Abstract: Methods of inhibiting cell proliferation in a patient suffering from such disorder comprising the use of a styryl-substituted heteroaryl compound wherein the heteroaryl group is a monocyclic ring with 1 or 2 heteroatoms, or a bicyclic ring with 1 to about 4 heteroatoms, said compound optionally substituted or polysubstituted, with the proviso that when said ring is polysubstituted, the substituents do not have a common point of attachment to said ring, and those compounds wherein no substituent on the heteroaryl group is a carboxy group or an ester group, and pharmaceutical compositions comprising such compounds.

Abstract: A method of inhibiting cell proliferation in a patient suffering from such disorder comprising the administration to the patient of a pharmaceutically effective amount of a pharmaceutical composition containing, in admixture with a pharmaceutically acceptable carrier, a compound, or a pharmaceutically acceptable salt thereof, of the formula ##STR1## wherein the radicals are defined in the specification.

Abstract: The present invention relates to new compounds of formula ##STR1## wherein A is a bicyclic ring chosen from naphthalene, tetrahydronaphthalene, quinoline, isoquinoline and indole.B is a R.sup.2 substituted benzene ring or an unsubstituted pyridine or thiophene ring;R is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy or a group NR.sup.3 R.sup.4 wherein each of R.sup.3 and R.sup.4 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy or a group NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are as defined above;n is zero or an integer of 1 to 2;x is zero or an integer of 1 to 5;and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful as tyrosine kinase inhibitors.

Abstract: A compound of structure (I), in which A.sup.1 is O, S(O).sub.n in which n is 0, 1 or 2, NR, CH.sub.2, or CH(OH); A.sup.2 is a bond or CH.sub.2 ; or A.sup.1 A.sup.2 is CH.dbd.CH; R is hydrogen or C.sub.1-4 alkyl; R.sup.1 is an optionally substituted 6- to 10-membered aryl or heteroaryl ring; suitably R.sup.1 is an optionally substituted 6- 10-membered aryl ring such as phenyl or naphthyl; suitably R.sup.1 is optionally substituted 6- to 10-membered heteroaryl ring, containing from 1 to 4 nitrogen atoms; R.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl, CN, NO.sub.2 or CF.sub.3 ; R.sup.3 is C(R.sup.4)(R.sup.5)CH.sub.2 NR.sup.6 R.sup.7, --CH.dbd.NNHC(NH)NH.sub.2 or a; R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-4 alkyl; R.sup.6 and R.sup.7 are the same or different and are each hydrogen or C.sub.1-4 alkyl or together with the nitrogen atom to which they are attached form a ring; R.sup.8 is hydrogen, C.sub.1-4 alkyl, or C.sub.

Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.

Abstract: Compounds of formulaA--X--Y--NH--Bwherein A is derived from optionally substituted benzothiophene, indole, 4-aza-and 7-aza-benzothiophene or-indole, A bearing in position 5 hydrogen, halogen, optionally substituted alkyl, hydroxy, nitro, amino, alkylamino, acylamino, alkoxycarbonyl, sulfamoyl, cyano, trimethylsilyl, carboxy, carbamoyl, phosphate, oxycarbamoyl, heterocyclic radical or ether or ester group, X-Y is --CR.sub.8 .dbd.N-- or CH(R.sub.8)--NH-- wherein R.sub.8 is -H or alkyl and attached at position 3 of A, and B is a heterocyclic radical or a residue ##STR1## wherein R.sub.10 is H, optionally substituted alkyl, cycloalkyl, aryl, adamantyl, acyl or carbamoyl and X.sub.2 is alkylthio or NR.sub.3 R.sub.10 wherein R.sub.3 is H or alkyl or R.sub.3 and R.sub.10 together with the nitrogen atom to which they are attached form a heterocyclic radical, in free form or in salt form, have pharmacological activity, e.g. for treating gastrointestinal disorders.

Abstract: Dye-donor element for use according to thermal dye transfer comprising least one dye corresponding to the general formula (I): ##STR1## wherein Z is --CN, --COOR.sup.1 or --CONR.sup.2 R.sup.3 ; R.sup.1 is --H, (cyclo)alkyl, or aryl; R.sup.2 and R.sup.3 is --H, (cyclo)alkyl, aryl, or R.sup.2 and R.sup.3 together represent the atoms necessary to complete a heterocyclic nucleus; R.sup.4 and R.sup.5 is --H, (cyclo)alkyl, aryl, a heterocyclic ring, SO.sub.2 R.sup.8, COR.sup.8, CSR.sup.8, POR.sup.8 R.sup.9, OR.sup.6, NR.sup.6 R.sup.7, SR.sup.6, or R.sup.4 and R.sup.5 together represent the atoms necessary to complete a aliphatic ring, a heterocyclic ring including a heterocyclic ring carrying a fused-on aliphatic or aromatic ring; R.sup.6 and R.sup.7 is (cyclo)alkyl, aryl, alkenyl, aralkyl, aryl, a heterocyclic group, or R.sup.6 and R.sup.7 together represent the atoms necessary to complete a 5- or 6-membered ring; R.sup.8 and R.sup.

Abstract: Dye-donor element for thermal dye transfer comprising at least one magenta dye having extremely low side absorption in the blue and red regions of the spectrum, said dye corresponding to the general formula (I): ##STR1## wherein R.sup.1 is H, (cyclo)alkyl, or aryl; X represents the atoms completing a heterocycle; Z is an electron-withdrawing group; Y is an electron-withdrawing group or --N(R.sup.2)R.sup.3 ; R.sup.2 and R.sup.3 together represent the atoms completing a heterocycle; or R.sup.2 and R.sup.3 together represent .dbd.C(R.sup.4)R.sup.5, or each of R.sup.2 and R.sup.3 represents (same or different) (cyclo)alkyl, aryl, or an electron-withdrawing group; each of R.sup.4 and R.sup.5 (same or different) represents H, (cyclo)alkyl, aryl, a heterocycle, SO.sub.2 R.sup.6, COR.sup.6, CSR.sup.6, POR.sup.6 R.sup.7, OR.sup.8, NR.sup.8 R.sup.9, SR.sup.8, or R.sup.4 and R.sup.5 together represent the atoms completing an aliphatic ring or a heterocycle, each of R.sup.6 and R.sup.

Abstract: This invention provides a method of selectively antagonizing the 5-HT.sub.1A receptor in mammals by administering aryloxypropanolamines. Aryloxypropanolamines are also claimed.

Abstract: Amidines derived from 3-aminoethyl indoles of formula (I) ##STR1## where R.sub.1 is an atom of hydrogen or a lower alkyl or alkenyl group: R.sub.2 is an atom of hydrogen or a lower alkyl or alkenyl , aryl, arylalkyl or cycloalkyl group; R.sub.3 and R.sub.4 may be the same or different and are an atom of hydrogen or a lower straight or branched chain alkyl group; and R.sub.5 is an atom of hydrogen; a straight or branched chain alkyl, alkenyl or alkynyl group, which may be substituted with an hydroxy group, alkoxy, alkoxycarbonyl, carboxyl, trifluoromethyl, halogen, carbonyl, cyano; a cyano group, phenyl, aryl, cycloalkyl, heterocycle or arylalkyl, optionally substituted with a hydroxy, alkoxy, halogen, amino, alkoxycarbonyl, carboxyl, trifluoromethyl, carbonyl, cyano, nitro, lower alkyl, lower alkenyl, or may form an optionally substituted heterocycle with R.sub.4 and with the nitrogen atom; and the physiologically acceptable salts thereof.

Abstract: Disclosed is a novel UV light absorbing compound which can preferably be employed in the art of colored molding plastics, resin films, heat-sensitive transfer materials, liquid crystal display materials, color photographs and the like, and method for producing thereof. The UV light absorbing compound is characterized by the general formula: ##STR1## wherein R.sup.1 represents linear or branched alkyl or aralkyl group, and R.sup.2 represents --CN or --COOR.sup.3, wherein R.sup.3 represents substituted or unsubstituted alkyl or aralkyl group.

Abstract: Heteroarylethenediyl compounds wherein the heteroaryl group can be mono- or icyclic heteroaryl and the aryl group can be or mono- or bicyclic carbocyclic, said compound optionally substituted or polysubstituted, with the proviso that the heteroaryl group is not furyl or thienyl when the ethenediyl group has geminal cyano substituents, and pharmaceutical compositions comprising said compounds, and the use thereof for inhibiting a protein tyrosine kinase portion of a receptor selected from epidermal growth factor and platelet derived growth factor in a patient suffering from such disorder.

Abstract: The present invention relates to 2-substituted-1-hydroxyindoles of the following formula: ##STR1## wherein, R.sup.1 is an electron withdrawing group,R.sup.2 is an alkenyl having 2-10 carbon atoms, and N-substituted .alpha.-iminobenzyl group wherein the substituents are selected from the group consisting of phenyl, anilino and dimethylamino, an unsubstituted aromatic group, and an aromatic group having meta or para substituents which are nitro, trifluoromethyl, fluoro, formyl, hydroxyiminomethyl and carbamoyl,R.sup.3 is a halogen atom, andn is 0, 1, or 2,provided that when R.sup.2 is either phenyl or nitro substituted phenyl and n is 0, then R.sup.1 is not cyano.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, lower alkenyl, aryl or ar(lower)alkyl,R.sup.4 is imidazolyl, which may have alkyl or imino-protective group as substituents, or pyridyl,A is lower alkylene, andis single bond or double bond, and pharmaceutically acceptable salts thereof, having 5-HT antagonism.

Abstract: Azaporphyrin derivatives of the formula ##STR1## where R.sup.1 and R.sup.2 are each, independently of one another, hydrogen, unsubstituted or substituted C.sub.1 -C.sub.20 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl or unsubstituted or substituted phenyl, or two adjacent R.sup.1 radicals form, together with the carbon atoms to which they are bonded, an unsaturated or aromatic 5- to 7-membered carbocyclic ring,X are each hydrogen or C.sub.1 -C.sub.4 -alkyl andp are each 1 or 2, andbiladienes of the formula ##STR2## where R.sup.1, R.sup.2, X and p each have the abovementioned meanings, m and n are each 0 or 1 and An.sup..crclbar. is an anion, as intermediates therefor, are used for preparing vinylogous porphyrin derivatives.

Abstract: 1-Hydroxyindoles of the following formula are useful in controlling fungi: ##STR1## wherein: R.sup.1 is hydrogen or an electron withdrawing group;R.sup.2 is selected from the group consisting of alkenyl having 2-10 carbon atoms, N-substituted-.alpha.-iminobenzyl, an unsubstituted or substituted aromatic group and acyl of 2-16 carbon atoms,R.sup.3 is selected from the group consisting of halogen atoms, andn is 0 to 4.

Abstract: Substituted indolyl compounds of the formula ##STR1## are potent inhibitors of the lipoxygenase enzymes and are useful as agents for the treatment of allergies and inflammatory disease states.

Abstract: A process for preparing .alpha.-formylamino nitriles of the formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or unsubstituted or substituted, with substituents which are inert under the reaction conditions, aliphatic or heteroaliphatic radicals with 1 to 10, cycloaliphatic or heterocycloaliphatic radicals with 3 to 6, araliphatic radicals with 7 to 12, heteroaraliphatic radicals with 4 to 12, aromatic radicals with 6 to 10 or heteroaromatic radicals with 3 to 10 carbon atoms, by reacting cyanohydrins of the formula II ##STR2## with the formamide III ##STR3## in the presence of acids, entails adding at least one ammonium salt to the reaction mixture.

Abstract: A process for preparing .alpha.-formylamino nitriles of the formula Ia ##STR1## and Ib ##STR2## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different and each is hydrogen or unsubstituted or substituted, with substituents which are inert under the reaction conditions, aliphatic or heteroaliphatic radicals with 1 to 10, cycloaliphatic or heterocycloaliphatic radicals with 3 to 6, araliphatic radicals with 7 to 12, heteroaraliphatic radicals with 4 to 12, aromatic radicals with 6 to 10 or heteroarometic radicals with 3 to 10 carbon atoms, with the priviso that at least one of R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 is hydrogen, comprises reacting an iminodiacetonitrile of the formula II ##STR3## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the abovementioned meanings, with formamide of the formula III ##STR4## in the presence of formic acid or with a compound which provides formic acid, in the presence of acids.

Abstract: Disclosed is a composition comprising 1,3,5-trioxane, and more particularly a stability-improved trioxane composition.

Abstract: Indole derivatives are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl; R.sub.2 is a hydrogen, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, phenyl, phen(C.sub.1-4)alkyl or C.sub.5-7 cycloalkyl; R.sub.3 and R.sub.4 are hydrogen, C.sub.1-3 alkyl or propenyl groups or together form an aralkylidene group; Alk is C.sub.2 -C.sub.3 alkylene chain and A is C.sub.2 -C.sub.5 alkylene chainand its physiologically acceptable salts and solvates.The compounds may be prepared, for example, by cyclization of a compound of general formula (II): ##STR2## where Q is the group NR.sub.3 R.sub.4 or a protected derivative thereof or a leaving group and R.sub.1 l, R.sub.2, R.sub.3, R.sub.4, A and Alk are as defined for formula (I).The compounds have a selective vosoconstrictor action and are useful in treating pain such as migraine. The compounds may be formulated as pharmaceutical compositions in conventional manner, preferably for oral administration.

Abstract: Members of a novel class of organic nitriles related to an indole alkaloid of Dithyrea wislizenii (Cruciferae) have been discovered to be patent feeding inhibitors of the fall armyworm and European corn borer.

Abstract: Use of a compound of formula ##STR1## wherein A is an aromatic-heterocyclic ring which contains an oxygen or nitrogen atom, and n is 1 or 2, for controlling insects and plant-destructive nematodes and to a composition containing such a compound. The compounds of this invention are particularly suitable for controlling sucking insects.

Abstract: Members of a novel class of organic nitriles related to an indole alkoaloid of Dithyrea wislizenii (Cruciferae) have been discovered to be potent feeding inhibitors of the fall armyworm and European corn borer.

Abstract: The present invention relates to the synthesis of nitriles having an amine function on the adjacent carbon.

Abstract: Compounds are disclosed of the general formula (I) ##STR1## wherein R.sub.1 represents halogen, alkyl, alkoxy or hydroxyl, or a group NR.sub.a R.sub.b or CON.sub.a R.sub.b, where R.sub.a and R.sub.b are hydrogen, alkyl or alkenyl or with the nitrogen atom form a saturated monocyclic 5 to 7-membered ring;R.sub.2 represents hydrogen or alkyl;R.sub.3 and R.sub.4 represent hydrogen, C.sub.1-3 alkyl or propenyl or R.sub.3 and R.sub.4 together form an aralkylidene group; Alk represents a C.sub.2-3 alkylene chain;n and m, are integers of 1 to 4 or n is zero, and their physiologically acceptable salts and solvates.The compounds are described as useful in treating pain originating from dilatation of the cranial vasculature in particular migraine and cluster headache and can be formulated in conventional manner as pharmaceutical compositions with carriers or excipients for administration by any convenient route.

Abstract: A compound selected from the group consisting of all possible isomeric forms, optically active isomers and racemic mixtures of compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, --OH, --CF.sub.3 and --NO.sub.2, R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, aralkyl of 7 to 12 carbon atoms, benzoyl and acyl of an alkanoic acid of 1 to 12 alkyl carbon atoms and ##STR2## is selected from the group consisting of ##STR3## and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity as well as cerebral oxygenating and vaso regulating activity.

Abstract: A process for the asymmetric preparation of a compound of the formula ##STR1## wherein the hydrogen at 3a and 7a are of cis or trans configuration and their non-toxic, pharmaceutically acceptable acid addition salts comprising submitting a compound of the formula ##STR2## to a Hoffman reaction and reacting the resulting product with formaldehyde in the presence of cyanide ions and acid halide of benzoic acid or an aliphatic carboxylic acid of 1 to 5 carbon atoms to obtain a compound of the formula ##STR3## wherein R is acyl of benzoic acid or aliphatic carboxylic acid of 1 to 5 carbon atoms, cyclizing the latter to form a compound of the formula ##STR4## selectively hydrolyzing the latter with a dilute aqueous mineral acid to obtain a compound of the formula ##STR5## subjecting the latter to hydrolysis with a concentrated aqueous mineral acid to form the acid addition salt of a compound of claim 1 and optionally forming the free base.

Abstract: Indoles are disclosed of formula (I): ##STR1## wherein R.sub.1 represents R.sub.5 R.sub.6 NCOCH.sub.2 --, R.sub.5 CONH(CH.sub.2).sub.p --,R.sub.5 R.sub.6 NSO.sub.2 (CH.sub.2).sub.p -- or R.sub.7 SO.sub.2 NH(CH.sub.2).sub.p --, (where R.sub.5 and R.sub.6 each represents a hydrogen atom or a C.sub.1-3 alkyl group, R.sub.7 represents C.sub.1-3 alkyl and p is zero or one),R.sub.2 is hydrogen or C.sub.1-3 alkyl;R.sub.3 and R.sub.4 each represents hydrogen atom, C.sub.1-3 alkyl, or 2-propenyl;m is zero or an integer from 1 to 4; andn is an integer from 2 to 5; and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. They may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers of excipients for administration by any convenient route.Various methods for the preparation of the compounds (I) are disclosed.

Abstract: The present invention provides compounds of the general formula: ##STR1## wherein Ar is a substituted or unsubstituted aromatic or heteroaromatic radical, A is a straight-chained or branched alkylene chain containing up to 8 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms, B is a straight-chained mono- or bicyclic, optionally branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms and/or up to two --CH.sub.2 -- groups of which can be replaced by an oxygen or a sulphur atom or by an --S(.dbd.O) or --S(.dbd.O).sub.2 group, X is a valency bond, an oxygen atom or an --NR.sup.1 group, in which R.sup.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl or nitroxyalkyl radical containing up to 6 carbon atoms or R.sup.1, together with the nitrogen atom of the --NR.sup.

Abstract: Polymethine dyes are disclosed containing an acidic electron accepting terminal nucleus comprised of an isocyano group. The dyes are useful as spectral sensitizers in ultravioilet responsive imaging compositions.

Abstract: A compound of the formula ##STR1## wherein A is the residue of a ACOOH pyrethrinoid acid, Z is selected from the group consisting of hydrogen, --CN, --C.tbd.CH, --CH.sub.3 and alkyl of 1 to 3 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, cycloalkyl, cycloalkenyl and cycloalkynyl of 3 to 8 carbon atoms, aryl of 6 to 14 carbon atoms and aralkyl of 7 to 18 carbon atoms and R.sub.2 is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, cycloalkyl, cycloalkenyl and cycloalkynyl of 3 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms, --CN, --CF.sub.3, --NO.sub.2 and --COOAlK and AlK is alkyl of 1 to 18 carbon atoms having pesticidal activities.

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: This invention provides a series of novel keto sulfones of formula I ##STR1## in which the group .dbd.A-- is selected from .dbd.C(Ra)-- and .dbd.N-- and the other radicals have the meanings defined in the following specification.The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.

Abstract: This invention relates to a color-shifted dye compounds containing at least one thermally unstable carbamate moiety which are useful in thermal imaging. These compounds may be represented by the formula [M--(X).sub.q ].sub.p D wherein M is a carbamate moiety; X is --N.dbd., --SO.sub.2 -- or --CH.sub.2 --; D taken with X and M represents the radical of a color-shifted organic dye, said carbamate moiety M comprising a tert-alkoxycarbonyl group, ##STR1## wherein R' is halomethyl or alkyl.

Abstract: Indole derivatives of the general formula (I) are disclosed: ##STR1## where R.sub.1 is H or an alkyl or alkenyl group, R.sub.2 is H, or an alkyl, alkenyl, aryl, aralkyl or cycloalkyl group;R.sub.3 is H or an alkyl group;R.sub.4 and R.sub.5 are independently H or an alkyl or propenyl group or together form an aralkylidene group; andAlk is an optionally substituted alkylene chain; and their physiologically acceptable salts and solutes.These compounds are potentially useful for the treatment of migraine and may be formulated as pharmaceutical compositions in conventional manner.Various methods for the production of the compounds are disclosed including a Fischer-indole cyclization process.

Abstract: Compounds of the formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 and R.sup.2, which are the same or different, are hydrogen, cyano or halogen (fluorine, chlorine, bromine or iodine) or optionally substituted alkyl; V is either oxygen or sulphur; W, X, Y and Z, which may be the same or different, are hydrogen, halogen, nitro, cyano, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted aryl, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted arylalkoxy, optionally substituted alkenyl S(O).sub.n R.sup.3 (wherein n is 0, 1 or 2), or optionally substituted heteroaryl, or W, X or X, Y or Y, Z together form methylenedioxy; and R.sup.3 is optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl or optionally substituted heteroaryl.

Abstract: Indole derivatives are disclosed of formula (I): ##STR1## wherein R.sub.1 represents H, alkyl or alkenyl;R.sub.2 represents H, alkyl, alkenyl, cycloalkyl or phenyl or phenyl alkyl the phenyl ring being optionally substituted by halogen, alkyl, alkoxy, hydroxyl or by a group --NR.sub.a R.sub.b, or --CONR.sub.a R.sub.b, wherein R.sub.a and R.sub.b are H, alkyl, alkenyl, or with the nitrogen atom form a saturated monocyclic ring;R.sub.3 and R.sub.4 are H, alkyl or propenyl or together form an aralkylidene group;Alk represents a Cf.sub.2-3 alkyl chain optionally substituted by one or two alkyl groups; andA.sup.1 represents a C.sub.2-5 alkenyl chain and salts and solvates thereof.The compounds have selective vasoconstrictor activity and are useful in treating and/or preventing pain resulting from dilatation of the cranial vasculature, particularly migraine. The compounds may be formulated in conventional manner with pharmaceutically acceptable carriers or excipients.

Abstract: Cationic hydrazone dyestuffs of the general formula ##STR1## in which R.sub.1 stands for hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 - to C.sub.4 -alkoxy, nitro or halogen,R.sub.2 stands for hydrogen, C.sub.1 - to C.sub.4 -alkyl, C.sub.1 - to C.sub.4 -alkoxy, halogen or phenylazo,R.sub.3 stands for C.sub.1 - to C.sub.3 -alkyl andA.sup.- stands for an anion,are prepared by quaternarizing azo bases of the general formula ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 have the abovementioned meaning, with dialkyl sulphates of the general formula(R.sub.3 --O).sub.2 SO.sub.2 IIIin whichR.sub.3 has the abovementioned meaning,in the presence of water and alkali metal sulphate or alkaline earth metal sulphate and, where appropriate, by replacing the alkylsulphate anion by another anion.

Abstract: A process for preparing indoles in high yield by reacting anilines and 1,2-glycols in a liquid phase in the presence of a cadmium bromide or iodide/potassium bromide or iodide catalyst. The used catalyst can be easily recovered and when reused, exhibits excellent performance.

Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalkyl- or haloalkyl-1H-indole with an amine.

Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalky- or haloalkyl-1H-indole with an amine.

Abstract: A process for the production of an ergot alkaloid comprising intramolecularly cyclizing a 3-iminoethyl-4-trans-buta-1',3'-dienylindole to produce an 8-ergolene and as necessary converting the resultant ergolene into the desired ergot alkaloid.

Abstract: The present invention provides aminopropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkanoyl or an aroyl radical, R.sub.2 is a lower alkyl radical or a radical of the general formula: ##STR2## wherein X is a valency bond, a methylene group or an oxygen or sulphur atom, Ar is a monocyclic, carbo- or heterocyclic aryl radical, R.sub.6 and R.sub.7, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.8 and R.sub.9, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, alkenyl radicals, alkynyl radicals, alkyl radicals, lower alkoxy radicals, aralkoxy radicals, alkenyloxy radicals, alkynyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or acylamino radicals; or R.sub.2 is a 1,4-benzodioxan-2-ylmethyl radical, R'.sub.2 is a hydrogen atom or a benzyl radical, R.sub.

Abstract: The compounds of formula I, ##STR1## where R.sub.1, R.sub.2 and R.sub.3 have various significances, and physiologically acceptable hydrolyzable derivatives thereof having the hydroxy group in the 2 position of the 3-aminopropoxy side chain in esterified form, are useful as cardiotonic, antiarrhythmic, .alpha.- and .beta.-adrenoceptor blocking agents.

Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom, an aralkyl radical or a radical of the general formula: ##STR2## in which B is a reactive group or, together with R.sub.5, represents a valency bond, and R.sub.5 is a hydrogen atom or an aliphatic or aromatic acyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen atom, a methyl radical or a --CH.sub.2 --O--R.sub.5 radical, R.sub.5 having the same meaning as above, and R.sub.4 is an aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, with the proviso that R.sub.1 is not an aralkyl radical when R.sub.4 is a formyl radical. The present invention also provides processes for the preparation of these compounds. Furthermore, the present invention is concerned with the use of these compounds for the preparation of compounds with a heart and circulatory activity.

Abstract: There are disclosed herein certain indole derivatives which are useful in the treatment of peptic ulcer diseases.

Abstract: Novel indole derivatives of the general formula I can be obtained by reacting, directly or indirectly, N,N-dimethyl-3-indolemethylamine with a Schiff base of the general formula II, ##STR1## in which R.sup.1 is cyano or methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl or butoxycarbonyl, and .phi. is phenyl. The successive hydrolysis of the indole derivatives of the general formula I in the presence of an acid and of a base gives tryptophane.

Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalky- or haloalkyl-1H-indole with an amine.