EPISYNCHRONS FOR PRECISION MEDICINE

Title:

EPISYNCHRONS FOR PRECISION MEDICINE

Document Type and Number:

WIPO Patent Application WO/2023/167813

Kind Code:

A4

Abstract:

This invention relates to the field of peptide diagnostics and therapeutics, and more particularly to novel structures and uses of a ligand-modified species of immodulin peptides herein termed "episynchrons" — end-modified immodulin peptides capable of driving the enhanced formation of RXR heterodimers in the nucleus of living mammalian cells — to modulate immunoregenerative processes, among other uses. The covalent addition of the exemplified nuclear receptor ligands to the carboxyterminus of a peptide prior to full chain elongation during peptide synthesis is novel and relevant to the cost of production of these agents at scale. Moreover, the facile and organelle-specific 'on-demand' reprogramming of transcriptional sets within target tissues is a technical breakthrough relevant to the future of precision medicine. Pre-designed tissue-specific epigenetic synchrony made possible by the unique structure of episynchrons in combination with the formulation of episynchrons in zip-coded microparticles or nanoparticles delivered in a location-specific manner, is a powerful and novel concept for twenty-first century medicine. The compositions and methods provided herein demonstrate new and surprising biological activities for episynchrons that are useful in treating a wide range of dysfunctions and perturbations in mammals in the context of organ- and stress-specific precision medicine.

Inventors:

MASCARENHAS DESMOND (US)

Application Number:

PCT/US2023/013908

Publication Date:

November 09, 2023

Filing Date:

February 26, 2023

Export Citation:

Click for automatic bibliography generation Help

Assignee:

MASCARENHAS DESMOND (US)

International Classes:

A61K47/64; A61K38/00; C12P21/02; A61P35/00; A61P37/02

Download PDF:

View/Download PDF PDF Help

Claims:

AMENDED CLAIMS received by the International Bureau on 18 September 2023 (18.09.2023)

What is claimed is:

1. A modified peptide formed by covalent amide bond linkage of the moieties “E” and “C-lig” wherein:

[a] “E” moiety is a synthetic peptide, 20-60 amino acids in length, comprising an amino acid sequence corresponding to SEQ ID NO:8 or SEQ ID NO:9 and having a lysine residue at its C-terminus;

[b] “C-lig” moiety is a nuclear receptor ligand independently capable of binding at least one nuclear receptor isoform with submillimolar affinity in vitro;

[c] “C-lig” moiety is selected from a group consisting of tamibarotene, HX600, GW7647, GW3965, palovarotene, GW4064, GW501516, AM580, sobetirome, AC-55649, GW9578 and LG100754; and

[d] said covalent amide bond linkage between “E” and “C-lig” between the carboxyl group of “C-lig” and the epsilon amino group of the C-terminal lysine of “E” moiety is formed prior to completion of the amino acid chain elongation steps during peptide synthesis.

2. The modified peptide according to Claim 1 comprising an amino acid sequence corresponding to SEQ ID NO:6.

3. The modified peptide according to Claim 1 comprising an amino acid sequence corresponding to SEQ ID NOT.

4. The modified peptide according to Claim 1 comprising tamibarotene.

5. The modified peptide according to Claim 1 comprising HX600.

6. The modified peptide according to Claim 1 comprising GW7647.

7. The modified peptide according to Claim 1 comprising GW3965.

8. A formulation comprising the modified peptide according to Claim 1 and acceptable pharmaceutical excipients.

9. The formulation of Claim 8 comprising human serum albumin covalently attached to a homing peptide via a covalent bond wherein said homing peptide comprises an amino acid sequence corresponding to any one of SEQ ID NOs: 10-16.

10. The formulation of Claim 8 comprising a natural antioxidant or antimicrobial compound selected from a group consisting of: resveratrol, quercetin, curcumin, ursolic acid, berberine, tannic acid, chitosan compound, menthol, anisic acid, verbenone, linalool, ferulic acid, glycyrrhizic acid and levulinic acid.

11. A method for administering the modified peptide of Claim 1 in the treatment of a subject suffering from bodily dysfunction.

12. Use of the modified peptide according to claim 1 in the treatment of a subject suffering from bodily dysfunction.

13. Use of the modified peptide according to claim 1 in the manufacture of a medicament for treatment of a subject suffering from bodily dysfunction.

19

AMENDED SHEET (ARTICLE 19)

Previous Patent: AIR STRIPPING DEVICE

Next Patent: METHOD OF MANUFACTURING A CARTRIDGE FOR A FLUID MIXTURE DISPENSING SYSTEM