Compositions and methods of treating retinal disease

Patent metadata

Field	Value
Publication number	US-9650342-B2
Application number	US-201615049890-A
Country	US
Kind code	B2
Filing date	Feb 22, 2016
Priority date	May 26, 2005
Publication date	May 16, 2017
Grant date	May 16, 2017

Abstract

Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed.

First claim

What is claimed is:

1. A method of treating macular degeneration or a retinal disease mediated by the accumulation of N-retinylidene-N-retinylethanolamine (A2E) and/or lipofuscin, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula (I):

or a pharmaceutically acceptable salt thereof,

wherein
W, X, Y, and Z are each independently N, S, O, CU, CH, or C with the —NH 2 , wherein at least one of W, X, Y and Z is N;
A is selected from the group consisting of

wherein
D is an unbranched C 1-6 alkyl, wherein each D can be the same or different; and
R is a substituted or unsubstituted C 1-8 straight chain alkyl or C 3-8 branched chain alkyl;
U is selected from halogen, cyano, lower alkyl, and aryl, wherein one or more hydrogen atoms on the lower alkyl or aryl are optionally substituted by substituents selected from the group consisting of halogen, hydroxyl, carbamoyl, amino and aryl, and
n is 0, 1, 2, 3, or 4.

2. The method of claim 1 , wherein A is

wherein D is an unbranched C 1-6 straight chain alkyl.

3. The method of claim 2 , wherein each D is methyl.

4. The method of claim 1 , wherein n is 0 or 1.

5. The method of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

6. The method of claim 1 , where the compound is

7. The method of claim 1 , wherein the macular degeneration is age-related macular degeneration (AMD).

8. The method of claim 7 , wherein the AMD is wet AMD or dry AMD.

9. The method of claim 1 , wherein the macular degeneration is Stargardt's disease.

10. The method of claim 1 , wherein U is a halogen.

11. The method of claim 10 , wherein the halogen is chloro or bromo.

Assignees

• Aldeyra Therapeutics Inc

Inventors

• Jordan Thomas A
• Dowling John E
• Chabala John Clifford

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P27/02

  Ophthalmic agents · CPC title

• A61P27/00

  Drugs for disorders of the senses · CPC title

• A61K31/423

  condensed with carbocyclic rings · CPC title

• A61K31/426

  1,3-Thiazoles · CPC title