Compounds for inhibiting neovascularization factors and use thereof

Patent metadata

Field	Value
Publication number	US-12545695-B2
Application number	US-202017784969-A
Country	US
Kind code	B2
Filing date	Dec 16, 2020
Priority date	Dec 16, 2019
Publication date	Feb 10, 2026
Grant date	Feb 10, 2026

Abstract

The present specification relates to compounds for inhibiting neovascularization factors and use thereof. Furthermore, the present specification relates to methods for treating neovascularization diseases using the compounds.

First claim

What is claimed is:

1 . A compound of structure represented by the following [Chemical Formula 1], a pharmaceutically acceptable salt or a prodrug thereof:

wherein,
R 1 is H, C 1-5 alkyl, C 2-5 alkenyl, or C 2-5 alkynyl;
R 3 and R 4 are independently C 1-5 alkoxy;
R 2 and R 5 are independently hydroxy, alkoxy or halogen and at least one of R 2 and R 5 is halogen;
L is —(CH 2 ) n —; and
n is an integer from 5 to 12.

2 . The compound of claim 1 , wherein the compound of represented by [Chemical Formula 1] is selected from [Chemical Formula 2] to [Chemical Formula 5]:

3 . A method of treating a neovascular ocular disease in a subject in need thereof, comprising administering to said subject a therapeutically effective amount of a compound of a structure represented by the following [Chemical Formula 1], a pharmaceutically acceptable salt or a prodrug thereof:

wherein,
R 1 is H, C 1-5 alkyl, C 2-5 alkenyl, or C 2-5 alkynyl;
R 3 and R 4 are independently C 1-5 alkoxy;
R 2 and R 5 are independently hydroxy, alkoxy or halogen and at least one of R 2 and R 5 is halogen;
L is —(CH 2 ) n —; and
n is an integer from 5 to 12.

4 . The method of claim 3 , wherein the [Chemical Formula 1] is selected from [Chemical Formula 2] to [Chemical Formula 5]:

5 . The method of claim 3 , wherein the compound is formulated for eye drops.

6 . The method of claim 3 , wherein the neovascular ocular disease is selected from choroidal neovascular disease, retinal neovascular disease, subretinal neovascular disease, corneal neovascular disease, iris neovascular disease and neovascular glaucoma.

7 . The method of claim 3 , wherein the neovascular ocular disease is a retinal neovascular disease selected from diabetic retinopathy, retinopathy of prematurity, and retinal vein occlusion.

8 . The method of claim 3 , wherein the neovascular ocular disease is wet age-related macular degeneration (wet AMD).

Assignees

• Ulsan Nat Inst Science & Tech Unist
• Smartin Bio Inc

Inventors

• Kang Byoung Heon
• Kim So-Yeon
• Yoon Nam Gu
• Lee Changwook
• Park Dong Ho

Classifications

• A61K9/0048

  Eye, e.g. artificial tears · CPC title

• A61P27/02 Primary

  Ophthalmic agents · CPC title

• C07F9/5456

  Arylalkanephosphonium compounds · CPC title

• A61K9/08

  Solutions {(composition of solutions A61K47/00)} · CPC title

• C07F9/5442 Primary

  Aromatic phosphonium compounds (P-C aromatic linkage) · CPC title