Abstract: This invention relates to novel compounds, their synthesis and use as selective .alpha..sub.1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the .alpha..sub.1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: 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.

Abstract: 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.

Abstract: Compounds of general formula: ##STR1## are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and related disorders such as glaucoma.

Abstract: 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.

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

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

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

Abstract: 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.

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

Abstract: 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.

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

Abstract: 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.

Abstract: 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.

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

Abstract: 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.