Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S-- where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.

Abstract: Compounds of the tautomeric formula ##STR1## wherein R, R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is straight or branched alkyl, optionally interrupted by heteroatoms such as oxygen, sulfur or nitrogen; straight or branched alkenyl; alkynyl; cyano; cycloalkyl or cycloaliphatic alkyl; a bicyclic group; aryl; or a heterocyclic group; orR.sub.2 and R.sub.3, together with each other and the nitrogen atoms to which they are attached, form a heterocyclic group;R.sub.4 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; andHet is a substituted or unsubstituted heterocycle containing two or three heteroatoms;tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.

Abstract: 2,3-Unsaturated nitrogen-containing heterocyclic compounds with a 3-nitro group and a 2-heterocyclyl alkylamino group. The alkyl group of 2-position substituents is preferably interrupted by sulfur or oxygen. The compounds of the invention are preferably dihydropyrroles or tetrahydropyrridines or pyrimidines. The compounds of the invention are histamine H.sub.2 -receptor antagonists.

Abstract: A process for the preparation of a urea derivative having the formula: ##STR1## in which A represents a straight- or branched-chain alkyl group having 1-20 carbon atoms, an aryl group, or a heterocyclic group, and each of R.sup.1 and R.sup.2 represents hydrogen, a straight- or branched-chain alkyl group having 1-20 carbon atoms, an alicyclic group, or an aryl groups, which comprises:reacting sodium salt of an N-halogenamide with a quaternary ammonium salt to obtain its addition salt and then,reacting said addition salt with an amine derivative in the absence or presence of an organic solvent.

Abstract: 1-Heterocyclic-2-pyrrolidinone analogs, and intermediates thereof, as aquatic and terrestrial herbicides and aquatic algicides. The compounds and intermediates can also be used together with one or more herbicides to provide useful terrestrial herbicidal combinations.

Abstract: This invention relates to new N-(5-aminomethyl-2-oxazoline-2-yl)-N'-phenylureas, the method for producing them and their application in therapy, particularly in treating convulsions, rhythm troubles, ulcerous disorders or inflammatory or edematous conditions.The products of this invention have the general formula: ##STR1## wherein R.sub.1 and R.sub.2 independently represent an alkyl radical of C.sub.1 to C.sub.4, or a carbocyclic alkyl radical having 3 or less rings, or a carbocyclic radical having 3 or less rings; R.sub.1 and R.sub.2 can form, with the nitrogen atom to which they are attached, a 4 to 7 member heterocycle containing 1 or 2 nitrogen atoms and 1 or 0 oxygen atoms, said heterocycle can be substituted by R with R being an alkyl radical of C.sub.1 to C.sub.4, allyl, benzyl, pyridyl, phenyl substituted or not by one or more substituents such as halogen, trihalomethyl, alkyl of C.sub.1 to C.sub.4, hydroxy, or alkoxy having a C.sub.1 to C.sub.4 alkyl radical.

Abstract: This invention relates to new 2-amino-5-aminomethyl-2-oxazolines, the method of preparing them, and their pharmacological properties making possible their application in cardiovascular, psychotropic, antiinflammatory antiallergic, antihistamine, antiH.sub.2 therapy.These new products have the general formula: ##STR1## wherein R.sub.1 and R.sub.2 independently represent an alkyl radical of C.sub.1 to C.sub.4, or a carbocyclic alkyl radical having less than 4 rings, or a carbocyclic radical having less than 4 rings; R.sub.1 and R.sub.2 can form, with the nitrogen atom to which they are attached, a 4 to 7 member heterocycle containing 1 or 2 nitrogen atoms, and either 1 or 0 oxygen atoms. This heterocycle can be substituted by R with R being a lower alkyl, allyl, benzyl, pyridyl, phenyl substituted or not by one or more substituents such as halogen, trifluoromethyl, methyl, methoxy, hydroxy.

Abstract: Described are oxazolyl (or thiazolyl) hydrazinoalkyl nitrile compounds of the formula ##STR1## wherein R is hydrogen or loweralkyl, R.sub.1 and R.sub.2 independently of one another denote hydrogen, loweralkyl, or phenyl or naphthyl substituted with halo, loweralkyl or loweralkoxy, X is oxygen or sulfur, n and m are each an integer from 0 to 3 inclusive, or pharmaceutically acceptable salts thereof. The compounds are useful as anti-inflammatory agents.

Abstract: The invention relates to a guanidine derivative of the formula: ##STR1## in which W is a 2-6C alkylene chain optionally substituted by 1 or 2 1-4C alkyls; E is O, S, SO, SO.sub.2 or NR.sup.3 in which R.sup.3 is H or 1-6C alkyl; R.sup.1 is H or a straight chain 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls; or R.sup.1 and R.sup.3 are joined to form a morpholine, pyrrolidine, piperidine or piperazine ring; X, P, Y, Q and R.sup.2 are as defined in the specification, and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing process, pharmaceutical compositions and intermediates are also described. The compounds of the formula I are histamine H-2 antagonists.

Abstract: Novel antibacterially-active esters of antibiotic nodusmicin. Activity is demonstrated against Staphylococcus aureus, Streptococcus pyogenes, and Sarcina lutea. Thus, these esters can be used in various known environments, using well-known procedures, to eradicate or control susceptible microbes.

Abstract: The compounds are novel N-substituted-N'-heterocyclic alkylthioureas, guanidines and 1-nitro-2,2-diaminoethylene compounds which are histamine H.sub.2 -antagonists.

Abstract: Cephalosporin broad spectrum antibiotics possessing a 7.beta.-[2-[(2-aminooxazol)-4-yl]-2-(substituted oximino)]acetamido side chain and a variety of substituents at the 3-position of the cephalosporins are claimed. Also claimed are intermediates in the synthesis of the above cephalosporin antibiotics.

Abstract: Cephalosporin broad spectrum antibiotics possessing a 7.beta.-[2-[(2-aminooxazol)-4-yl]-2-(substituted oximino)acetamido side chain and a variety of substituents at the 3-position of the cephalosporins are claimed. Also claimed are intermediates in the synthesis of the above cephalosporin antibiotics.

Abstract: 5-Membered, 6-membered and 7-membered heterocyclic derivatives of guanidine having hypoglycemic activity.

Abstract: A compound, with hypoglycaemic activity, having formula (II) or a pharmaceutically acceptable acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur;R.sup.1 R.sup.2 are the same or different and represent hydrogen, halogen, C.sub.1-6 alkyl, phenyl, benzyl,C.sub.3-6 cycloalkyl, carbo-C.sub.1-6 alkoxy or C.sub.1-6 carboxy or R.sup.1 and R.sup.2 represent the remaining members of a benzene ring;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, phenyl or benzyl;R.sup.4 represents hydrogen or C.sub.1-6 alkyl;R.sup.5 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.4 and R.sup.5 together represent the remaining members of a 5- or 6- membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl; andR.sup.

Abstract: 3-Nitro-2-substituted aminopyrroles are histamine H.sub.2 -receptor antagonists. The 2- position substituent is a fully-unsaturated heterocyclyl alkyl group preferably with alkyl group interrupted by sulfur or oxygen. The 4- and 5- positions of the pyrrole ring can also be substituted.

Abstract: Oxothia compounds, especially 2-oxo-2,3-dihydro-benzo[b]-thiophene compounds of the formula ##STR1## in which Ph represents an optionally substituted 1,2-phenylene radical, X represents oxygen or sulphur, R.sub.1 represents an organic radical bonded via a carbon atom and R.sub.2 denotes hydrogen or an optionally substituted hydrocarbon radical of aliphatic character, and their salts are useful as peripheral analgetics and/or as antiphlogistic uricosuric and/or thrombolytic agents.

Abstract: Broad spectrum cephalosporin antibiotics represented by the formula, ##STR1## pharmaceutical compositions of the antibiotics, and a method for treating infections are provided. In the formula, R is 2-aminooxazol-4-yl, 5-amino-1,2,4-oxadiazol-3-yl or 5-aminoisoxazol-3-yl; R' is eg. C.sub.1 -C.sub.4 alkyl; R.sub.1 is H, NH.sub.2, chloro, C.sub.1 -C.sub.4 NH--, (C.sub.1 -C.sub.4).sub.2 N--, etc. The antibiotics are best prepared by reacting a pyrazine with a 3-iodomethyl cephalosporin.

Abstract: Broad spectrum cephalosporin antibiotics represented by the formula ##STR1## wherein R is a 3-aminoisoxazol-5-yl, 2-aminooxazol-4-yl, or a 5-amino-1,2,4-oxadiazol-3-yl group; R.sub.1 is isoquinolinium or substituted isoquinolinium; and R' is C.sub.1 -C.sub.4 alkyl, an N-substituted carbamoyl group, or a carboxy-substituted alkyl or cycloalkyl group; and the pharmaceutically acceptable non-toxic salts thereof; are prepared by the reaction of a 3-iodomethyl cephalosporin, having the above 2-(amino-substituted heterocyclic)-2-oximinoacetyl side chain, with isoquinoline or a substituted isoquinoline. Pharmaceutical formulations of the antibiotics and a method for treating bacterial infections with the antibiotics are provided.

Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which one of R.sub.1 and R.sub.2 represents hydrogen, halogen or a C.sub.1-4 alkyl group which may be optionally substituted by hydroxy or C.sub.1-4 alkoxy, and the other represents the group R.sub.4 R.sub.5 NAlk-- in which R.sub.4 represents hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, heteroaralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkylamino or cycloalkyl, and R.sub.5 represents hydrogen or a C.sub.1-4 alkyl group or R.sub.4 and R.sub.5 may, together with the nitrogen atom to which they are attached, form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.

Abstract: Broad spectrum cephalosporin antibiotics represented by the formula ##STR1## are provided. In the formula, R represents a 2-aminooxazol-4-yl, 5-amino-1,2,4-oxadiazol-3-yl, or 5-aminoisoxazol-3-yl heterocyclic group; R' is hydrogen, C.sub.1 -C.sub.4 alkyl, a carboxy-substituted alkyl or cycloalkyl group or a C.sub.1 -C.sub.4 alkyl ester or carboxy-protecting ester derivative thereof; or an N-substituted carbamoyl group; and R.sub.1 and R.sub.2 are independently hydrogen or a substituent group, eg. halo, hydroxy, amino, carbamoyl, alkyl, or trifluoromethyl. The antibiotics are useful in a method for treating bacterial infections and can be formulated into pharmaceutical formulations for such use.

Abstract: 1-(2,6-disubstituted benzoyl)-3-(4-alkoxycarbonyl-5-oxazolyl)ureas useful as insecticides.

Abstract: This invention relates to trifluorethylamines and to a process for producing the same.These trifluorethylamines are substituted on the nitrogen atom with a lower alkyl or a cyclo lower alkyl radical.They are endowed with interesting pharmacological properties.

Abstract: Amidinosulphonic acid derivatives carrying an unsaturated nitrogen heterocycle-containing substituent, representative of which are N-methyl-N'[2-(5-methyl-4-imidazolylmethylthio)- ethyl] amidinosulphonic acid and N-methyl-N'-[2-(3-chloropyrid-2-ylmethylthio) ethyl] amidinosulphonic acid, are histamine H.sub.2 -receptor antagonists.

Abstract: Bisamidines carrying one unsaturated nitrogen heterocyclo-containing substituent, representative of which i; 1-[N'-(2-(5-methyl-4-imidazolyl)methylthio)ethyl)guanidino]-8-[N'-methylgu anidino]octane, are histamine H.sub.2 -antagonists.

Abstract: Guanidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. These derivatives have the formula: ##STR1## in which X is oxygen or sulphur;Y is nitrogen or a CH radical;n is 1, 2, 3 or 4;m is 0 or 1;R.sup.1 is, for example, hydrogen or alkyl of 1-6 carbons; andR.sup.2 is, for example, ##STR2## and are characterized by the guanidino and cycloalkyl substituents which are attached directly to the heterocyclic ring.

Abstract: This invention provides a convenient and commercially adaptable process for the preparation of vinylcyclopropane derivatives in high yield. For the process an alkylating agent and activated methylene compound are reacted in the presence of an alkylene oxide derivative and alkali metal compound. Water can also be present and/or the reaction may be carried out in an inert organic diluent.

Abstract: This invention provides a convenient and commercially adaptable process for the preparation of vinylcyclopropane derivatives in high yield. For the process an alkylating agent and activated methylene compound are reacted in the presence of a cyclic polyether compound and alkali metal compound. Water can also be present and/or the reaction may be carried out in an inert organic diluent.

Abstract: A class of novel compounds is disclosed which has utility as plant growth regulators, having the general formula: ##STR1## in which X is O or S,Y is one of the group: ##STR2## R is H or CH.sub.3, Q is phenyl or chlorophenyl whenQ' is hydrogen, or Q and Q' together may form the remainder of a benzene ring.

Abstract: This invention relates to novel substituted aryl lower alkamine and more precisely to arylmethylamine, the methyl group of which is substituted with one more polyfluoromethyl radicals.This invention also relates to the process for producing said compounds.The resulting compounds have pharmacological utility and may be used as a drug in human and veterinary medicine.

Abstract: Certain phenyl amines have been prepared wherein the "methyl" carbon is substituted with a polyfluoroalkyl radical. The compounds form acid addition salts, exist in resolvable stereoisomeric forms, and are useful for treating hypertension. Formulations for human and veterinary medicine are described, as well as methods of use.

Abstract: The guanidine derivative has the formula: ##STR1## where X is O or S: Y is N, CH or CCH.sub.3 : m is 0 or 1: R.sup.1 is hydrogen and R.sup.2 cyano, trifluoroacetyl, C.sub.1-6 alkanoyl, 4,5-dihydro-4-oxothiazol-2-yl or A-B where A is 3,4-dioxocyclobutene-1,2-diyl or C.dbd.Z where Z is oxygen, sulphur, NCN, NNO.sub.2, CHNO.sub.2, NCONH.sub.2, C(CN).sub.2, NCOR.sup.6, NCO.sub.2 R.sup.6, NSO.sub.2 R.sup.6 or NR.sup.7 where R.sup.6 is C.sub.1-6 alkyl and R.sup.7 is hydrogen or C.sub.1-6 alkyl and B is C.sub.1-6 alkyl, alkoxy or alkylthio or NR.sup.8 R.sup.9 where R.sup.8 and R.sup.9 are hydrogen, C.sub.1-10 alkyl, C.sub.3-10 -alkenyl, alkynyl or alkoxyalkyl, C.sub.2-6 (primary hydroxy)alkyl, or, when R.sup.9 is hydrogen, R.sup.8 is 2-[[5-dimethylaminomethylfuran-2-yl]methylthio]-ethylamino or R.sup.8 and R.sup.9 are together a 5- or 6-membered non-aromatic ring optionally containing an additional N or O; or R.sup.1 and R.sup.2 are together imidazolidin-2-ylidene: R.sup.3 is hydrogen or fluorine: R.sup.

Abstract: The compounds are ethylene derivatives which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A compound of this invention is 1-nitro-2-methylamino-2-[2-((4-methyl-5-imidazolyl)methylthio)-ethylamino] ethylene.

Abstract: Described are acyl glycine oxazolines of the formula: ##STR1## where R is lauryl, C.sub.11 H.sub.23, oleyl or stearyl; and R' is hydrogen or lower alkyl. Also disclosed are motor fuel compositions in the gasoline boiling range containing a corrosion-inhibiting and detergent amount of the above compounds.

Abstract: Certain arylmethyl amines have been prepared wherein the "methyl" carbon is substituted with a polyfluoroalkyl radical. The compounds form acid addition salts, exist in resolvable stereoisomeric forms, and are useful for treating hypertension. Formulations for human and veterinary medicine are described, as well as methods of use.

Abstract: This invention provides a convenient and commercially adaptable process for the preparation of vinylcyclopropane derivatives in high yields. The process involves reacting an alkylating agent and an activated methylene compound in the presence of an onium compound, an alkali metal compound and water, which while only necessary in trace amounts can be present in substantial quantities.

Abstract: A compound, with hypolgycaemic activity, having formula (II) or a pharmaceutically acceptable quaternary ammonium or acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur; n.sub.7 represents zero or 1;R.sup.7 represents hydrogen or C.sub.1-6 alkyl;R.sup.1 and R.sup.2 are the same or different and represent hydrogen, C.sub.1-6 alkyl, phenyl, benzyl, or C.sub.3-6 cycloalkyl;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, phenyl or benzyl;R.sup.4 represents hydrogen or C.sub.1-6 alkyl;R.sup.5 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.4 and R.sup.5 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.

Abstract: Spin labels, especially dianionic aromatic spin labels which can bind to the first specific high-affinity bilirubin-binding site on serum albumin, and which are quantitatively displaceable into solution from said site in the presence of bilirubin, can be used in an assay for bilirubin-binding capacity. In the assay, an excess of spin label is mixed with the serum albumin or serum and is titrated with standard bilirubin. ESR spectroscopy indicates a change in the rate of spin label release with addition of bilirubin, giving a value indicative of bilirubin-binding capacity. Novel dianionic aromatic spin labels are also disclosed.

Abstract: Organic chemical compounds based upon the urea molecule are disclosed which have potent gastric secretion inhibitory properties. The urea is substituted with a heterocyclic ring which may be substituted with one or more loweralkyl groups. The urea is also substituted with loweralkyl and a lower-alkylamino loweralkyl group. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.

Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.

Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-guanidines which are inhibitors of histamine activity.

Abstract: Novel compounds are described of the formula ##STR1## where R is C.sub.2-6 alkyl, R.sup.1 and R.sup.2 are hydrogen or C.sub.1-4 alkyl and n is 3 to 6. The compounds are useful in the prophylactic treatment of immediate hypersensitivity diseases including asthma.

Abstract: A class of novel 2-oxazolyl ureas and carbamates having anti-allergic activity are described together with methods of making such compounds and pharmaceutical compositions containing the active compounds of the invention.

Abstract: Photographic silver halide emulsions show increased speed and reduced latent image fading when a compound of the following structure is incorporated: ##STR1## wherein: X is ##STR2## Y.sup.1 and Y.sup.2 individually represent hydrogen or an aromatic nucleus or together represent the atoms completing a fused aromatic nucleus;Z is ##STR3## R is hydrogen or lower alkyl of from 1 to 5 carbon atoms; and R.sup.1 is hydrogen or methyl.