Compounds characterized generally as amino acyl amino propargyl diol derivatives are useful in treatment of glaucoma. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b,b,b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrog...

The present invention provides a method for treating anxiety in humans using heterocyclic compounds.

Compounds such as [5-chloronicotine, 5-fluoronornicotine, anabaseine, 5-fluoroanabaseine, 2-acetoxymethylquinuclidine or]2-(3-pyridyl)-quinuclidine are useful as locally acting and highly selective muscle relaxants. Each compound, when administered intravenously, acts to bind to musculoskeletal nicotinic receptor sites in a reversible manner causing transient depolarization, and hence provides for reversible muscle relaxation to a patient during anesthesia.

The present invention relates to the use of certain NK-1 receptor antagonists (e.g., substance P receptor antagonists) to treat cancer patients, particularly cancer patients afflicted with a small cell lung carcinoma, APUDoma, astrocytoma, neuroendocrine tumor or extrapulmonary small cell carcinoma.

Compounds of structural formula (I): ##STR1## are squalene synthestase inhibitors useful in inhibiting the biosynthesis of cholesterol in the treatment of hypercholesterolemia and related disorders.

A method of treatment of migraine, cluster headaches and trigeminal neuralgia, radiation or cytotoxic agent induced nausea and vomiting and/or cardiac arrhythmia in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is C.sub.1-6 alkyl; R.sub.2 is amino or C.sub.1-7 acylamino; R.sub.3 is halo; one of R.sub.4 and R.sub.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phen...

Compounds such as 2-acetoxymethylquinuclidine are useful as locally acting and highly selective muscle relaxants. Each compound, when administered intravenously, acts to bind to musculoskeletal nicotinic receptor sites in a reversible manner causing transient depolarization, and hence provides for reversible muscle relaxation to a patient during anesthesia.

A method for the treatment of xerostomia not caused by Sjogren's syndrome comprising administering to an affected individual an effective amount of a derivative of spirooxathiolane-quinuclidine.

Compounds of general formula I: ##STR1## wherein: X represents oxygen or sulphur; R.sup.1 represents loweralkyl; R.sup.2 represents hydrogen, halo, 4,5-benzo, loweralkoxy, amino, methylamino or dimethylamino; R.sup.3 represents hydrogen or loweralkyl; and n is 1 or 2 and their pharmaceutically acceptable acid addition salts have anxiolytic activity. In particular, they have activity against anxiety induced by the withdrawal from ingested substances such as narcotics (e.g. cocaine), alcohol and n...

2-Alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl) benzamides and thiobenzamides having the formula ##STR1## wherein X is oxygen or sulphur; R.sub.1 is loweralkyl; and R.sub.2 is hydrogen, halo, 4,5-benzo, alkoxy or Am wherein Am is amino, methylamino or dimethylamino, and n is 1 or 2, and the pharmaceutically acceptable acid addition salts thereof have antischizophrenic activity.