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Generated: January 23, 2018

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Title: Thiophene sulfonamides useful as carbonic anhydrase inhibitors
Abstract:Thiophene 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)
Filing Date:Nov 27, 1990
Application Number:07/618,765
Claims:1. A compound selected from the group consisting of:

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

3,4-Dihydro-4-methoxy-2-[2-(4-morpholino)ethyl]-4H-thieno[3,2-e]-1,2-thiazi ne-6-sulfonamide-1,1-dioxide,

3,4-Dihydro-4-ethylamino-2-methyl-4H-thieno[3,2-e]-1,2-thiazine-6-sulfonami de-1,1-dioxide;

3,4-Dihydro-4-ethylamino-2-allyl-4H-thieno[3,2-e]-1,2-thiazine-6-sulfonamid e-1,1-dioxide;

3,4-Dihydro-4-ethylamino-2-n-propyl-4H-thieno[3,2-e]-1,2-thiazine-6-sulfona mide-1,1-dioxide;

3,4-Dihydro-4-ethylamino-2-(2-methoxyethyl)-4H-thieno[3,2-e]-1,2-thiazine-6 -sulfonamide-1,1-dioxide; and

3,4-Dihydro-4-hydroxy-2-[2-(4-morpholino)ethyl]-4H-thieno[3,2-e]-1,2-thiazi ne-6-sulfonamide-1,1-dioxide.

2. The compound of claim 1 which is

3,4-Dihydro-4-ethylamino-2-methyl-4H-thieno[3,2-e]-1,2-thiazine-6-sulfonami de-1,1-dioxide.

3. (+)-3,4-Dihy dro-4-ethylamino-2-methyl-4H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-d ioxide.

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

5. The formulation of claim 4 wherein the compound concentration is between about 0.1 and 10% by weight.

6. A formulation for controlling intraocular pressure comprising a therapeutically effective amount of the compound of claim 3 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 method for controlling intraocular pressure which comprises topically administering to the affected eye a therapeutically effective amount of the compound of claim 1.

9. A method for controlling intraocular pressure which comprises topically administering to the affected eye a therapeutically effective amount of the compound of claim 3.

10. A method for controlling intraocular pressure which comprises topically administering the formulation of claim 1.

11. A formulation for controlling intraocular pressure, comprising between about 0.25 wt % and 5.0 wt % (+)-3,4-Dihydro-4-ethylamino-2-methyl-4H-thieno[3,2-e]-1,2-thiazine-6-sulf onamide-1,1-dioxide in a pharmaceutically acceptable carrier.
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