Abstract: Hydroxyindole-3-carboxylic acid amide compounds of the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, the same or different, respectively a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or a heteroaryl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 are respectively groups which are combined to each other taken together with the adjacent nitrogen atom to form a heterocyclic group, R.sup.5 is an alkyl group, R.sup.6 is a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group or an aralkyl group and X is a hydrogen atom, a halogen atom or a lower alkanoyl group, or their acid addition salts.These compounds are of use as diuretics or a therapeutic medicine for circulation system diseases.

Abstract: Carboxyalkyl urea compounds and derivatives thereof are disclosed which are useful as angiotensin converting enzyme (ACE) inhibitors and as antihypertensives. These compounds and derivatives are represented by the general formula: ##STR1## An illustrative specie falling within this general formula is:N-(2-carboxy-4-phenylbutyl-N-isopropylaminocarbonyl-L-tryptophan.

Abstract: The compound of formula (I): ##STR1## N-cyclohexyl-N"-4-(2-methylthioquinolyl)-N'-2-thiazolyl-guanidine and pharmaceutically acceptable salts thereof is a valuable antiinflammatory, analgesic and antipyretic agent.The compound of the invention may be formulated with conventional pharmaceutically acceptable carriers or diluents to provide a pharmaceutical composition.

Abstract: Quinoline-8-carboxylic acid azolides of the formula ##STR1## where A, X and R have the meanings given in the disclosure, and their use as herbicides.

Abstract: The invention provides compounds of the formulaD--DHC].sub.n (I)and the nontoxic pharmaceutically acceptable salt thereof, wherein D is the residue of a centrally acting drug containing at least one reactive functional group selected from the group consisting of amino, hydroxyl, mercapto, carboxyl, amide and imide, said residue being characterized by the absence of a hydrogen atom from at least one of said reactive functional groups in said drug; n is a positive integer equal to the number of said functional groups from which a hydrogen atom is absent; and [DHC] is the reduced, biooxidizable, blood-brain barrier penetratring lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier, said carrier comprising a bivalent radical of the formula ##STR1## wherein the alkylene group can be straight or branched and can contain 1 to 3 carbon atoms; R.sub.

Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.

Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur; A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 or --S(O).sub.n R.sup.3 groups; any two of the groups A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.

Abstract: New original derivatives are described of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutasnoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl.The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatitis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.

Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are:(a) compounds of the formula[D--DHC] (I)wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier, with the proviso that when [DHC] is ##STR1## wherein R is lower alkyl or benzyl and [D] is a drug species containing a single NH.sub.2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH.sub.

Abstract: A compound of D-phenylalanine derivative for hypoglycemic use, represented by the general formula ##STR1## R.sup.1 is selected from hydrogen, alkyl of 1 to 5 carbon atoms, aryl of 6 to 12 carbon atoms, aralkyl of 6 to 12 carbon atoms, ##STR2## --CH.sub.2 CO.sub.2 R.sup.3, --CH(CH.sub.3)--OCO--R.sup.3, and --CH.sub.2 --OCO--C(CH.sub.3).sub.3 ; R.sup.2 is selected from groups comprising aryl of 6 to 12 carbon atoms, a hetero six-membered ring, a hetero five-membered ring, cycloalkyl, or cycloalkenyl, any of which groups may have one or more substituents; and R.sup.3 is selected from hydrogen and alkyl of 1 to 5 carbon atoms; the salts thereof, and precursors which can be converted thereto in the human or animal body.Some of the compounds are novel per se.

Abstract: p-Aminophenols are provided having the structure ##STR1## wherein m is 0 to 5; X is CH or N; R.sup.1 and R.sup.2 may be the same or different and are H, lower alkyl, aryl, hydroxy, hydroxyalkyleneoxy, alkylthio, alkoxy, alkanoyloxy, aryloxy, halo, carboxy, alkoxycarbonyl or amido; R.sup.3 is H, lower alkyl, alkanoyl or aroyl; and R.sup.4 is H, lower alkyl or alkanoyl, and including acid-addition salts thereof, with the proviso that when X is CH, m is 0 and R.sup.1 is H, and when R.sup.4 is H, R.sup.2 is other than alkoxy, H or hydroxy, and when R.sup.4 is benzoyl, R.sup.2 is other than H.These compounds together with the compounds defined in the above proviso are useful as inhibitors of leukotriene production and as such are useful as antiallergy, anti-inflammatory and anti-psoriatic agents.

Abstract: The invention concerns compounds of formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy; R.sub.2 represents hydrogen or lower alkyl; A represents an alkylene, oxoalkylene or hydroxyalkylene chain each having 2 to 6 carbon atoms, R.sub.3 and R.sub.4 may be in the same or different rings and independently represent hydrogen, lower alkyl, lower alkoxy, amino or halogen and one of X and Y represents nitrogen the other represents CR.sub.5 wherein R.sub.5 is one of the values for R.sub.3 or R.sub.5 is the bond to the NHCO group; or a pharmaceutically acceptable salt thereof, which compounds possess antihypertensive activity while exhibiting reduced CNS depressant properties. Also disclosed are processes for preparing the compounds and pharmaceutical compositions containing them.

Abstract: Quinoline derivatives of the formula ##STR1## where R.sup.1, X, Y and Z have the meanings given in the disclosure, herbicides containing these compounds as active ingredients, and a process for combating unwanted plant growth.

Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed. The oxazepinones and oxazepinethiones prepared by the process have utility as antihistaminics with low sedative potential. Novel intermediate compounds are also disclosed.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 -polymethylene;either R.sub.3 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together are a bond;R.sub.5 is hydrogen C.sub.1-6 alkyl optionally substituted by halogen hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C.sub.1-6 alkyl groups, or C.sub.2-6 alkenyl, amino optionally substituted by a C.sub.1-6 alkyl or C.sub.1-6 alkenyl group or by a C.sub.1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen, or aryl or hetroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C.sub.1-6 alkyl, C.sub.

Abstract: The invention provides an improved process for the preparation of substituted and unsubstituted 2-carbamoyl nicotinic and 3-quinolinecarboxylic acids.

Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## X.sup.-, wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.

Abstract: There are disclosed compounds of the formula ##STR1## wherein W represents a covalent bond or ##STR2## X is N or CR.sup.2 ; Y is O, S, NR.sup.2 or C(R.sup.2).sub.2 when n=0, or N or CR.sup.2 when n=1Z is ##STR3## R.sup.1 is hydrogen, lower alkyl, trifluoromethyl, nitro, hydroxy, lower alkoxy, mercapto, loweralkylthio or halo;R.sup.2 is hydrogen or lower alkyl;n is 0-1;m is 1-6 with the proviso that m is 0-5 when W represents a covalent bond;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, in psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other immediate hypersensitivity reactions.

Abstract: Novel 2-carbamoylnicotinic and 3-quinolinecarboxylic acids and esters are useful intermediate compounds for the preparation of 2-(2-imodazoline-2-yl) pyridine and quinoline herbicides.

Abstract: A novel quinaldinamide derivative having the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents a lower alkyl group or R.sup.1 and R.sup.2 are combined together with the adjacent nitrogen atom to form a 5-7 membered ring; and X represents the hydrogen atom, a lower alkyl group or a lower alkoxy group, and its acid-addition salt, which show prominent central muscle relaxant effect, namely rigidity relieving effect on anemic decerebrated rigidity.

Abstract: Novel compositions are prepared from (1) nitrogen-containing aromatic heterocyclic compound having at least one group of either (a) a carboxylic acid, (b) carboxylic acid ester, (c) carboxylic acid anhydride, (d) carboxylic acid halide, (e) or combination thereof, such as 2-pyridinecarboxylic acid, and (2) an organic fatty amine such as a mixture of C.sub.10 to C.sub.21 fatty amines. These novel compositions are useful as oil and gas well corrosion inhibitors.

Abstract: A compounds of the general formula (I): ##STR1## wherein R.sup.1 is alkyl, lower alkenyl, lower alkynyl, aralkyl, haloalkyl, lower alkoxy-lower alkyl, lower alkylthio-lower alkyl or lower alkoxycarbonyl-lower alkyl group; R.sup.2 is aryl group which may be substituted by one or more groups of halogen atom, lower alkyl, lower alkoxy, lower alkoxycarbonyl, trifluoromethyl, cyano and nitro group; R.sup.3 and R.sup.4 are, the same or different, lower alkyl, aralkyl, haloalkyl or cycloalkyl, or aryl group which may be substituted by one or more groups of halogen atom, lower alkyl, lower alkoxy, trifluoromethyl, cyano or nitro group; R.sup.5 is hydrogen atom, halogen atom, lower alkyl, phenyl which may be substituted or aralkyl which may be substituted; or R.sup.4 and R.sup.5 may be combined to form a group of --(CH.sub.2).sub.n - in which n is 3 or 4, or its 1-oxide or addition salt. which is useful as a plant growth inhibitory agent.

Abstract: A method for the preparation of substituted and unsubstituted 2-[(1-carbamoyl-1,2-dimethyl-propyl) carbamoyl]-3-quinolinecarboxylic, nicotinic and benzoic acids.

Abstract: Quinoline derivatives of the formula ##STR1## where X, n, R.sup.1, R.sup.2 and Y have the meanings given in the description, are used for controlling undesirable plant growth.

Abstract: Compounds of the formula: ##STR1## in which R.sub.1 is C.sub.1-6 alkyl, phenyl, C.sub.3-6 cycloalkyl, phenylalkyl, cycloalkyl-alkyl or ##STR2## R.sub.3 and R.sub.4 being H or alkyl, R.sub.5 being alkenyl or alkynyl, and the sum of the carbon atoms in R.sub.3, R.sub.4 and R.sub.5 being 2 to 5, R.sub.2 is as defined for R.sub.1 and may also represent ##STR3## in which n is 0, 1, 2 or 3, it also being possible for R.sub.1 and R.sub.2 to form, with the nitrogen atom to which they are attached, a 5-, 6- or 7-membered heterocyclic radical which can contain another hetero-atom chosen from O and N and which can carry 1 or 2 substituents, Z is phenyl, pyridinyl, thienyl, thiazol-2-yl or substituted phenyl, X and R.sub.0 are H, halogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, nitro or CF.sub.3, A represents N or CH and E represents N or CH, some of which are known compounds, are therapeutically useful compounds useful in the treatment of anxiety states or of pulmonary, renal, circulatory or cardiovascular disorders.

Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## W is --O--, --S--, ##STR3## when n=0, or W is ##STR4## when n=1, and the dotted line represents an optional double bond; Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, ##STR5## n is 0-1; R.sup.1 is hydrogen, loweralkyl, loweralkoxy, lower alkanoyl, halo, trifluoromethyl, cyano or nitro;R.sup.2 is hydrogen or loweralkyl;R.sup.3 is loweralkyl, perfluoroloweralkyl or perfluorophenyl, with the proviso that when X=N, W=O or S and n=0, R.sup.3 is other than loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and in antithrombotic therapy.

Abstract: There are provided novel 2-(2-imidazolin-2-yl)pyridine and quinoline compounds, a process and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.

Abstract: Herein is disclosed bicyclic-substituted aminoethanol derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for treating hypertension in a mammal.

Abstract: Guanidine derivatives of the formula ##STR1## in which R.sup.2 represents a six-membered aromatic heterocyclic structure which contains at least one nitrogen atom and is substituted by halogen, amino, cyano or formyl and/or by optionally substituted radicals from the series comprising alkyl, alkoxy, alkylamino, dialkylamino, alkylcarbonyl and alkoxycarbonyl, and/or is optionally fused,R.sup.3 represents hydrogen, an optionally substituted radical from the series comprising alkyl, cycloalkyl, alkenyl, alkinyl and aralkyl, or the radical --S(O).sub.n --R.sup.6,the other radicals can have varied meanings, andacid adducts and salts thereof,which possess herbicidal and plant growth regulating activity.

Abstract: Compounds of the formula: ##STR1## wherein X is oxygen or sulfur; Z is oxygen or sulfur; R is pyridyl optionally substituted with 1 to 3 substituents independently selected from halogen, lower alkyl or lower alkoxy optionally substituted with 1 to 3 of the same or different halogen atoms or nitro; R.sup.1 is lower alkyl; and R.sup.2 is a 5- or 6-membered heterocyclic ring containing 1 to 3 ring nitrogens and the remainder of the ring atoms carbon atoms, a quinoline ring or a phenyl ring, all optionally substituted with 1 to 3 substituents independently selected from halogen, trihalomethyl, lower alkyl or lower alkoxy are fungicidal.

Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.

Abstract: The invention provides a process for the preparation of substituted and unsubstituted 2-carbamoyl nicotinic and 3-quinolinecarboxylic acids.

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: Salicylic acid derivatives of the formula I ##STR1## wherein R.sup.1, W, X, Y and Z have the meanings indicated or a physiologically tolerated salt thereof, processes for their preparation, pharmaceutical formulations based on these compounds and their use as antidiabetic agents.

Abstract: 1:2 Nickel or 1:2 copper complexes of a naphthostyril of the formula ##STR1## or of tautomers thereof, in which A, X and Y are as defined in claim 1, are suitable for pigmenting high molecular weight organic material.

Abstract: An improved process for preparing tetrahydroquinolines and related compounds especially 5,6,7,8-tetrahydroquinoline-8-nitriles, amides and thioamides is described. The nitriles and thioamides are anti-ulcer and/or anti-secretory agents. Typically a compound of formula A ##STR1## where M is sodium, potassium, lithium or MgHal where Hal is chlorine, bromine or iodine, is reacted, e.g., in an ether solvent, with a silyl compound R.sub.x.sup.a Si(NCY).sub.4-x (III) wherein R.sup.a is alkyl, cycloalkyl, aralkyl, or aryl, at least one group R.sup.a being a branched chain alkyl, cycloalkyl, aryl or branched chain aralkyl, Y is oxygen or sulphur, x has a value from 1 to 3, then subjecting the product to hydrolysis or alcoholysis, to obtain the corresponding nitrile, amide or thioamide, provided that when a nitrile is desired the molar ratio of compound III to compound A is at least 2:1 and x is 3 and Y is S. The products may be obtained as acid addition salts.Compound A may contain various substituents, e.g.

Abstract: Herein is disclosed bicyclic-substituted aminoethanol derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for treating hypertension in a mammal.

Abstract: 3-Chloro-8-cyanoquinolines of the formula ##STR1## where R.sup.1 is --NR.sup.2 R.sup.3, and R.sup.2 and R.sup.3 are identical or different and are each hydrogen, C.sub.1 -C.sub.8 -alkyl, formyl, cyclohexyl, or phenyl, or together are tetramethylene or pentamethylene, and one methylene group in these radicals can be replaced by oxygen, nitrogen or --N(CH.sub.3), are used for controlling undesirable plant growth.

Abstract: Hydrolysis of nitrile to amide by use of a quaternary ammonium hydroxide at 60.degree. to 95.degree. C.

Abstract: Compounds with the formula: ##STR1## in which R.sub.1 and R.sub.2 represent independently, a linear or branched alkyl, cycloalkyl, phenylalkyl or cycloalkylalkyl group. R.sub.1 and R.sub.2 may also represent an alkenyl or alkynyl group. R.sub.1 and R.sub.2 may also represent a group of the formula --R.sub.3 --Z--R.sub.4 in which R.sub.3 represents an alkylene group, on condition that at least 2 carbon atoms separate the nitrogen atom from the group Z; R.sub.4 represents an alkyl group, and Z an atom of oxygen, sulphur or the group >N--R.sub.5, R.sub.5 representing a hydrogen atom or an alkyl group. R.sub.1 and R.sub.2 may form, with the nitrogen atom to which they are attached, a heterocyclic ring. Ar represents a phenyl, pyridyl or thienyl group, or a substituted phenyl group, A and B representing independently, N or CH--, the group C representing the residue of a benzene or thiophene ring. These compounds can be used as medicaments, in particular, for the various applications of benzodiazepines.

Abstract: Dichloroquinoline derivatives of the formula ##STR1## are prepared as described, and are used as herbicides.

Abstract: Novel 3-quinoline-carboxamides of the formula ##STR1## wherein R is in 6 or 7-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, --CF.sub.3, --SCF.sub.3 and CH.sub.3 S--, R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, phenyl and benzyl, R.sub.2 is --NHR.sub.4, R.sub.4 is selected from the group consisting of alkyl of 2 to 6 carbon atoms, substituted aryl of 6 to 10 carbon atoms and substituted heterocycle of an aromatic character of 3 to 5 carbon atoms with the proviso that when R.sub.4 is a mono substituted aryl or heterocycle, the substituent is different from R of the quinoline when it is a halogen and R.sub.

Abstract: This invention relates to improved hydrocarbon lubricating oil compositions. More particularly this invention relates to hydrocarbon oil compositions which possess improved oxidation inhibition properties through the presence of a new additive functioning as an antioxidant or as an antioxidant catalyst which acts as a chain terminating species for oxidation reactions.

Abstract: The invention concerns compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O,S,--CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or defined substituents and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocyclic or heterocyclic ring optionally carrying one or more defined substituents; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is --CO-- or --CH.sub.

Abstract: The invention relates to urea compounds which are useful as antihypertensives.

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: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2, which may be the same of different, each represent hydrogen, C.sub.1 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino alkylamino dialkylamino or cycloalkyl or R.sub.1 and R.sub.2 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.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom which is oxygen or sulphur;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms,Q represents a furan or thiophene ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5- positions, the furan ring optionally bearing a further substituent R.sub.

Abstract: There is disclosed pharmaceutical preparations and a method of using same in the treatment of inflammation and/or pain, e.g., treating rheumatic affections, with novel substituted alkylidene-aminooxyalkyl carboxylic acid esters.

Abstract: Phenylacetic acid derivatives of the formula ##STR1## wherein A is an aryl radical optionally substituted by halogen, trifluoromethyl, alkyl, alkoxy, alkenyloxy, alkoxyalkoxy, alkyl-substituted amino or aryloxy, or a heterocyclic ring system optionally substituted by halogen, alkyl or alkoxy,Y is a valency bond or an optionally branched alkylene radical containing up to 3 carbon atoms, andR.sub.1 and R.sub.2 each independently is hydrogen or a lower alkyl radical,or a physiologically compatible salt or ester thereof, exhibit marked hypoglycaemic and hypolipidaemic activity.