Abstract: This invention relates to novel amide derivatives of certain 2,6-methano-2H-quinolizine-type compounds, to the intermediates and processes for their preparation, to their ability to antagonize the effects of serotonin at the 5HT.sub.3 receptors, and to their end-use application in the treatment of chemotherapeutically-induced nausea and vomiting, as anti-anxiety agents, in the symptomatic treatment of pain associated with migraine, as anti-arrhythmic agents, in the treatment of cognitive disorders, in treating hallucinatory endogenous psychoses of the type manifested in patients suffering from schizophrenia, and mania, in the treatment of glaucoma, for stimulating gastric motility, to combat drug abuse, to treat sleep apnea and to treat irritable bowel syndrome.

Abstract: This invention relates to the manufacture of certain esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one and hexahydro-8-hydroxy-2,6-methano-2H-quinolizines and their use as medicaments in the treatment of cognitive disorders.

Abstract: This invention relates to 5-chloro-2,3-dihydro-2,2-dimethylbenzofuran-7-carboxylic acid-octahydro-3-hydroxy-2,6-methano-2H-quinolizin-8-yl ester (I), a novel 5-HT.sub.3 -receptor antagonist, its method of preparation, and to its end-use application in the treatment or radio- and chemo-therapeutically-induced nausea and vomiting, in the treatment or pain associated with migraine, in the treatment of cognitive disorders, in treating hallucinatory endogenous psychoses or the type manifested in patients suffering from schizophrenia and mania, for irritable bowel syndrome, and to combat drug abuse.

Abstract: The present invention is directed to the use of esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one and hexahydro-8-hydroxy-2,6-methano-2H-quinolizines in the manufacture of a medicament for the treatment of anxiety, psychosis, glaucoma and for the stimulation of gastric motility.

Abstract: Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I ##STR1## wherein: R.sub.1 represents methoxy, ethoxy or hydroxy,R.sub.2 represents methoxy, ethoxy, hydroxy or hydrogen;each R.sub.3 independently represents methyl or ethyl;R.sub.4 represents hydrogen or methyl;R.sub.5 represents hydrogen or methyl; andn represents 2 or 3, and a pharmacologically acceptable acid addition salt thereof (a) have anxiolytic activity, (b) antagonize the anxiogenic activity of benzodiazepine inverse agonists, (c) reduce chronic abnormally high brain levels of serotonin or its metabolite 5-hydroxy-indoleacetic acid and (d) have antibacterial and antiviral activity. These activities are believed to be related to a reduction in serotonin turnover caused by blocking the depolarisation activation of tryptophan hydroxylase. Novel compositions comprise the compounds with a benzodiazepine agonist or benzodiazepine inverse agonist.

Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.

Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.

Abstract: Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I ##STR1## wherein: R.sub.1 represents methoxy, ethoxy or hydroxy,R.sub.2 represents methoxy, ethoxy, hydroxy or hydrogen;each R.sub.3 independently represents methyl or ethyl;R.sub.4 represents hydrogen or methyl;R.sub.5 represents hydrogen or methyl; andn represents 2 or 3,and a pharmacologically acceptable acid addition salt thereof (a) have anxiolytic activity, (b) antagonize the anxiogenic activity of benzodiazepine inverse agonists, (c) reduce chronic abnormally high brain levels of serotonin or its metabolite 5-hydroxy-indoleacetic acid and (d) have antibacterial and antiviral activity. These activities are believed to be related to a reduction in serotonin turnover caused by blocking the depolarization activation of tryptophan hydroxylase. Novel compositions comprise the compounds with a benzodiazepine agonist or benzodiazepine inverse agonist.

Abstract: The present invention is directed to a group of esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(3H)-ones and related compounds. The compounds are prepared from the appropriate carboxylic acids and alcohols by standard procedures or, where steric factors are significant, a new process which makes use of heavy metal salts of super acids can be used. The compounds involved are useful in the treatment of migraine and similar disorders and in cytotoxic drug-induced vomiting.

Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.

Abstract: Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I ##STR1## wherein: R.sub.1 represents methoxy, ethoxy or hydroxy,R.sub.2 represents methoxy, ethoxy, hydroxy or hydrogen;each R.sub.3 independently represents methyl or ethyl;R.sub.4 represents hydrogen or methyl;R.sub.5 represents hydrogen or methyl; andn represents 2 or 3,and a pharmacologically acceptable acid addition salt thereof (a) have anxiolytic activity, (b) antagonize the anxiogenic activity of benzodiazepine inverse agonists, (c) reduce chronic abnormally high brain levels of serotonin or its metabolite 5-hydroxy-indoleacetic acid and (d) have antibacterial and antiviral activity. These activities are believed to be related to a reduction in serotonin turnover caused by blocking the depolarization activation of tryptophan hydroxylase. Novel compositions comprise the compounds with a benzodiazepine agonist or benzodiazepine inverse agonist.

Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.

Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.

Abstract: Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I ##STR1## wherein: R.sub.1 represents methoxy, ethoxy or hydroxy,R.sub.2 represents methoxy, ethoxy, hydroxy or hydrogen;each R.sub.3 independently represents methyl or ethyl;R.sub.4 represents hydrogen or methyl;R.sub.5 represents hydrogen or methyl; andn represents 2 or 3,and a pharmacologically acceptable acid addition salt thereof (a) have anxiolytic activity, (b) antagonize the anxiogenic activity of benzodiazepine inverse agonists, (c) reduce chronic abnormally high brain levels of serotonin or its metabolite 5-hydroxy-indoleacetic acid and (d) have antibacterial and antiviral activity. These activities are believed to be related to a reduction in serotonin turnover caused by blocking the depolarization activation of tryptophan hydroxylase. Novel compositions comprise the compounds with a benzodiazepine agonist or benzodiazepine inverse agonist.

Abstract: This invention relates to aromatic .omega.-alkylimino-tetrahydro-6H-1,3-thiazine-6-one derivatives, to a process for the preparation of same, and to their use as anxiolytic and antihypertensive agents.

Abstract: This invention relates to 4-(2-pyrimidinyl)-1-piperazinyl heterocyclic carbonyl derivatives, to a process for their preparation, and to their use as anxiolytic agents.

Abstract: Glutarimide derivatives of the formula which are useful antihypertensive and antianxiety agents ##STR1## wherein R.sub.1 and R.sub.2 each independently represent hydrogen, a 1 to 4 carbon alkyl, a 1 to 4 carbon alkoxy, halogen, nitro, hydroxy, SO.sub.3 H, SO.sub.2 NH.sub.2, and when R.sub.1 and R.sub.2 are taken together, form a fused phenyl group at the 1,2- or 3,4- positions, with the proviso that when R.sub.1 and R.sub.2 are identical they each represent a hydrogen, a 1 to 4 carbon alkyl, a 1 to 4 carbon alkoxy, hydroxy or a halogen group; A and B independently represent an oxo, a thio or an imino group having the formula --N(R.sub.6)-- wherein the R.sub.6 group is hydrogen or a 1 to 4 carbon alkyl group; R.sub.3 is a hydrogen, a 1 to 4 carbon alkyl or hydroxyethyl group; n is an integer of from 2 to 5; and R.sub.4 and R.sub.5 represent methyl groups or when taken together form a cyclopentane or cyclohexane ring; its enantiomers; and the pharmaceutically acceptable acid addition salts thereof.

Abstract: Migraine is treated with a tropyl benzoate derivative of the following general formula: ##STR1## wherein: R.sub.1 represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen;R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen; andR.sub.3 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen, provided that R.sub.3 is hydrogen when R.sub.2 is hydrogen, or a pharmaceutically acceptable salt thereof.Additionally, some novel tropyl benzoate derivatives are disclosed.

Abstract: Migraine is treated with a tropyl benzoate derivative of the following general formula: ##STR1## wherein: R.sub.1 represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen;R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen; andR.sub.3 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen, provided that R.sub.3 is hydrogen when R.sub.2 is hydrogen, or a pharmaceutically acceptable salt thereof.Additionally, some novel tropyl benzoate derivatives are disclosed.

Abstract: Novel 1,4-dihydropyridine derivatives have the following general Formula: ##STR1## and are calcium antagonists, useful for treating cardiovascular diseases.