IP Library Granted Patent US 10,202,348
Granted Patent B2
US 10,202,348 · App. 15/861,332 · Granted Feb 12, 2019

Compositions and methods of treating retinal disease

Inventors: Thomas A. Jordan (Lexington, MA); John E. Dowling (Boston, MA); John Clifford Chabala (Scotch Plains, NJ)
Assignee: Aldeyra Therapeutics, Inc.
C07D215/38A61K31/41A61K31/423A61K31/426A61K31/435A61K31/44A61K31/4418A61K31/47A61K31/4706C07C215/68C07C229/56C07C229/60C07D277/40C07D277/56
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Quick Facts
Patent No.
US 10,202,348
App. No.
15/861,332
Granted
Feb 12, 2019
Kind
B2
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.

Claims (30)

1. A compound of formula:

or a pharmaceutically acceptable salt thereof

wherein,

X is CH;

Y is C with the —NH 2 attached to Y;

Z is N;

A is

 and

D is a 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 compound of claim 1 , wherein A is:

3. The compound of claim 1 which is:

or a pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition comprising a compound of formula:

or a pharmaceutically acceptable salt thereof

wherein,

X, Y, and Z are each, independently, N, CH, or C with the —NH 2 attached, wherein at least one of X, Y and Z is N;

A is

D is a unbranched lower alkyl;

R is substituted or unsubstituted C1, C2, C3, C4, C5, C6, C7, or C 8 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; and

a pharmaceutically acceptable carrier.

5. The pharmaceutical composition of claim 4 , wherein

X is CH;

Y is C with the —NH 2 attached to Y; and

Z is N.

6. The pharmaceutical composition of claim 4 , wherein A is:

7. The pharmaceutical composition of claim 6 , wherein each D is methyl.

8. The pharmaceutical composition of claim 4 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

9. The pharmaceutical composition of claim 5 , wherein A is:

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 3, 2019
From: JORDAN, THOMAS A.; DOWLING, JOHN E.; CHABALA, JOHN CLIFFORD
To: NEURON SYSTEMS, INC.
Reel/Frame 047892/0298 →
CHANGE OF ADDRESS Recorded Jan 3, 2019
From: NEURON SYSTEMS, INC.
To: NEURON SYSTEMS, INC.
Reel/Frame 048004/0258 →
CHANGE OF NAME Recorded Jan 3, 2019
From: NEURON SYSTEMS, INC.
To: ALDEXA THERAPEUTICS, INC.
Reel/Frame 048007/0294 →
CHANGE OF NAME Recorded Jan 3, 2019
From: ALDEXA THERAPEUTICS, INC.
To: ALDEYRA THERAPEUTICS, INC.
Reel/Frame 048007/0346 →
Continuity (8)
Continuation 15488205 · Apr 14, 2017
Continuation 15049890 · Feb 22, 2016
Continuation 14581462 · Dec 23, 2014
Continuation 13175218 · Jul 1, 2011
Continuation 11441848 · May 26, 2006
Provisional Application 60723577 · Oct 4, 2005
Provisional Application 60685460 · May 26, 2005
Related Publication 20180194733A1 · Jul 12, 2018
Cited By (1)
US 12,240,816