# US 7,314,865 B2 · Compositions and methods for promoting lipid mobilization in humans

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- Number: US 7,314,865 B2
- Document ID: US7314865B2
- Status: Granted
- Kind: B2
- Application number: 10/869,768
- Filed: 2004-06-16
- Published: 2004-11-11
- Granted: 2008-01-01
- Earliest claimed: 2002-02-07
- Assignees: BLM Group
- Inventors: Bernice Schacter; Lee P. Schacter
- Web page: https://patentgrep.com/patent/US7314865B2

## CPC

- G01N 33/5038: {involving detection of metabolites per se}
- A61K 38/1767: {from invertebrates}
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 7/06: having 5 to 11 amino acids
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- G01N 33/5008: {for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics}
- G01N 33/5044: {involving specific cell types}
- G01N 33/5061: {Muscle cells}
- G01N 33/5067: {Liver cells}
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)
- 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

The invention provides methods of using polypeptide compounds based on the structures of insect peptides of the adipokinetic hormone family to mobilize lipids in humans. The compositions and methods described in the application are useful for modulating human body weight, such as inducing weight loss. The invention also includes screening methods for identifying other compounds effective for modulating lipid mobilization in humans.

## Claims

### Claim 1

A pharmaceutical composition comprising a peptide having the formula
Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-X-Z,
or a pharmaceutically acceptable salt thereof, wherein:
Xaa1 is a glutamine residue;
Xaa2 is one of a leucine residue, an isoleucine residue, a valine residue, a phenylalanine residue, and a tyrosine residue;
Xaa3 is one of an asparagine residue and a threonine residue;
Xaa4 is one of a phenylalanine residue and a tyrosine residue;
Xaa5 is one of a threonine residue and a serine residue;
Xaa6 is one of a proline residue, a serine residue, a threonine residue, and an alanine residue;
Xaa7 is one of a glycine residue, an asparagine residue, a serine residue, an aspartate residue, a valine residue, and a tryptophan residue;
Xaa8 is a tryptophan residue;
X is from 0 to 10 amino acid residues; and
Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety.

### Claim 2 (depends on 1)

The composition of claim 1, wherein:
Xaa2 is one of a leucine residue and a valine residue;
Xaa6 is one of a proline residue, a serine residue, and a threonine residue;
Xaa7 is one of a glycine residue, an asparagine residue, and a serine residue;
Xaa8 is a tryptophan residue;
X is from 0 to 3 amino acid residues; and
Z is an (—NH2) radical.

### Claim 3 (depends on 2)

The composition of claim 2, wherein Xaa4 is a phenylalanine residue.

### Claim 4 (depends on 1)

The composition of claim 1, wherein:
X is 0 amino acid residues; and
Z is an (—NH2) radical.

### Claim 5 (depends on 1)

The composition of claim 1, wherein X is a glycine residue.

### Claim 6 (depends on 5)

The composition of claim 5, wherein Z is one of a hydrogen radical and an (—NH2) radical.

### Claim 7 (depends on 1)

The composition of claim 1, wherein X has the chemical structure
Xaa9-Xaa10
wherein:
Xaa9 is a glycine residue; and
Xaa10 is one of a threonine residue, a glycine residue, a tryptophan residue, a serine residue, and an asparagine residue.

### Claim 8 (depends on 7)

The composition of claim 7, wherein Xaa10 is a threonine residue.

### Claim 9 (depends on 7)

The composition of claim 7, wherein Z is an (—NH2) radical.

### Claim 10 (depends on 1)

The composition of claim 1, wherein X has the chemical structure
Xaa9-Xaa10-Xaa11
wherein:
Xaa9 is glycine;
Xaa10 is one of a threonine residue, a glycine residue, a tryptophan residue, a serine residue, and an asparagine residue; and
Xaa11 is a lysine residue.

### Claim 11 (depends on 1)

The composition of claim 1, wherein X has the chemical structure
Xaa9-Xaa10-Xaa11-(Xaa12)n
wherein
n is from 0 to 7
Xaa9 is a glycine residue,
Xaa10, when present, is one of a threonine residue, a glycine residue, a tryptophan residue, a serine residue, and an asparagine residue;
Xaa11, when present, is a lysine residue; and
each Xaa12, when present, is any amino acid residue.

### Claim 12

A pharmaceutical composition comprising a peptide having the formula
Xaa1-Xaa22-Xaa23-Xaa24-Xaa25-Xaa26Xaa27-Xaa28-X-Z,
or a pharmaceutically acceptable salt thereof, wherein:
Xaa1 is a glutamine residue;
Xaa22 is an amino acid residue having a non-polar side chain;
Xaa23 is an amino acid residue having a non-ionic polar side chain;
Xaa24 is an amino acid residue having an aromatic side chain;
Xaa25 is an amino acid residue having a non-ionic polar side chain;
Xaa26 is any amino acid residue;
Xaa27 is any amino acid residue;
Xaa28 is an amino acid residue having an aromatic side chain;
X is from 0 to 10 amino acid residues; and
Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety.

### Claim 13 (depends on 12)

The composition of claim 12, wherein:
Xaa26 is one of a proline residue, a serine residue, a threonine residue, and an alanine residue.

### Claim 14 (depends on 12)

The composition of claim 12, wherein:
Xaa27 is one of a glycine residue, an asparagine residue, a serine residue, a glutamate residue, a valine residue, and a tryptophan residue.

### Claim 15 (depends on 1)

The composition of claim 1 wherein X is glycine and Z is a hydrogen radical.

### Claim 16

A pharmaceutical composition comprising a peptide of the formula:
Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-X-Z,
or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier; wherein:
Xaa1 is a pyroglutamate residue, a glutamate residue or glutamine residue;
Xaa2 is one of a leucine residue, an isoleucine residue, a valine residue, a phenylalanine residue, and a tyrosine residue;
Xaa3 is one of an asparagine residue and a threonine residue;
Xaa4 is one of a phenylalanine residue and a tyrosine residue;
Xaa5 is one of a threonine residue and a serine residue;
Xaa6 is one of a proline residue, a serine residue, a threonine residue, and an alanine residue;
Xaa7 is one of glycine residue, an asparagine residue, a serine residue, an aspartate residue, a valine residue, and a tryptophan residue;
Xaa8 is a tryptophan residue;
X is from 0 to 10 amino acid residues; and
Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety, which composition is either
in a form selected from the group consisting of a tablet, a hard or soft capsule, a cachet, a troche, a lozenge, an oily suspension, an emulsion, a suppository, a cream, a paste, a composition in which the said peptide is in microcrystalline form, a dry powder including a solid fine powder diluent, and a liposomal preparation;
or is added to a food or foodstuff.

### Claim 17

A pharmaceutical composition comprising a peptide of the formula:
Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-X-Z,
or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier; wherein:
Xaa1 is a pyroglutamate residue, a glutamate residue or glutamine residue;
Xaa2 is one of a leucine residue, an isoleucine residue, a valine residue, a phenylalanine residue, and a tyrosine residue;
Xaa3 is one of an asparagine residue and a threonine residue;
Xaa4 is one of a phenylalanine residue and a tyrosine residue;
Xaa5 is one of a threonine residue and a serine residue;
Xaa6 is one of a proline residue, a serine residue, a threonine residue, and an alanine residue;
Xaa7 is one of glycine residue, an asparagine residue, a serine residue, an aspartate residue, a valine residue, and a tryptophan residue;
Xaa8 is a tryptophan residue;
X is from 0 to 10 amino acid residues; and
Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety,
which composition is in the form of a powdered or granular formulation comprising one or more of a dispersing or wetting agent, a suspending agent, and a preservative.

### Claim 18

A pharmaceutical composition comprising a peptide of the formula:
Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-X-Z,
or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier; wherein:
Xaa1 is a pyroglutamate residue, a glutamate residue or glutamine residue;
Xaa2 is one of a leucine residue, an isoleucine residue, a valine residue, a phenylalanine residue, and a tyrosine residue;
Xaa3 is one of an asparagine residue and a threonine residue;
Xaa4 is one of a phenylalanine residue and a tyrosine residue;
Xaa5 is one of a threonine residue and a serine residue;
Xaa6 is one of a proline residue, a serine residue, a threonine residue, and an alanine residue;
Xaa7 is one of glycine residue, an asparagine residue, a seine residue, an aspartate residue, a valine residue, and a tryptophan residue;
Xaa8 is a tryptophan residue;
X is from 0 to 10 amino acid residues; and
Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety,
which composition is in the form of a sterile solution for parenteral administration comprising a non toxic parenterally acceptable diluent or solvent and one or more of a dispersing agent, a wetting agent and a suspending agent.

### Claim 19

A pharmaceutical composition comprising a peptide of the formula:
Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-X-Z,
or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier; wherein:
Xaa1 is a pyroglutamate residue, a glutamate residue or glutamine residue;
Xaa2 is one of a leucine residue, an isoleucine residue, a valine residue, a phenylalanine residue, and a tyrosine residue;
Xaa3 is one of an asparagine residue and a threonine residue;
Xaa4 is one of a phenylalanine residue and a tyrosine residue;
Xaa5 is one of a threonine residue and a seine residue;
Xaa6 is one of a proline residue, a seine residue, a threonine residue, and an alanine residue;
Xaa7 is one of glycine residue, an asparagine residue, a serine residue, an aspartate residue, a valine residue, and a tryptophan residue;
Xaa8 is a tryptophan residue;
X is from 0 to 10 amino acid residues; and
Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety,
which composition is in the form of a sterile solution for parenteral administration comprising a preservative.