# US 8,569,241 B2 · Composition for improving brain function and method for improving brain function

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- Number: US 8,569,241 B2
- Document ID: US8569241B2
- Status: Granted
- Kind: B2
- Application number: 13/532,394
- Filed: 2012-06-25
- Published: 2012-11-01
- Granted: 2013-10-29
- Earliest claimed: 2009-12-28
- Assignees: Calpis Co., Ltd.
- Applicants: Kazuhito Ohsawa; Naoto Uchida; Kohji Ohki; Hiroaki Goto
- Inventors: Kazuhito Ohsawa; Naoto Uchida; Kohji Ohki; Hiroaki Goto
- Web page: https://patentgrep.com/patent/US8569241B2

## CPC

- A61K 38/04: Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof ({enzyme inhibitors A61K38/005;} gastrins {A61K38/2207}, somatostatins A61K38/31, melanotropins A61K38/34 {; protease inhibitors A61K38/55})
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/24: Antidepressants
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- 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
- 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

Provided are a composition for improving the brain function, which can be orally taken at a low dose, and a method therefor. The composition for improving the brain function contains, as the active ingredient, X-Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu-Y (wherein X is nil or represents Ile or Asn-Ile; and Y is nil or represents Val-Met), X-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu-Y (wherein X is abscent or represents Thr-Gln-Thr-Pro, Pro-Leu-Thr-Gln-Thr-Pro, Leu-Thr-Gln-Thr-Pro or Pro; and Y is abscent or represents Val-Met), or a salt of the same. The method for improving the brain function comprises administering said peptide or a salt of the same.

## Claims

### Claim 1

A composition for improving brain function, comprising, as an active ingredient, a peptide consisting of the amino acid sequence of X-Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu-Y (SEQ ID NO: 20) or a salt thereof, wherein
i. X is Asn-Ile, Y is absent or represents Val-Met, or
ii. X is absent or represents Ile, and Y is absent.

### Claim 2 (depends on 1)

The composition for improving brain function according to claim 1, wherein said active ingredient is a peptide consisting of the amino acid sequence of Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:1) or a salt thereof.

### Claim 3 (depends on 1)

The composition for improving brain function according to claim 1, wherein said active ingredient is a peptide consisting of the amino acid sequence of Ile-Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:2) or a salt thereof.

### Claim 4 (depends on 1)

The composition for improving brain function according to claim 1, wherein said active ingredient is a peptide consisting of the amino acid sequence of Asn-Ile-Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:3) or a salt thereof.

### Claim 5 (depends on 1)

The composition for improving brain function according to claim 1, wherein said active ingredient is a peptide consisting of the amino acid sequence of Asn-Ile-Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu-Val-Met (SEQ ID NO:6) or a salt thereof.

### Claim 6

A composition for improving brain function, comprising, as an active ingredient, a peptide consisting of the amino acid sequence of X-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu-Y (SEQ ID NO: 21) or a salt thereof, wherein
X is absent or represents Leu-Thr-Gln-Thr-Pro (SEQ ID NO: 24) or Pro
Y is absent.

### Claim 7 (depends on 6)

The composition for improving brain function according to claim 6, wherein said active ingredient is a peptide consisting of the amino acid sequence of Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:9) or a salt thereof.

### Claim 8 (depends on 6)

The composition for improving brain function according to claim 6, wherein said active ingredient is a peptide consisting of the amino acid sequence of Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:10) or a salt thereof.

### Claim 9 (depends on 6)

The composition for improving brain function according to claim 6, wherein said active ingredient is a peptide consisting of the amino acid sequence of Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:11) or a salt thereof.

### Claim 10

An isolated polypeptide consisting of the amino acid sequence of X-Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu-Y (SEQ ID NO: 20) or a salt thereof, wherein i) X is Asn-Ile and Y is absent or represents Val-Met or ii) X is absent or represents Ile and Y is absent.

### Claim 11 (depends on 10)

The isolated polypeptide according to claim 10, wherein said polypeptide consists of the amino acid sequence of Asn-Ile-Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val- Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:3) or a salt thereof.

### Claim 12 (depends on 10)

The isolated polypeptide according to claim 10, wherein said polypeptide consists of the amino acid sequence of Asn-Ile-Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu-Val-Met (SEQ ID NO:6) or a salt thereof.

### Claim 13 (depends on 10)

The isolated polypeptide according to claim 10, wherein said polypeptide consists of the amino acid sequence of Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:1) or a salt thereof.

### Claim 14 (depends on 10)

The isolated polypeptide according to claim 10, wherein said polypeptide consists of the amino acid sequence of Ile-Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:2) or a salt thereof.

### Claim 15

An isolated polypeptide consisting of the amino acid sequence of X-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO: 25) or a salt thereof, wherein X is absent or represents Leu-Thr-Gln-Thr-Pro (SEQ ID NO: 24) or Pro.

### Claim 16 (depends on 15)

The isolated polypeptide according to claim 15, wherein said polypeptide consists of the amino acid sequence of Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:9) or a salt thereof.

### Claim 17 (depends on 15)

The isolated polypeptide according to claim 15, wherein said polypeptide consists of the amino acid sequence of Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:10) or a salt thereof.

### Claim 18 (depends on 15)

The isolated polypeptide according to claim 15, wherein said polypeptide consists of the amino acid sequence of Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu (SEQ ID NO:11) or a salt thereof.
