Abstract: Novel 1-aryloxy-4-amino-2-butanols of the formulaArO--CH.sub.2 --CHOH--CH.sub.2 --CH.sub.2 --NR.sup.1 R.sup.2wherein Ar is 1-naphthyl, 2-naphthyl, indene-4(or 5-)yl, 3-(or 5-)chloro-2-pyridyl, phenyl, monosubstituted phenyl or di-substituted phenyl, R.sup.1 is lower alkyl, phenyl, phenylalkyl, 2-hydroxymethyl-2-propyl, adamantyl or lower-cycloalkyl, R.sup.2 is hydrogen or lower alkyl, wherein R.sup.1 and R.sup.2 together with the adjacent nitrogen from a heterocyclic residue and the pharmaceutically acceptable acid addition salts thereof having local anesthetic, beta-adrenergic blocking, antihypertensive and antiarrhythmic properties are disclosed. The compounds are prepared by reacting novel 1-aryloxy-4-chloro-2-butanols with amines. Methods for the preparation of the novel 1-aryloxy-4-chloro-2-butanol intermediates are also disclosed.

Abstract: Co-extruded insecticidal pet collars contain one or more active insecticidal components in a desired relationship to the skin of the animal. The outside layer (away from the skin) contains carbamate, organo-phosphate chlorinated hydrocarbon or other insecticide that is irritating to the skin, or a cholinesterase inhibitor. The inside layer acts as a barrier to the insecticide. The layers of a multi-layered collar which is prepared by extrusion may also contain different insecticidal systems. A co-extruded collar is prepared by preparing two blends which have varying concentrations of active and/or inert ingredients, depending on the end product which is desired. Each of the blends is fed into an extruder wherein the polyvinyl chloride is fused. The melt blend from extruder B is then transferred to the die of extruder A where it becomes an integral part of the extruded strip from extruder A.

Abstract: Substituted dialkanolamines, oxazine and sulfur analogs thereof, useful in treating shipping fever syndrome in mammals are disclosed having the formula: ##STR1## wherein: Ar is ##STR2## Z is oxygen or sulfur; R is selected from hydrogen, loweralkyl or ##STR3## R.sup.1 R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are selected from hydrogen or loweralkyl; and ##STR4## when taken together may form a lowercycloalkyl ring or R.sup.5 with --ZR.sup.2 when taken together may form a 5-membered saturated oxygen or sulfur containing heterocyclic ring;X is selected from hydrogen, halo, loweralkoxy, loweralkyl, trifluoromethyl or dimethylamino and when X is more than 1, it may be the same radical or different;y is 0, 1 or 2;n is one, or zero and when n is 1, the stereoisomers thereof and when n is zero the dotted line becomes an oxygen-carbon bond forming an oxazine ring and the pharmaceutically acceptable acid addition salts thereof.

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: 2-Amino-3-aroyl-.gamma.-oxobenzenebutanoic acids and derivatives having the formula: ##STR1## wherein X is hydrogen, halogen, or loweralkyl; Y is hydrogen, halogen, loweralkyl, loweralkoxy, nitro, or trifluoromethyl; n is 1 or 2; and R is hydrogen, loweralkyl, or a pharmaceutically acceptable cation, are disclosed having anti-inflammatory activity.

Abstract: A process is described wherein pyrido[1,4]benzodiazepines having the formula: ##STR1## wherein Q is NR.sup.1 R.sup.2 or ##STR2## are prepared from unsubstituted pyridobenzodiazepinones by alkylation reaction with halo-alkyl-Q followed by acylation of the other nitrogen; breaking the ring with an aryl Grignard reagent and recyclizing to add the aryl radical and form the azepine ring. Novel intermediates are thereby 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: 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: N-(Arylthioalkyl)-N'-(aminoalkyl)ureas and thioureas and oxidation derivatives having the formula ##STR1## wherein B is thio, sulfinyl or sulfonyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, cycloalkyl, 2-furanyl, phenyl, substituted phenyl or phenyl-loweralkyl and R.sup.3 and R.sup.4 are hydrogen, loweralkyl, phenyl or phenyl-loweralkyl wherein phenyl is optionally substituted, or R.sup.3 and R.sup.4 taken with the adjacent nitrogen form a heterocyclic residue. The compounds are useful in the treatment of cardiac arrhythmia.

Abstract: A method of controlling emesis caused by anticancer drugs with 2-alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl) benzamide-N-oxides having the formula: ##STR1## wherein R.sub.1 is loweralkyl, and R.sub.2 is selected from the group consisting of hydrogen, halo, 4,5-benzo, methylsulfonyl, loweralkoxy or Am and n is 1 or 2, and the pharmaceutically acceptable acid addition salts thereof is disclosed.

Abstract: A method of treating depression with 5-(aminoalkyl)-11-phenyl-5H-dibenzo[b,e][1,4]diazepines having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are selected from hydrogen or methyl and X is selected from hydrogen, chlorine, bromine or fluorine is disclosed.

Abstract: A method is disclosed for treating pain and/or inflammation by transdermal administration of 2-amino-3-benzoylbenzeneacetic acids, salts and esters having the formula ##STR1## wherein R.sup.1 is hydrogen, loweralkyl or a pharmaceutically acceptable cation; R.sup.2 is hydrogen, halogen, loweralkyl or loweralkoxy; R.sup.3, R.sup.4 and R.sup.5 are hydrogen or loweralkyl; X is hydrogen, halogen, loweralkyl, hydroxy, loweralkoxy, nitro, trifluoromethyl or loweralkylthio; Y is hydrogen, loweralkyl, loweralkoxy, nitro or trifluoromethyl and hydrates and alcoholates thereof.

Abstract: This invention relates to novel compounds having the formula: ##STR1## wherein; R.sup.1 is fluoro, chloro, bromo, lower-alkyl or nitro,R.sup.2 is lower alkyl, lower alkoxy, fluoro, chloro, bromo, nitro or trifluoromethyl, andm and n are 0-2 with the proviso that when R.sup.1 or R.sup.2 are tertiary butyl or a sterically hindering lower alkyl radical, m and/or n are 1. These compounds are intermediates in the preparation of 2-aminobiphenylacetic acids, esters and metal salts thereof.

Abstract: Pyrido[1,4]benzodiazepines having antidepressant activity of the formula ##STR1## wherein Ar is 2, 3 and 4-pyridinyl, 2 or 3-thienyl, phenyl or a substituted phenyl; R is hydrogen, loweralkyl or an amine on the end of a hydrocarbon chain; Z is hydrogen, halogen, trifluoromethyl, loweralkyl, lower-alkoxy, hydroxy or nitro; and Y is hydrogen, loweralkyl, loweralkoxy or hydroxy; and the pharmaceutical salts are prepared from [2-[(aminopyridinyl)amino]phenyl]arylmethanones which also have antidepressant activity.

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: Novel pyrrolidine, piperidine and homopiperidinecarboxamide and thiocarboxamide compounds having the formula: ##STR1## wherein X is --S--, --S(O)-- or --S(O).sub.2 --; A is a loweralkalene chain and A.sup.1 and A.sup.2 are alkalene chains when p and d are one; R, R.sup.1 and R.sup.2 are hydrogen, loweralkyl, phenyl cycloalkyl or phenylalkyl and R.sup.1 and R.sup.2 may form a heterocyclic residue with the adjacent nitrogen atom; Q is a selected aromatic radical, and the pharmaceutically acceptable acid addition salts useful as cardiac antiarrhythmia agents are disclosed.Novel chemical intermediates, unsubstituted on pyrrolidine, piperidine and homopiperidine nitrogen but with --(A.sup.2).sub.p --X--(A.sup.2).sub.d --Q side chain are also disclosed.

Abstract: Intermediates for preparing pyrido [1,4] benzodiazepines having antidepressant activity are disclosed of the formula ##STR1## wherein, R is hydrogen, loweralkyl, --alk.sup.1 --NR.sup.1 R.sup.2, --alk.sup.1 --N.dbd.CH--OC.sub.2 H.sub.5 or ##STR2## R.sup.1 and R.sup.2 are loweralkyl, --C(O)--O--loweralkyl or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom may form a 1-piperidinyl, 1-phthalimido, 1-pyrrolidinyl, 4-morpholino, 1-piperazinyl or 4-substituted-1-piperazinyl;Ar is 2, 3 or 4-pyridinyl, 2 or 3-thienyl, phenyl or phenyl substituted by 1 to 3 radicals selected from halo, loweralkyl, loweralkoxy, trifluoromethyl or nitro and may be the same or different;alk.sup.1 is a straight or branched hydrocarbon chain containing 1-8 carbon atoms;Z is hydrogen, halogen, loweralkyl, loweralkoxy, hydroxy or nitro;Y is hydrogen or 1-2 radicals selected from loweralkyl, loweralkoxy or hydroxy and may be the same or different,and the acid addition salts thereof.

Abstract: A pharmaceutical method for improving memory or correcting memory deficiency is disclosed, utilizing compounds having the formula: ##STR1## wherein m and n are zero and one and when m is zero, the dotted line represents a double bond; X is oxygen or sulfur; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, phenyl or phenylloweralkyl, or R.sup.1 and R.sup.2 taken together may form a fused second ring with the nitrogen atoms having three or four methylene groups to which may be attached at any second ring carbon atom thereof, a loweralkyl or phenyl radical; R.sup.3 is hydrogen or loweralkyl; Ar is phenyl, pyridyl, furanyl, thienyl, methoxy-1H-benzotriazolyl, indolinyl, methoxyindolinyl, methoxypyrimidinyl, aminomethoxypyrimidinyl, 1,3-benzodioxolyl or naphthalenyl, the active optical isomers; and the pharmaceutically acceptable acid addition salts thereof.

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: N-(arylthioalkyl)-N'-(aminoalkyl)ureas and thioureas and oxidation derivatives having the formula ##STR1## wherein B is thio, sulfinyl or sulfonyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, cycloalkyl, 2-furanyl, phenyl, substituted phenyl or phenyl-loweralkyl and R.sup.3 and R.sup.4 are hydrogen, loweralkyl, phenyl or phenyl-loweralkyl wherein phenyl is optionally substituted, or R.sup.3 and R.sup.4 taken with the adjacent nitrogen form a heterocyclic residue.