# US 10,118,955 B2 · C-terminal fragments of glucagon-like peptide-1 (GLP-1)

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 10,118,955 B2
- Document ID: US10118955B2
- Status: Granted
- Kind: B2
- Application number: 14/539,578
- Filed: 2014-11-12
- Published: 2015-05-14
- Granted: 2018-11-06
- Earliest claimed: 2008-11-07
- Assignees: The General Hospital Corporation
- Applicants: The General Hospital Corporation
- Inventors: Joel F. Habener; Tatsuya Yano; Eva Tomas Falco
- Web page: https://patentgrep.com/patent/US10118955B2

## CPC

- C07K 14/605: Glucagons
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 7/12: Antidiuretics, e.g. drugs for diabetes insipidus (ADH A61P5/10)
- C07K 14/005: from viruses
- C12N 7/00: Viruses; Bacteriophages; Compositions thereof; Preparation or purification thereof (preparing medicinal viral antigen or antibody compositions, e.g. virus vaccines, A61K39/00)
- 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)
- C07K 2319/10: containing a tag for extracellular membrane crossing, e.g. TAT or VP22
- C12N 2740/16033: Use of viral protein as therapeutic agent other than vaccine, e.g. apoptosis inducing or anti-inflammatory
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- 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)

## Abstract

C-Terminal Fragments of Glucagon-Like Peptide-1 (GLP 1), and methods of use thereof, e.g., for the treatment of obesity and obesity-related disorders, e.g., diabetes and the metabolic syndrome.

## Claims

### Claim 1

A method of treating metabolic syndrome in a subject, the method comprising administering to the subject a therapeutically effective amount of a peptide consisting of the amino acid sequence of (Phe/Tyr)-Ile-Ala-Trp-Leu-Val-(Lys/Arg)-Gly-Arg-Xaa (SEQ ID NO:1), wherein Xaa is Gly-Arg or Gly-Arg-Gly, wherein one or more amino acids of the peptide are alkylated, acylated, or biotinylated.

### Claim 2 (depends on 1)

The method of claim 1, wherein the peptide is amidated.

### Claim 3

A method of treating obesity in a subject, the method comprising administering to the subject a therapeutically effective amount of a peptide consisting of the amino acid sequence of (Phe/Tyr)-Ile-Ala-Trp-Leu-Val-(Lys/Arg)-Gly-Arg-Xaa (SEQ ID NO:1), wherein Xaa is Gly-Arg or Gly-Arg-Gly, wherein one or more amino acids of the peptide are alkylated, acylated, or biotinylated.

### Claim 4 (depends on 3)

The method of claim 3, wherein the peptide is amidated.

### Claim 5

A method of treating metabolic syndrome in a subject, the method comprising administering to the subject a therapeutically effective amount of a fusion peptide comprising a first portion consisting of the amino acid sequence of (Phe/Tyr)-Ile-Ala-Trp-Leu-Val-(Lys/Arg)-Gly-Arg-Xaa (SEQ ID NO:1), wherein Xaa is Gly-Arg or Gly-Arg-Gly, fused to a cell-penetrating peptide, wherein one or more amino acids of the fusion peptide are alkylated, acylated, or biotinylated.

### Claim 6 (depends on 5)

The method of claim 5, wherein the cell-penetrating peptide is fused to the C-terminus of the first portion.

### Claim 7 (depends on 5)

The method of claim 5, wherein the cell-penetrating peptide is selected from the group consisting of HIV-derived TAT peptides, penetratins, transportans, SS peptides, and hCT derived cell-penetrating peptides.

### Claim 8

A method of treating obesity in a subject, the method comprising administering to the subject a therapeutically effective amount of a fusion peptide comprising a first portion consisting of the amino acid sequence of (Phe/Tyr)-Ile-Ala-Trp-Leu-Val-(Lys/Arg)-Gly-Arg-Xaa (SEQ ID NO:1), wherein Xaa is Gly-Arg or Gly-Arg-Gly, fused to a cell-penetrating peptide, wherein one or more amino acids of the fusion peptide are alkylated, acylated, or biotinylated.

### Claim 9 (depends on 8)

The method of claim 8, wherein the cell-penetrating peptide is fused to the C-terminus of the first portion.

### Claim 10 (depends on 8)

The method of claim 8, wherein the cell-penetrating peptide is selected from the group consisting of HIV-derived TAT peptides, penetratins, transportans, SS peptides, and hCT derived cell-penetrating peptides.

### Claim 11 (depends on 1)

The method of claim 1, wherein Xaa is Gly-Arg.

### Claim 12 (depends on 3)

The method of claim 3, wherein Xaa is Gly-Arg.

### Claim 13 (depends on 5)

The method of claim 5, wherein Xaa is Gly-Arg.

### Claim 14 (depends on 8)

The method of claim 8, wherein Xaa is Gly-Arg.

### Claim 15 (depends on 1)

The method of claim 1, wherein Xaa is Gly-Arg-Gly.

### Claim 16 (depends on 3)

The method of claim 3, wherein Xaa is Gly-Arg-Gly.

### Claim 17 (depends on 5)

The method of claim 5, wherein Xaa is Gly-Arg-Gly.

### Claim 18 (depends on 8)

The method of claim 8, wherein Xaa is Gly-Arg-Gly.