IP Library Granted Patent US 7,687,539
Granted Patent B1
US 7,687,539 · App. 11/593,714 · Granted Mar 30, 2010

Method of treating ocular allergy

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Quick Facts
Patent No.
US 7,687,539
App. No.
11/593,714
Granted
Mar 30, 2010
Kind
B1
Abstract

The topical use of 5,6,7-trihydroxyheptanoic acid and analogs alone or in combination with histamine antagonists and/or mast cell stabilizers is disclosed for the treatment of ocular allergy.

Claims (20)

1. A method for the treatment of ocular allergy in a mammal, which comprises topically administering to the eye of the mammal a composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound of formula I:

wherein

R 1 is C 2 H 5 , CO 2 R, CH 2 OR 4 , or a carboxylate salt of formula CO 2 − R + ;

R + is Li + , Na + , K + , or NH 4 + ;

R is H, CH 3 , C 2 H 5 , n-C 3 H 7 , or i-C 3 H 7 ;

R 4 is H, COCH 3 , or CH 3 ; and

R 7 , R 8 , R 9 are independently H, CH 3 , or CH 3 CO;

or R 7 and R 8 or R 8 and R 9 together constitute a carbonyl group (C═O), thus forming a cyclic carbonate;

or OR 8 R 1 together form a cyclic ester (a lactone); and

indicates that the OR 9 substituent can be arranged to afford the R or S absolute configuration:

2. The method of claim 1 , wherein the compound of formula I has the configuration:

3. The method of claim 1 , wherein the compound of formula I has the configuration:

4. The method of claim 2 , wherein a compound of formula I is used to treat seasonal or perennial allergic conjunctivitis.

5. The method of claim 2 , wherein a compound of formula I is used to treat vernal keratoconjunctivitis, atopic keratoconjunctivitis, or giant papillary conjunctivitis.

6. The method of claim 5 , wherein the compound of formula I is used in combination with a histamine receptor antagonist and/or a mast cell stabilizer.

7. The method of claim 6 , wherein the histamine receptor antagonist and/or mast cell stabilizer is selected from the group consisting of: emedastine; levocabastine; mequitazine; chlorpheniramine; brompheniramine; astemizole; cetirizine; terfenadine; rocastine; loratadine; desloratadine [that is, 8-chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine]; 5-[2-[4-bis(4-fluorophenyl)hydroxymethyl-1-piperidinyl]ethyl]-3-methyl-2-oxazolidinone ethanedioate; pyrilamine; clemastine; azelastine; epinastine; ketotifen; olopatadine; mapinastine; lodoxamide; cromolyn sodium; and nedocromil disodium salt.

8. The method of claim 4 or claim 5 , wherein the compound of formula I is selected from the group consisting of:

9. The method of claim 7 , wherein the compound of formula I is selected from the group consisting of:

10. The method of claim 1 , wherein the pharmaceutically effective amount of the compound of formula I is from 0.00003 to 0.01% (w/v).

11. The method of claim 10 , wherein the pharmaceutically acceptable carrier comprises one or more ingredients selected from the group consisting of surfactants; tonicity agents; buffers; preservatives; co-solvents; and viscosity building agents.

Assignments (2)
MERGER Recorded Jul 21, 2008
From: ALCON MANUFACTURING, LTD.
To: ALCON RESEARCH, LTD.
Reel/Frame 021266/0729 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 7, 2006
From: KLIMKO, PETER G.; BEAUREGARD, CLAY
To: ALCON MANUFACTURING, LTD.
Reel/Frame 018546/0559 →