Abstract: Disclsoed herein is dye suitable for use in dyeing denim cotton yarns. The dye comprises at least one quinophthalone derivative represented by the following general formula (I) or (II): ##STR1## wherein X means H, Br or Cl and Y denotes H, COOR or --COOC.sub.2 H.sub.4 OR (R: alkyl), or a combination of said at least one quinophthalone derivative and an idigo dye. A dyeing process making use of the above dye and denim cotton yarns thus dyed are also disclosed.

Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.

Abstract: A compound of formula (I) ##STR1## in which R is (a) a hydrogen atom;(b) a linear or branched (C.sub.1 -C.sub.6) alkyl group; an allyl group; a cycloalkylmethyl group in which the cycloalkyl moiety has from 3 to 6 carbon atoms; a phenylmethyl group unsubstituted or substituted with one to three substituents chosen from halogen atoms and trifluoromethyl, nitro, amino, dimethylamino, cyano, aminocarbonyl, linear or branched (C.sub.1 -C.sub.3) alkyl, linear or branched (C.sub.1 -C.sub.3) alkoxy and linear or branched (C.sub.1 -C.sub.3) alkylthio groups; a 2-phenylethyl group; a 3-phenylpropyl group; a 3-phenyl-2-propenyl group; a phenylcarbonylmethyl group; a naphthylmethyl group; a pyridylmethyl group; a furylmethyl group; or a thienylmethyl group; or(c) a linear or branched (C.sub.2 -C.sub.

Abstract: Novel 4-amino-6,7-dimethoxy-2-(6,7-disubstituted-1,2,3,4-tetrahydroisoquinol-2-y l)quinoline compounds have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. Preferred compounds include 4-amino-6,7-dimethoxy-2-(6-hydroxy-7-methoxy-1,2,3,4-tetrahydroisoquinol-2 -yl)quinoline and 4-amino-6,7-dimethoxy-2-(7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinol-2 -yl)quinoline. Methods for preparing these compounds from known starting materials are provided.

Abstract: The present invention relates to new naphthyl derivatives of general formula ##STR1## wherein N represents the number 1 or 2,A represents a --CH.sub.2 --, --CO--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## while the atom marked with an x is linked to the phenyl nucleus, E represents a straight chained alkylene group optionally substituted by an alkyl group,G represents a straight chained alkylene group optionally substituted by an alkyl group,L represents a bond or an oxygen atom, if G represents a straight chained alkylene group with 2 to 5 carbon atoms optionally substituted by an alkyl group,R.sub.1 and R.sub.2, which may be identical or different, represent alkyl or alkoxy groups or R.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, or an alkyl or an allyl group,R.sub.4, R.sub.5 and R.sub.

Abstract: New pyri(mi)dyl-oxy- or -thio-benzoic acid derivatives of the formula ##STR1## are taught which have herbicidal and plant growth regulating activity. In the formula Z can be Ch or N, X is oxygen or sulphur, A is oxygen, sulphur, a radical R.sup.5 --N.dbd.or a radical R.sup.6 O--N.dbd.and B is oxygen, sulphur, a radical ##STR2## with the proviso that at least one of the radicals R.sup.1, R.sup.2 or R.sup.3 represents alkyl or a part of a 3- to 6-membered fused carbocyclic ring.

Abstract: Certain substituted sulfonamide quinolines and isoquinolines are disclosed having anti-allergic activity. A preferred use is for the treatment of chronic obstructive lung disease, and in particular, asthma.

Abstract: A and A' are each hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy or aryloxy;X is cyano, nitro, COOR, SR, SOR or SOOR;R is H, C.sub.1-6 alkyl or aryl;n n' and n" are each 0 to 4; andm, m' and m" are each 1 to 4, have calcium channel blocking activity.

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: The invention relates to a class of tetrahydroisoquinolinylalkanoic acids containing an aryl sulphonamide group which have activity as thromboxane A.sub.2 antagonists.

Abstract: A compound of formula 1, or a solvate or salt thereof: ##STR1## in which: RCO is an acyl group in which the group R comprises a substituted or unsubstituted carbocyclic or heterocyclic aromatic ring and R.sub.1 and R.sub.2 are independently C.sub.1-6 alkyl groups or together form a C.sub.3-6 polymethylene or alkenylene group, is useful for treating pain.

Abstract: An efficient synthesis of quanidines, e.g. of the formula (III), by oxidizing a thiourea, e.g. of the following formula (II): ##STR1## with H.sub.2 O.sub.2 and a molybdenum catalyst to yield an aminoiminomethane sulfonic acid which can then be reacted with an amine followed by optional transamination steps.

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: A compound of formula I: ##STR1## or a solvate or salt thereof in which: R is an acyl group containing a substituted or unsubstituted carbocyclic or heterocyclic aromatic ring and R.sub.1 and R.sub.2 are independently C.sub.1-6 alkyl groups or together form a C.sub.3-6 polymethylene or alkenylene group, is useful for treating pain in mammals.

Abstract: Methine dyes (I) which conform in one of their tautomeric forms to the general formula ##STR1## where Y.sup.1 is in both or either case an electron-attracting group and the other Y.sup.1 is hydrogen,Y.sup.2 is in each case, independently of the others, hydrogen, --CN, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl, phenyl, pyridyl or together with a further Y.sup.2 a five- or six-membered ring which may have a fused-on benzene ring,R is hydrogen, C.sub.1 -C.sub.20 -alkyl, C.sub.7 -C.sub.10 -aralkyl or .beta.

Abstract: Thiazole derivatives have been made, for example, by reacting a 2-aryl-2,2-dialkoxyethylamine with an appropriately substituted aryl acetyl halide followed by treating the resulting amide with diphosphoryl pentasulfide. The thiazole derivatives are found to be effective immunoregulants.

Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.

Abstract: The present invention are 2-(2-aryl-2-oxo-alkylidene) analogs of 1,2,3,4-tetrahydropyridine-3,5-pyridinecarboxylic acids and particularly esters thereof having valuable calcium antagonist and positive inotropic activity useful in the treatment of cardiovascular disorders, pharmaceutical compositions and methods of use therefor.

Abstract: This invention relates to novel isoquinolinesulfonamide derivatives of Formula (I): ##STR1## wherein A is a C.sub.0-10 alkylene group or a C.sub.0-10 alkylene group having a C.sub.1-10 alkyl group, a phenyl group, a substituted phenyl group or a phenylalkyl group; R.sub.1 and R.sub.2 each is a hydrogen atom; or R.sub.1 and R.sub.2 are linked directly to form an ethylene group unsubstituted or substituted with a C.sub.1-4 alkyl group;R.sub.3 and R.sub.4 each is a hydrogen atom, a C.sub.1-6 alkyl group or linked directly to form a C.sub.2-6 alkylene group; and the pharmaceutically acceptable acid addition salt thereof, and to a process for preparing them. The isoquinoline derivatives possess a relaxatory action for vascular smooth muscle and action for increasing blood flow and are useful as a vasodilator and a hypotensor.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently --H or lower alkoxy;R.sub.3 and R.sub.4 are each independently lower alkyl; andR.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--and pharmaceutically acceptable acid addition salts thereof are calcium channel blockers useful for treating cardiovascular disorders including angina, hypertension and congestive heart failure.

Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: A, B, D and E are selected from CH, N and N-Z wherein Z is selected from oxygen and the group YAn wherein Y is selected from alkyl and benzyl and An is an anion, and provided that no more than three of A, B, D and E are selected from N and N-Z and no more than one of A, B, D and E is selected from N-Z;W is a saturated or unsaturated C.sub.2 to C.sub.5 hydrocarbon chain;X and X.sup.1 are independently selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, alkanoyloxy, benzyloxy, substituted benzyloxy, amino, substituted amino and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof, or two of X.sup.1 on the same carbon atom may form an oxo group;R.sup.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 and each independently --H or lower alkoxy; R.sub.3 and R.sub.4 are each independently lower alkyl; and R.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--, and pharmaceutically acceptable acid addition salts thereof are prepared by cyclizing, deoxygenating, coupling, or hydrogenating the intermediates disclosed herein.

Abstract: This invention relates to novel 2-acetyl- and 2-propionylpyridine selenosemicarbazones. These compounds are useful as antimalarial and antileukemic agents. Also disclosed are several synthetic procedures used to prepare the selenosemicarbazones.

Abstract: The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.

Abstract: Acylanilides of the formula ##STR1## wherein R.sup.1 and R.sup.2, the same or different, each is cyano, carbamoyl, nitro, halogeno, perfluoroalkyl or other defined substituents;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or alkyl, or is joined to R.sup.5 ;R.sup.5 is hydrogen, hydroxy, alkoxy or acyloxy or is joined to R.sup.4 ;R.sup.6 is alkyl or halogenoalkyl, or has the formula --A.sup.3 --R.sup.8 or --A.sup.4 --X.sup.2 --A.sup.5 --R.sup.9 ;A.sup.1 and A.sup.4, the same or different, each is alkylene;A.sup.2, A.sup.3 and A.sup.5, the same or different, each is a direct link or alkylene;X.sup.1 and X.sup.2, the same or different, each is oxygen, sulphur, sulphinyl, sulphonyl, imino or alkylimino;R.sup.7 and R.sup.9, the same or different, each is alkyl, alkenyl, hydroxyalkyl, cycloalkyl, phenyl optionally substituted, naphthyl or heterocyclic optionally substituted;and R.sup.8 is phenyl, naphthyl or heterocyclic as defined above for R.sup.7 or R.sup.

Abstract: Compounds of formula (I): ##STR1## wherein: A represents a CH-NO.sub.2 group or a N-CN group;B represents CH.sub.2, O, S or a direct bond;R represents a bicyclic or polycyclic residue, variously substituted and functionalized;R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or C.sub.1 -C.sub.4 alkyl groups; andn and m, which may be the same or different, are 0, 1, 2, 3 or 4;are valuable pharmacological agents.

Abstract: This invention relates to novel isoquinolinesulfonamide derivatives of Formula (I): ##STR1## wherein A is a C.sub.0-10 alkylene group or a C.sub.0-10 alkylene group having a C.sub.1-10 alkyl group, a phenyl group, a substituted phenyl group or a phenylalkyl group; R.sub.1 and R.sub.2 each is a hydrogen atom; or R.sub.1 and R.sub.2 are linked directly to form an ethylene group unsubstituted or substituted with a C.sub.1-4 alkyl group;R.sub.3 and R.sub.4 each is a hydrogen atom, a C.sub.1-6 alkyl group or linked directly to form a C.sub.2-6 alkylene group; and the pharmaceutically acceptable acid addition salt thereof, and to a process for preparing them. The isoquinoline derivatives possess a relaxatory action for vascular smooth muscle and action for increasing blood flow and are useful as a vasodilator and a hypotensor.

Abstract: The invention relates to new 1-cyclohexyl-3,4-dihydroisoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hydrogen, hydroxyl or alkoxy having from 1 to 6 carbon atoms,X is oxygen andZ is a .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is hydrogen or alkyl having from 1 to 6 carbon atoms; orX represents an .dbd.NR.sup.4 group, in which R.sup.4 is hydrogen or hydroxyl, andZ is a .dbd.CH--CN, .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is as defined above,and acid addition salts thereof.The compounds of formula (I) are pharmaceutically active, in particular show antispasm, analgesic, gastric acid secretion inhibiting, sedative and hypnotic activity and effectively reduce the alcoholic narcosis time. According to a further aspect of the invention there is provided a process for the preparation of these compounds. The invention further relates to pharmaceutical compositions containing them as active ingredient.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently --H or lower alkoxy;R.sub.3 and R.sub.4 are each independently lower alkyl; andR.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--and pharmaceutically acceptable acid addition salts thereof are calcium channel blockers useful for treating cardiovascular disorders including angina, hypertension and congestive heart failure.

Abstract: Novel 2,4-diaminopyrimidines having substituted heterobicyclomethyl moieties in the 5-position have superior antibacterial properties.

Abstract: Compounds of the formula (II) ##STR1## or a salt, N-oxide or acyl derivative thereof, wherein Y is a group ##STR2## which is optionaly substituted and which optionally contain a nitrogen atom at one of positions A, B, C, D or E, in which the dotted line represents aromatic rings unless one of the rings contains a nitrogen atom in which case this ring is either aromatic or partially saturated, have antimicrobial properties. Processes for making these compounds, pharmaceutical compositions containing them and the medical use of the compounds are also disclosed.

Abstract: New derivatives of the general formula (I) in which:R=H or Cl and either R.sub.1 and R.sub.2 form a tetrahydroquinoxaline, tetrahydroquinoline, tetrahydroisoquinoline, dihydrobenzoxazine, tetrahydro-1H-benzazepine or isoindoline ring, it being possible for all these rings to be substituted by one or more halogen, carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, trifluoromethyl, cyano, nitro, alkoxy, alkylthio or alkyl, substituted by carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, hydroxyl, amino, alkylamino or dialkylamino, or R.sub.1 =alkyl and R.sub.2 =alkyl substituted by phenyl which is itself unsubstituted or substituted by one or more halogen, alkyl, alkoxy, alkylthio, hydroxy, amino, alkylamino, dialkylamino, carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, trifluoromethyl, cyano or nitro, all the alkyls having 1 to 4 C in a straight or branched chain.These new products are used as antirheumatics.

Abstract: The invention relates to novel N-aminomethyl-3-phenyl-4-cyanopyrrole derivatives of the formula I ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen, halogen, methoxy or methylthio,Z is a group ##STR2## wherein R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by cyano, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkoxycarbonyl; or are C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, benzyl or benzyl which is substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl and/or C.sub.1 -C.sub.6 alkoxy, or phenyl or phenyl which is substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl and/or C.sub.1 -C.sub.6 alkoxy, with the proviso that only one of R.sub.3 or R.sub.4 can be hydrogen,R.sub.5 and R.sub.6 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.

Abstract: N-substituted amino acids are described which when coupled with 1,2,3,4-tetrahydroisoquinolines result in substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids as anti-hypertensive agents. The novel intermediates are in turn prepared by reacting an amino acid such as alanine with 2-bromo-4-phenyl butanoic acid or an ester thereof.

Abstract: 2-Acyl-1,3,4,6,7,11b-hexahydro-2H-pyrazino-[2,1-a]-4-isoquinoleinones having anthelmintic activity of the formula ##STR1## are prepared from 4-acyl-2,6-dioxopierazines by reaction with a phenethyl halide, selective reduction of one of the oxo groups and cyclization, by the novel intermediates of formula ##STR2## in which Y represents O or H, OH.

Abstract: A class of bicyclic nitrogen heterocyclic ether and thioether compounds exhibiting pharmacological activity including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.

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: Bicyclic imino acids, particularly 2-carboxylic acid derivatives of azabicycloalkanes and process for preparing them.These compounds have therapeutical activity and may be used as medicines, particularly as cardiovascular and antihypertensive drugs in human or veterinary medicine.

Abstract: 1-Aroyl-2-phenylamino-2-imidazolines of the general formula ##STR1## where R.sup.1 and R.sup.2 are identical or different and each is chlorine, bromine, fluorine, methyl, ethyl, methoxy, trifluoromethyl or cyano,R.sup.3 has the meanings given for R.sup.1 and R.sup.2 or is hydrogen andAr is an unsubstituted or substituted monocyclic or bicyclic heteroaromatic radical containing 1, 2 or 3 nitrogen and/or oxygen and/or sulfur atoms, their salts with physiologically tolerated acids, their preparation, and drugs containing these compounds.The compounds have, inter alia, a blood pressure-reducing action.

Abstract: Isoquinolines are disclosed of the formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbomoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.

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: Oxime ether derivatives of the formula (I): ##STR1## wherein Het is a monocyclic heteroaromatic group containing two hetero atoms at least one of which is nitrogen, or a bicyclic heteroaromatic group containing one or two hetero atoms at least one of which is nitrogen, Ar is a phenyl or a 5- or 6-membered monocyclic heteroaromatic group, and R is an alkyl, alkenyl, alkynyl, cyanoalkyl, carbamidoalkyl or aminoalkyl group, or N-oxides thereof, have anti-ulcer activity in the gastro-intestinal tract of mammals.

Abstract: Novel isoquinoline derivatives of the general formula ##STR1## wherein R represents a lower alkyl group, a lower cycloalkyl group, or a group of the formula ##STR2##in which R.sup.2 represents a hydrogen atom, a halogen atom, a methyl group, a trifluoromethyl group, a methoxy group, a methylamino group or a dimethylami no group;R.sup.1 represents a hydrogen atom or a lower alkyl group; andY represents a carboxyl group, a cyano group, a carbamoyl group, a lower alkoxycarbonyl group or a lower alkylaminocarbonyl group;or a salt thereof; a process for the production thereof.The above compound is useful as an anti-inflammatory and analgesic agent.

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 method of synthesizing fused ring pyridines (annulated) by co-oligomerization of .alpha.,.omega.-diynes with about molar equivalents of nitriles using a Co.sup.+1 catalyst preferably cyclopentadienyl cobalt dicarbonyl. Additionally, new compounds of tricyclic quinolizine-4-ones were produced where excess cyanoacetic ester starting materials were utilized (about 2:1 equivalent nitriles:diyne). The results with the catalyst employed indicated a stepwise mechanism in which cobalt(I) catalyst first forms a metallocycle intermediate derived from the bisacetylene. This cobalt(III) intermediate reacts preferentially with nitriles to give the product annulated pyridines in good yield. Generally, preferred conditions indicated roughly molar equivalents of reactants with no substantial excess of either reactant for the bicyclic compounds.

Abstract: Compounds corresponding to the formula ##STR1## are disclosed, wherein Alk represents a C.sub.2 -C.sub.5 -alkylene groups optionally substituted by a hydroxy group and Ar represent an optionally substituted phenyl, naphthyl, tetrahydronaphthyl, indanyl or indenyl radical or a monocyclic or condensed bicyclic or tricyclic heterocyclic radical which is optionally substituted, the heterocyclic radical consisting of individual rings having 5 or 6 members and optionally containing from 1 to 4 hetero atoms, and the acid addition salts thereof. A process for producing these compounds is also disclosed. These substituted aminoalkyl guanidines block the .beta.-receptors of the adrenergic nerve system, and also reduce blood pressure.

Abstract: A compound effective in the treatment of diabetic angiopathy, i.e. a selective .beta.-receptor blocker has the formula ##STR1## wherein: R.sup.2 is a hydrogen or alkyl having one to five carbon atoms,R.sup.3 is alkyl having one to five carbon atoms, cycloalkyl or phenyl optionally substituted with hydroxyl or phenyl, or R.sup.2 and R.sup.3 together form a five- to eight-membered ring optionally containing also other heteroatoms and/or fused with another ring, preferably phenyl, naphthyl, quinolyl, isoquinolyl, pyridyl, pyrazolyl,R.sup.5 is hydrogen or alkyl having one to four carbon atoms, cycloalkyl or phenyl optionally substituted with halogen, alkoxy having one to four carbon atoms or alkyl having one to four carbons,R.sup.6 is hydrogen, alkyl having one to four carbon atoms or phenyl, m=0, 1 or 2, and n=0, 1 or 2.

Abstract: Isoquinolines are disclosed of the formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbomoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.