# US 11,439,693 B2 · Vasoconstrictive and antibacterial combination treatment for rosacea

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- Number: US 11,439,693 B2
- Document ID: US11439693B2
- Status: Granted
- Kind: B2
- Application number: 16/339,812
- Filed: 2017-10-05
- Published: 2019-10-10
- Granted: 2022-09-13
- Earliest claimed: 2016-10-07
- Assignees: Migreos Human Health B.V.
- Applicants: Micreos Human Health B.V.
- Inventors: Mark Leonard Offerhaus; Bjorn Lars Herpers
- Web page: https://patentgrep.com/patent/US11439693B2

## CPC

- A61K 38/47: acting on glycosyl compounds (3.2), e.g. cellulases, lactases
- A61K 31/4164: 1,3-Diazoles
- A61K 31/4174: Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
- A61K 31/498: Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
- A61K 38/4886: {Metalloendopeptidases (3.4.24), e.g. collagenase}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/14: Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
- A61P 17/00: Drugs for dermatological disorders
- A61P 31/04: Antibacterial agents
- C12Y 302/01017: Lysozyme (3.2.1.17)
- C12Y 304/24075: Lysostaphin (3.4.24.75)
- 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
- C12Y: ENZYMES

## Abstract

The invention relates to the field of medicine, specifically to the field of treatment of rosacea. The invention relates to a novel composition and a novel kit of parts, both comprising a vasoconstrictive compound and a compound specifically targeting a bacterial cell, preferably a gram positive bacterial cell. The invention further relates to said composition and/or kit of parts for medical use, preferably for treating an individual suffering from rosacea.

## Claims

### Claim 1

A method for treating rosacea in a patient in need thereof comprising the sequential or simultaneous administration of a first compound and a second compound to the patient,
wherein said first compound is a vasoconstrictive compound selected from the group consisting of alpha(1)- and alpha(2)-adrenergic agonists and said second compound is a compound specifically targeting a Staphylococcus cell, and comprises one or more enzymatic active domains exhibiting peptidoglycan hydrolase activity.

### Claim 2 (depends on 1)

The method according to claim 1, wherein said second compound further comprises at least one cell wall binding domain which specifically binds to the peptidoglycan cell wall of said Staphylococcus cell.

### Claim 3 (depends on 2)

The method according to claim 2, wherein said cell wall binding domain originates from or is a homologue of a Staphylococcus phage endolysin, an S. simulans lysostaphin and/or an S. capitis ALE-1 bacteriocin.

### Claim 4 (depends on 2)

The method according to claim 2, wherein said second compound comprises a cell wall binding domain that has at least 80% identity to SEQ ID NO: 6.

### Claim 5 (depends on 1)

The method according to claim 1, wherein said one or more enzymatic active domains is selected from the group consisting of a cysteine, histidine dependent amidohydrolase/peptidase domain, an endopeptidase domain, an amidase domain and a glycosylhydrolase domain, and combinations thereof.

### Claim 6 (depends on 1)

The method according to claim 1, wherein said second compound is a naturally occurring endolysin.

### Claim 7 (depends on 1)

The method according to claim 1, wherein said second compound is a recombinant polypeptide comprising the one or more enzymatic active domains exhibiting peptidoglycan hydrolase activity.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the alpha(1)- and alpha(2)-adrenergic agonist is selected from the group consisting of Brimonidine, Tetrahydrozoline and Oxymetazoline.