Abstract: Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(1S-oxo-3R-thiolanylthio)-2-penem-3-carboxylic acid and 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio )-2-penem-3-carboxylic acid, and pharmaceutically-acceptable salts and in vivo hydrolyzable esters thereof, useful as systemic antibacterial agents; and intermediates and processes which are useful in the said synthesis of said diastereoisomers.

Abstract: 1S,4S and 1R,4R-2-alkyl-2,5-diazabicyclo[2.2.1]-heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures.

Abstract: A series of novel 5-substituted imidazolidinedione derivatives and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. 5-Naphthalimido-imidazolidine-2,4-dione and 5-[3-(4'-bromo-2'-fluorobenzyl)-3,4-dihydro-4-oxophthalazin-1-yl]-imidazol idine-2,4-dione represent typical and preferred member compounds. Methods for preparing all these compounds from known starting materials are provided.

Abstract: A method for treating depression in humans using a compound of the formula ##STR1##

Abstract: Improved processes for the synthesis of tigogenin beta-cellobioside, a known hypocholesterolemic agent, using cellobiose heptaacetate and tigogenin as starting materials.

Abstract: In the disclosed process, an O.sup.2, 2' anhydro-1-(.beta.-D-arabinofuranosyl)thymine is formed by condensing a 2-amino-.beta.-arabinofurano[1',2':4,5,]-2-oxazoline with a compound of the formula ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.4 alkyl; X is halogen or OR.sub.2, wherein R.sub.2 is H, C.sub.1 -C.sub.4 alkyl or phenyl; in the presence of a suitable solvent at about 0.degree. C. to about 150.degree. C. Catalytic agents such as dimethylaminopyridine and triethylamine may also be added to accelerate the reaction.Protected intermediates of the anhydronucleosides and aminooxazolines are also disclosed.

Abstract: This invention relates to the use of tenidap, 5-chloro-2,3-dihydro-2-oxo-3-(2-thienylcarbonyl)-indole-1-carboxamide, and the pharmaceutically-acceptable base salts thereof to inhibit activation of collagenase in a mammal and to inhibit the activity of myeloperoxidase in a mammal. This invention also relates to the use of tenidap and its salts for treating collagenase mediated disorders and diseases such as bone resorption disorders, corneal ulceration, periodontal disease, inflammatory disease and wounds of the skin and burns in mammals. The methods of this invention comprise administering an effective amount of tenidap or salts thereof to a mammal.

Abstract: Platelet activating factor antagonists of formula (I), (II) or (III): ##STR1## where A is optionally substituted benzene, pyridine, naphthalene, quinoline, thiophene, benzothiophene, pyrazole or isothiazole,X is O, S or NHY is 1,4 phenylene or a group of formula ##STR2## R.sup.1 is H or optionally substituted C.sub.1 -C.sub.4 alkyl, R.sup.2 and R.sup.3 are H or C.sub.1 -C.sub.4 alkyl,B is an optionally fused 5- or 6-membered ring containing nitrogen atoms,Het is an optionally substituted 5-membered heterocyclic ring containing nitrogen or a pyridine ring, the ring optionally being fused to benzene or nitrogen-containing heterocyclic ring.

Abstract: Compounds of the formula ##STR1## where Y is alkyl, aryl or heterocyclic, n is 1-7, R is hydrogen, alkyl, aralkyl or carboxymethyl, R.sub.1 is acetoxy, thiophenoxy, hydrogen, halo, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen, alkyl or alkanoyl and X is C.dbd.O, CH.sub.2, NH, O or S as antiallergy and antiinflammatory agents.

Abstract: This invention relates to the use of tenidap, 5-chloro-2,3-dihydro-2-oxo-3-(2-thienylcarbonyl)-indole-1-carboxamide, and the pharmaceutically-acceptable base salts thereof to inhibit the release of elastase by neutrophils in a mammal. This invention also relates to the use of tenidap and its salts for treating elastase-mediated diseases and dysfunctions such as arteritis, proteinuria and pulmonary emphysema in mammals. The methods of this invention comprise administering an effective amount of tenidap or salts thereof to a mammal.

Abstract: Novel 5-alkanesulphonamido-2-[N-(4-alkanesulphonamidophenoxyalkyl)-N-methylamino ]indane and 5-alkanesulphonamido-2-[N-(4-alkanesulphonamidophenyl-alkyl)-N-methylamino ]indane compounds have been prepared, including their pharmaceutically acceptable salts and various key novel intermediates therefor. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. The most preferred member compouned is 5-methanesulphonamido-2-[N-(4-methanesulphonamidophenethyl)-N-methylamino] indane. Methods for preparing these compounds from known starting materials are provided.

Abstract: A novel three-step process for resolving a racemic spiro-hydantoin compound into its optical antipodes is disclosed, which involves (1) reacting said racemic compound with an optically-active asymmetric isocyanate of the formula RNCO, wherein R is (S)- or (R)-1-phenylethyl or (S)-or (R)-1-(1-naphthyl)ethyl, to form the corresponding diastereomeric ureido compound; (2) separating the resulting diastereomeric mixture into its component parts, and (3) thereafter converting the separated ureido diasteromers obtained in step (b) to the corresponding asymmetric hydantoin compounds by treatment with an alkali metal lower alkoxide (C.sub.1 -C.sub.4), followed by acidification, whereupon the desired optical isomer is obtained.

Abstract: The bone prosthesis of the present invention comprises a first body member or stem for placement into a bone cavity, such as an intramedullary canal. The body member is configured and dimensioned so as to provide a nonuniform interference press-fit. The apparatus further comprises a second body member or broach for placement into the broach configured and dimensioned so as to prepare and removal from a bone cavity, the bone cavity so as to provide a nonuniform interference press-fit with the stem. THe apparatus further comprises a distal sleeve configured and dimensioned so as to be attached to the stem so as to centralize the stem in the bone cavity. The distal sleeve preferably is provided with an interior conical slope and an exterior conical slope on a portion thereof to aid in insertion into the canal. The stem further comprises at least one groove and preferably a plurality of grooves along its corners.

Abstract: A modular apparatus for use in the preparation of bone surfaces and the implantation of a modular total knee prosthesis in a patient, which apparatus comprises cutting guides, templates, alignment devices, a distractor and clamping instruments which provide modularity and facilitate bone resection and prosthesis implantation.

Abstract: An oral drug delivery system having delayed gastrointestinal transit comprising a non-continuous compressible element and an attached controlled release device and which in the expanded form resists gastrointestinal transit; and a modular system for use therein comprising a non-continuous compressible element and an attached receptacle means for receiving and holding a drug-containing orally administrable controlled release device and which in the expanded form resists gastric transit.

Abstract: Plants and trees are effectively treated with erythorbic acid or salts thereof to reduce ozone damage to their crops.

Abstract: 2-substitutedmethylamino-amino 5-(hydroxy or alkoxy) pyridines and derivatives thereof are disclosed. The compounds are inhibitors of leukotriene synthesis and are therefore useful for the treatment of pulmonary, inflammatory, dermatological, allergic and cardiovascular diseases.

Abstract: An amine substituion process for 2-(1-pentyl-3-guanidino)-4-(2-methyl-4-imidazolyl)thiazole, for precursor N-(pentylamidino)thiourea, and for analogs thereof of said compounds.

Abstract: Crystalline 2-(1-pentyl-3-guanidino)-4-(2-methyl-4-imidazolyl)thiazole dihydrochloride trihydrate having advantageous properties.

Abstract: A water based slurry for use as backup coat on a wax model has colloidal silica and milled zircon as primary ingredients. The slurry is utilized as a backup coat on a wax model used in a lost wax investment casting technique. The slurry comprises of colloidal silica, a latex glue, ammonium alginate, a wetting agent, milled zircon, tabular alumina, glass rock and an anti-foaming agent.