Abstract: Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is methyl, hydroxymethyl, ethyl, n-propyl or isopropyl; R is ##STR2## where at least one of R.sup.3, R.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six; and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl, they are methyl or ethyl.Said amides are potent sweeteners having advantages over the prior art, edible compositions containing them, methods for their use in edible compositions and novel amine and amide intermediates useful in their production.

Abstract: 6-Halo- and 6,6-dihalo-1,1-dioxopenicillanoyloxymethyl 6-[D-2-(2-alkoxycarbonyl-1-methylvinylamino- and 1-methyl-3-oxo-1-butenylamino)-2-phenylacetamido]penicillanates and analogs; process for their conversion to sultamicillin and analogs; and process for their preparation.

Abstract: 6-(1-Carbamoyl-1-hydroxymethyl)penicillanic acid derivatives are useful as antibacterials and/or beta-lactamase inhibitors.

Abstract: Oxophthalazinyl acetic acids having aldose reductase inhibitory properties of the formula ##STR1## wherein Z is hydrogen or methyl, U is S, CH.sub.2 or a covalent bond, and R.sup.1, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as herein defined, are prepared by reacting an intermediate oxophthalazinyl acetic acid ester having a cyano or alkylamido group with an aniline derivative of the formula ##STR2## Processes for the preparation of the intermediate oxophthalazinyl acetic esters are disclosed.

Abstract: Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.

Abstract: Intermediates and a stepwise process for the conversion of ethyl 4-chloro-3R-hydroxybutyrate to optically active compounds of the formula ##STR1## wherein R is (C.sub.1 -C.sub.3)alkyl, phenyl or tolyl. The later compounds are in turn useful as an intermediate in the preparation of penem antibiotic 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acic and corresponding pharmaceutically acceptable salts and esters.

Abstract: A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl)alkylamine derivatives have been prepared, including their pharmaceutically acceptable salts, wherein the heterocyclic moiety is a 5- or 6-membered nitrogen-containing heterocyclic group which is attached to the adjacent carbon atom by a carbon or nitrogen atom and optionally contains a further heteroatom selected from oxygen and nitrogen, said nitrogen-containing heterocyclic group being either (i) substituted by a phenyl or benzyl group or (ii) fused at two adjacent carbon atoms to a benzene ring, with the resulting heterocyclic ring moiety also being optionally substituted. These particular compounds are useful in therapy as highly effective anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrythmias. The most preferred member compound of the series is 2-hydroxy-2-(4-methanesulphonamidophenyl)-N-methyl-N-[2-(6-chloro-2H-isoin dolin-1-on-2-yl)ethyl]ethylamine.

Abstract: Certain substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones are highly potent gabaergic agents, valuable in the treatment of individuals suffering from schizophrenia or reversing the side effects of a previously or concurrently administered neuroleptic agent; or in the treatment of epilepsy. A wider class of substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones, together with 1-phenyl-3-(2-pyrrolidinylidene)-2(1H,3H)-indolones, and homologs thereof, are valuable in the treatment of anxiety.

Abstract: This invention relates to the use of certain 3-substituted-2-oxindole-1-carboxamides of the formula ##STR1## and the pharmaceutically-acceptable base salts thereof wherein X is H, Cl or F; Y is H or Cl; and R is benzyl or thienyl to inhibit interleukin-1 biosynthesis in a mammal. This invention also relates to the use of such compounds for treating interleukin-1 mediated disorders and dysfunctions such as bone and connective tissue metabolism disorders and immune dysfunction in a mammal. The methods of this invention comprise administering an interleukin-1 biosynthesis inhibiting amount of the compounds and salts of this invention to such a mammal.

Abstract: Certain N-substituted nicotinamide compounds having formula (I) below ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is 1-piperidyl, 1-(3-indolyl)ethyl, C.sub.1-4 alkyl, phenyl, 1-(1-phenylethyl), benzyl or mono-substituted benzyl wherein the substituent is methyl, methoxy, chloro or fluoro; and R.sup.2 is bicyclo[2.2.1]hept-2-yl or ##STR2## wherein Y is hydrogen, fluoro or chloro; and X is hydrogen, fluoro, chloro, methoxy, trifluoromethyl, cyano, carboxy, carbo (C.sub.1-4 alkoxy), methylcarbamoyl or dimethylcarbamoyl function as selective inhibitors of calcium-independent phosphodiesterase and are useful as antidepressants.

Abstract: Antibacterial compounds have the formula ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p-aminophenyl; or A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five to seven membered ring which is optionally substituted; and R.sup.2 is a bridged-diazabicycloalkyl group.

Abstract: A method for enhancing the unrolling of a rolled active agent-containing laminate device in an aqueous use environment which comprises coating one side of the device with an elastomer prior to constraining it in a rolled configuration; and the devices so treated.

Abstract: Quaternary 8-(alkyldithio)-1-(2-pyrimidyl)-quinolinium salts, inhibitors of the H.sup.30 /K.sup.+ ATPase enzyme, are useful in the treatment of ulcers.

Abstract: Polypeptides and derivatives thereof containing homocyclostatine and cyclostatine are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.

Abstract: 4-Aryl-3-alkoxycarbonyl-6-methyl-5-carbamyl-2-triazolylalkoxymethyl-1,4-dih yd ropyridines as anti-allergic and anti-inflammatory agents.

Abstract: A high strength, low modulus, ductile, biocompatible titanium base alloy containing one or more isomorphous beta stabilizers, eutectoid beta stabilizers and optional alpha stabilizers, characterized by a modulus of elasticity not exceeding 100 GPa; a method for the preparation of said alloy and prostheses made from said alloy.

Abstract: A catheter for facilitating the restoration of patency to a blood vessel occluded with an atheroma or other similar lesion or thrombus comprising an outer flexible plastic tubular member having a plurality of ports proximate its distal end and concentrically surrounding an inner flexible plastic tubular member having a cutting loop at its distal end. The distal end portion of the inner tubular member is journaled for rotation in the distal end portion of the outer tubular member. A motor is provided at the proximal end of the catheter assembly for rotatably driving the inner tubular member and the cutting loop thereof while flushing the treatment site and aspirating the flushing liquid, blood and any debris loosened during the procedure.

Abstract: Antibacterial 12,12'-anhydro-9R-hydroxy-9-deoxoerythromycin A derivatives, intermediate therefor and process of 12,12'-dehydration.

Abstract: Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is methyl, ethyl, n-propyl or isopropyl; R is a branched member selected from the group consisting of fenchyl, diisopropylcarbinyl, d-methyl-t-butylcarbinyl, d-ethyl-t-butylcarbinyl, di-t-butylcarbinyl, 2-methylthio-2,4-dimethylpentan-3-yl, ##STR2## where at least one of R.sup.3, R.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, X is O, S, SO, SO.sub.2, C.dbd.O or CHOH; m is zero or 1-4, n and p are each zero, 1, 2 or 3 where the sum of n+p is not greater than 3 and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six, and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl they are methyl or ethyl, ##STR3## where one of R.sup.7, R.sup.8, R.sup.

Abstract: Polypeptides containing fluorinated cyclostatine derivatives as antihypertensive agents.