Modulators of G-Protein Coupled Receptors
US-2024383960-A1 · Nov 21, 2024 · US
US10947290B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10947290-B2 |
| Application number | US-201816209128-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 4, 2018 |
| Priority date | Apr 28, 2014 |
| Publication date | Mar 16, 2021 |
| Grant date | Mar 16, 2021 |
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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 method of stabilizing a bioactive peptide against protease hydrolysis, the method comprising replacing the amide bond formed between the first and second amino acid residues from the N-terminus of the bioactive peptide with a thioamide bond, wherein the protease comprises at least one selected from the group consisting of DPP-4 and carboxypeptidase. 2. The method of claim 1 , wherein the bioactive peptide comprises at least one selected from the group consisting of GIP, OCM, GLP-1, NPY, GHRH, ENT, and BNP. 3. The method of claim 1 , wherein the thioamide-modified peptide has equivalent biological activity or longer in vivo half-life to the bioactive peptide.
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
Glucagons · 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
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