Abstract: This invention provides a group of antiarrythmic agents of the formula: ##STR1## in which R.sub.1 is --CO.sub.2 H, --CO.sub.2 (CH.sub.2).sub.n --NR.sub.4 R.sub.5, --CONR.sub.6 R.sub.7, --NHCO.sub.2 R.sub.8 or --NHCO.sub.2 (CH.sub.2).sub.o --NR.sub.9 R.sub.10 where R.sub.4 and R.sub.5 are H or alkyl of 1 to 6 carbon atoms and n is 1 to 6; R.sub.6 and R.sub.7 are H or alkyl of 1 to 6 carbon atoms; R.sub.8 is alkyl of 1 to 6 carbon atoms; and R.sub.9 and R.sub.10 are alkyl of 2 to 6 carbon atoms and o is 1 to 6;R.sub.2 and R.sub.3 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; andm is one of the integers 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof, and a method for their use.

Abstract: The compounds: ##STR1## in which R.sup.1 is hydrogen, halogen, hydroxy, or alkyl;R.sup.2 is substituted or unsubstituted pyridinyl, pyrazinyl, quinolinyl or quinoxalinyl and said substituents are alkyl, alkoxy, alkoxycarbonyl, halogen, cyano or nitro; andn is 2, 3, 4, 5 or 6;or a pharmaceutically acceptable salt thereof, are antipsychotic and anxiolytic agents.

Abstract: 2-(2,3-Dihydro-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole, or a pharmaceutically acceptable salt thereof, is useful in the treatment of hyperprolactinemic states in warm-blooded animals.

Abstract: Novel benzoxazocines of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1 represents hydrogen, or one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro, amino acylamino, mono- or di- (lower)alkyl-amino or cyano substituents, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each represent hydrogen or lower alkyl or R.sup.3 and R.sup.4 together represent --(CH.sub.2).sub.3 --or --(CH.sub.2).sub.4 --, R.sup.5 represents hydrogen, lower alkyl, phenyl(lower)alkyl or cycloalkyl(lower)alkyl, and Ar is a phenyl radical optionally substituted by one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro or amino groups exhibit activity on the central nervous system, particularly as antidepressants. The compounds can be prepared from novel alcohols of formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Ar are as defined above and X is fluorine, chlorine or bromine.

Abstract: Pharmaceutical compositions produced with liquid, hydrophilic lubricants possessing markedly improved dissolution rates.

Abstract: 4-(2,3-dichloro-6-fluorophenyl)-1,4,5,6,7,8-hexahydro-2-methyl-5-oxo-1,7-na phthyridine-3-carboxylic acid 2-(2,3-dichlorophenoxy)ethyl ester and pharmaceutically acceptable salts thereof are useful antihypertensive agents.

Abstract: Compounds of the formula: ##STR1## in which Z is ##STR2## where R is hydrogen, alkyl, polyfluorinated alkyl, --CN, cyanoalkyl, cycloalkyl or cycloalkylalkyl;R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7, independently, are hydrogen, alkoxy, trifluoromethyl or halo;R.sup.8 is hydrogen or alkyl;or a pharmaceutically acceptable salt thereof, are useful as anti-arrhythmic agents.

Abstract: This application discloses certain substituted phenylacetonitriles of the formula: ##STR1## in which the dotted line represents optional unsaturation, and R.sub.4 is hydrogen or alkyl;R.sub.5 and R.sub.6, one of which may be hydrogen, are ortho or para substituents, independently selected from the group consisting of hydroxyl, alkyl, alkoxy, aralkoxy, alkanoyloxy, alkylmercapto, halo or trifluoromethyl;R.sub.7 is hydrogen or alkyl; andn is one of the integers 0, 1, 2, 3 or 4;which are useful in the production of antidepressant agents.

Abstract: The invention provides novel silyl reagents of Formula IR.sup.b R.sup.c R.sup.d SiNCYwherein R.sup.b is a branched chain alkyl of 3-10 carbon atoms, cycloalkyl of 4-8 carbon atoms or branched chain aralkyl of 8-12 carbon atoms and R.sup.c and R.sup.d are selected from alkyl of 1-10 carbon atoms, cycloalkyl of 4-8 carbon atoms, aralkyl of 7-12 carbon atoms or aryl with the proviso that R.sup.c and R.sup.d are not the same group as R.sup.b, and Y is oxygen or sulphur. A further novel compound tri-isopropylsilyl isothiocyanate is also included. These silyl reagents are useful in preparing tetrahydroquinoline 8-nitriles, amides and thioamides as described in Ser. No. 506,279.

Abstract: This invention provides a group of hydroxycycloalkanephenoxyethylamine antidepressant derivatives of the following structural formula: ##STR1## in which R.sub.1 is hydrogen or alkyl of 1 to 6 carbon atoms;R.sub.2 is alkyl of 1 to 6 carbon atoms;R.sub.3 and R.sub.4 are independently hydrogen, hydroxyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, alkanoyloxy of 2 to 7 carbon atoms, halo or trifluoromethyl;R.sub.5 is hydrogen, alkyl of 1 to 6 carbon atoms or alkanoyl of 2 to 7 carbon atoms;and n is one of the integers 0, 1, 2 or 3;or a pharmaceutically acceptable salt thereof.

Abstract: Ready-to-use parenteral formulations of Dezocine containing from about 0.2 to about 2.0 percent wt/vol. Dezocine; about 30 to about 45 percent wt/vol. propylene glycol; about 0.5 to about 2.0 percent wt/vol. lactic acid buffered with a pharmaceutically acceptable base to a pH of from about 3.5 to about 5.0 and 0 to 0.02 percent wt/vol. sodium metabisulfite, in water for injection.

Abstract: 1,4,5,6,7,8-Hexahydro-2-alkyl-4-aryl-5-oxo-1,7-naphthyridine-3-carboxylic acid aromatic esters and pharmaceutically acceptable acid addition salts thereof are useful antihypertensive agents.

Abstract: The invention concerns novel compounds of formula IIIAR.sub.x.sup.a Si(NCS).sub.4-x IIIAwherein R.sup.a is selected from electron donating substituents consisting of alkoxy of 1-10 carbon atoms, cycloalkoxy of 4-8 carbon atoms, aralkoxy of 7-12 carbon atoms, phenoxy which may be substituted by alkyl of 1-10 carbon atoms, alkoxy of 1-10 carbon atoms or trifluoromethyl, the group R.sup.b R.sup.c N-wherein R.sup.b and R.sup.c are selected from alkyl of 1-6 carbon atoms, cycloalkyl of 4-6 carbon atoms, phenyl which may be substituted by alkyl of 1-10 carbon atoms, alkoxy of 1-10 carbon atoms or trifluoromethyl, and aralkyl of 7-12 carbon atoms or R.sup.b and R.sup.

Abstract: An anti-arrhythmic agent which is N-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-N-(1-methylethyl)- 2,3,4-trimethoxy-benzenesulfonamide or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to the preparation of 1-bromo-2-D-alkylpropanoyl-L-proline derivatives and analogous compounds which are useful as chemical intermediates to angiotensin converting enzyme (ACE) inhibitors and to the stereospecific synthesis of such ACE inhibitors having the formula: ##STR1## wherein R.sup.1 is lower alkyl and R.sup.4 and R.sup.5 are both hydrogen or together with the carbons to which they are attached represent a benzene ring optionally substituted by defined substituents. Intermediates of formula ##STR2## are also disclosed wherein R.sup.1, R.sup.4, R.sup.5 are as defined above and B.sup.+ is a cation.

Abstract: The invention provides new silyl derivatives of 5,6,7,8-tetrahydroquinolines and related compounds. The tetrahydroquinolines are substiuted at the 8-position by the group SiR.sub.3 where R may be one of various hydrocarbon groups or an electron donating substituent. The 8-position may also carry a lithium, sodium or potassium atom. The new silyl derivatives may be prepared by treating a corresponding 8-lithio, sodio or potassio tetrahydroquinoline with a silyl halide R.sub.3 SiHal followed by a metal compound R*M where M is sodium, potassium or lithium and R* is alkyl, cycloalkyl, aralkyl or aryl or an amine residue. The new silyl derivatives are useful intermediates for the preparation of known 5,6,7,8-tetrahydroquinline-8-nitriles, amides and thioamides employing an alkyl silyl isothiocyanate or cyanate. The nitriles and thioamides are anti-ulcer agents. The related compounds may be made by analogous methods.

Abstract: Improved parenteral formulations of 1-cis-2(.alpha.-dimethylamino-m-hydroxybenzyl)cyclohexanol containing from about 20 to about 40 percent propylene glycol (USP).

Abstract: 7-(Substituted)-1,4,5,6,7,8-hexahydro-2-alkyl-4-aryl-5-oxo-1,7-naphthyridin e-3-carboxylic acid esters and pharmaceutically acceptable acid addition salts thereof are useful antihypertensive agents.

Abstract: This invention provides a group of antiarrhythmic agents of the formula: ##STR1## in which R.sub.1 is --CO.sub.2 H, --CO.sub.2 (CH.sub.2).sub.n --NR.sub.4 R.sub.5, --CONR.sub.6 R.sub.7, --NHCO.sub.2 R.sub.8 or --NHCO.sub.2 (CH.sub.2).sub.o --NR.sub.9 R.sub.10 where R.sub.4 and R.sub.5 are H or alkyl of 1 to 6 carbon atoms and n is 1 to 6; R.sub.6 and R.sub.7 are H or alkyl of 1 to 6 carbon atoms; R.sub.8 is alkyl of 1 to 6 carbon atoms; and R.sub.9 and R.sub.10 are alkyl of 2 to 6 carbon atoms and o is 1 to 6;R.sub.2 and R.sub.3 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; andm is one of the integers 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof, and a method for their use.

Abstract: 1,4,5,6,7,8-Hexahydro-4-heterocyclyl-5-oxo-quinoline derivatives and corresponding acridine derivatives and pharmaceutically acceptable salts thereof are useful antihypertensive agents.