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US 7,314,865 B2Granted
Compositions and methods for promoting lipid mobilization in humans
AssigneeBLM Group
InventorsBernice Schacter, Lee P. Schacter
Life of this patent
Estimating the term…
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.
Claims19
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.
10 more elements
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.
10 more elements
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.
13 more elements
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.
12 more elements
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.
12 more elements
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.
12 more elements
Dependencies are inferred from the claim text.