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US 2010/0075907 A1Published application
Neuromedin u receptor agonists and uses thereof
OwnerDonald J. Marsh, Antonello Pessi +4inventors
InventorsDonald J. Marsh, Antonello Pessi, Maria A. Bednarek, Elisabetta Bianchi, Paolo Ingallinella, Andrea M. Peier
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Abstract
Neuromedin U receptor agonists for use in the treatment of metabolic disorders such as obesity and diabetes are disclosed.
Claims25
A neuromedin U receptor agonist, which has the formula
- Z1-peptide-Z2
- wherein the peptide has the amino acid sequence X1-X2-X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16-X17-X18-Phe-Leu-Phe-Arg-Pro-Arg-Asn (SEQ ID NO:1), wherein amino acids 1 to 17 can be any amino acid or absent amino acid X18 is absent, Tyr, Trp, Phe, a des-amino acid or an acyl group,
- and the peptide further includes a cysteine residue at the N-terminus of the peptide in which the thiol group of the cysteine residue is covalently joined to one or more molecules selected from the group consisting of PEG, cholesterol, N-ethylmaleimidyl, and palmitoyl;
- Z1 is an optionally present protecting group that, if present, is joined to the N-terminal amino group;
- Z2 is NH2 or an optionally present protecting group that, if present, is joined to the C-terminal carboxy group;
- and pharmaceutically acceptable salts thereof.
3 more elements
3-4. (canceled)
(canceled)
16-18. (canceled)
A method for treating a metabolic disorder in an individual administering to the individual a therapeutically effective amount of a neuromedin U receptor agonist that has the formula
- Z1-peptide-Z2
- wherein the peptide has the amino acid sequence X1-X2-X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16-X17-X18-X19-X20-X21-X22-X23-X24-X25 (SEQ ID NO:27) X1-X2-X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16-X17-X18-Phe-Leu-Phe-Arg-Pro-Arg-Asn (SEQ ID NO:1), wherein amino acids 1 to 17 can be any amino acid or absent;
- wherein amino acid X18 is absent, Tyr, Trp, Phe, a des-amino acid or an acyl group,
- and the peptide further includes a cysteine residue at the N-terminus of the peptide in which the thiol group of the cysteine residue is covalently joined to one or more molecules selected from the group consisting of PEG, cholesterol, N-ethylmaleimidyl, and palmitoyl;
- Z1 is an optionally present protecting group that, if present, is joined to the N-terminal amino group;
- Z2 is NH2 or an optionally present protecting group that, if present, is joined to the C-terminal carboxy group and pharmaceutically acceptable salts thereof;
- to treat the disorder in the individual.
4 more elements
(canceled)
25-28. (canceled)
Dependencies are inferred from the claim text.