Merck + Co., Inc.

Kenneth L Shepard

Samuel L Graham

John J Baldwin

Gerald S Ponticello

Theresa M Williams

William J Paleveda, Jr

Wasyl Halczenko

Marcia E Christy

Sandor L Varga

Robert G Strachan

Daniel G Brenner

George D Hartman

Edward J Cragoe, Jr

Daniel F Veber

Jacob M Hoffman, Jr

Cecilia A Hunt

Harvey Schwam

Frederick W Holly, Deceased

Charles M Habecker

Ronald J Hudcosky

Conformationally constrained tricyclic thienothiopyran compounds are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.

Tricyclic thienothiopyran carbonic anhydrase inhibitors

Substituted 4,5-dihydrothieno[2,3-b]thiophene-2-sulfonamides and 6,6-dioxides thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.

Substituted 4,5-dihydrothieno(2,3-b)thiophene-2-sulfonamides and

Intermediates are described for preparing conformationally constrained tricyclic thienothiopyran compounds that are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.

Tricyclic thienothiopyrans as pharmaceutical intermediates

Thieno[2,3-b][1,4]thiazine-6-sulfonamides having the structural formula: ##STR1## wherein Z, R.sup.1, R.sup.2, and n are as hereinafter defined, are carbonic anhydrase inhibitors useful in the topical treatment of elevated intraocular pressure and glaucoma.

Substituted thieno(2,3-B)(1,4)thiazine-6-sulfonamides as antiglaucoma

4-Alkylamino-6-(C.sub.3-5 -hydrocarbyl)thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxides wherein the 4-alkylamino group is an ethylamino or propylamino are powerful carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith. These compounds have the formula ##STR1##

4-alkylamino-6-(C.sub.3-5

Aryl (or aralkyl)-sulfonylthiophene-2-sulfonamides containing a basic functional group as a substituent are efficacious in the treatment of elevated intraocular pressure and glaucoma following topical ocular administration.

Thiophene sulfonamide antiglaucoma agents

Novel 2-sulfamoyl-1H-indoles and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in pharmaceutical compositions designed for systemic or topical ophthalmic administration.

2-Sulfamoyl-1H-indole derivatives for the treatment of elevated

Novel 2-sulfamoylbenzo[b]thiopenes and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.

2-Sulfamoylbenzo(b)thiophene derivatives pharmaceutical compositions and

Thienopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.

Thienopyridine sulfonamides and their ophthalmological formulation

Thiophene-2-sulfonamides with a 5-alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.

Substituted thiophene-2-sulfonamide antiglaucoma agents

Benzenesulfonamides with a substituted-alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.

Substituted benzenesulfonamides

Novel 2-sulfamoylbenzo[b]thiophenes and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.

Elevated intraocular pressure lowering benzo-[b]-thiophene-2-sulfonamide

5-[2(or 3)-Hydroxyphenylsulfonyl]thiophene-2-sulfonamides are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are disclosed.

5-[2(Or 3)-hydroxyphenylsulfonyl]thiophene-2-sulfonamides for the

Novel 2-sulfamoylbenzo[b]furans and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including opthalmic drops and inserts.

2-Sulfamoylbenzo[b]furan derivatives for the treatment of elevated

5-[Phenylsulfonyl(or sulfinyl)]thiophene-2-sulfonamides are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are disclosed.

Growing community of inventors

North Wales, PA, United States of America

Kenneth L Shepard