Merck + Co., Inc.

Jacob M Hoffman, Jr

William A Bolhofer

Edward J Cragoe, Jr

Clarence S Rooney

Walfred S Saari

John S Wai

William J Greenlee

Otto W Woltersdorf, Jr

Theresa M Williams

William C Lumma, Jr

Philip E Sanderson

Kenneth L Shepard

Joel R Huff

Terrence M Ciccarone

Suresh K Balani

Sandor L Varga

Mark E Goldman

Anthony G Zacchei

Ling L Lee

Anthony D Theoharides, Deceased

Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Inhibitors of HIV reverse transcriptase

Novel aminopyridones inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

4-(2-Methyl-2-hydroxypropylamino)-5,6-dihydrothieno[2,3-b]thiopyran-2-sulfo namide-7,7-dioxide is a major mammalian metabolite of 4-(2-methylpropylamino)-5,6-dihydrothieno[2,3-b]thiopyran-2-sulfonamide-7, 7-dioxide and is itself an active carbonic anhydrase inhibitor useful in the treatment of ocular hypertension by topical administration.

4-(2-methyl-2-hydroxypropylamino)-5,6-dihydrot

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

Furopyridine sulfonamides and their opthalmological compositions

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

Novel ethers of hydroxy-2-benzothiazolesulfonamide are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions include drops and inserts.

Ethers of hydroxybenzothiazole-2-sulfonamide for the topical treatment

There are disclosed novel 1,2,4,6-thiatriazine-1,1-dioxides and related compounds which are connected to a substituted phenyl or heterocyclic group through a linear or cyclic connecting group. Processes are provided for the preparation of such compounds. The compounds are useful for the suppression of gastric acid secretions in mammals and compositions for such uses are also disclosed.

Thiatriazine dioxides as gastric anti-secretory agents

A process is disclosed for preparing intermediates which are useful for obtaining sulfamylamidine antisecretory agents.

Process for preparing sulfamylamidine antisecretory agents

There are disclosed novel compounds described as aminoalkyl pyridine derivatives in which the aminoalkyl pyridine is connected to a guanidine moiety or a functional equivalent thereof, either directly or through a linear connecting group. Processes for the preparation of such compounds are also disclosed. The compounds are useful for the suppression of gastirc acid secretions in mammals and compositions for such uses are also disclosed.

Aminoalkyl pyridine derivatives

There are disclosed novel substituted pyridopyrimidine compounds and processes for preparing such compounds. These compounds are useful as gastric secretion inhibitors in mammals.

Substituted pyridopyrimidines as gastric secretion inhibitors

Organic chemical compounds based upon the naphthyridine molecule are disclosed which have potent gastric secretion inhibitory properties. The naphthyridinone is substituted with a substituted amino alkyl group at the 1-position, and variously substituted at the remaining positions. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.

Substituted naphthyridinones and processes for their preparations

There are disclosed novel compounds described as imidazole cyanoguanidines in which the imidazole moiety is connected to the cyanoguanidine moiety through a cyclic group which may optionally contain one or two alkylene linkages. The cyclic groups may be phenyl, cyclohexyl, thienyl and the like. Processes for the preparation of such compounds are also disclosed. The compounds are useful for the suppression of gastric acid secretion in mammals, and compositions for such uses are also disclosed.

Cyclic imidazole cyanoguanidines

Compounds of the formula ##STR1## have been found to inhibit gastric secretion in mammalian species.

Growing community of inventors

North Wales, PA, United States of America

Jacob M Hoffman, Jr