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Generated: September 21, 2017

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Title: Topical ophthalmic formulations for treating allergic eye diseases
Abstract:Topical ophthalmic formulations of the invention contain as an active ingredient 11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid or a pharmaceutically acceptable salt thereof. The formulations are useful for treating allergic eye diseases such as allergic conjunctivitis, vernal conjunctivitis, vernal keratoconjunctivitis, and giant papillary conjunctivitis.
Inventor(s): Hayakawa; Eiji (Susono, JP), Nakakura; Masashi (Shizuoka-ken, JP), Robertson; Stella M. (Arlington, TX), Yanni; John Michael (Burleson, TX)
Assignee: Alcon Laboratories, Inc. (Fort Worth, TX) Kyowa Hakko Kogyo Co. Ltd. (Tokyo, JP)
Application Number:08/469,729
Patent Claims: 1. A method for treating allergic eye diseases in humans comprising stabilizing conjuctival mast cells by topically administering to the eye a composition comprising a therapeutically effective amount of 11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz(b,e)oxepin-2-acetic acid or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 wherein the composition is a solution and the amount of 11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid is from about 0.0001 w/v. % to about 5% (w/v).

3. The method of claim 2 wherein the amount of 11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid is from about 0.001 to about 0.2% (w/v).

4. The method of claim 3 wherein the amount of 11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid is about 0.1% (w/v).

5. The method of claim 1 wherein the 11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid is (Z)-11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid, substantially free of (E)-11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid.

6. The method of claim 5 wherein the amount of (Z)-11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid is from about 0.0001 to about 5% (w/v).

7. The method of claim 6 wherein the amount of (Z)-11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid is from about 0.001 to about 0.2% (w/v).

8. The method of claim 7 wherein the amount of (Z)-11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid is 0.1% (w/v).

9. The method of claim 1 wherein the 11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid is (E)-11-(3-dimethylaminopropylidene) -6,11 -dihydrodibenz[b,e]oxepin-2-acetic acid, substantially free of (Z)-11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid.

10. The method of claim 9 wherein the amount of (E)-11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid is from about 0.0001 to about 5% (w/v).

11. The method of claim 10 wherein the amount of (E)-11-(3-dimethylaminopropylidene)-6,11-dihydredibenz[b,e]oxepin-2-acetic acid is from about 0.001 to about 0.2% (w/v).

12. The method of claim 11 wherein the amount of (E)-11-(3-dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid is about 0.1% (w/v).
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