Abstract: The compounds of the described invention are potent ACAT inhibitors and are useful in pharmaceutical compositions for the treatment of atherosclerosis and have the formulas: ##STR1## when Q is a double bond wherein: R.sup.1 and R.sup.2 are each H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.4 -C.sub.10 -C.sub.10 cyloalkylalkyl, C.sub.7 -C.sub.14 aralkyl, 2-,3- or 4-pyridinyl, 2-thienyl, 2-furanyl, phenyl optionally substituted by F, Cl, Br, OH, CN, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.8 alkyl, CH.sub.3 S(O).sub.r, NO.sub.2, CF.sub.3 NR.sup.7 R.sup.8 or NR.sup.7 C(O)R.sup.8 ;R.sup.3 is N.C.sub.1 -C.sub.6 alkyl, allyl or benzyl or phenyl both optionally substituted F, Cl, CH.sub.3, CH.sub.3), or CF.sub.3 ; C.sub.1 -C.sub.4 carboalkyl;R.sup.4 is H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.1 -C.sub.3 perfluoroalkyl or, benzyl or phenyl both optionally substituted by C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.4 -alkoxy, F, Br, Cl, NH.sub.

Abstract: There are provided, novel no or low wax formulations for amantadine hydrochloride and methods for preparing such formulations.

Abstract: This invention relates to imidazoles as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT), processes for their preparation, and their use as antihypercholesterolemic agents or antiatherosclerotic.The compounds for use in the described method are compounds of Formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are selected independently from H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.7 -C.sub.14 araalkyl, phenyl optionally substituted with 1 to 3 groups selected from F, Cl, Br, OH, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, CH.sub.3 S(O).sub.r, NO.sub.2, CF.sub.3, or NR.sup.7 R.sup.8 ; R.sup.3 is H, C.sub.1 -C.sub.6 alkyl, allyl, benzyl, or phenyl optionally substituted with F, Cl, CH.sub.3, CH.sub.3 O, or CF.sub.3 ; R.sup.4 is straight chain C.sub.1 -C.sub.8 alkyl optionally substituted with F; C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.

Abstract: A process for the preparation of 1,5-(alkylimino)-1,5-dideoxy-D-glucitol and derivatives of the formula: ##STR1## wherein R is hydrogen, alkyl of 1 to 13 carbon atoms, and aralkyl wherein alkyl is a lower alkyl of 2 to 6 carbon atoms, and aryl is phenyl, unsubstituted or substituted with lower alkyl of 1 to 6 carbon atoms, halo, lower alkoxy of 1 to 4 carbon atoms or thio lower alkyl of 1 to 4 carbon atoms by the steps of: treating L-sorbose with 2,2-dimethoxypropane to yield 1,2:4,6-di-O-(1-methylethylidene)-.alpha.-L-sorbanose; treating the compound with sulfuric acid in a solvent to produce 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; consecutively treating with sulfonyl chloride and with an amine to yield 6-(substituted amino)-6-deoxy-1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; adsorbing the compound on an ion exchange resin and hydrogenating to produce compounds of the above formula.

Abstract: This invention is a process for purifying nucleoside-5'-diphosphates containing substituents other than primary amines (hereinafter designated as NDPs) from complex mixtures by contacting the aqueous solution mixture with a strongly basic ion exchange resin in the chloride form, eluting certain absorbed impurities with an alkali metal salt solution, converting the column to the hydroxide form by contacting the resin with an alkali metal hydroxide solution such that the effluent becomes basic, and eluting absorbed NDP with a weakly acidic alkali metal salt solution such that solutions of highly pure NDP are obtained in basic effluent fractions. The new process is particularly valuable for purification of NDPs directly from chemical synthesis reaction media.

Abstract: A process for the production of .sup.32 P-labeled nucleotides in accordance with an enzymatic pathway utilizing phosphotransacetylase and acetate kinase.

Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.

Abstract: Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-oxa or thio-lH-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetamide, possess useful antibacterial activity.

Abstract: Aminomethyl oxooxazolidinyl aza cycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-3-aza-1H-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetam ide, possess useful antibacterial activity.

Abstract: Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-oxa or thia-1H-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetamide, possess useful antibacterial activity.

Abstract: Described is a process for preparing a racemic or chiral aryloxypropanolamine (1) or arylethanolamine (2) of the formula ##STR1## wherein Ar is aryl, substituted aryl, heteroaryl, or aralkyl and R is alkyl, substituted alkyl, aralkyl, or WB wherein W is a straight or branched chain alkylene of from 1 to about 6 carbon atoms and wherein B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, where R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.sub.5 are not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.3 or --NR.sub.3 COOR.sub.5, or R.sub.3 and R.sub.4 may together with N form a 5- to 7-membered heterocyclic group.The process can be used to prepare beta-blocking agents, useful in the treatment of cardiac conditions.

Abstract: An easily opened package is provided, formed of a substantially rigid, foldable sheet, such as cardboard, and having an opening on one side of the sheet. A plastic film is sealed about the opening and is stretchable to form a pouch for receiving an item to be stored in the package. To form the package, the plastic film is heated and stretched about the item and the cardboard sheet is folded over and sealed together. Prior to forming the package, a pair of opposing cuts are formed in the edges of the film, the cuts facilitating tearing of the film when it is desired to open the package. To further facilitate opening, indicia can be placed on the edges of the cardboard sheet to indicate the point at which tearing is easiest, or notches can be cut in one side of the sheet.

Abstract: Aminomethyl oxooxazolidinyl ethenylbenzene derivatives, including the nitriles, sulfoxides, acetamides and nitro compounds, such as l-N-[3-[4-(E-1-methyl-2-cyanoethenyl)phenyl]-2-oxooxazolidin-5-ylmethyl]ac etamide, possess useful antibacterial activity.

Abstract: In accordance with the present invention, disclosed herein are compounds of the formula ##STR1## wherein R is hydrogen, straight or branched loweralkyl, cycloalkyl, amino, loweralkoxy or acylamino, and R.sub.1 is straight or branched loweralkyl, amino, cyclohexyl phenyl or phenyl substituted with loweralkyl, loweralkoxy or halo, benzyl, morpholino, piperidino, tetrahydrofuranyl, dihydrofuranyl, furanyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolidinyl, tetrahydrooxazolyl, and dihydrooxazolyl, R.sub.2 is hydrogen or --COR.sub.3 wherein R.sub.3 is straight or branched loweralkyl, provided, however, when R.sub.1 is loweralkyl or cyclohexyl, R.sub.2 is not hydrogen, and pharmaceutically acceptable salts thereof. The compounds are useful in the treatment of glaucoma.

Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.

Abstract: Aminomethyl oxooxazolidinyl aroylbenzene derivatives, such as l-N-[3-[4-(2,4-difluorobenzoyl)phenyl]-2-oxooxazolidin-5-ylmethyl]acetamid e, possess useful antibacterial activity.

Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S-- where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A) is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.

Abstract: Novel compounds of the general formula ##STR1## wherein R.sub.1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxymethyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the ##STR2## group may be the same or different; Ar is heterocyclic, unsubstituted aromatic or aromatic substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.

Abstract: A method for the preparation of clindamycin phosphate by first preparing the novel intermediate, clindamycin phosphoryl benzylate. The method can be used to make other, structurally related compounds.

Abstract: The present invention relates to new compositions for the preservation of organs prior to implantation comprising hydroxyethyl starch substantially free of ethylene glycol, ethylene chlorohydrin and acetone in a pharmaceutically acceptable organ perfusate.