# US 12,758,642 B2 · Peptide exhibiting botulinum toxin-like activity, and use thereof

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- Number: US 12,758,642 B2
- Document ID: US12758642B2
- Status: Granted
- Kind: B2
- Application number: 18/009,388
- Filed: 2021-06-11
- Published: 2024-08-29
- Granted: 2026-10-13
- Earliest claimed: 2020-06-12
- Assignees: Caregen Co., Ltd.
- Applicants: Caregen Co, Ltd.
- Inventors: Yong Ji Chung; Eun Mi Kim; Eung Ji Lee; Young Min Lee; Han A Kang
- Web page: https://patentgrep.com/patent/US12758642B2

## CPC

- A61K 47/551: {one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid}
- A61K 8/498: {having 6-membered rings or their condensed derivatives, e.g. coumarin}
- A61K 8/64: Proteins; Peptides; Derivatives or degradation products thereof
- A61K 31/353: 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
- A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- A61P 21/02: Muscle relaxants, e.g. for tetanus or cramps
- A61Q 19/08: Anti-ageing preparations
- C07K 7/06: having 5 to 11 amino acids
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- A61K 2800/57: Compounds covalently linked to a(n inert) carrier molecule, e.g. conjugates, pro-fragrances
- 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
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)

## Abstract

The present invention relates to a trolox-peptide conjugate which exhibits activity that relieves muscle contraction and increases the extracellular matrix, and which can be used as an active ingredient of a drug, a quasi-drug or a cosmetic product for muscle relaxation, neuromuscular disorder prevention or treatment, or the improvement of skin conditions including skin wrinkles.

## Claims

### Claim 1

A trolox-peptide conjugate in which a peptide having an amino acid sequence of SEQ ID NO: 1 and trolox are conjugated, wherein a carboxyl group of the trolox is peptide-bound with an N-terminus of the peptide.

### Claim 2 (depends on 1)

A method for muscle relaxation in a subject in need thereof comprising administering an effective amount of the trolox-peptide conjugate according to claim 1 to the subject.

### Claim 3 (depends on 2)

The method for muscle relaxation of claim 2, wherein the trolox-peptide conjugate relieves muscle contraction by inhibiting a release of a neurotransmitter.

### Claim 4 (depends on 1)

A method for treating a neuromuscular disorder in a subject in need thereof comprising administering an effective amount of the trolox-peptide conjugate according to claim 1 to the subject.

### Claim 5 (depends on 4)

The method for treating neuromuscular disorder of claim 4, wherein the neuromuscular disorder is selected from the group consisting of myoclonus, hemifacial spasm, spasmodic torticollis, anal fissure, blepharospasm, facial spasm, cerebral palsy, strabismus, temporomandibular disorder, neuralgia, myalgia, overactive bladder, urge urinary incontinence, dystonia, and hyperhidrosis.

### Claim 6 (depends on 1)

A method for improving a skin condition in a subject in need thereof comprising administering an effective amount of the trolox-peptide conjugate according to claim 1 to the subject,
wherein the skin condition improved by the trolox-peptide conjugate is selected from the group consisting of reduction of an appearance of fine lines, reduction of an appearance of wrinkles, widening of the eyes, lifting a corner of the mouth of the subject, reduction of muscle mass, reduction of facial asymmetry, and flattening of a line extending from the upper lip of the subject, and
wherein the trolox-peptide conjugate improves wrinkles by i) increasing an expression of ColIα1 (collagen type I alpha 1), ii) increasing an expression of a fibronectin gene, or iii) increasing an expression of an elastin gene.

### Claim 7 (depends on 6)

The method for improving a skin condition of claim 6, wherein the trolox-peptide conjugate relieves contraction of facial muscles by inhibiting a release of a neurotransmitter.