Compositions and methods of treating retinal disease

Patent metadata

Field	Value
Publication number	US-9265759-B2
Application number	US-201414581462-A
Country	US
Kind code	B2
Filing date	Dec 23, 2014
Priority date	May 26, 2005
Publication date	Feb 23, 2016
Grant date	Feb 23, 2016

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 and other forms of retinal disease mediated by the accumulation of A2E and/or lipofuscin in a subject, the method comprising administering to the subject a composition comprising a compound of formula Ia:

or a pharmaceutically acceptable salt of Ia,

wherein
X is CH;
Z is N;
Y is C with the —NH 2 attached to Y;
p is 1, 2, or 3;
B is a halogen atom, hydroxyl, carbamoyl, substituted or unsubstituted aryl or amino wherein substituted aryl has one or more substituents selected from halogen, hydroxyl, alkoxy, alkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aryloxycarbonyloxy, carboxylate, alkylcarbonyl, alkylaminocarbonyl, aralkylaminocarbonyl, alkenylaminocarbonyl, arylcarbonyl, aralkylcarbonyl, alkenylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylthiocarbonyl, phosphate, phosphonato, phosphinato, cyano, amino, alkylamino, dialkylamino, arylamino, diarylamino, alkylarylamino, acylamino, alkylcarbonylamino, arylcarbonylamino, carbamoyl, ureido, amidino, imino, sulfhydryl, alkylthio, arylthio, thiocarboxylate, sulfates, alkylsulfinyl, sulfamoyl, sulfonamido, nitro, trifluoromethyl, azido, heterocyclyl, alkylaryl, an aromatic moiety and a heteroaromatic moiety;
A is

D is unbranched lower alkyl; and
R is substituted or unsubstituted C1, C2, C3, C4, C5, C6, C7, or C8 straight chain alkyl, or substituted or unsubstituted C3, C4, C5, C6, C7or C8 branched chain alkyl wherein said substituted straight chain alkyl or said substituted branched chain alkyl has one or more substituents selected from alkyl, alkenyl, alkynyl, halogen, hydroxyl, alkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aryloxycarbonyloxy, carboxylate, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkylthiocarbonyl, alkoxyl, phosphate, phosphonato, phosphinato, cyano, amino, alkylamino, dialkylamino, arylamino, diarylamino, alkylarylamino, acylamino, alkylcarbonylamino, arylcarbonylamino, carbamoyl, ureido, amidino, imino, sulfhydryl, alkylthio, arylthio, thiocarboxylate, sulfates, alkylsulfinyl, sulfamoyl, sulfonamido, trifluoromethyl, azido, heterocyclyl, alkylaryl, an aromatic moiety and a heteroaromatic moiety.

2. The method of claim 1 , wherein p is 1.

3. The method of claim 2 , wherein A is

4. The method of claim 3 , wherein D is CH 3 .

5. The method of claim 4 , wherein B is a halogen atom.

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

• C07D215/38 Primary

  Nitrogen atoms (nitro radicals C07D215/18) · CPC title