# US 11,298,327 B2 · Methods and compositions for treating and preventing arthritis

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- Number: US 11,298,327 B2
- Document ID: US11298327B2
- Status: Granted
- Kind: B2
- Application number: 17/017,999
- Filed: 2020-09-11
- Published: 2020-12-31
- Granted: 2022-04-12
- Earliest claimed: 2014-11-07
- Assignees: Albert Einstein College of Medicine
- Applicants: Albert Einstein College of Medicine
- Inventors: Hui B. Sun; Daniel J. Leong; Neil J. Cobelli; David M. Hirsh; John A. Hardin; Karen E. Sperling; Sun J. Kim; David C. Spray; Chandan Guha; Marwa Choudhury
- Web page: https://patentgrep.com/patent/US11298327B2

## CPC

- A61K 31/05: Phenols {(cannabinoids A61K31/658)}
- 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 9/0019: {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 31/12: Ketones
- A61K 31/353: 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- 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

Methods and formulations are provided for treating or preventing arthritis, in particular osteoarthritis, where the formulation to be administered to a subject for treating or preventing arthritis comprises carvacrol, curcumin, epigallocatechin-3-gallate and oligomeric procyanidins.

## Claims

### Claim 1

A method of treating osteoarthritis in a subject in need thereof, comprising administering to the subject as active agents:
a therapeutically-effective amount of carvacrol;
a therapeutically-effective amount of curcumin;
a therapeutically-effective amount of epigallocatechin-3-gallate; and
a therapeutically-effective amount of oligomeric procyanidins,
wherein the therapeutically-effective amounts of carvacrol, curcumin, epigallocatechin-3-gallate, and oligomeric procyanidins are selected to synergistically increase expression of Cbp/p300 interacting transactivator with ED-rich tail 2 (CITED2) in the subject, and
wherein the carvacrol, the curcumin, the epigallocatechin-3-gallate, and the oligomeric procyanidins are present in a molar ratio of 1:1:100:50 or in a weight ratio of 10:10:1:10.

### Claim 2 (depends on 1)

The method of claim 1, wherein the active agents are in a pharmaceutical formulation and the pharmaceutical formulation further comprises a pharmaceutically acceptable carrier.

### Claim 3 (depends on 1)

The method of claim 1, wherein the carvacrol, the curcumin, the epigallocatechin-3-gallate, and the oligomeric procyanidins are present in the molar ratio of 1:1:100:50.

### Claim 4 (depends on 1)

The method of claim 1, wherein the carvacrol, the curcumin, the epigallocatechin-3-gallate, and the oligomeric procyanidins are present in the weight ratio of 10:10:1:10.

### Claim 5 (depends on 1)

The method of claim 1, wherein the administering is by injection.

### Claim 6 (depends on 1)

The method of claim 1, wherein the administering is topical.

### Claim 7 (depends on 1)

The method of claim 1, wherein the administering is oral.

### Claim 8 (depends on 1)

The method of claim 1, wherein the administering reduces cartilage degradation associated with the osteoarthritis in the subject.

### Claim 9 (depends on 1)

The method of claim 1, wherein the administering reduces inflammation associated with the osteoarthritis in the subject.

### Claim 10 (depends on 1)

The method of claim 1, wherein the administering reduces pain symptoms associated with the osteoarthritis in the subject.

### Claim 11 (depends on 1)

The method of claim 1, wherein the administering suppresses expression of a cartilage degradation enzyme in the subject.

### Claim 12 (depends on 1)

The method of claim 1, wherein the administering suppresses expression of matrix metalloproteinase-1 (MMP-1) in the subject.

### Claim 13 (depends on 1)

The method of claim 1, wherein the administering suppresses expression of matrix metalloproteinase-3 (MMP-3) in the subject.

### Claim 14 (depends on 1)

The method of claim 1, wherein the administering suppresses expression of matrix metalloproteinase-13 (MMP-13) in the subject.

### Claim 15 (depends on 1)

The method of claim 1, wherein the administering suppresses expression of ADAM metallopeptidase with thrombospondin type 1 motif 5 (ADAMTS5) in the subject.

### Claim 16 (depends on 1)

The method of claim 1, wherein the administering suppresses expression of tumor necrosis factor-alpha (TNF-α) in the subject.