# US 8,772,449 B2 · Cell-penetrating peptides

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- Number: US 8,772,449 B2
- Document ID: US8772449B2
- Status: Granted
- Kind: B2
- Application number: 13/321,176
- Filed: 2010-05-19
- Published: 2012-03-15
- Granted: 2014-07-08
- Earliest claimed: 2009-05-20
- Assignees: Toray Industries, Inc.
- Applicants: Mariko Morishita; Kozo Takayama; Reiji Nishio; Nobuo Ida
- Inventors: Mariko Morishita; Kozo Takayama; Reiji Nishio; Nobuo Ida
- Web page: https://patentgrep.com/patent/US8772449B2

## CPC

- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/007: {Pulmonary tract; Aromatherapy}
- 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 38/10: Peptides having 12 to 20 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 14/43581: {from Drosophila}
- 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)
- 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

A cell-penetrating peptide of (A) to (D) below gives cell membrane permeability and transmucosal absorbability to a physiologically active substance: (A) a peptide having the amino acid sequence of SEQ ID NO:1; (B) a peptide represented by SEQ ID NO:1 except that one or several basic amino acids are changed; (C) a peptide represented by SEQ ID NO:1 except that 1 to 5 amino acids are changed; (D) a peptide having: the reverse sequence of any of (A) to (C); an amino acid sequence which is the same as the reverse sequence of (A) except that one or several basic amino acids are changed; or an amino acid sequence which is the same as the reverse sequence of (A) except that 1 to 5 amino acids are changed.

## Claims

### Claim 1

A cell-penetrating peptide, comprising:
(A) a peptide having the amino acid sequence of SEQ ID NO:1; or
(B) a peptide having an amino acid sequence of SEQ ID NO:1 except that up to 3 basic amino acids are substituted with any other basic amino acid, deleted from SEQ ID NO:1, inserted into SEQ ID NO:1 and/or added to SEQ ID NO:1, which peptide has cell membrane permeability.

### Claim 2 (depends on 1)

The cell-penetrating peptide according to claim 1, wherein said peptide (B) has the amino acid sequence of any of SEQ ID NOs: SEQ ID NO:2, SEQ ID NO:9, and SEQ ID NO:10.

### Claim 3 (depends on 1)

A pharmaceutical composition comprising the cell-penetrating peptide according to claim 1 and a hydrophilic physiologically active substance.

### Claim 4 (depends on 3)

The pharmaceutical composition according to claim 3, wherein said hydrophilic physiologically active substance is a peptide, protein or nucleic acid.

### Claim 5 (depends on 1)

A method of administering a pharmaceutical composition, which comprises:
combining the cell-penetrating peptide according to claim 1 and a hydrophilic physiologically active substance into a composition which is pharmaceutically acceptable for nasal or oral administration; and
administering the pharmaceutically acceptable composition by nasal or oral administration.