Abstract: The invention provides a compound of formula I ##SPC1##or an acid addition salt thereof, wherein R.sup.1, R.sup.2 and R.sup.4 are the same or different and represent hydrogen, or a lower alkyl radical, R.sup.5 represents hydrogen or single or multiple substitution by lower alkyl radicals, X is cyano, CONHR.sup.3, CSNHR.sup.3 or CO.sub.2 R.sup.3 wherein R.sup.3 is hydrogen or a lower alkyl radical, m is 1, 2 or 3 and R.sup.6 is hydrogen, a lower alkyl radical or a lower alkanoyl radical or an alkali-metal salt of a compound in which X is CO.sub.2 H.Compounds of formula I wherein X is CN or CSNHR.sup.3 and R.sup.6 is lower alkyl are anti-ulcer agents. The other compounds of formula I are intermediates.

Abstract: The present invention encompasses compounds of the formula ##SPC1##Wherein R represents hydrogen or lower alkyl having 1-7 carbon atoms and wherein one X represents (nitrogen) N and the other X represents methylidyne. The compounds of the present invention are prepared by the methods set out in the following scheme: ##SPC2##Wherein R and X are as defined above. Compounds of the present invention are useful anti-inflammatory agents.

Abstract: Polymerizable monomers of the formula I ##SPC1##whereinX denotes --O-- or --NH--,R denotes H--, --COOH or --COOR.sub.3,R.sub.1 denotes --H or --CH.sub.3 andR.sub.2 denotes H-- or --CH.sub.3, said monomers are obtained by acylation of 2-[4-hydroxyphenyl]-2-[5-(8-hydroxyquinolyl)]-propane or 2-[4-aminophenyl]-2-[5-(8-hydroxyquinolyl)]-propane with acid halides of the formula.

Abstract: The invention concerns 7.beta.-amino-cepham-3-ol-4-carboxylic acid compounds, particularly esters thereof, and the N-substituted, especially N-acylated derivatives of such compounds, as well as the 3-O-esters of these compounds. They can be used as intermediates, for example, for the manufacture of the corresponding 3-unsubstituted 7.beta.-amino-3-cephem-4-carboxylic acid compounds, which show outstanding pharmacological effects.

Abstract: 4-[3-(3-vinyl-1-acetyl-4-piperidyl)-1-propenyl]-6-methoxyquinoline, the corresponding epoxide and related compounds, useful in the synthesis of Cinchona alkaloids, are prepared by introducing an ylid group in the 4-position of a suitably substituted quinoline and reacting this ylid with an N-acetyl-4-piperidineacetaldehyde.

Abstract: A compound having the formula: ##EQU1## and a 7-amihocephalosporanic acid derivative having the formula: ##SPC1##Are reacted in a homogeneous aqueous solution of the reactants to prepare a reaction of the formula: ##SPC2##In the formulas, R may be H or other defined substituents such as carboxyl group; R.sub.1 is H, an alkyl of 1-4 carbons or other defined substitents; R.sub.2 is H or phenyl or when taken together with R.sub.1 form a defined cyclicradical; R.sub.3 is H or other defined substituents and M is an alkali metal cation, ammonium cation or H.

Abstract: A class of amino alicyclylmethyl penicillins, their salts, esters, method of preparation and oral compositions containing them are described. The penicillins give high and prolonged blood levels on oral administration and are active against both Gram-positive and Gram-negative bacteria.

Abstract: Compounds of the formula ##SPC1##Wherein ##EQU1## where R.sub.1 is hydrogen, straight or branched aliphatic acyl of 1 to 12 carbon atoms, methoxy-substituted straight or branched aliphatic acyl of 1 to 12 carbon atoms, benzoyl, halo-benzoyl, carbalkoxy of 2 to 7 carbon atoms, carbcycloalkoxy of 4 to 7 carbon atoms, benzyl, methylbenzyl, phenylsulfonyl, halo-phenylsulfonyl, tolylsulfonyl, alkenyl of 2 to 6 carbon atoms, phenyl, trifluoroacetyl, amidino, amido, thioamido, phenoxycarbonyl, benzyloxycarbonyl, methylsulfonyl or--B -- XwhereB is straight or branched alkylene of 1 to 6 carbon atoms, andX is hydrogen, hydroxyl, methoxy, carboxyl, cyano, dimethylaminocarbonyl, morpholino-carbonyl or carbalkoxy of 2 to 6 carbon atoms,R.sub.2 is hydrogen, hydroxyl, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkanoyloxy of 1 to 3 carbon atoms, alkoxycarbonyloxy of 2 to 4 carbon atoms, amino, dimethylamino, morpholino or halogen,R.sub.

Abstract: In the preparation of vincadifformine and derivatives thereof, such as 3-oxo-1,2-dehydroaspidospermidine and 1,2-dehydro-aspidospermidine, 2-hydroxy-tryptamine or a derivative thereof substituted in the benzene ring is condensed with dimethyl 4-ethyl-4-formyl-pimelate to form an oxindolic lactam-ester as the first step of the process. By means of this process, vincadifformine and its derivatives can be obtained in a smaller number of steps than in known processes.

Abstract: 7-[D-(.alpha.-Amino-.alpha.-phenyl-, 2-thienyl- and 3-thienylacetamido)]-3-(thiazol-2-yl)carbonylthiomethyl-3-cephem-4-carboxy lic acid and 7-[D-(.alpha.-amino-.alpha.-phenyl-, 2-thienyl- and 3-thienylacetamido)]-3-(5-methylthiazol-2-yl)carbonylthiomethyl-3-cephem-4 -carboxylic acid and their pharmaceutically acceptable salts are valuable as antibacterial agents, as nutritional supplements in animal feeds, as agents for the treatment of mastitis in cattle and as therapeutic agents in poultry and animals, including man. The compounds are especially useful in the treatment, particularly by oral administration, of infectious diseases caused by many Gram-positive and Gram-negative bacteria. Also included within the invention are easily cleavable esters of the above acids and pharmaceutically acceptable acid addition salts of said esters.

Abstract: 7-Acylamido-3-alkylsulfonyloxy (and phenyl or substituted phenylsulfonyloxy)-3-cephem-4-carboxylic acids and esters thereof are provided via sulfonation of 3-hydroxy-3-cephem esters. The 3-cephem-3-sulfonate esters are useful antibacterial compounds.

Abstract: Novel isoquinoline derivatives of the formula ##SPC1##Wherein R.sub.1 is H or, together with R.sub.2, a C--N bond; R.sub.2 is H, R.sub.8 or, together with R.sub.1, a C--N bond; R.sub.3 is H, methyl or ethyl; R.sub.4 and R.sub.5 each are H or collectively a C--C bond; and R.sub.6 and R.sub.7 each are H or methoxy; R.sub.8 being acyl of 1-10 carbon atoms or alkyl of 1-17 carbon atoms optionally mono- or polysubstituted by phenyl, OH, ArCOO--, ArCONH--, piperidino, 3,4-dehydropiperidino, morpholino, carboxy, carbomethoxy and/or carbethoxy, Ar being 3,4,5-trimethoxyphenyl; and the physiologically acceptable acid addition salts and quaternary ammonium salts thereof, have cardiovascular activity and can be prepared by acylating a corresponding primary amine lacking the COAr group with 3,4,5-trimethoxybenzoic acid or a functional derivative thereof.

Abstract: Certain substituted 6,7-dihydro-7-hydroxy-1-oxo-1H,5H-benzo[ij]quinolizine-2-carboxylic acids and salt and ester derivatives thereof are described. These compounds are useful antibacterial agents.

Abstract: Amino acids having masked amino groups react with amino acids having masked carboxyl groups to form peptide derivatives in good yields if the reaction medium contains an isonitrile. Isonitriles also are effective in causing condensation of amino acids having masked amino groups with compounds having active hydroxyl groups to the corresponding amino acid esters. The yields of the first-mentioned reaction are enhanced if the reaction mixture additionally contains one of the compounds having active hydroxyl groups. Both the peptide derivatives and the amino acid esters of the compounds having active hydroxyl groups are useful for peptide synthesis.

Abstract: Sulfonyl-ureas of the formula X--CO--NH--A--SO.sub.2 --NH--CO--NH--R.sup.1, in which R.sup.1 represents cyclopentylmethyl, alkyl-cyclopentylmethyl or dialkyl-cyclopentylmethyl, having up to 2 carbon atoms in the alkyl rest, or cyclopentylethyl, X represents a. ##SPC1##In which R.sup.2 represents hydrogen, F, Cl, Br, CF.sub.3, CH.sub.3 or OCH.sub.3,b. ##SPC2##In which R.sup.3 represents hydrogen, Cl or CH.sub.3,c. ##SPC3##In which R.sup.4 represents hydrogen, Cl or Br,A represents one of the groupings ##SPC4##And their physiologically tolerated salts, process for preparing them and pharmaceutical preparations containing them.

Abstract: Mono-esters of .alpha.-carboxypenicillins and their preparation are described including intermediates for the mono-esters. The mono-esters are esterified on the .alpha.-carboxy group. They are well absorbed orally and de-esterified in vivo to give high serum concentrations of the parent .alpha.-carboxypenicillins.

Abstract: A process is described for the preparation of pyrimidine derivatives having therapeutic properties. They have the general formula: ##SPC1##Wherein A represents an alkylene or alkenylene grouping which together with the carbon atoms of the pyrimidine nucleus to which it is attached forms a homocyclic ring containing five to seven carbon atoms, which homocyclic ring may carry one or more halogen, lower alkyl and/or lower alkoxy substituents and R represents an amino, lower alkylamino or di(lower)alkylamino group, or a nitrogen-, oxygen- or sulphur-containing saturated or unsaturated mononuclear heterocyclic group linked to the pyrimidine ring either through a carbon atom or, when the group contains a nitrogen atom, either through the nitrogen atom or a carbon atom and are prepared by reacting a cycloaliphatic(A)oaminonitrile with a nitrile of the formula R-CN where A and R have the above meanings in the presence of a basic alkali metal-containing compound and then reacting the resultant intermediate with water.

Abstract: A process for the preparation of methyl 3-(2-quinoxalinylmethylene)carbazate N.sup.1,N.sup.4 -dioxide which comprises contacting a 2-quinoxalinecarboxaldehyde N.sup.1,N.sup.4 -dioxide nitrone with at least about an equimolar proportion of methyl carbazate in acidic solvent medium until reaction is substantially complete.

Abstract: Iminoisoindolinone pigments of the formula ##SPC1##WhereinX represents halogen atoms,Y represents a halogen atom, an alkoxy, cycloalkoxy, aralkoxy, aryloxy, alkylthio or arylthio group,R represents an aromatic radical containing a cyclic bound -CONH group, andQ represents an O-atom or the group =N--R and are useful for coloring plastics and lacquers in yellow shades having excellent fastness properties.

Abstract: Racemic 3-aminomethylene-6,7-dimethoxy-2-methyl-4-oxo-1,2,3,4-tetrahydro-1-quinoli ne carboxylic acid, alkyl, phenyl and benzyl esters as analgesic agents, synthesized from 3-hydroxymethylene-6,7-dimethoxy-2-methyl-4-oxo-1,2,3,4-tetrahydro-1-quino line carboxylic acid, alkyl, phenyl and benzyl esters and the dextrorotatory enantiomer 3-aminomethylene-6,7-dimethoxy-2-methyl-4-oxo-1,2,3,4-tetrahydro-1-quinoli ne carboxylic acid, ethyl ester, an outstanding analgesic agent.