Abstract: The present invention also provides novel compositions of matter. In particular, the present invention provides novel 3-substituted compounds of formula I which are from among the selected 5,6,7,8-tetrahydroquinolines and 5,6-dihydropyrindines having use as inhibitors of the synthesis of leukotrienes and as inhibitors of the action of lipoxygenase in mammalian metabolism.

Abstract: Isoindolazines which, in one of their tautomeric structures, have the formula ##STR1## where the rings designated X and T can be substituted andA.sup.1 and A.sup.2 represent the divalent radical of a compound having two replaceable hydrogen atoms on a C or N atom, in particular the divalent radical of an active methylene compound, of an amine, of a hydrazine, of a hydrazide or of a hydrazone,salts and complexes of these compounds, processes for their preparation, and their use as pigments.

Abstract: Carbostyril derivative or a pharmaceutically acceptable acid addition salt thereof, having excellent platelate aggregation inhibitory effect, calcium antagonism, hypotensive effect and phosphodiesterase inhibitory effect are useful as prophylactic or treating agents for thrombosis, circulation improving agents for coronary blood flow such as coronary vasodilators, hypotensive agents and phosphodiesterase inhibitors. Furthermore, the carbostyril derivatives are weak in heart rate increasing activity and also in cardiac muscle contraction increasing activity, and the carbostyril derivatives are useful agents for curing and treating heart diseases such as cardiac angina and myocardial infarction caused by hypercoagulability of the platelets. Processes are disclosed for preparation of the carbostyril derivatives.

Abstract: 4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R.sup.1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R.sup.2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR.sup.3, --SCOR.sup.3 or --S(O).sub.n --R.sup.3 (R.sup.3 being a hydrocarbyl group and n an integer 1 or 2), R.sup.4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO.sub.3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.

Abstract: Compounds of the formula: ##STR1## wherein, R is H, alkyl, cycloalkyl, aryl, or heteroaryl;R.sub.1 is H, alkyl, cycloalkyl, aryl, heteroaryl, substituted heteroaryl, aralkyl, substituted aryl, halo, OR.sup.2, SR.sup.2, NR.sub.2, CF.sub.3, NO.sub.2, CN, COOR.sup.2, CHO, SO.sub.3 H or SO.sub.2 NH.sub.2,whereinR.sup.2 is H, methyl, ethyl or propyl;Y is ##STR2## Z is O, S, NH or CH.sub.2 ; X is --CH.sub.2 --, ##STR3## or --(CH.sub.2).sub.n CHOH(CH.sub.2).sub.n --; whereinR.sup.2 is H, methyl, ethyl or propyl;n is 1-10, and pharmaceutically acceptable salts thereof have antiallergy and antiinflammatory activity.

Abstract: Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula --OR.sub.5, ##STR2## or --S--S--R.sub.5 wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.

Abstract: Cyclohexane-1,3-dione derivatives of the formula ##STR1## where A is an unsubstituted or substituted, saturated or unsaturated 4-membered to 7-membered heterocyclic structure which contains from 1 to 3 nitrogen atoms and may be fused to an aromatic radical, R.sup.1 is hydrogen, methoxycarbonyl, ethoxycarbonyl, methyl or cyano, R.sup.2 is alkyl and R.sup.3 is alkyl, haloalkenyl or propargyl, and salts of these compounds, are useful for controlling undesirable plant growth.

Abstract: Acylanilides of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are substituents defined in claim 1; wherein R.sup.4 is hydrogen or alkyl of up to 4 carbon atoms, or is joined to R.sup.5 as stated below;wherein R.sup.5 is hydrogen, hydroxy, or alkoxy or acyloxy each of up to 15 carbon atoms, or is joined to R.sup.4 to form an oxycarbonyl group such that together with the --N--CO--C-- part of the molecule it forms an oxazolidinedione group;wherein R.sup.6 is alkyl or halogenoalkyl of up to 4 carbon atoms;and wherein R.sup.7 is 5- or 6- membered saturated or unsaturated heterocyclic which contains one, two or three hetero atoms selected from oxygen, nitrogen and sulphur, which heterocyclic may be a single ring or may be fused to a benzo-ring, and which heterocyclic is unsubstituted or bears one or two substituents defined in claim 1;processes for their manufacture and pharmaceutical compositions containing them. The compounds possess antiandrogenic activity.

Abstract: X is in the 8 position and is O(CH.sub.2).sub.n, N(CH.sub.2).sub.n ;Y is O(CH.sub.2).sub.n, N(CH.sub.2).sub.n ;R.sub.2 is monosubstituted or independently disubstituted H, carboxyl, or alkylcarboxy;Z is 0; andn is 0 to 10 inclusive,useful in the treatment of ischemic heart disease and hypertriglyceridemia.

Abstract: 4-Hydroxy-2-quinolone derivatives are useful for their anti-inflammatory, anti-allergenic, antitussive and expectorant activity. Pharmaceutical compositions containing said compounds and pharmaceutically acceptable salts thereof and methods of treating humans and animals are described herein.

Abstract: Animal feeds and drinks containing small amounts of compounds of the formula Ia or Ib ##STR1## where R.sup.1 is hydrogen, low molecular weight alkyl or alkoxy, or halogen, R.sup.2 is hydrogen or low molecular weight alkyl and R.sup.3 and R.sup.4 are hydrogen or a low molecular weight aliphatic or araliphatic radical. The compounds of the formulae Ia and Ib promote growth without exerting an antibiotic action.

Abstract: Quinolinone derivatives of the formula (I) ##STR1## in which X represents oxy or a direct bond, R.sub.1 represents an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical or hydrogen, Ph represents an optionally additionally substituted 1,2-phenylene radical containing the group R.sub.1 --X--C(O)--, and one of the radicals R.sub.2 and R.sub.3 represents an optionally esterified or amidated carboxy group R.sub.4 and the other represents hydrogen or an aliphatic radical or, in the case of a radical R.sub.3, hydroxy, and in which either R.sub.A and R.sub.B together represent oxo, R.sub.C and R.sub.D together represent an additional bond, or, when R.sub.2 represents a radical R.sub.4, R.sub.C is hydrogen and R.sub.3 and R.sub.D together represent oxo, and R.sub.E represents a radical R.sub.5 which represents hydrogen or an aliphatic, cycloaliphatic, araliphatic heterocyclic-aliphatic radical, or R.sub.A represents an optionally etherified hydroxy group and R.sub.

Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is hydroxy, C.sub.1-4 alkoxy or an in-vivo hydrolysable acyloxy group:R.sub.2 is hydrogen, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy or an in-vivo hydrolysable acyloxy group;R.sub.4 is benzofuryl, benzothienyl, indolyl, quinolyl, isoquinolyl,2,3-dihydrobenzofuryl, 2,3-dihydrobenzylthienyl or 2,3-dihydroindolyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, hydroxy or acyloxy, trifluoromethyl, halogen or nitro; andA is a bond or C.sub.1-6 alkylene,a process for their preparation, and pharmaceutical compositions containing them.

Abstract: The invention concerns novel compounds of the formula I ##STR1## The compounds are herbicides and in further embodiments the invention provides herbicidal compositions containing as active ingredient a compound of formula I and a process for severely damaging or killing unwanted plants by applying to the plants or to the growth medium of the plants an effective amount of a compound of formula I.

Abstract: Novel carbostyril derivative and its salt represented by the general formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a phenyl-lower alkyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a group of the formula ##STR2## wherein A is a lower alkylene group; R.sup.3 is a lower alkyl group, a hydroxy lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkanoyloxy-lower alkyl group or a benzoyloxy-lower alkyl group; and R.sup.4 is a C.sub.3-10 -cycloalkyl group which may have at least one hydroxyl group as the substituent(s) in the cycloalkyl ring, a C.sub.3-10 -cycloalkyl-lower alkyl group, a phenyl group, a phenyl-lower alkyl group which may have at least one lower alkoxy group as the substituent(s) in the phenyl ring, a lower alkyl group which may have at least one hydroxyl group as the substituent(s), a heterocyclic ring residue or a lower alkyl group having one heterocyclic ring residue as the substituent; further, R.sup.3, R.sup.

Abstract: Novel 3-methoxy-2-oxoazetidine derivatives, which are shown by the following formula ##STR1## wherein R.sub.1 is amino, acylated amino or protected amino, are of value as intermediates for the synthesis of useful compounds represented by the formula ##STR2## wherein R.sub.1 has the same meaning as defined above, as drugs in the treatment of bacterial infections.

Abstract: Described are compounds of the formula ##STR1## wherein R.sub.2 -R.sub.8 independently of one another denote hydrogen, loweralkyl, phenyl, alkoxy, halo, hydroxy, nitro, trifluoromethyl, ##STR2## with the proviso that at least one but no more than one of the substituents R.sub.2 -R.sub.8 is ##STR3## and with the further provisos that at least four of the substituents R.sub.2 -R.sub.8 are hydrogen and R.sub.2 cannot be ##STR4## when R.sub.3 -R.sub.8 are hydrogen, and pharmaceutically acceptable salts thereof.The compounds are effective as antiinflammatory and antiasthma agents.

Abstract: Compounds are prepared which correspond to the formula ##STR1## wherein R represents a nitrogen containing heterocyclic radical corresponding to one of the formulae ##STR2## each X independently represents chloro, fluoro, bromo, nitro, alkyl of 1 to 4 carbon atoms, amino, mono- or dialkylamino wherein each alkyl group independently contains from 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 carbon atoms, alkylsulfinyl of 1 to 4 carbon atoms, alkylsulfonyl of 1 to 4 carbon atoms, cyano, trifluoromethyl, trichloromethyl, phenoxy or substituted phenoxy of the formula ##STR3## wherein each Z independently represents chloro, fluoro, bromo, nitro, cyano, alkoxy of 1 to 4 carbon atoms or alkylthio of 1 to 4 carbon atoms, with the proviso that when either n is 2 or 3, all X groups are sterically compatible with each other and all Z groups are sterically compatible with each other; Y represents oxygen or sulfur; each n can independently represent an integer of from 0 to 3, inclusive; R.sup.

Abstract: A process for the preparation of aromatic sulfohalides by reacting an aqueous solution, containing a hydrogen halide, of an aromatic diazonium halide with sulfur dioxide, wherein(a) the aqueous solution, containing the hydrogen halide, of a diazonium salt which is derived from the corresponding aromatic amine and the halogen of the desired sulfohalide is reacted with sulfur dioxide in the presence of an inert organic solvent which is immiscible or only partially miscible with water,(b) the diazonium salt is decomposed, simultaneously or subsequently, by means of a catalyst for diazonium salt decomposition and(c) the resulting reaction mixture, or the organic phase thereof after removal of the aqueous phase, is treated with an oxidizing agent.

Abstract: An improved process for selectively N-acylating hydroxy-amino-arylsulfonic acids is disclosed wherein the hydroxy-amino-arylsulfonic acid is dissolved in water by treatment with an alkaline lithium salt, such as lithium hydroxide, and the acylation is conducted while maintaining the pH at about 3-6. The N-acyl-hydroxy-amino-arylsulfonic acids are useful as dyestuff precursors.

Abstract: The known synthesis for the production of aromatic substituted acetonitriles by reaction of aromatic substances with cyanogen chloride in the gas phase is improved by feeding the starting materials in gaseous form and separated from each other into the reactor. The process can be used to synthesize in general aromatic and especially hetero-aromatic substituted acetonitrile.

Abstract: There is disclosed a process for the preparation of dihydroxyquinoline and certain derivatives thereof. The compounds have the structure: ##STR1## where X=Cl, Br, I, NO.sub.2, HY=--CN, --H --COOHThe process comprises the reaction of isatoic anhydride or its derivatives with alkyl esters of cyanoacetic acid to form an intermediate compound such as 2-(2'-aminobenzoyl)cyanoacetate which subsequently undergoes cyclization to form 3-cyano-2,4-diydroxyquinoline (when X is hydrogen) or its derivatives (where X is Cl, Br, I or NO.sub.2). The cyano group may be cleaved under alkaline conditions to convert Y from --CN to --H or under acid conditions to convert Y from --CN to --COOH.

Abstract: Heterocyclic ethanolamines of the formulaHet--CHOH--CH.sub.2 --NH--aralkylwhere het is a 10 membered N heterocycle are disclosed. The compounds are useful as pharmaceuticals.

Abstract: The invention concerns novel compounds of formula IX--A--S--Y (I)wherein X is a radical selected from imidazolyl, pyridyl, quinolyl, tetrahydropyridyl or piperidyl any of which may be substituted and Y is any of the above radicals or a pyridinium radical, A is alkylene of 1-6 carbon atoms. Most of the compounds are anti-ulcer agents but some have anti-hypertensive activity, eg where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.

Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## and functional derivatives thereof, are anti-inflammatory agents.

Abstract: 9-Amino-1-hydroxyoctahydrobenzo[c]quinoline derivatives of formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein R is hydrogen, COR.sub.7 or SO.sub.2 R.sub.8 where R.sub.7 is hydrogen, alkyl, having from one to five carbon atoms; alkenyl and alkynyl each having from two to six carbon atoms; trifluoromethyl, benzyl, furyl, thienyl, pyridyl or R.sub.9 C.sub.6 H.sub.4 where R.sub.9 is H, NH.sub.2, F, Cl, Br, CH.sub.3 or OCH.sub.3 ; R.sub.8 is alkyl having from one to five carbon atoms or R.sub.9 C.sub.6 H.sub.4 ; R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl having from one to five carbon atoms or --CO--(CH.sub.2).sub.p --NR.sub.2 R.sub.3 wherein p is 0 or an integer from 1 to 4; each of R.sub.2 and R.sub.3 when taken individually is hydrogen or alkyl having from one to four carbon atoms; R.sub.2 and R.sub.

Abstract: Compositions which contain a quinolone compound of the general formula ##STR1## wherein n is 0, 1 or 2; R.sub.1 is lower alkyl optionally substituted by hydroxy or C.sub.1-4 alkoxycarbonyl; allyl; propynyl or phenyl- lower alkyl in which the phenyl ring is optionally substituted by 1 or 2 C.sub.1-4 alkoxy groups; R.sub.2 is C.sub.1-4 alkyl with the proviso that when n is 0, R.sub.2 is methyl; and R.sub.3, R.sub.4 and R.sub.5, which may be the same or different, are hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, halo, trifluoromethyl or lower alkylthio show antihypertensive activity.Compounds of general formula ##STR2## in which n, R.sub.1 R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as described above are novel subject to the following provisos (a) when R.sub.3, R.sub.4 and R.sub.4 and R.sub.5 are hydrogen R.sub.2 is methyl and R.sub.1 is lower alkyl, R.sub.1 contains more than one carbon atom, and(b) when R.sub.3 and R.sub.4 are hydrogen, R.sub.5 is hydrogen or 7-methyl, and R.sub.1 is ethyl, R.sub.

Abstract: Imidazolylethoxy derivatives of quinoline-2- or 4-methanols having the general formula ##STR1## and their acid addition salts are useful as antifungal and antibacterial agents.

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: 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: Compounds of the formula ##STR1## where B is oxygen, sulfur, imino or >N--R.sup.1, the ring A may be substituted, and R, Y.sup.1 to Y.sup.4 and Z are conventional dye substituents.The compounds according to the invention give brilliant, very fast dyeings on polyesters and mass-colorations of plastics.

Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## and functional derivatives thereof, are anti-inflammatory agents.

Abstract: A process is provided for preparing pyrazolo-[1,5-c]quinazoline derivatives of the structure ##STR1## wherein X is O or S; R.sup.1 is hydrogen, lower alkyl, hydroxymethyl, phenyl-lower alkyl, phenyl or phenyl substituted with halogen, lower alkyl, lower alkoxy, or trifluoromethyl; R.sup.2 is lower alkoxy, phenyl-lower alkoxy, phenoxy, or phenoxy substituted with lower alkyl or lower alkoxy; and R.sup.3 and R.sup.4 are the same or different and are selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, lower alkanoyloxy of 1 to 4 carbons, nitro, benzyloxy, benzyloxy having a single monolower alkoxy substituent, halogen, hydroxy, and trifluoromethyl, wherein quinolone compounds of the structure ##STR2## which are new intermediates, are reacted with a hydrazine compound to form a 5-(2-aminophenyl)-pyrazole which is then cyclized to the product.In addition, the above product may be reacted with a halogen acid to form the corresponding hydroxymethyl compound.

Abstract: The compounds are amino- or cyano-bearing dihydroquinolines, which have either of the combinations of (a) 2-amino, 3-carboxylic and 4-oxo functions, or (b) 2-oxo, 3-cyano and 4-hydroxy functions, and may be optionally substituted at 1 or 2 of the 5, 6, 7 or 8 positions, eg 1-allyl-2-amino-1,4-dihydro-6,7-dimethoxy-4-oxo-quinoline-3-carboxylic acid ethyl ester, and 1-allyl 3-cyano-1,2-dihydro-4-hydroxy-6,7-dimethoxy-2-oxo-quinoline. The compounds are useful as pharmaceuticals.

Abstract: Certain sulfonamidoquinolines and metal complexes thereof both of which are soluble in essentially water-immiscible organic solvents. The sulfonamidoquinolines have the structural formula ##STR1## where the R, R.sup.1 and R.sup.2 groups and m and n are as defined in the specification and claims hereof. Solutions of the sulfonamidoquinolines and the metal complexes thereof in essentially water-immiscible organic solvents.

Abstract: Imidazolylethoxy derivatives of quinoline-3-methanols having the general formula ##STR1## and their acid addition salts are useful as antifungal and antibacterial agents.

Abstract: Anti-allergic 4-hydroxy-3-nitro-quinoline-2(1H)-ones are prepared by reacting an isatoic anhydride with the carbanion resulting from the treatment of nitro acetic acid alkyl esters with a proton abstracting agent.

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: 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: New quinolone derivatives of the Formula I ##STR1## wherein R.sup.1 and R.sup.2 are each H, F, Cl, Br, CF.sub.3 or CH.sub.3 O or a physiologically acceptable acid addition salt thereof possess pharmacological properties including thrombocyte aggregation inhibiting action.

Abstract: A compound having the formula ##STR1## wherein A denotes an optionally substituted aromatic, isocyclic or heterocyclic residue; R is H, an alkyl residue having from 1 to 6 carbon atoms, an aryl residue having from 6 to 10 carbon atoms or an aralkyl residue having from 7 to 10 carbon atoms; Q is H or a methyl group; X and Y are the same or different and each is a non-water solubilizing group, or X and Y together form a fused aromatic ring system; and R.sub.1 and R.sub.2 are the same or different and each is H or an alkyl radical having from 1 to 22 carbon atoms, and R.sub.3 is hydrogen, an alkyl radical having from 1 to 22 carbon atoms or an aryl radical having from 6 to 10 carbon atoms, the alkyl radicals in R.sub.1, R.sub.2 and R.sub.3 being unsubstituted and uninterrupted or being substituted by an OH, NH.sub.2 or CN group and/or being interrupted by an ethylenic group or an oxygen, sulphur or nitrogen bridge, or two or all three of R.sub.1, R.sub.2 and R.sub.

Abstract: 8-(1H-Tetrazol-5-ylcarbamoyl)quinolines and pharmaceutically acceptable salts thereof are potent anti-allergic agents.

Abstract: 1:1-Metal complexes of azomethines of the formula I ##STR1## wherein A and B are isocyclic or heterocyclic aromatic radicals, with however only one of the radicals A and B being a benzene ring, R represents a hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or an aryl radical, and the complexing metal ions are bivalent cations of the transition metals, zinc ions or cadmium ions which are useful for pigmenting high molecular organic material.

Abstract: Benzenesulfonyl ureas of the formula ##STR1## in which R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Y have the defined meanings, and the salts thereof, process for preparing them, pharmaceutical preparations containing them and their use for lowering the blood sugar level.

Abstract: Anti-allergic 4-hydroxy-3-sulfonyl-quinolin-2(1H)-ones are prepared by reacting an isatoic anhydride with the carbanion resulting from the treatment of sulfonyl acetic acid alkyl esters with a proton abstracting agent.

Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.

Abstract: Anti-allergic 4-hydroxy-3-sulfinyl-quinolin-2(1H)-ones are prepared by reacting an isatoic anhydride with the carbanion resulting from the treatment of sulfinyl acetic acid alkyl esters with a proton abstracting agent.