Claims for Patent: 8,034,839

Summary for Patent: 8,034,839

Title:	Method of treating ocular allergy
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.
Inventor(s):	Klimko; Peter G. (Fort Worth, TX), Beauregard; Clay (Burleson, TX)
Assignee:	Alcon Research, Ltd. (Fort Worth, TX)
Application Number:	12/702,030
Patent Claims:	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: ##STR00010## wherein R.sup.1 is CONR.sup.2R.sup.3 or CH.sub.2NR.sup.5R.sup.6, where: R.sup.2, R.sup.3 are independently H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, benzyl, phenyl, OH, OCH.sub.3, or OC.sub.2H.sub.5, provided that at most only one of R.sup.2, R.sup.3 is OH, OCH.sub.3, or OC.sub.2H.sub.5; R.sup.5, R.sup.6 are independently H, C(O)R.sup.14, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, benzyl, phenyl, OH, OCH.sub.3, or OC.sub.2H.sub.5, provided that at most only one of R.sup.2, R.sup.3 is OH, OCH.sub.3, or OC.sub.2H.sub.5; R.sup.7, R.sup.8, and R.sup.9 are independently H, CH.sub.3, C.sub.2H.sub.5, C(O)R.sup.14, or CO.sub.2R.sup.15; or R.sup.7 and R.sup.8 or R.sup.8 and R.sup.9 together constitute a carbonyl group (C.dbd.O), thus forming a cyclic carbonate; or OR.sup.8R.sup.1 together form a cyclic ester (a lactone); R.sup.14 is H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, benzyl, or phenyl; R.sup.15 is C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, benzyl, or phenyl; and indicates that the OR.sup.9 substituent can be arranged to afford the R or S absolute configuration: ##STR00011## 2. The method of claim 1 wherein for the compound of formula I: R.sup.7, R.sup.8, R.sup.9 are independently H, CH.sub.3, or CH.sub.3CO; or R.sup.7 and R.sup.8 or R.sup.8 and R.sup.9 together constitute a carbonyl group (C.dbd.O), thus forming a cyclic carbonate; or OR.sup.8R.sup.1 together form a cyclic ester (a lactone). 3. The method of claim 2 wherein the compound of formula I has the configuration: ##STR00012## 4. The method of claim 2, wherein the compound of formula I has the configuration: ##STR00013## 5. The method of claim 3, wherein a compound of formula I is used to treat seasonal or perennial allergic conjunctivitis. 6. The method of claim 3, wherein a compound of formula I is used to treat vernal keratoconjunctivitis, atopic keratoconjunctivitis, or giant papillary conjunctivitis. 7. The method of claim 6, wherein the compound of formula I is used in combination with a histamine receptor antagonist and/or a mast cell stabilizer. 8. The method of claim 7, 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-oxazolidino- ne ethanedioate; pyrilamine; clemastine; azelastine; epinastine; ketotifen; olopatadine; mapinastine; lodoxamide; cromolyn sodium; and nedocromil disodium salt. 9. 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). 10. The method of claim 9, 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.

Details for Patent 8,034,839

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Jubilant Hollisterstier Llc	N/A	positive skin test control-histamine	Injection	103891	03/13/1924		2025-11-07