# US 2021/0330623 A1 · Active ingredient consisting of a mixture of polylysine compounds and use in the prevention of strokes and the treatment of the post-stroke inflammatory phase

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- Number: US 2021/0330623 A1
- Document ID: US20210330623A1
- Status: Published application
- Kind: A1
- Application number: 16/613,963
- Filed: 2018-05-14
- Published: 2021-10-28
- Earliest claimed: 2017-05-16
- Assignees: Polyneuros
- Applicants: Polyneuros
- Inventors: Michel GEFFARD; Arturo MANGAS MARTIN; Laëtitia VIDAL
- Web page: https://patentgrep.com/patent/US20210330623A1

## CPC

- A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00)
- A61K 38/063: {Glutathione}
- 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 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- A61K 9/0095: {Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006)}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 31/355: Tocopherols, e.g. vitamin E
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 47/645: {Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT}
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- 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 invention relates to an active ingredient consisting of several polylysine compounds, said polylysine compounds consisting of at least one small molecule conjugated to a polylysine, said active ingredient comprising at least the following polylysine compounds: Coenzyme Q10-Polylysine Retinoic Acid-Polylysine Cysteine-Polylysine Taurine-Polylysine Glutathione-Polylysine, for use in humans or animals, to prevent strokes and/or treat the inflammatory phase following a stroke.

## Claims

### Claim 1

An active ingredient consisting of several polylysine compounds, said polylysine compounds consisting of at least one small molecule conjugated to a polylysine, said active ingredient comprising at least the following polylysine compounds:
Coenzyme Q10-Polylysine,
Retinoic Acid-Polylysine,
Cysteine-Polylysine,
Taurine-Polylysine, and
Glutathione-Polylysine,
for use in humans or animals, to prevent strokes and/or treat the inflammatory phase following a stroke.

### Claim 2 (depends on 1)

An active ingredient for use according to claim 1, for reducing inflammation in the arteries to prevent strokes in patients at risk and/or treat the inflammatory phase following a stroke.

### Claim 3 (depends on 1)

An active ingredient for use according to claim 1, for reducing the destruction of viable neurons by the immune cells during treatment in the inflammatory and apoptotic phase following a stroke.

### Claim 4 (depends on 1)

An active ingredient for use according to claim 1, characterized in that it also comprises at least one of the following polylysine compounds:
α-Tocopherol-Polylysine
Ascorbic Acid-Polylysine
Methionine-Polylysine.

### Claim 5 (depends on 1)

An active ingredient for use according to claim 1, characterized in that it consists exclusively of the following polylysine compounds:
Coenzyme Q10-Polylysine
Retinoic Acid-Polylysine
Cysteine-Polylysine
Taurine-Polylysine
Glutathione-Polylysine
α-Tocopherol-Polylysine
Ascorbic Acid-Polylysine
Methionine-Polylysine.

### Claim 6 (depends on 1)

An active ingredient for use according to claim 1, characterized in that the polylysine is Poly-L-lysine.

### Claim 7 (depends on 1)

An active ingredient for use according to claim 1, characterized in that the concentrations of each of said small molecules are between 1×10−4 and 1×10−3 M.

### Claim 8 (depends on 1)

An active ingredient for use according to claim 1, characterized in that all the polylysine compounds have the same concentration of small molecules.

### Claim 9 (depends on 1)

A composition for use in humans or animals, to prevent strokes and/or treat the inflammatory phase following a stroke, comprising at least 7 mg by weight of an active ingredient according to claim 1.

### Claim 10 (depends on 9)

A composition for use according to claim 9, characterized in that it is in dry form.

### Claim 11 (depends on 10)

A composition for use according to claim 10, characterized in that it is in the form of a tablet to be swallowed, a sublingual tablet, a gastro-resistant capsule, a powder, a dermal patch, or a suppository.

### Claim 12 (depends on 10)

A composition for use according to claim 10, characterized in that the active ingredient is present at between 5 and 15 mg per 100 mg of composition.

### Claim 13 (depends on 9)

A composition for use according to claim 9, characterized in that it is in liquid form.

### Claim 14 (depends on 13)

A composition for use according to claim 13, characterized in that it is in the form of an oral or injectable solution.

### Claim 15 (depends on 13)

A composition for use according to claim 13, characterized in that the therapeutic active ingredient is present at a concentration of between 5 and 15 mg per ml of composition.