Abstract: A method of treating animals to obtain muscle relaxation and/or to relieve anxiety is disclosed utilizing novel and known 3-aryloxy and 3-arylthioazetidinecarboxamides having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo substituted pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, aryl, allyl groups, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl and diloweralkylaminoalkyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen atom may form a heterocyclic amine radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof and pharmaceutical salts thereof and hydrates thereof when they are possible.

Abstract: A method of treating animals to obtain muscle relaxation and/or to relieve anxiety is disclosed utilizing novel and known 3-aryloxy and 3-arylthioazetidinecarboxamides having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo substituted pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, aryl, allyl groups, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl and diloweralkylaminoalkyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen atom may form a heterocyclic amine radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof and pharmaceutical salts thereof and hydrates thereof when they are possible.

Abstract: Novel compounds of the formula: ##STR1## wherein R and R.sup.1 are C.sub.1 -C.sub.6 alkyl or cycloalkyl and R.sup.2 and R.sup.3 are independently selected from C.sub.1 -C.sub.6 alkyl or aryl or --NR.sup.2 R.sup.3 forms a heterocyclic group which may be further substituted are disclosed. These compounds were found to possess muscle relaxant properties.

Abstract: A method of treating cardiac arrhythmias and muscle tension and spasticity with N-(1-methyl-3-pyrrolidinyl)-1-(phenylmethyl)-1H-benzimidazol-2-amine and analogs and the pharmaceutical compositions are herein disclosed. Illustratively, the compound having the structure: ##STR1## corrects an induced arrhythmia in 7 out of 8 dogs at 7 mg/kg IV and has an ED.sub.50 of 21 mg/kg in the mouse Straub-tail test.

Abstract: The present invention relates to novel 3-(2-chlor-4-trifluoromethylphenoxy)-1-azetidine carboxamides having the formula: ##STR1## wherein R1 and R2, same or different, are selected from hydrogen, C.sub.1 -C.sub.4 alkyl, and allyl.In a series of 3-(substitutedphenoxy)-1-azetidinecarboxamides, introduction of a chlorine atom at the 2-position of the phenoxy group of the corresponding 4-trifluoromethylphenoxy-1-azetidinecarboxamides resulted in unexpected increased potency in anticonvulsant pharmacological tests.

Abstract: A method of treating animals to obtain muscle relaxation and/or to relieve anxiety is disclosed utilizing novel and known 3-aryloxy and 3-arylthioazetidinecarbonxamides having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo substituted pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, aryl, allyl groups, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloakylloweralkyl, arylloweralkyl and diloweralkylaminoalkyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen atom may form a heterocyclic amine radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof and pharmaceutical salts thereof and hydrates thereof when they are possible.

Abstract: Novel compounds of the formula: ##STR1## Where R.sup.1 is loweralkyl and R.sup.2 and R.sup.3 are independently H, loweralkyl, aryl, or--NR.sup.2 R.sup.3 forms a heterocyclic group such as imidazole, morpholine, piperidine, or piperazine were found to exhibit cardiac arrhythmia correcting properties.

Abstract: Novel 4-aryl-N-[2-(dialkylamino and heterocyclicamino)alkyl]-1-piperazinecarboxamides of the formula: ##STR1## wherein B is oxygen or sulfur; Ar is selected from ##STR2## or 2, 3 or 4-pyridyl; X is selected from hydrogen, halogen, loweralkyl, loweralkoxy, amino, dimethylamino, nitro, trifluoromethyl, cyano, acetyl, acetylamino, aminocarbonyl, carboxy or loweralkylcarboxylic acid ester; Y is selected from hydrogen, halogen, loweralkyl, loweralkoxy, nitro, trifluoromethyl, cyano, acetylamino, aminocarbonyl, carboxy or loweralkyl carboxylic acid ester; Z is selected from hydrogen, loweralkyl or loweralkoxy; Q is selected from ##STR3## m is 1 to 3 inclusive; n is zero or 1; p is zero to 3 inclusive; R.sup.1, R.sup.2 and R.sup.3 are loweralkyl and may be the same or different, or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom may be form a heterocyclic residue; and the pharmaceutically acceptable salts thereof are disclosed.

Abstract: Novel 3-aryloxy and 3-arylthioazetidinecarboxamides having utility in a method of treating convulsions and epilepsy and compositions therefor are disclosed having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo-substituted-pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, aryl, allyl, substituted allyl, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl, diloweralkylaminoloweralkyl, and R.sup.1 and R.sup.2 when taken with the adjacent nitrogen atom may form a heterocyclic radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof, excepting that when R.sup.3 is hydrogen, Z is oxygen, B is oxygen, and Ar is phenyl or phenyl substituted by trifluoromethyl or aminocarbonyl, then R.sup.1 and R.sup.2 cannot be a combination of hydrogen and loweralkyl, and the further exception that when R.sup.

Abstract: This invention is directed to compounds having the formula: ##STR1## wherein: A represents an aromatic or heterocyclic ring having two of its carbon atoms held mutually with the oxazepine, thiazepine or diazepine moiety selected from the group consisting of benzene, naphthalene, a quinoline, a pyridine in any of its four positions, any of which rings are optionally substituted by one or two Y radicals selected from the group consisting of halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, lower acylamino, trilfuoromethyl, phenyl or phenyl substituted by one to three Y' groups selected from halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracylamino or trifluoromethyl,E is selected from oxygen, sulfur or ##STR2## B is selected from the group consisting of loweralkyl, cycloalkyl or phenyl-loweralkyl wherein phenyl is optionally substituted by one or two radicals selected from halo, loweralkyl, loweralkoxy, nitro or trifuoromethyl,N is 1 or 2,R.sup.4 and R.sup.

Abstract: Aromatic azepinones and thiones having the formula ##STR1## wherein; A is benzene, naphthalene, quinoline or pyridine;B is oxygen or sulfur; ##STR2## E is oxygen, sulfur or n is 1, 2 or 3;Z is an amino or a heterocyclic nitrogen-containing radical;R is hydrogen, loweralkyl, cycloalkyl or phenyl-loweralkyl;Y is halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracetylamino, trifluoromethyl, phenyl or phenyl substituted by one to three Y' radicals selected from halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracylamino or trifluoromethyl;and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.

Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed. The oxazepinones and oxazepinethiones prepared by the process have utility as antihistaminics with low sedative potential. Novel intermediate compounds are also disclosed.

Abstract: Aromatic tetrahydroazepinones and thoines having the formula: ##STR1## wherein Q is carbon or nitrogen;B is oxygen or sulfur;R is loweralkyl, cycloalkyl or phenylloweralkyl;Z is an amino or a heterocyclic amino containing radical; andY is halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, phenyl or trifluorophenyl;and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.

Abstract: Novel aromatic-spiropiperidineoxazepinones and thiones exhibiting antihistamine activity are disclosed having the formula: ##STR1## wherein A represents an aromatic ring, selected from benzo when Z is carbon or pyrido[3,2-f] when Z is nitrogen either of which rings may be optionally substituted on carbon;B is selected from oxygen or sulfur;R.sup.1 is selected from the group consisting of loweralkyl, cycloalkyl, cycloalkyl-loweralkyl or phenyl-loweralkyl of which phenyl may be optionally substituted;R is selected from the group consisting of loweralkyl, cycloalkyl or phenyl-loweralkyl of which phenyl may be optionally substituted and the pharmaceutically acceptable salts thereof and novel chemical intermediates in the preparation thereof.

Abstract: Chemical intermediates having the formula: ##STR1## wherein A represents an aromatic or heterocyclic ring system selected from benzene, a naphthalene, a quinoline or a pyridine in any of its four positions, any of the rings systems are optionally substituted by one or two Y radicals selected from the group consisting of halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro or trifluoromethyl;R is selected from the group consisting of loweralkyl, cycloalkyl or phenylloweralkyl wherein phenyl is optionally substituted by one or two radicals selected from halo, loweralkyl, loweralkoxy, nitro or trifluoromethyl;R.sup.4 and R.sup.5 are selected from hydrogen or loweralkyl;n is 1 or 2;X is selected from chlorine, bromine, or fluorine and E is selected from sulfur, oxygen or ##STR2## and chemical intermediates having the formula: ##STR3## wherein A, R, R.sup.4, R.sup.5, E and n are as defined above and Q is selected from the group consisting of ##STR4## wherein R.sup.

Abstract: Aromatic azepinones and thiones having the formula ##STR1## wherein; A is benzene, naphthalene, quinoline or pyridine;B is oxygen or sulfur;E is oxygen, sulfur or ##STR2## n is 1, 2 or 3; Z is an amino or a heterocyclic nitrogen-containing radical;R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl;Y is halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracetylamino, trifluoromethyl, phenyl or phenyl substituted by one to three Y' radicals selected from halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracylamino or trifluoromethyl;and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.

Abstract: Aromatic azepinones and thiones having the formula ##STR1## wherein: A is benzene, naphthalene, quinoline or pyridine;B is oxygen or sulfur;E is oxygen, sulfur or ##STR2## n is 1, 2 or 3; Z is an amino or a heterocyclic nitrogen containing radical;R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl;and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.

Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed.

Abstract: A method of counteracting the effects of histamine with aromatic azepinones and diazepinones and thiones thereof having the formula ##STR1## wherein: A is benzene, naphthalene, quinoline or pyridine;B is oxygen or sulfur:E is oxygen, sulfur or loweralkyl substituted nitrogen;n is 1, 2 or 3;Z is an amino or a heterocyclic nitrogen containing radical;R is hydrogen, loweralkyl, cycloalkyl or phenyl-loweralkyl;and compositions therefor are disclosed.

Abstract: Aromatic azepinones and thiones having the formula ##STR1## wherein; A is benzene, naphthalene, quinoline or pyridine;B is oxygen or sulfur;E is oxygen, sulfur or ##STR2## n is 1, 2 or 3; Z is an amino or a heterocyclic nitrogen containing radical;R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl;and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.