Abstract: 1-Aryloxy-3-[(3-indolyl)-tert.-butyl]amino-2-propanols having a heterocyclic aryl-attached substituent or aryl-fused heterocyclic ring are antihypertensive agents having vasodilator and adrenergic .beta.-receptor blocking action.

Abstract: Novel phthalimide intermediates are reduced to 5-sulfamoyl-6-halo-3-oxoisoindole compounds bearing a substituted 1-phenylalkyl-4-piperidinyl moiety as the isoindole N-substituent. Preferred compounds such as 6-chloro-2,3-dihydro-3-oxo-2-[1-(phenylmethyl)-4-piperidinyl]-1H-isoindole -5-sulfonamide exhibit diuretic and antihypertensive properties.

Abstract: 6-(1H-Tetrazol-5-yl)thiazolo[3,2-a]pyrimidin-5-ones, 3-(1H-tetrazol-5-yl)-4H-pyrimido[2,1-b]benzothiazol-4-ones, and the corresponding imidazo- and triazolo- pyrimidines, thiones, and imines are useful as antiallergy and antiasthmatic compounds by virtue of their inhibitory action on the immediate hypersensitivity reaction in mammals and relaxant action on the tracheal muscle. Intermediates in the synthesis of these substances from 2-aminoazoles and ethoxymethylene malononitrile also have smooth muscle relaxant and immediate hypersensitivity reaction inhibitory activity.

Abstract: Imidazopyrimidinones and other diazaheterocyclopyrimidinones having an additional fused imidazole or triazole ring have utility as bronchodilators, mediator release inhibitors, phosphodiesterase inhibitors, and peripheral vasodilators. They are orally active and useful in the prophylaxis and treatment of asthma. A preferred compound is 4-[(4-chlorophenyl)methyl]-6,7-dihydro-3H-imidazo[1,2-a]purin-9(4H)-one.

Abstract: Phenoxyalkyl substituted-1,2,4-triazolones having anti-depressant properties typified by 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-4-(2-phenoxyethyl)- 2H-1,2,4-triazol-3(4H)-one are disclosed.

Abstract: 2-[4-[4-Arylpiperazin-1-yl]butyl]-1,2,4-triazolo[4,3-a]pyridin-3(2H)-ones are anti-psychotic agents.

Abstract: Non-disintegrating theophylline tablets having a pair of opposing substantially planar surfaces and a very thin cross-section have a high bioavailability on ingestion and a relatively steady release rate permitting a 12 hr. dosing interval for maintenance of non-toxic therapeutic blood theophylline concentrations. Excipients or tableting aids are not required, but trace amounts of a tableting lubricant are preferably included to facilitate continuous large scale production.

Abstract: A process for resolving a racemic modification of .beta.-adrenergic aryl- or hetaryl-oxypropanolamines such as (.+-.)-2-[2-hydroxy-3-[[2-(1H-indol-3-yl)-1,1-dimethylethyl]amino]propoxy] benzonitrile into its individual enantiomers is described. The process comprises converting the racemic modification into a pair of diastereomeric urea derivatives by reaction with a chiral aralkylisocyanate; separation into the individual diastereomers; and facile regeneration of the starting amine by cleavage of the intermediate urea compound using hydrazine. This final step is improved by the addition of an .alpha.-keto carboxylic acid, such as pyruvic acid, which functions as a scavenger of nucleophilic by-products.

Abstract: Piperazinyl derivatives containing a spiro-2,4-thiazolidinedione heterocyclic component with relatively selective psychotropic properties are disclosed. The compound 2-[4-[4-(7,9-dioxo-6-thia-8-azaspiro[4.4]nonan-8-yl)butyl]-1-piperazinyl]p yridine-3-carbonitrile which has selective anti-psychotic activity constitutes a typical embodiment of the invention.

Abstract: An improved process for the preparation of 4-methoxy-2'-{2-(1-methyl-2-piperidyl)ethyl}benzanilide has been developed. The process comprises essentially three steps starting with methyl anthranilate and 2-picoline and features a novel low-pressure hydrogenation sequence.

Abstract: Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is benzisothiazol-3-yl or benzisoxazol-3-yl and the other is alkylene attached to heterocycles such as azaspiro[4.5]decanedione, dialkylglutarimide, thiazolidinedione and spirocyclopentylthiazolidinedione or butyrophenone-like groups. The compounds have psychotropic properties and 8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5]deca ne-7,9-dione is a typical embodiment having selective antipsychotic activity.

Abstract: Buspirone and its pharmaceutically acceptable salts are useful in alleviation of extrapyramidal motor disorders which can take the form of clinical syndromes such as Parkinsonism and neuroleptic-induced extrapyramidal symptoms (EPS).

Abstract: Loss of potency of estradiol cream compositions found to be due to unexpected oxidation of estradiol. Improved cream composition comprises 1% or less 17.beta.-estradiol in the presence of stabilizing members selected from phenolic-type antioxidants, metal chelating agents, and suspending agents.

Abstract: 1-[4-(4,4-Dialkyl-2,6-piperidinedion-1-yl)butyl]piperazines with 2-pyrimidyl substituents in the 4- position have been synthesized and demonstrate useful anxiolytic properties. The compound 4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedi one, which has selective anxiolytic activity, constitutes the preferred embodiment of the invention.

Abstract: This invention concerns an isethionic acid addition salt of the non-adrenergic bronchodilating agent 9-cyclohexyl-2-propoxy-9H-purine-6-amine. The salt is comprised of a 2:1 molecular ratio of the isethionic acid to the adenine base. The salt of the invention is characterized in having improved water solubility and stability.

Abstract: Novel spiro-quaternary ammonium halides are disclosed. The new compounds are particularly valuable as intermediates in preparation of N-(2-pyrimidinyl)piperazinylalkyl derivatives of azaspiroalkanediones such as the psychopharmacologic agent 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dio ne.

Abstract: A series of 1,4-dihydropyrid-5-yl cyclic imidate esters have been prepared possessing the general formula ##STR1## wherein R and R.sup.1 are independently selected from hydrogen, lower alkyl or alkoxyalkyl groups; R.sup.2 is lower alkyl, aryl, or hetaryl; R.sup.3 is cycloalkyl, aryl or hetaryl, generally with electron-withdrawing substituents; R.sup.4 is lower alkyl, alkoxyalkyl, aminoalkyl, haloalkyl, or dialkylaminoalkyl; R.sup.5 is lower alkyl or aryl; m is 0 or 1; and n is 0, 1, or 2. Compounds of this series demonstrate blockage of calcium ion flux in tissue preparations in vitro and vasodilation in animal testing in vivo.

Abstract: Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is benzisothiazol-3-yl or benzisoxazol-3-yl and the other is alkylene attached to heterocycles such as azaspiro[4.5]decanedione, dialkylglutarimide, thiazolidinedione and spirocyclopentylthiazolidinedione or butyrophenone-like groups. The compounds have psychotropic properties and 8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspior[4.5]deca ne-7,9-dione is a typical embodiment having selective antipsychotic activity.

Abstract: Imidazopyrimidinones and other diazaheterocyclopyrimidinones having an additional fused imidazole or triazole ring have utility as bronchodilators, mediator release inhibitors, phosphodiesterase inhibitors, and peripheral vasodilators. They are orally active and useful in the prophylaxis and treatment of asthma. A preferred compound is 4-[(4-chlorophenyl)methyl]-6,7-dihydro-3H-imidazo[1,2-a]-purin-9(4H)-one.