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

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

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: (Hydroxybenzoyl)thiophenesulfonamide and acyl derivatives thereof are useful for the topical treatment of elevated intraocular pressure in ophthalmic compositions including drops and inserts.

Abstract: Novel acyloxy derivatives of [phenylsulfonyl(or sulfinyl)]thiophenesulfonamides are useful for the topical treatment of elevated intraocular pressure in ophthalmic compositions including drops and inserts.

Abstract: There are disclosed cyclic octapeptide analogs of the tridecapeptide, neurotensin.

Abstract: There are disclosed metabolically protected linear analogs of the carboxy terminal pentapeptide fragment of the tridecapeptide, neurotensin.

Abstract: Benzocycloheptapyridines with an imine bridge in the cycloheptane ring, derivatives and pharmaceutically acceptable salts thereof are useful as anxiolytics, antidepressants, anticonvulsants, muscle relaxants and in the treatment of mixed anxiety-depression, minimal brain dysfunction and extrapyramidal disorders such as Parkinson's disease. They are prepared, for example, by treatment of a benzo[5,6]cyclohepta[1,2-c]pyridin-11-one with ammonia to give the 11-imine, acylation of the imine, treatment of the protected imine with an alkyllithium to provide the 11-alkyl-11-acylamino compound, treatment with acid or base to cause ring closure to an 11-alkyl-6,11-acylimino compound followed by removal of the protecting group, either hydrolytically or hydrogenolytically.

Abstract: 10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease. They are prepared by treatment of a 5H-dibenzo[a,d]cyclohepten-5-one with ammonia to give the 5-imine, acylation of the imine, treatment of the protected imine with an organolithium to provide the 5-substituted-5-acylamino compound, treatment with acid or base to cause ring closure to a 5-substituted-5,10-acylimino compound followed by removal of the protecting group, either hydrolytically or hydrogenolytically.

Abstract: Benzocycloheptapyridines with an imine bridge in the cycloheptane ring, derivatives and pharmaceutically acceptable salts thereof are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease.

Abstract: Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt; ester and amide or derivatives; and methods of treatment comprising administering such compounds and compositions.

Abstract: Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt, ester and amide derivatives; and methods of treatment comprising administering such compounds and compositions.

Abstract: Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt, ester and amide derivatives, and methods of treatment comprising administering such compounds and compositions.

Abstract: Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt, ester and amide derivatives; and methods of treatment comprising administering such compounds and compositions.

Abstract: Novel 4-phenyl-4-substituted-5-oxo-7-aryl-heptanoic acids are prefaced by either of two synthetic processes. The first method involves the reaction of a 4-phenyl-4-substituted-5-oxo-hexanoic acid with an arylcarboxyaldehyde. The second method involves reaction of an arylcarboxaldehyde with an appropriate ketone, treatment of the product with an acrylic acid ester, followed by hydrolysis of the resulting ester. The compounds of the invention are prostaglandin antagonists and are particularly useful as topical anti-inflammatory agents.