HIF-1α inhibitor, preparation method therefor, and pharmaceutical composition for preventing or treating angiogenesis-associated eye disease, containing same as active ingredient

Patent metadata

Field	Value
Publication number	US-12006283-B2
Application number	US-201917057297-A
Country	US
Kind code	B2
Filing date	Aug 12, 2019
Priority date	Aug 31, 2018
Publication date	Jun 11, 2024
Grant date	Jun 11, 2024

Abstract

Disclosed are a novel hypoxia-inducible factor 1α (HIF-1α) inhibitor, a method of preparing the same, and a pharmaceutical composition for preventing or treating an angiogenesis-related eye disease containing the same as an active ingredient. The compound of Example provided according to an embodiment of the present invention is capable of effectively inhibiting HIF-1α and is thus useful as a pharmaceutical composition for preventing or treating an angiogenesis-related eye disease.

First claim

The invention claimed is:

1. A compound represented by the following Formula (1), or a solvate, hydrate, optical isomer or pharmaceutically acceptable salt thereof:

A 1 and A 2 are methoxy or A 1 is H and A 2 is F;
B 1 is —H, or C 1-10 straight- or branched-chain alkoxy; and
R 1 is C 3-10 cycloalkyloxy, heterocycloalkyl of a 5- to 10-membered ring containing at least one heteroatom selected from the group consisting of N, O and S, or benzylamino unsubstituted or substituted with —CN.

2. The compound or a solvate, hydrate, optical isomer, or pharmaceutically acceptable salt thereof according to claim 1 , wherein B 1 is C 1-10 straight- or branched-chain alkoxy, and R 1 is heterocycloalkyl of a 5-membered ring containing N.

3. The compound or a solvate, hydrate, optical isomer, or pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound of Formula 1 is selected from the group consisting of the following compounds:

4. A method of treating or preventing an angiogenesis-related eye disease in a subject, the method comprising administering a pharmaceutically effective amount of the compound according to claim 1 to the subject.

5. The method according to claim 4 , wherein the angiogenesis-related eye disease is age-related macular degeneration, diabetic retinopathy, retinopathy of prematurity, or neovascular glaucoma.

Assignees

• Seoul Nat Univ R&Db Foundation

Inventors

• Suh Youngger
• Lee Seungbeom
• Kim Jeonghun

Classifications

• C07D265/30

  not condensed with other rings · CPC title

• C07D211/22

  by oxygen atoms · CPC title

• C07D207/08 Primary

  with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms · CPC title

• C07C255/59

  the carbon skeleton being further substituted by singly-bound oxygen atoms · CPC title

• C07C225/22

  having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton · CPC title