# US 11,998,523 B2 · Ascorbic acid and quinone compounds for treating Chagas disease

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 11,998,523 B2
- Document ID: US11998523B2
- Status: Granted
- Kind: B2
- Application number: 16/466,931
- Filed: 2017-12-05
- Published: 2019-11-14
- Granted: 2024-06-04
- Earliest claimed: 2016-12-06
- Assignees: IC-MedTech Corp.
- Applicants: IC-MedTech Corp.
- Inventors: Sueli de Oliveira Silva Lautenschlager; Vânia Cristina Desoti; Celso Vataru Nakamura; Valdecir Farias Ximenes
- Web page: https://patentgrep.com/patent/US11998523B2

## CPC

- A61K 31/375: Ascorbic acid, i.e. vitamin C; Salts thereof
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
- A61K 31/4168: having a nitrogen attached in position 2, e.g. clonidine
- A61K 31/541: Non-condensed thiazines containing further heterocyclic rings
- A61P 33/02: Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P 33/14: Ectoparasiticides, e.g. scabicides
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

Provided herein is a method of treating, preventing, or alleviating one or more symptoms of Chagas disease in a subject, comprising administering to the subject (i) ascorbic acid, or a single enantiomer, a mixture of enantiomers, or a mixture of diastereomers thereof; or a pharmaceutically acceptable salt, solvate, or hydrate thereof; and (ii) a quinone compound, or a single enantiomer, a mixture of enantiomers, or a mixture of diastereomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof.

## Claims

### Claim 1

A method of treating, preventing, or alleviating Chagas disease in a subject, comprising administering to the subject: (i) ascorbic acid, or a single enantiomer, a mixture of enantiomers, or a mixture of diastereomers thereof; or a pharmaceutically acceptable salt, solvate, or hydrate thereof; and (ii) a quinone compound, or a single enantiomer, a mixture of enantiomers, or a mixture of diastereomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof; wherein the quinone compound is vitamin K3.

### Claim 2 (depends on 1)

The method of claim 1, wherein the ascorbic acid is administered orally.

### Claim 3 (depends on 1)

The method of claim 1, wherein the quinone compound is administered orally.

### Claim 4 (depends on 1)

The method of claim 1, wherein the ascorbic acid and the quinone compound are administered together in a single composition comprising ascorbic acid, or a single enantiomer, a mixture of enantiomers, or a mixture of diastereomers thereof; or a pharmaceutically acceptable salt, solvate, or hydrate thereof; and a quinone compound, or a single enantiomer, a mixture of enantiomers, or a mixture of diastereomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof.

### Claim 5 (depends on 1)

The method of claim 1, wherein the ascorbic acid and the quinone compound are formulated together in a single oral dosage form.

### Claim 6 (depends on 5)

The method of claim 5, wherein the single oral dosage form is a tablet.

### Claim 7 (depends on 5)

The method of claim 5, wherein the single oral dosage form is a capsule.

### Claim 8 (depends on 7)

The method of claim 7, wherein the capsule comprises about 500 mg of ascorbic acid, or a single enantiomer, a mixture of enantiomers, or a mixture of diastereomers thereof; or a pharmaceutically acceptable salt, solvate, or hydrate thereof; and about 5 mg of a quinone compound, or a single enantiomer, a mixture of enantiomers, or a mixture of diastereomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof.

### Claim 9 (depends on 7)

The method of claim 7, wherein the ascorbic acid is L-ascorbic acid or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate or hydrate thereof.

### Claim 10 (depends on 1)

The method of claim 1, wherein the ascorbic acid is L-ascorbic acid or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate or hydrate thereof.

### Claim 11 (depends on 10)

The method of claim 10, wherein the ascorbic acid is an alkali or alkaline earth metal salt of L-ascorbic acid, or a pharmaceutically acceptable solvate or hydrate thereof.

### Claim 12 (depends on 11)

The method of claim 11, wherein the ascorbic acid is sodium L-ascorbate, potassium L-ascorbate, calcium L-ascorbate, or magnesium L-ascorbate, or a pharmaceutically acceptable solvate or hydrate thereof; or a mixture thereof.

### Claim 13 (depends on 11)

The method of claim 11, wherein the ascorbic acid is magnesium L-ascorbate, or a pharmaceutically acceptable solvate or hydrate thereof.

### Claim 14 (depends on 1)

The method of claim 1, wherein vitamin K3 is 1,2,3,4-tetrahydro-2-methyl-1,4-dioxo-2-naphthalenesulfonic acid or a pharmaceutically acceptable salt thereof; or a pharmaceutically acceptable solvate or hydrate thereof.

### Claim 15 (depends on 1)

The method of claim 1, wherein vitamin K3 is 2-methyl-1,4-naphthalenedione; or a pharmaceutically acceptable solvate or hydrate thereof.

### Claim 16 (depends on 1)

The method of claim 1, wherein the molar ratio of the ascorbic acid to the quinone compound is ranging from about 50 to about 500.

### Claim 17 (depends on 1)

The method of claim 1, wherein the molar ratio of the ascorbic acid to the quinone compound is about 100, about 200, or about 400.

### Claim 18 (depends on 1)

The method of claim 1, wherein the ascorbic acid is administered once, twice, three times, four times, five times, or six times a day.

### Claim 19 (depends on 1)

The method of claim 1, wherein the quinone compound is administered once, twice, three times, four times, five times, or six times a day.

### Claim 20 (depends on 1)

The method of claim 1, wherein the ascorbic acid is administered in an amount ranging from about 500 mg to about 30,000 mg per day, and the quinone compound is administered in an amount ranging from about 3 mg to about 1,200 mg per day.

### Claim 21 (depends on 1)

The method of claim 1, wherein the ascorbic acid and the quinone compound are administered as one or more capsules, each comprising about 500 mg of sodium L-ascorbate and about 3 mg of sodium 1,2,3,4-tetrahydro-2-methyl-1, 4-dioxo-2-naphthalenesulfonate.

### Claim 22 (depends on 1)

The method of claim 1, wherein the ascorbic acid and the quinone compound are administered as one or more capsules, each comprising about 1,000 mg of calcium L-ascorbate and about 10 mg of 2-methyl-1,4-naphthal enedione.

### Claim 23 (depends on 1)

The method of claim 1, further comprising administering an additional therapeutic agent.

### Claim 24 (depends on 23)

The method of claim 23, wherein the additional therapeutic agent is an anti-parasite agent.

### Claim 25 (depends on 24)

The method of claim 24, wherein the additional therapeutic agent is benznidazole or nifurtimox.

### Claim 26 (depends on 1)

The method of claim 1, wherein the Chagas disease is chronic Chagas disease.