Abstract: Cephalosporins with a .alpha.-amino-(ureidophenyl)acetamido substituent at position 7 are prepared by acylation of a 7-aminocephalosporin with a derivative of .alpha.-amino-p(or m)-ureidophenylacetic acid. These compounds are antibacterial agents.

Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1 denotes optionally substituted phenyl, thienyl, furyl or 1,4-cyclohexadienyl, R.sub.2 represents a free carboxyl group or an esterified carboxyl group which can be split physiologically, R.sub.3 represents hydrogen, lower alkoxy or an optionally substituted methyl group, and B represents a monosubstituted or polysubstituted six-membered ring with 1 to 3 ring nitrogen atoms which is bonded to the carbonyl group --C(.dbd.O)-- by one of its ring carbon atoms, and the salts of such compounds which have salt-forming groups, which compounds possess antibiotic properties.

Abstract: A compound of the following formula ##STR1## wherein R represents an alkyl group containing 1 to 4 carbon atoms or a phenyl group; X.sub.1 represents a chlorine or bromine atom; Y represents the group of the formula ##STR2## WHEREIN X.sub.2 and X.sub.3 each represent a chlorine or bromine atom, and n is an integer of 2 to 4; and ring A may be substituted by an alkyl group containing 1 to 4 carbon atoms and or a halogen atom.The compound of formula (I) can be easily produced by reacting a quinoline derivative of the formula ##STR3## wherein R, X.sub.1 and the ring A are the same as defined above, with an aryldicarboxylic acid or its reactive derivatives.The compounds of formula (I) are useful as yellow organic pigments.

Abstract: Novel 1,2-dihydro-2-oxoquinol-4-ylalkanoic acid derivatives bearing a variety of substituents on the quinoline nucleus but including, at position 1, an aromatic radical linked directly or through a C.sub.1-4 -alkylene or a C.sub.2-4 -alkenylene radical. Representative compounds of the invention are 1-(3,4-dichlorobenzyl)-3-methyl-1,2-dihydro-2-oxoquinol-4-ylacetic acid and .alpha.-(1-benzyl-1,2-dihydro-2-oxoquinol-4-yl)propionic acid. The compounds possess anti-inflammatory or analgesic properties, or are inhibitors of the enzyme aldose reductase.

Abstract: New semisynthetic cephalosporins are described whose structures are characterized by having an .alpha.-oxyimino group in the 7-acetamido moiety and a sulfosubstituted tetrazolylthiomethyl group at position 3. The compounds are active antibacterial agents especially against Gram negative organisms.

Abstract: A series of novel 7-(D-.alpha.-acylaminoarylacetamido)-.DELTA..sup.3 -cephem derivatives have been prepared wherein the acyl moiety contains an epoxy group immediately adjacent to the carbonyl carbon atom. These compounds are useful as antibacterial agents for the treatment of diseases caused by Gram-negative and Gram-positive bacteria. Preferred members include 7-[D-.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]-3-(1-meth yl-1,2,3,4-tetrazol-5-ylthiomethyl)-.DELTA..sup.3 -cephem-4-carboxylic acid and 7-[D.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]cephalospor anic acid. Alternate methods of preparation are provided for these compounds and the principal synthetic route is described in detail.

Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

Abstract: Compounds of the formula ##STR1## wherein A is hydrogen, hydroxy, methyl or methoxy,R.sup.1 is hydrogen, sodium or potassium,R.sup.2 is carboxyl or 2-furyl or an aliphatic, aromatic or heterocyclic radical to which there is also attached a strongly acidic group in the form of its sodium or potassium salt, andR.sup.3 is tetrazol-5-yl, 1,2,4-thiadiazol-5-yl, 1,3,4-thiadiazol-2-yl, 1,3,4-oxadiazol-3-yl or 1,2,4-triazol-5-yl, each of such groups being unsubstituted or substituted with one or two lower alkyl groups of one to four carbon atoms are prepared by reacting the appropriate aldehyde with the corresponding amphoteric cephalosporin. Preferred products have the structure ##STR2## in which A is --H or --SO.sub.3 Na.

Abstract: [[[(2,4-Dioxo-1-imidazolidinyl)amino]carbonyl]amino]-acetylcephalosporin derivatives having the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; R.sub.2, R.sub.3 and R.sub.5 each is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cyclo-lower alkyl, cyclo-lower alkenyl, cyclo-lower alkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR3## or certain heterothio groups; are useful as antibacterial agents.

Abstract: Compounds of the formula ##STR1## wherein A is hydrogen, hydroxy, methyl or methoxy,R.sup.1 is hydrogen, sodium or potassium, andR.sup.2 is 1,2,3-triazol-5-yl, such group being unsubstituted or substituted with one or two lower alkyl groups of one to four carbon atoms are prepared by reacting the appropriate aldehyde with the corresponding amphoteric cephalosporin.

Abstract: Novel 2-substituted-1-methylamino adamantanes of formula: ##STR1## where X is hydroxyl or halogeno, and R.sup.1, R.sup.2 and R.sup.3 are hydrogen or C.sub.1-4 alkyl or R.sup.2 and R.sup.3 together with the nitrogen form a heterocyclic ring, having anti-Parkinsonian activity, pharmaceutical formulations containing the active adamantanes and novel 4-protoadamantane spiro oxirane and 1,2-difunctionalized intermediates useful in the preparation of the final products of the invention.

Abstract: Compounds of the formula ##STR1## in which W is quinolyl or lower alkyl quinolyl;A is alkylene of 1 to 6 carbon atoms;R is phenyl, halophenyl, lower alkoxy phenyl or lower alkyl phenyl;Or a pharmaceutically acceptable acid addition salt thereof, are hypotensive and bradycardial agents.

Abstract: Antibacterial 3-carbamoylbenzyl cephems and 3-(carbamoylpyridylmethyl) cephems, pharmaceutically acceptable salts and in vivo hydrolyzable esters thereof; pharmaceutical compositions containing antibacterially effective amounts of such cephems and intermediates therefor. Minimum inhibitory concentrations against various bacteria are given. The cephems and compositions containing the same are suitable for administration in conventional forms to humans.

Abstract: 3-Carbamoyloxymethyl and 3-N-methylcarbamoyloxymethyl cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## where R is thienyl, furyl or phenyl; R.sup.a is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl or phenyl, and R.sup.b is hydrogen, carboxy, C.sub.2 -C.sub.5 carbalkoxy or any of the groups designated for R.sup.a, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; exhibit broad spectrum antibiotic activity charcterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases. The compounds, which are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer, have particularly high in vitro activity against strains of Escherichia coli, Haemophilus influenzae and Proteus organisms; and also shown unusually high activity against Pseudomonas organisms.

Abstract: Novel antibacterial agents; namely, 7-(.alpha.-acylamino-arylacetamido)-cephalosporanic acid derivatives having the formula: ##STR1## wherein R.sup.1 is thienyl, 2-furyl, phenyl, substituted thienyl or substituted phenyl; R is hydroxyl; R.sup.2 is hydrogen, hydroxy, acetoxy, carbamoyloxy, N-pyridyl, azido or heterocyclic thio group; R and R.sup.2 when taken together represent an oxygen atom; R.sup.3 is sulpho or COOR.sup.4' wherein R.sup.4' is hydrogen or R.sup.4 wherein R.sup.4 is lower alkyl, 5-indanyl, naphthyl, phenyl, or substituted phenyl, CONR.sup.5 R.sup.6, wherein each of R.sup.5 and R.sup.6 is hydrogen, lower alkyl or cycloalkyl; or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a saturated heterocyclic group; X is oxygen or sulphur, a direct link, carbonyl, methylene, hydroxymethylene, sulphinyl, sulphonyl or an imino group of the formula --NR.sup.7 --, wherein R.sup.7 is hydrogen, lower alkyl, lower alkenyl, or benzyl; and each of alk.sup.1 and alk.sup.

Abstract: This invention concerns novel aminoalkylthiopyridazine compounds useful for inhibiting the aggregation of blood platelets in animals and a process for preparing the compounds from an isothiuronium salt generated in situ from an aminoalkyl halide and thiourea. The compounds also have fungicidal and nematocidal properties.

Abstract: Sodium 7-(D-2-hydroxy-2-phenylacetamido)-3-(1-methyl-1H-tetrazole-5-ylthiomethyl) -3-cephem-4-carboxylate is obtained as a pharmaceutically acceptable crystalline anhydrate via crystalline methanolate or crystalline monohydrate forms.

Abstract: Thiazolo[5,4-f]quinoline-8-carboxylic acid derivatives having either the general formula (I): ##STR1## wherein R.sub.1 is a lower alkyl group, a lower alkenyl group or a benzyl group; or the general formula (III-a): ##STR2## WHEREIN R.sub.3 is a lower alkyl group and X is a halogen atom; and methods for the preparation thereof. The compounds of the general formula (I) are useful as antibacterial agents against gram-negative and gram-positive bacteria. The compounds of the general formula (III-a) are useful as antifungal agents against eumycetes and also as an intermediate in a peparation of the compounds of the general formula (I).

Abstract: Compounds of the class of benzylisoquinoline derivatives of the formula ##STR1## wherein R.sup.1 is selected from the group consisting of hydrogen and methyl, and R.sup.2 is selected from the group consisting of methyl, ethyl, n-propyl and isopropyl, and therapeutically acceptable salts thereof, useful as active ingredients of pharmaceutical preparations for the treatment of cardiac arrhythmias.

Abstract: Indolinone compounds which exhibit anti-inflammatory activity have the following formula ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5, and n are as defined herein.