmaceutically acceptable salt thereof, the hydrate thereof or the solvate thereof inhibits the expression of one or more of iNOS and COX-2.

### Claim 4 (depends on 1)

The method according to claim 1, wherein the 5-adamantan-1-yl-N-(2,4-dihydroxybenzyl)-2,4-dimethoxybenzamide of Chemical Formula 1, the pharmaceutically acceptable salt thereof, the hydrate thereof or the solvate thereof inhibits the activity of one or more of the transcription factors NF-κB and AP-1.

### Claim 5 (depends on 1)

The method according to claim 1, wherein the 5-adamantan-1-yl-N-(2,4-dihydroxybenzyl)-2,4-dimethoxybenzamide of Chemical Formula 1, the pharmaceutically acceptable salt thereof, the hydrate thereof or the solvate thereof inhibits the expression of the proinflammatory cytokine IL-1β.

### Claim 6 (depends on 1)

The method according to claim 1, wherein the 5-adamantan-1-yl-N-(2,4-dihydroxybenzyl)-2,4-dimethoxybenzamide of Chemical Formula 1, the pharmaceutically acceptable salt thereof, the hydrate thereof or the solvate thereof is administered in a form of composition, and the amount of 5-adamantan-1-yl-N-(2,4-dihydroxybenzyl)-2,4-dimethoxybenzamide of Chemical Formula 1, the pharmaceutically acceptable salt thereof, the hydrate thereof or the solvate thereof is 0.01-20 wt % based on the total weight of the composition.

### Claim 7 (depends on 6)

The method according to claim 6, wherein the composition is a cosmetic composition.

### Claim 8 (depends on 6)

The method according to claim 6, wherein the composition is a food composition.

### Claim 9 (depends on 6)

The method according to claim 6, wherein the composition is a pharmaceutical composition.