Apratyramide therapeutic agents and methods of treatment

Patent metadata

Field	Value
Publication number	US-11358989-B2
Application number	US-201816765969-A
Country	US
Kind code	B2
Filing date	Nov 21, 2018
Priority date	Nov 22, 2017
Publication date	Jun 14, 2022
Grant date	Jun 14, 2022

Abstract

The invention is directed towards Apratyramide linear depsipeptide compounds, pharmaceutical compositions thereof, and methods of affecting wound healing, and methods of affecting the biological processes involved in wound healing (e.g., inflammation, cell proliferation, tissue granulation, remodeling of scar tissue, etc.).

First claim

What is claimed:

1. A compound according to the formula:

or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, or stereoisomer thereof.

2. The compound or pharmaceutically acceptable salt, solvate, hydrate, prodrug, or stereoisomer thereof of claim 1 , wherein the compound is:

3. A pharmaceutical composition comprising the compound of claim 1 , or pharmaceutically acceptable salt, solvate, hydrate, prodrug, or stereoisomer thereof, and a pharmaceutically acceptable carrier.

4. A topical pharmaceutical composition comprising the compound of claim 1 , or pharmaceutically acceptable salt, solvate, hydrate, prodrug, or stereoisomer thereof, and a pharmaceutically acceptable topical carrier.

5. A method of treating a subject suffering from or susceptible to a wound, comprising administering to said subject in need thereof, an effective amount of a compound of claim 1 , or pharmaceutically acceptable salt, solvate, hydrate, prodrug, or stereoisomer thereof.

6. The method of claim 5 , wherein the wound is a chronic wound.

7. The method of claim 5 , wherein the wound is a diabetic foot ulcer [DFU], pressure ulcer [PU], or chronic venous leg ulcer [VU].

8. A method of treating a subject suffering from or susceptible to a disorder or disease mediated by VEGF, comprising administering to said subject in need thereof, an effective amount of a compound of claim 1 , or pharmaceutically acceptable salt, solvate, hydrate, prodrug, or stereoisomer thereof, wherein the disorder or disease is a wound.

9. The method of claim 8 , wherein the disorder or disease is mediated by VEGF-A.

10. The method of claim 8 , wherein the wound is a chronic wound.

11. The method of claim 8 , wherein the wound is a diabetic foot ulcer [DFU], pressure ulcer [PU], or chronic venous leg ulcer [VU].

12. A method of inducing VEGF expression in a subject, comprising administering to said subject an effective amount of a compound of claim 1 , or pharmaceutically acceptable salt, solvate, hydrate, prodrug, or stereoisomer thereof.

Assignees

• Univ Florida
• Smithsonian Inst

Inventors

• Luesch Hendrik
• Cai Weijing
• Paul Valerie J
• Salvador Lilibeth A

Classifications

• C07K11/00 Primary

  Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof · CPC title

• A61K38/00

  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

• A61P17/02 Primary

  for treating wounds, ulcers, burns, scars, keloids, or the like · CPC title