Modulators of G-Protein Coupled Receptors
US-2024383960-A1 · Nov 21, 2024 · US
US10189884B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10189884-B2 |
| Application number | US-201515305681-A |
| Country | US |
| Kind code | B2 |
| Filing date | Apr 28, 2015 |
| Priority date | Apr 28, 2014 |
| Publication date | Jan 29, 2019 |
| Grant date | Jan 29, 2019 |
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The invention includes a thioamide-modified peptide, wherein the thioamide modification increases the in vivo half-life of the peptide. The invention further includes methods of treating or preventing a disease or disorder in a subject in need thereof, the method comprising administering to the subject a thioamide-modified peptide of the invention.
Opening claim text (preview).
What is claimed is: 1. A peptide comprising the thioamide-modified amino acid sequence of SEQ ID NO:2, or a salt or solvate thereof, wherein residue 1 of SEQ ID NO:2 is the N-terminus residue of the peptide. 2. A pharmaceutical composition comprising at least one peptide of claim 1 and a pharmaceutically acceptable carrier. 3. The composition of claim 2 , further comprising at least one additional agent useful for treating or preventing a disease or disorder in a subject. 4. The composition of claim 3 , wherein the disease or disorder comprises at least one selected from the group consisting of diabetes and obesity. 5. The peptide of claim 1 , wherein the C-terminus of the peptide is amidated. 6. The peptide of claim 1 , wherein the C-terminus of the peptide is esterified. 7. The peptide of claim 1 , wherein at least one NH group in the peptide backbone is methylated. 8. The peptide of claim 1 , wherein the N-terminus amino group is methylated or acetylated.
Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) · CPC title
by reversible modification of the secondary, tertiary or quarternary structure, e.g. using denaturating or stabilising agents · CPC title
Glucagons · CPC title
Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00) · CPC title
Glucagons · CPC title
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