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US 2015/0307550 A1Published application
Improved peptide pharmaceuticals
AssigneeEumederis Pharmaceuticals, Inc.
InventorJohn J. NESTOR
Life of this patent
Estimating the term…
Abstract
Described herein are methods of syntheses and therapeutic uses of covalently modified peptides and/or proteins. The covalently modified peptides and/or proteins allow for improved pharmaceutical properties of peptide and protein-based therapeutics.
Claims47
A peptide product comprising a surfactant X, covalently attached to a peptide, the peptide comprising a linker amino acid U and at least one other amino acid:
- wherein X is
- wherein
- A is a hydrophobic group;
- and
- B is a hydrophilic group covalently attached to the peptide via a linker amino acid U.
2 more elements
A peptide product having a structure of Formula II:
- aa1-aa2-aa3-aa4-aa5-Z Formula II
- wherein:
- each of aa1, aa2, aa3, aa4, and aa5 is independently absent, a D- or L-natural or unnatural amino acid, an N-alkylated amino acid, an N-acetylated amino acid, a CαR3 amino acid, a Ψ-amino acid, or a linker amino acid U covalently attached to a surfactant X;
- Z is —OH, —NH2 or —NHR3;
- each R3 is independently substituted or unsubstituted C1-C12 branched or straight chain alkyl, a PEG chain of less than 10 Da, or substituted or unsubstituted aralkyl chain;
- and
- X is
- wherein
- A is a hydrophobic group;
- and
- B is a hydrophilic group covalently attached to the peptide via a linker amino acid U;
- provided that one, or at least one of aa1, aa2, aa3, aa4, and aa5 is the linker amino acid U covalently attached to the surfactant X;
- and further provided that not all of aa1, aa2, aa3, aa4, and aa5 are absent.
10 more elements
A compound selected from compounds of Table 1 in FIG. 1.
Dependencies are inferred from the claim text.