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Claims for Patent: 6,248,735

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Claims for Patent: 6,248,735

Title: Ophthalmic compositions comprising combinations of a carbonic anhydrase inhibitor and a .beta.-adrenergic antagonist
Abstract:Combinations of a .beta.-adrenergic antagonist and a topical carbonic anhydrase inhibitor are particularly useful in the treatment of ocular hypertension, especially in patients insufficiently responsive to treatment with .beta.-adrenergic antagonists.
Inventor(s): Baldwin; John J. (Gwynedd Valley, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:08/833,067
Patent Claims: 1. A topical formulation for treatment of ocular hypertension or glaucoma comprising an opthalmologically acceptable carrier, 0.05 to 5% of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide, the individual diastereomers, enantiomers or mixtures thereof, or an ophthalmologically acceptable salt thereof, and 0.01 to 1.0% of (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol, or an ophthalmologically acceptable salt thereof.

2. A formulation of claim 1 wherein the salt of (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol is maleate.

3. A formulation of claim 1 wherein the salt of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide is the monohydrochloride salt.

4. A formulation of claim 3 wherein the concentration of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide is 0.5 to 3%.

5. A formulation of claim 2 wherein the concentration of (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol is 0.1 to 0.5%.

6. A formulation of claim 1 wherein the concentration of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide is 0.7 to 2.0% and the concentration of (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol is 0.5%.

7. A formulation of claim 6 which further contains a gum.

8. A formulation of claim 7 wherein the gum is gellan gum at a concentration of 0.1% to 2%.

9. A formulation of claim 1 which takes a form of solution, gel, ointment, suspension or solid insert.

10. A formulation of claim 6 wherein the ratio of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide to (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol is greater than one.

11. A formulation of claim 10 wherein the concentration of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide is 2% and (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol is 0.5%.

12. A topical formulation for treatment of ocular hypertension or glaucoma comprising an opthalmologically acceptable carrier, 2% of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide monohydrochloride, and 0.5% of (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol maleate, or an ophthalmologically acceptable salt thereof.

13. A formulation of claim 12 which further contains gellan gum at a concentration of 0.1% to 2%.

14. A method of treating ocular hypertension or glaucoma, which, comprises administration of an effective amount of a topical ophthalmic formulation to a patient in need thereof, comprising an ophthalmologically acceptable carrier, 0.05 to 5% of (S,S)-(-)-5,6dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-su lfonamide-7,7 dioxide, the individual diastereomers, enantiomers or mixtures thereof, or an ophthalmologically acceptable salt thereof, and 0.01 to 1.0% of (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol, or an ophthalmologically acceptable salt thereof.

15. A method of claim 14 wherein the salt of (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol is maleate.

16. A method of claim 14 wherein the salt of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide is the monohydrochloride salt.

17. A method of claim 16 wherein tie concentration of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide is 0.5 to 3%.

18. A method of claim 15 wherein the concentration of (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol is 0.1 to 0.5%.

19. A method of claim 14 wherein the concentration of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide is 0.7 to 2.0% and the concentration of (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol is 0.5%.

20. A method of claim 14 wherein the formulation contains a gum.

21. A method of claim 20 wherein the gum is gellan gum at a concentration of 0.1% to 2%.

22. A method of claim 14 wherein the formulation takes a form of solution, gel, ointment, suspension or solid insert.

23. A method of claim 14 wherein the formulation takes the form of a solution adapted for topical administration.

24. A method of claim 20 wherein the ratio of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-2,3-b]thiopyran-2-su lfonamide-7,7 dioxide to (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol is greater than one.

25. A method of claim 14 wherein the concentration of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide is 2% and (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol is 0.5%.

26. A method of treating ocular hypertension or glaucoma, which comprises administration of an effective amount of a topical ophthalmic formulation to a patient in need thereof, comprising an ophthalmologically acceptable carrier, 2% of (S,S)-(-)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno-[2,3-b]thiopyran-2-s ulfonamide-7,7 dioxide monohydrochloride, 0.5% of (s)-(-)-1-(tert-butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy-2-p ropanol maleate.

27. A method of claim 26 wherein the formulation contains gellan gum at a concentration of 0.1% to 2%.
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