Phenylquinoline compositions for treatment of ocular disorders and conditions

Patent metadata

Field	Value
Publication number	US-11337968-B2
Application number	US-201716097353-A
Country	US
Kind code	B2
Filing date	Apr 28, 2017
Priority date	Apr 29, 2016
Publication date	May 24, 2022
Grant date	May 24, 2022

Abstract

Compositions containing a phenylquinoline derivative compound having peroxisome proliferator-activated receptor a (PPARα) agonistic activity, and methods of their use in enhancing PPARα activity in retinal cells, and in treating ocular disorders or conditions, such as but not limited to retinal inflammation, retinal neovascularization, retinal vascular leakage, retinopathy of prematurity, diabetic retinopathy, age-related macular degeneration, and diabetic macular edema are disclosed.

First claim

What is claimed is:

1. A method of treating an ocular disorder or condition in a subject, comprising:
administering to the subject a phenylquinoline derivative compound having peroxisome proliferator-activated receptor α (PPARα) agonistic activity, the compound having the chemical structure I:

wherein:
R 1 is CH 3 , R 2 is selected from Cl, F, Br, and I, R 5 is a carboxylic acid group, and R 3 , R 4 , and R 6 -R 11 are H; and
wherein the ocular disorder or condition is selected from the group consisting of retinopathy of prematurity (ROP), diabetic retinopathy (DR), age-related macular degeneration (AMD), and diabetic macular edema (DME).

2. A method of treating an ocular disorder or condition in a subject, comprising:
administering to the subject a phenylquinoline derivative compound having peroxisome proliferator-activated receptor α (PPARα) agonistic activity, the compound having the chemical structure I:

wherein:
R 1 is CH 3 , R 2 is Cl, R 5 is a carboxylic acid group, and R 3 , R 4 , and R 6 -R 11 are H;
and wherein the ocular disorder or condition is selected from the group consisting of retinopathy of prematurity (ROP), diabetic retinopathy (DR), age-related macular degeneration (AMD), and diabetic macular edema (DME).

3. A method of treating an ocular disorder or condition in a subject, comprising:
administering to the subject a phenylquinoline derivative compound having peroxisome proliferator-activated receptor α (PPARα) agonistic activity, the compound having the chemical structure I:

wherein:
R 1 is CH 3 , R 2 is F, R 5 is a carboxylic acid group, and R 3 , R 4 , and R 6 -R 11 are H;
and wherein the ocular disorder or condition is selected from the group consisting of retinopathy of prematurity (ROP), diabetic retinopathy (DR), age-related macular degeneration (AMD), and diabetic macular edema (DME).

4. The method of claim 1 , wherein R 2 is Br.

5. The method of claim 1 , wherein R 2 is Iodine (I).

Assignees

• Univ Oklahoma

Inventors

• Ma Jian-Xing
• Moran Elizabeth
• Deng Guotao
• Duerfeldt Adam S

Classifications

• C07D413/12

  linked by a chain containing hetero atoms as chain links · CPC title

• C07D215/52

  with aryl radicals attached in position 2 · CPC title

• A61K9/0048

  Eye, e.g. artificial tears · CPC title

• C07D405/04

  directly linked by a ring-member-to-ring-member bond · CPC title

• C07D215/48

  Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen · CPC title