# US 11,298,353 B2 · Anti-inflammatory composition

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- Number: US 11,298,353 B2
- Document ID: US11298353B2
- Status: Granted
- Kind: B2
- Application number: 16/719,913
- Filed: 2019-12-18
- Published: 2021-03-04
- Granted: 2022-04-12
- Earliest claimed: 2019-08-30
- Assignees: Osteoneurogen Inc.
- Applicants: Osteoneurogen Inc.
- Inventors: Byung Soo Youn; Han Soo Kim; Ik Hwan Kim; Ho Sup Yoon; Moon Kee Maeng; Baik Lin Seong; Min Ju Ham; Hyeong Deok Choi
- Web page: https://patentgrep.com/patent/US11298353B2

## CPC

- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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 an anti-inflammatory composition, and more particularly to an anti-inflammatory composition containing, as an active ingredient, a compound represented by Formula 1 or a salt thereof, wherein the anti-inflammatory composition may inhibit inflammatory response even at an early stage by inhibiting the interaction between CD14 and LPS and blocking the expression of CD14 and the expression of TNFα and IL-1β, which are the key factors in inflammatory response, and may also regulate the expression of important factors, such as CCL2 (MCP-1), CCL7 (MCP-3), CXCL2, CHOP and NOX1, which are involved in inflammatory response.

## Claims

### Claim 1

A method of treating an inflammatory disease in a subject in need thereof, comprising:
administering to the subject in need there of a composition comprising, as an active ingredient, a compound represented by the Formula 1:
or a salt thereof,
wherein R1 is C1-5 alkyl, C5-6 cycloalkyl, C5-6 heterocycloalkyl, C6-12 aryl or C5-6 heteroaryl, where the C5-6 heterocycloalkyl or C5-6 heteroaryl each independently contain at least one heteroatom selected from the group consisting of oxygen and nitrogen;
R2 is hydrogen, ethyl, acetyl, acetoxy, carboxy, benzoyloxy or 3,4,5-trihydroxybenzoyloxy;
R3 is hydrogen, hydroxy, methyl, methoxy, acetoxy, carboxy or benzoyloxy;
R4 is hydrogen, hydroxy, methyl, methoxy, acetoxy, carboxy or benzoyloxy; and
R5 is hydrogen, hydroxy, methyl, methoxy, acetoxy, carboxy or benzoyloxy,
wherein the inflammatory disease is selected from the group consisting of Crohn's disease, ulcerative colitis, rheumatoid arthritis, lupus, multiple sclerosis and psoriasis.

### Claim 2 (depends on 1)

The method of claim 1, wherein R1 is methyl, ethyl, cyclopentyl, cyclohexyl or phenyl.

### Claim 3 (depends on 1)

The method of claim 1, wherein
R1 is methyl;
R2 is hydrogen;
R3 is hydrogen, hydroxy or methoxy;
R4 is hydroxy or methoxy; and
R5 is hydrogen, hydroxy or methoxy.

### Claim 4 (depends on 1)

The method of claim 1, wherein the compound is selected from the group consisting of Formula 2, Formula 3, Formula 4 and Formula 5:
or a salt thereof.

### Claim 5 (depends on 1)

The method of claim 1, wherein the composition is a pharmaceutical composition, a quasi-drug composition, a food composition, a food additive composition, a feed composition, a feed additive composition, or a cosmetic composition.
