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US 11,141,455 B2Granted
Peptide analogues with branched amino acid probe(s)
AssigneeTXP Pharma GmbH
InventorThomas Boesen
Life of this patent
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Abstract
The present invention relates to peptide analogues comprising one or more branched amino acid probes and a peptide, native or variants thereof.
Claims18
A peptide analogue comprising a peptide and one or more branched amino acid probes,
- wherein said peptide is selected from the group consisting of glucagon-like peptide-1 (GLP-1), GLP-1 (7-37), GLP-1 (7-33) and exendin-4,
- wherein said one or more branched amino acid probes comprises a first amino-alkyl amino acid residue,
- said first amino-alkyl amino acid residue optionally being covalently linked to a second amino-alkyl amino acid residue, or to a second and a third amino-alkyl amino acid residue, to form a linear chain of 2 or 3 amino-alkyl amino acid residues,
- wherein the side chain of one or more of said first, second and/or third amino-alkyl amino acid residues are each modified by attaching to the side chain amino group a molecule independently selected from the group consisting of AAAq-AAA (SEQ ID NO:
- 168);
- (aa3)p-AAAq (SEQ ID NOs:
- 169-174);
- AAAq-(aa3)p (SEQ ID NOs:
- 175-180);
- [(aa3)-AAA]p (SEQ ID NOs:
- 181 and 182);
- and [AAA-(aa3)]p (SEQ ID NOs:
- 183 and 184);
- wherein q is a number selected from 0, 1, 2 and 3;
- p is a number selected from 1, 2 and 3;
- AAA is an amino-alkyl amino acid residue;
- and (aa3) is an amino acid residue independently selected from Arg, His, Gly and Ala,
- wherein said amino-alkyl amino acid residues are optionally acetylated,
- wherein said first amino-alkyl amino acid residue is covalently linked to the N-terminus of said peptide, covalently linked to the C-terminus of said peptide, or attached to the side chain amino group of an amino-alkyl amino acid residue within said peptide,
- with the proviso that said one or more branched amino acid probes consists of 2 to 9 amino acid residues.
17 more elements
Dependencies are inferred from the claim text.