# US 11,433,080 B2 · Antiviral treatment

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- Number: US 11,433,080 B2
- Document ID: US11433080B2
- Status: Granted
- Kind: B2
- Application number: 17/562,973
- Filed: 2021-12-27
- Published: 2022-05-12
- Granted: 2022-09-06
- Earliest claimed: 2020-05-29
- Assignees: Cebina GmbH
- Applicants: CEBINA GmbH
- Inventors: Eszter Nagy; Gabor Nagy; Valeria Szijarto; Robert Konrat
- Web page: https://patentgrep.com/patent/US11433080B2

## CPC

- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K 9/0043: {Nose}
- A61K 9/0073: {Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy; (nasal sprays A61K9/0043; inhalation of vapours of volatile or heated drugs, e.g. essential oils or nicotine, A61K9/007; devices A61M)}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 31/14: for RNA viruses
- 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

A method of treating a subject in need of anti-coronavirus treatment by providing a prophylactic or therapeutic treatment which includes an antiviral effective amount of an Azelastine compound, where the antiviral effective amount is 0.1-500 μg per dose. An Azelastine compound can also be used as an antiviral substance in a medicinal product for treating a biological surface to prevent coronavirus infection and/or coronavirus spread, or as a viral disinfectant.

## Claims

### Claim 1

A method of treating a subject in need of anti-coronavirus treatment, comprising providing a prophylactic or therapeutic treatment which comprises an antiviral effective amount of an Azelastine compound, wherein the antiviral effective amount is 0.1-500 μg per dose, and wherein the Azelastine compound is not combined with a steroidal anti-inflammatory agent.

### Claim 2 (depends on 1)

The method of claim 1, wherein said anti-coronavirus treatment is against one or more β-coronaviruses or SARS coronaviruses selected from the group consisting of SARS-CoV-2, MERS-CoV, SARS-CoV-1, HCoV-OC43, and HCoV-HKU1, and/or against one or more α-coronaviruses selected from the group consisting of HCoV-NL63, HCoV-229E and PEDV, and/or against one or more naturally-occurring variants or mutants of any of the foregoing.

### Claim 3 (depends on 2)

The method of claim 2, wherein said one or more viruses are naturally-occurring SARS-CoV-2 variants or mutants.

### Claim 4 (depends on 3)

The method of claim 3, wherein said SARS-CoV-2 variants or mutants comprise one or more mutations of the SARS-CoV-2 S-protein selected from the group consisting of K417N, L452R, N501Y, D614G, P681H, P681R, E484K, E484Q, and a 69/70 deletion in SEQ ID NO:4.

### Claim 5 (depends on 3)

The method of claim 3, wherein said SARS-CoV-2 variants or mutants are selected from the group consisting of B.1.1.7 (UK), B.1.351 (South Africa), P.1 (Brazil), B.1.617 (India), and B.1.618 (Bengal).

### Claim 6 (depends on 1)

The method of claim 1, wherein the subject has a disease or condition which is caused by or associated with an infection by β-coronaviruses or SARS viruses selected from the group consisting of any one or more of SARS-CoV-2, MERS-CoV, SARS-CoV-1, HCoV-OC43, and HCoV-HKU1, and/or by α-coronaviruses selected from the group consisting of any one or more of HCoV-NL63, HCoV-229E, and PEDV, and/or by any one or more naturally-occurring variants or mutants of any of the foregoing.

### Claim 7 (depends on 6)

The method of claim 6, wherein the subject has a disease or condition which is caused by or associated with an infection by one or more naturally-occurring SARS-CoV-2 variants or mutants.

### Claim 8 (depends on 7)

The method of claim 7, wherein said SARS-CoV-2 variants or mutants comprise one or more mutations of the SARS-CoV-2 S-protein one selected from the group consisting of K417N, L452R, N501Y, D614G, P681H, P681R, E484K, E484Q, and a 69/70 deletion in SEQ ID NO:4.

### Claim 9 (depends on 7)

The method of claim 7, wherein said SARS-CoV-2 variants or mutants are selected form the group consisting of B.1.1.7 (UK), B.1.351 (South Africa), P.1 (Brazil), B.1.617 (India), and B.1.618 (Bengal).

### Claim 10 (depends on 1)

The method of claim 1, wherein the antiviral effective amount is effective in preventing infection of susceptible cells by a coronavirus.

### Claim 11 (depends on 1)

The method of claim 1, wherein the Azelastine compound is applied into the subject's nose, and wherein the number of doses is 1 to 10 per day.

### Claim 12 (depends on 1)

The method of claim 1, wherein said Azelastine compound is comprised in a pharmaceutical preparation comprising said Azelastine compound and a pharmaceutically acceptable carrier.

### Claim 13 (depends on 12)

The method of claim 12, wherein said pharmaceutical preparation is formulated for local administration or systemic administration.

### Claim 14 (depends on 13)

The method of claim 13, wherein said local administration comprises application to the upper and lower respiratory tract, nasal administration, pulmonary administration, intraoral administration, ocular administration, or topical dermal application.

### Claim 15 (depends on 13)

The method of claim 13, wherein said systemic administration comprises intravenous administration, intramuscular administration, subcutaneous administration, intradermal administration, transdermal administration, or oral administration.

### Claim 16 (depends on 12)

The method of claim 12, wherein said pharmaceutical preparation is administered to the subject as a spray, a powder, a gel, an ointment, a cream, a foam, a liquid solution, a lotion, a gargle solution, an aerosolized powder, an aerosolized liquid formulation, granules, capsules, drops, tablet, syrup, lozenge, or a preparation for infusion or injection.

### Claim 17 (depends on 1)

The method of claim 1, wherein the Azelastine compound is the sole antiviral substance provided to the subject.

### Claim 18 (depends on 1)

The method of claim 1, wherein the Azelastine compound is the sole active substance provided to the subject.

### Claim 19 (depends on 1)

The method of claim 1, wherein treatment with the Azelastine compound is combined with a further treatment with one or more active substances.

### Claim 20 (depends on 19)

The method of claim 19, wherein said one or more active substances are selected from the group consisting of antiviral substances and antibiotic substances.

### Claim 21 (depends on 1)

The method of claim 1, wherein the subject has been infected with a coronavirus or is at risk of being infected with a coronavirus.

### Claim 22 (depends on 1)

The method of claim 1, wherein the subject has or is at risk of contracting a disease condition selected from the group consisting of a common cold, infection of the nose, sinusitis, infection of the throat and larynx, bronchiolitis, diarrhea, a skin rash, pneumonia, and/or acute respiratory distress syndrome (ARDS).

### Claim 23 (depends on 1)

The method of claim 1, wherein the subject is a human being, a dog, a cat, a horse, a camelid, a head of cattle or a pig.