Abstract: A series of novel [1,2,4]triazolo[4,3-a]quinoxaline-4-amine derivatives wherein the amine group is optionally substituted with lower alkyl, phenylalkyl having up to three carbon atoms in the alkyl moiety or alkanoyl having from two to five carbon atoms, or the amine group alternatively completes a piperazino ring, the quinoxaline ring is optionally substituted with fluorine, chlorine, bromine or methoxy, and the triazolo ring is optionally substituted with lower alkyl, lower perfluoroalkyl or phenyl are disclosed. These novel compounds are useful for treatment of symptoms associated with depression. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention.

Abstract: 1-Substituted-6-fluoro-7-aryl-(8-fluoro)-1,4-dihydroquinol-4-one 3-carboxylic acids having antibacterial activity are prepared by reacting the corresponding alkyl 1-substituted-6-fluoro-7-bromo-(8-fluoro)-1,4-dihydroquinol-4-one-3-carbox ylate with an arylmetallic compound and hydrolyzing the ester formed.

Abstract: Certain novel 1-(substituted-alkyl)-3-(3-hydroxyphenyl)piperidine compounds, and the pharmeceutically-acceptable acid-addition salts thereof, possess pharmaceutical activity as neuroleptic agents, and they are useful for treating psychotic disorders, e.g. schizophrenia, in human subjects. In particular, they are useful for alleviating such symptoms as anxiety, agitation, excessive aggression, tension and social or emotional withdrawal in psychotic patients.Certain 3-(3-methoxyphenyl)piperidine compounds are useful as chemical intermediates to the aforementioned neuroleptic agents.

Abstract: Methods for preparing purified, decolorized polydextrose having a lower caloric value, higher pH and less color than presently available commercial material, and the use of said improved product in edible foodstuffs and beverages.

Abstract: Hypoglycemic 5-furyl and 5-thienyl derivatives of oxazolidine-2,4-dione and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; and intermediates useful in the preparation of said compounds.

Abstract: Certain substituted-2-penem-3-carboxylic acid compounds, and pharmaceutically-acceptable salts thereof, can be prepared from the appropriate xanthate or trithiocarbonate by desulfurization, followed by halogenation and ring closure. The corresponding desulfurized and halogenated intermediates are disclosed.

Abstract: Certain 2-alkylthio-2-penem-3-carboxylic acid compounds are useful as antibacterials for treating mammals.

Abstract: Peptide-substituted heterocyclic compounds having the formula below, pharmaceutically acceptable salts thereof and intermediates therefor; processes for their preparation and use as immunostimulant and antiinfective agents. ##STR1## wherein R is a 5- or 6-membered N-containing heterocyclyl moiety which can have an additional hetero atom selected from N, S or O; R.sup.1 is hydrogen or (C.sub.1-4)alkyl; x is 0 or an integer from 1 to 5; and y is 0 or 1; provided that when y is 0, said N-containing heterocyclyl moiety is linked to the ##STR2## group at its N atom.

Abstract: Chiral sorbinil intermediates of the formula ##STR1## wherein R is hydrogen or benzyloxycarbonyl and Y is hydroxy or amino, processes therefor, and processes for the conversion thereof to sorbinil.

Abstract: Dihydropyridine derivatives of the formula: ##STR1## and their pharmaceutically acceptable acid addition salts; wherein R is a substituted aryl group;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.3 alkyl;Y is --(CH.sub.2).sub.n -- where n is 2, or --CH.sub.2 CH(CH.sub.3)--; and Het is a 6-membered aromatic heterocyclic group attached to the adjacent oxygen atom by a carbon atom.The compounds have utility as anti-ischaemic and anti-hypertensive agents.

Abstract: 1-substituted-1-haloaryl-1-('-[1H-1,2,4-triazol-1-yl]-cyclopropyl)-2-(1H-1, 2,4-triazol-1-yl)ethane compounds and pharmaceutical compositions thereof are useful in treating fungal infections in mammals and plants.

Abstract: A series of 5-(2-alkoxyphenyl)thiazolidinediones and pharmaceutically acceptable salts thereof useful as hypoglycemic agents, aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications; intermediates therefore; and process for preparation of said compounds.

Abstract: Compounds of the formula ##STR1## a pharmaceutically or agriculturally acceptable acid addition salt thereof wherein R is 5-chloro-2-pyridyl, phenyl or phenyl substituted by from 1 to 3 substituents, each independently selected from F, Cl, Br, I, CF.sub.3, (C.sub.1 -C.sub.4)alkyl and (C.sub.1 -C.sub.4)alkoxy; and R.sup.1 is H, Cl, phenyl, phenyl substituted by from 1 to 3 substituents each independently selected from F, Cl, Br, I and CF.sub.3 or a heterocyclic group linked to the adjacent CF.sub.2 group by a ring carbon atom; method for their use in combatting fungal infections in plants, seeds and animals, including humans, and pharmaceutical and agricultural compositions containing them.

Abstract: 1,4-Dihydropyridine derivatives of the formula: ##STR1## wherein R is aryl or heteroaryl: R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; Y is --(CH.sub.2).sub.n --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --; n is 1 to 3; and X is a 5 or 6 membered nitrogen containing aromatic heterocyclic ring which may optionally be substituted by one or more C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, CN, --N(R.sup.3).sub.2, (CH.sub.2).sub.m CO.sub.2 H, (CH.sub.2).sub.m CO.sub.2 (C.sub.1 -C.sub.4 alkyl) or (CH.sub.2).sub.m CON(R.sup.3).sub.2 group wherein each R.sup.3 is independently H or C.sub.1 -C.sub.4 alkyl and m is 0 or 1; and their pharmaceutically acceptable acid addition salts, and pharmaceutical preparation containing such compounds, have utility as anti-ischaemic and antihypertensive agents.

Abstract: Compounds of the general formula ##STR1## or a pharmaceutically or agriculturally acceptable acid addition salt thereof wherein R is 5-chloro-2-pyridyl, phenyl or phenyl substituted by from one to three substituents, each independently selected from F, Cl, Br, I, CF.sub.3, (C.sub.1 -C.sub.4)alkyl and (C.sub.1 -C.sub.4)alkoxy; and n is zero or an integer from 1 to 5; method for their use in combatting fungal infections in plants, seeds and animals, including humans; and pharmaceutical and agricultural compositions containing them.

Abstract: Certain 2-dioxacycloalkylthio-2-penem-3-carboxylic acid compounds are useful as antibacterials for treating mammals and have the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R is ##STR2## A is carbonyl, methylene or thiocarbonyl; B is alkylene having 2-5 carbon atoms;alk is alkylene having 1-6 carbon atoms;R.sub.1 is hydrogen or a group which results in an ester which is hydrolyzable in vivo; andn is zero or one.

Abstract: A series of novel derivatives of penicillanic acid 1,1-dioxide, having a disubstituted methyl group of the formula X-CH-Y at the 6-position, and the pharmaceutically-acceptable salts thereof and the pharmaceutically-acceptable esters thereof readily hydrolyzable in vivo, wherein X is hydroxy, acylated hydroxy or amino and Y is carboxy or esterified carboxy. The compounds of the invention are inhibitors of bacterial beta-lactamases, and they will protect certain beta-lactamase-susceptible beta-lactam antibiotics, e.g. ampicillin, against inactivation by beta-lactamases. Co-administration of a compound of the invention with a beta-lactam antibiotic such as ampicillin to a mammalian subject increases the effectiveness of the beta-lactam antibiotic against infections caused by beta-lactamase-producing bacteria.

Abstract: Certain novel 2-acetoxybenzoyl and ring-substituted .alpha.-arylpropionyl derivatives of 4-hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide and several other closely-related known oxicams have been prepared. These particular compounds are useful in therapy as non-steroidal anti-arthritic agents. Typical member compounds include 4-(2-acetoxybenzoyloxy)-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-ca rboxamide 1,1-dioxide, 4-[.alpha.-(4-isobutylphenyl)propionyloxy]-2-methyl-N-(2-pyridinyl)-2H-1,2 -benzothiazine-3-carboxyamide N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxyamide 1,1-dioxide, 4-[.alpha.-(3-benzoylphenyl)propionyloxy]-2-methyl-N-(2-pyridinyl)-2H-1,2- benzothiazine-3-carboxamide 1,1-dioxide, "d-4-[.alpha.-6-methoxynaphth-2-yl)propionyloxy]-2-methyl-N-(2-pyridinyl)- 2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide" to -- d-4-[.alpha.-(6-methoxynaphth-2-yl)propionyloxy]-2-methyl-N-(2-pyridinyl)- 2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide.

Abstract: A new antibiotic substance, which has been named nargenicin C.sub.1, has been isolated from fermentations of a species of the genus Nocardia. Nargenicin C.sub.1 can be used as an antibacterial agent against susceptible bacteria, especially susceptible strains of Staphylococcus aureus.