US2022304968A1PendingUtilityA1

Oxidative retinal diseases

72
Assignee: RETROTOPE INCPriority: Apr 26, 2011Filed: Mar 28, 2022Published: Sep 29, 2022
Est. expiryApr 26, 2031(~4.8 yrs left)· nominal 20-yr term from priority
A61K 45/06A61K 31/122A61K 31/66A61P 27/12A61K 31/375A61P 27/00A61K 31/12A61P 39/06A61P 27/02A61K 31/231A61P 9/10A61K 31/202A61P 3/10A61K 31/201A61P 43/00A61K 31/355A61K 31/23A61K 9/4858A61K 9/0048
72
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Claims

Abstract

Some aspects of the invention provide for a method of treating Wet and/or Dry Age-related Macular Degeneration, Retinitis Pigmentosa, Diabetic Retinopathy, cataracts, and/or Stargardt Disease using polyunsaturated fatty acids which are modified in certain positions to attenuate oxidative damage by Reactive Oxygen Species (ROS) and/or suppress the rate of formation of reactive products and toxic compounds.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A method of treating or preventing the progression of an oxidative retinal disease, comprising:
 administering an effective amount of a polyunsaturated substance to a Wet or Dry Age-related Macular Degeneration (AMD), Retinitis Pigmentosa (RP), Diabetic Retinopathy (DR), Cataracts, or Stargardt Disease (SD) patient in need of treatment, wherein the polyunsaturated substance is chemically modified such that one or more bonds is stabilized against oxidation;   wherein the polyunsaturated substance or a polyunsaturated metabolite thereof comprising said one or more stabilized bonds is incorporated into the patient's body following administration.   
     
     
         2 . The method of  claim 1 , wherein the polyunsaturated substance is a fatty acid, a fatty acid mimetic, or a fatty acid pro-drug. 
     
     
         3 . The method of  claim 2 , wherein the fatty acid, fatty acid mimetic, or fatty acid pro-drug is stabilized at one or more bis-allylic positions. 
     
     
         4 . The method of  claim 3 , wherein the stabilization comprises at least one  13 C atom or at least one deuterium atom at a bis-allylic position, wherein the at least one  13 C atom or the at least one deuterium atom is present at a level significantly above the naturally-occurring abundance level of said isotope. 
     
     
         5 . The method of  claim 4 , wherein the stabilized fatty acid, fatty acid mimetic, or fatty acid pro-drug comprise between about 10% and 50% of the total amount of fatty acids, fatty acid mimetics, or fatty acid pro-drugs administered to the patient. 
     
     
         6 . The method of  claim 4 , wherein the isotopically stabilized fatty acid, fatty acid mimetic, or fatty acid pro-drug comprise between about 10% and 30% of the total amount of fatty acids, fatty acid mimetics, or fatty acid pro-drugs administered to the patient. 
     
     
         7 . The method of  claim 4 , wherein the isotopically stabilized fatty acid, fatty acid mimetic, or fatty acid pro-drug comprise about 20% or more of the total amount of fatty acids, fatty acid mimetics, or fatty acid pro-drugs administered to the patient. 
     
     
         8 . The method of  claim 4 , wherein a cell or tissue of the patient maintains a sufficient concentration of the fatty acid, fatty acid mimetic, or fatty acid pro-drug to prevent autooxidation of the naturally occurring polyunsaturated fatty acid, mimetic, or ester pro-drug. 
     
     
         9 . The method of  claim 4 , wherein the polyunsaturated substance is an omega-3 fatty acid, fatty acid mimetic, or fatty acid pro-drug, or an omega-6 fatty acid, fatty acid mimetic, or fatty acid pro-drug. 
     
     
         10 . The method of  claim 9 , wherein the polyunsaturated substance is selected from the group consisting of 11,11-D2-linolenic acid, 14,14-D2-linolenic acid, 11,11,14,14-D4-linolenic acid, 11,11-D2-linoleic acid, 14,14-D2-linoleic acid, 11,11,14,14-D4-linoleic acid, 11-D-linolenic acid, 14-D-linolenic acid, 11,14-D2-linolenic acid, 11-D-linoleic acid, 14-D-linoleic acid, and 11,14-D2-linoleic acid. 
     
     
         11 . The method of  claim 9 , wherein the polyunsaturated substance is further stabilized at a pro-bis-allylic position. 
     
     
         12 . The method of  claim 4 , wherein the polyunsaturated substance is a fatty acid pro-drug ester. 
     
     
         13 . The method of  claim 12 , wherein the ester is a triglyceride, diglyceride, or monoglyceride. 
     
     
         14 . The method of  claim 2  further comprising co-administering an antioxidant. 
     
     
         15 . The method of  claim 14 , wherein the antioxidant is Coenzyme Q, idebenone, mitoquinone, mitoquinol, vitamin C, or vitamin E.

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