Abstract: 3-Isoxazolylurea derivatives of the formula: ##STR1## (wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.6 -C.sub.8 aryl; R.sup.1 represents hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.2 represents C.sub.1 -C.sub.6 alkyl, C.sub.6 -C.sub.8 aralkyl, or C.sub.6 -C.sub.8 aryl; or ##STR2## represents pyrrolidino, piperidino, morpholino, or 4-alkylpiperazino; X represents hydrogen or halogen; or R and X may optionally form C.sub.3 -C.sub.5 alkylene), are prepared by reacting a carboxamide of the formula: ##STR3## (wherein R and X each is as defined above) with an amine of the formula:R.sup.1 --NH--R.sup.2(wherein R.sup.1 and R.sup.2 each is as defined above) in the presence of an alkaline hypohalite and an alkaline hydroxide in an inert solvent medium.

Abstract: A mixture of minor diindole alkaloids from Vinca-containing vinblastine and 4-deacetoxy-vinblastine vines, are separated by subjecting the mixture to a deacetylation to correct the vinblastine to deacetyl-vinblastine prior to chromatographic separation of said mixture in a single stage.

Abstract: Cephalosporin compounds of the formula ##STR1## wherein R is 1-carboxymethyl-1,2,3,4-tetrazol-5-yl or 5-carboxymethyl-1,3,4-thiadiazol-2-yl,and non-toxic pharmaceutically acceptable salts thereof, and processes for preparing them. The compounds have superior antibacterial activity and excellent solubility in an aqueous medium, and are useful as antibacterial agent.

Abstract: Novel [2-(syn)-carbamoyloximinoacetamido]cephalosporins of the formula: ##STR1## [wherein, Y.sup.1 is hydrogen, hydroxyl, carbamoyloxy, acyloxy, quaternary ammonium or nitrogen-containing heterocyclic thio; R.sup.1 is alkyl, aralkyl or aryl; R.sup.2 is hydrogen or an ester residue; k is 0 or 1] and a salt thereof show strong antibacterial activities particularly against Gram-negative bacteria and they are useful as antibacterial agents.

Abstract: A novel process for preparing 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline by cyclizing N-acetyl-2,3-dichlorobenzylaminoacetaldehyde dimethyl acetal with a Lewis acid, reducing, and hydrolyzing the resulting acylated isoquinoline is disclosed.

Abstract: New indole derivatives of cephalosporin compounds have been prepared which are useful as antibiotics.

Abstract: 7-[.alpha.-(4-hydroxy-1,5-naphthyridine-3-carboxamido)-.alpha.-phenyl or thienyl (and substituted phenyl) acetamido]-3-(pyridiniummethyl)-3-cephem-4-carboxylates having on the pyridine ring an acidic group which is preferably --COOH or --SO.sub.3 H and also, if desired, having one or two methylene groups together with or without a hetero atom between the pyridine ring and the acidic group were synthesized and found to have potent antibacterial activity in vitro especially against many strains of Pseudomonas aeruginosa and also high solubility in water.

Abstract: Novel cephalosporin compounds, process of preparation thereof, intermediates useful in the preparation of the cephalosporins, pharmaceutical compositions formulated therefrom for administration and combinations of the cephalosporins in pharmaceutical composition form with clavulanic acid. The cephalosporin compounds are characterized by a 5-membered nitrogen-containing ring in the group in the 3-position of the sulphur-containing ring.

Abstract: A class of 3-carbamoyloxymethyl-7-.alpha.-acylureido cephalosporins have a broad spectrum of antibacterial activity.

Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, R' is selected from the group consisting of alkenyl and alkynyl of 2 to 4 carbon atoms, A is selected from the group consisting of hydrogen, alkali metal and equivalents of an alkaline earth metal or magnesium and an organic amine base and the OR' group is in the syn position having antibiotic activity and process for their preparation.

Abstract: 4-Desacetoxy-4.alpha.-hydroxyvinblastine, prepared by reduction of 4-desacetoxy-4-oxovinblastine, and derivatives thereof, useful as antimitotic agents.

Abstract: There are provided new compounds of the formula I ##STR1## wherein both R.sup.1 moieties stand for an alkyl group having 1 to 4 carbon atoms or form together a methylene bridge,R.sup.2 is cyano or an alkoxycarbonyl group having 1 to 4 carbon atoms in the alkoxy position,R.sup.3 is hydroxy or alkanoyloxy having 1 to 4 carbon atoms in the alkoxy position in .alpha.-position or .beta.-steric position,and acid addition salts thereof. There is also provided a process for the preparation of the compounds of the formula I.

Abstract: This invention relates to compounds having the formula: ##STR1## in which: R represents a C.sub.1-6 alkyl radical or a C.sub.1-6 alkenyl radical; A represents an indazol-2,3- or 4,5- or 6,7-diyl radical, which indazoldiyl radical may be substituted on the nitrogen atoms at 1- or 2-position with C.sub.1-6 alkyl or phenyl-(C.sub.1-6) alkyl radicals, and their salts with pharmaceutically acceptable bases.Said compounds are therapeutically useful as antibacterial agents.

Abstract: Disclosed are compounds which are 4-hydroxy-2-quinolinone-3-carboxylic acid esters, e.g., 1-methyl-4-hydroxy-2-quinolinone-3-carboxylic acid ethyl ester, useful as anti-allergic agents and intermediates for 1-alkyl-4-alkoxy-quinolin-2(1H)-ones, and prepared by reacting an isatoic anhydride with an alkali metal salt of a malonic ester.

Abstract: In spite of their pigment character, dyestuffs of the formula ##STR1## are outstandingly suitable for dyeing synthetic fibres, in particular polyester fibres, by customary methods, strong yellow dyeings with good fastness to light and sublimation being obtained. In the abovementioned formula:R.sub.1 and R.sub.3 denote hydrogen, alkyl, aralkyl, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl or aryl,R.sub.2 and R.sub.4 denote alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, --CN or --CONX.sub.1 X.sub.2,X.sub.1 denotes hydrogen, alkyl, aralkyl, aryl or cycloalkyl andX.sub.2 denotes hydrogen or alkyl.

Abstract: Leurosine derivatives of the formula (I), ##STR1## wherein R is hydrogen or formyl, or pharmaceutically acceptable acid addition salts thereof were prepared by oxidizing leurosine or an acid addition salt thereof, optionally formylating the thus-obtained product and then separating, and, if desired, converting any of the free bases into its acid addition salt. The new compounds of the invention possess strong cytostatic activity, and can be used in the human therapy with great advantage.

Abstract: Disclosed are compounds which are 4-hydroxy-2-quinolinone-3-carboxylic acids and salts thereof, e.g., 1-allyl-6,7-dimethoxy-4-hydroxy-2-quinolinone-3-carboxylic acid, useful as anti-allergic agents, and prepared by hydrolysis of the corresponding carboxylic acid esters.

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: 1-[.alpha.-(Carboxy)-4-hydroxybenzyl]-3.beta.-aminoazetidin-2-one esters are prepared by converting 2-acyl-3,3-dialkyl-7-oxo-.alpha.-[4-(benzyloxy)phenyl]-4-thia-2,6-diazabic yclo[3.2.0]-heptane-6-acetic acid esters with mercuric acetate in an aqueous organic solvent mixture, e.g., in aqueous methanol, to 7-oxo-3-phenyl-.alpha.-[4-benzyloxy)phenyl]-4-oxa-2,6-diazabicyclo[3.2.0]h ept-2-ene-1-acetic acid esters and the latter are reacted with PCl.sub.5 and pyridine to provide the monocyclic 1-[.alpha.-(carboxy)-4-benzyloxybenzyl]-3.beta.-(.alpha.-chlorobenzylidene amino)-4-chloroazetidin-2-one esters. Reduction of the dichloro azetidin-2-one with an organo tin hydride and azobisisobutyronitrile affords the deschloro, 1-[.alpha.-(carboxy)-4-benzyloxybenzyl]-3.beta.-benzylideneaminoazetidin-2 -one ester. The latter is hydrolyzed and the 4-benzyloxy group is cleaved via catalytic hydrogenolysis to yield an ester of 1-[.alpha.-(carboxy)-4-hydroxybenzyl]-3.beta.-aminoazetidin-2-one. The 3.beta.

Abstract: Cephalosporins in a series having the formula ##STR1## wherein R.sup.1 is alkyl containing 1-4 carbon atoms or a nontoxic pharmaceutically acceptable salt thereof, were synthesized and found to be potent antibacterial agents especially when in the form of the syn isomers essentially free of the corresponding anti isomer.