# US 11,439,640 B2 · Pharmaceutical composition comprising substance inhibiting enzymatic activity of peroxiredoxin 2 as effective ingredient for treatment of colorectal cancer

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- Number: US 11,439,640 B2
- Document ID: US11439640B2
- Status: Granted
- Kind: B2
- Application number: 16/728,100
- Filed: 2019-12-27
- Published: 2020-04-30
- Granted: 2022-09-13
- Earliest claimed: 2017-06-27
- Assignees: Ewha University-Industry Collaboration Foundation
- Applicants: Ewha University-Industry Collaboration Foundation
- Inventors: Sang Won Kang
- Web page: https://patentgrep.com/patent/US11439640B2

## CPC

- A61K 31/502: ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
- A61P 35/00: Antineoplastic agents
- 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 a pharmaceutical composition for treating colorectal cancer including a material inhibiting the enzyme activity of peroxiredoxin 2 as an active ingredient, and more specifically, to a pharmaceutical composition for treating colorectal cancer, which exhibits the effect of reducing colon polyps via increase of active β-catenin degradation by inhibiting the activity of peroxiredoxin 2, based on the mechanism that promotes colorectal tumor by the interaction between peroxiredoxin 2 (PrxII) and tankyrase (TNKS) in an APC-mutant cell.

## Claims

### Claim 1

A method for improving or treating colorectal cancer in a subject in need thereof, comprising the step of administering a pharmaceutically effective dose of a material inhibiting an enzyme activity of peroxiredoxin 2 to the subject,
wherein the material inhibiting the enzyme activity of peroxiredoxin 2 is a compound of the following Formula 1:
wherein in Formula 1 above,
R1 is —O—R2, a cyclic group, or hydrogen; and
R2 is a branched or unbranched C1 to C8 alkyl, a branched or unbranched C2 to C8 alkenyl, a branched or unbranched C2 to C8 alkynyl, or an aromatic or non-aromatic cyclic group that is substituted or unsubstituted.

### Claim 2 (depends on 1)

The method for improving or treating colorectal cancer of claim 1, wherein the material inhibiting the enzyme activity of peroxiredoxin 2 is one or more selected from the group consisting of Compound-1 to Compound-6 shown below:

### Claim 3 (depends on 1)

The method for improving or treating colorectal cancer of claim 1, wherein the material inhibiting the enzyme activity of peroxiredoxin 2 increases degradation of β-catenin.

### Claim 4 (depends on 1)

The method for improving or treating colorectal cancer of claim 1, wherein the material inhibiting the enzyme activity of speroxiredoxin 2 decreases degradation of Axin1 by tankyrase (TNKS).

### Claim 5 (depends on 1)

The method for improving or treating colorectal cancer of claim 1, wherein the material inhibiting the enzyme activity of peroxiredoxin 2 increases oxidative inactivation of tankyrase (TNKS).

### Claim 6 (depends on 5)

The method for improving or treating colorectal cancer of claim 5, wherein the oxidative inactivation of tankyrase (TNKS) occurs in cytoplasm of an APC-mutant cell.

### Claim 7 (depends on 1)

The method for improving or treating colorectal cancer of claim 1, wherein the material inhibiting the enzyme activity of peroxiredoxin 2 decreases interaction between peroxiredoxin 2 and tankyrase (TNKS) in cytoplasm of an APC-mutant cell.