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Claims for Patent: 5,240,923

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Claims for Patent: 5,240,923

Title: Sulfonamides useful as carbonic anhydrase inhibitors
Abstract:Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.
Inventor(s): Dean; Thomas R. (Weatherford, TX), Chen; Hwang-Hsing (Fort Worth, TX), May; Jesse A. (Fort Worth, TX)
Assignee: Alcon Laboratories, Inc. (Fort Worth, TX)
Application Number:07/775,313
Patent Claims: 1. A compound selected from the group consisting of:

3,4-Dihydro-2-(2-methoxy)ethyl-4-propylamino-2H- thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide;

2-(2-Ethoxyethyl-)-4-ethylamino-3,4-dihydro-2H-thieno[3,2-e]-1,2-thiazine-6 -sulfonamide 1,1-dioxide;

2-(2-Ethoxy)ethyl-3,4-dihydro-4-propylamino-2H-thieno[3,2-e]-1,2-thiazine-6 -sulfonamide 1,1-dioxide;

4-Ethylamino-3,4-dihydro-2-(3-methoxy)propyl-2H-thieno[3,2-e]-1,2-thiazine- 6-sulfonamide 1,1-dioxide;

3,4-Dihydro-2-(3-methoxy)propyl-4-propylamino-2H-thieno[3,2-e]-1,2-thiazine -6-sulfonamide 1,1-dioxide;

3,4-Dihydro-2-[2-(methoxyethoxy)ethyl]-4-propylamino-2H-thieno[3,2-e]-1,2-t hiazine-6-syulfonamide 1,1-dioxide; Ethylamino-3,4-dihydro-2-[2-(methoxyethoxy)ethyl]-2H-thieno[3,2-e]-1,2-thi azine-6-sulfonamide 1,1-dioxide;

4-Ethylamino-3,4-dihydro-2-[3-(methoxyethoxy)propyl]-2H-thieno[3,2-e]-1,2-t hiazine-6-sulfonamide 1,1-dioxide; and

3,4-Dihydro-2-[3-(methoxyethoxy)propyl]-4-propylamino-2H-thieno[3,2-e]-1,2- thiazine-6-sulfonamide 1,1-dioxide.

2. The compound of claim 10 which is

3,4-Dihydro-2-(2-methoxy)ethyl-4-propylamino-2H-thieno[3,2-e]-1,2-thiazine- 6-sulfonamide 1,1-dioxide.

3. The Compound of claim 1 which is 4-Ethylamino-3,4-dihydro-2-(3-methoxy)propyl-2H-thieno[3,2-e]-1,2-thiazine -6-sulfonamide -1,1-dioxide.

4. R-(+)-4-Ethylamino-3,4-di hydro-2-(2-methoxy)ethyl-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide.

5. R-(+)-3,4- Dihydro-2-(2-methoxy)ethyl-4-propylamino-2H-thieno[3,2-e]-1,2-thiazine-6-su lfonamide 1,1-dioxide.

6. A formulation for controlling intraocular pressure comprising a therapeutically effective amount of the compound of claim 1 in a pharmaceutically acceptable carrier.

7. The formulation of claim 6 wherein the compound concentration is between about 0.1 and 10% by weight.

8. A formulation for controlling intraocular pressure comprising a therapeutically effective amount of the compound of claim 4 in a pharmaceutically acceptable carrier.

9. The formulation of claim 8 wherein the compound concentration is between about 0.1 and 10% by weight.

10. The formulation of claim 9 wherein the concentration is between about 0.25 wt % and 5.0 wt %.

11. A formulation for controlling intraocular pressure comprising a therapeutically effective amount of the Compound of claim 5 in a pharmaceutically acceptable carrier.

12. The formulation of claim 11 wherein the compound concentration is between about 0.1 and 10% by weight.

13. The formulation of claim 12 wherein the concentration is between about 0.25 wt % and 5.0 wt %.

14. A method for controlling intraocular pressure which comprises topically administering to the affected eye a therapeutically effective amount of the compound of claim 1.
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