Abstract: Disclosed is a 4-step process for the preparation of alkyl esters of 1-methylcyclopropanecarboxylic acid which comprises the steps of (1) converting &ggr;-butyrolactone to &agr;-methyl-&ggr;-butyrolactone; (2) converting the &agr;-methyl-&ggr;-butyrolactone from step (1) to an alkyl 4-halo-2-methylbutyrate; (3) producing a xylene solution of the alkyl 4-halo-2-methylbutyrate; and (4) contacting the xylene solution of an alkyl 4-halo-2-methylbutyrate from step (3) with an alkali metal alkoxide under conditions of temperature and pressure which causes vaporization of (i) an alkanol as it is formed and (ii) an alkyl 1-methylcyclopropanecarboxylate as it is formed from the alkyl 4-halo-2-methylbutyrate. Also disclosed are processes whereby the alkyl 1-methylcyclopropanecarboxylate, prepared as described above, is converted to 1-methylcyclopropylamine.

Abstract: The invention relates to a process for the preparation of 2-methoxy-4-(N-t-butylaminocarbonyl)benzenesulfonyl chloride by sulfonating m-hydroxybenzoic acid, methylating the hydroxy group of the resulting sulfonic acid or its salt, transforming the carboxylic acid group and the sulfonic acid group to acid chloride groups and reacting the 4-chlorosulfonyl-3-methoxy-benzoyl chloride with t-butylamine, which comprises carrying out the sulfonation of the 3-methoxy-benzoic acid of general formula (II) with 96% sulfuric acid, separating the resulting 3-hydroxy-4-sulfobenzoic acid of general formula (III) in the form of its salt of general formula (IV), wherein Z stands for alkali metal or ammonium group, methylating the compound of general formula (IV) in the presence of a phase transfer catalyst at a pH value of about 11.

Abstract: Novel perfluoroalkyl-substituted mono-, di- and poly-amide compounds which are reaction products of a mono-, di- or polyamine of 60 to 2000 molecular weight with a perfluoroalkyl substituted unsaturated acid or its corresponding lower alkyl ester and optionally a non-fluorinated amino-reactive compound such as an acid, ester, anhydride, epichlorohydrin, isocyanate or urea, are useful as internally or externally applied paper sizes to impart oil and grease resistance to paper, and as oil proofing coatings on textiles, wood, masonry and the like, or as high-performance surface active agents.

Abstract: This invention relates to a method of making an incorporated photographic amide comprising a) continuously combining an amine capable of forming an incorporated photographic amide, an acid chloride, one or more acid-absorbing reagents, and one or more water-immiscible solvents to continuously form a reaction mixture; b) continuously reacting the amine and acid chloride to form an incorporated photographic amide; and c) separating the incorporated photographic amide from the reaction mixture.

Abstract: This invention relates to fluorophenyl-substituted alkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them. An embodiment of the invention embraces compounds of the formula I: and the pharmaceutically tolerated salts thereof. The disclosed compounds are valuable inhibitors of the cellular sodium/proton exchanger (Na+ /H+ exchanger) . They are therefore outstandingly suitable for the treatment of all diseases attributable to increased Na+ /H+ exchange.

Abstract: Substantive UV-absorbing water-soluble quaternary salts of cinnamidoalkylamine of formula I. Hair, skin and fabric care compositions containing the compounds of formula I; wherein R1 represents up to four substituents, same or different, selected from H, halo, —OH, —NH2, —NO2, —OCH3, —N(CH3)2, alkyl groups containing up to 6 carbon atoms, alkoxy groups containing up to 6 carbon atoms, alkylamino or N,N-dialkylamino groups containing up to 6 carbon atoms; R2 is selected from hydrogen, alkyl group containing up to 6 carbon atoms; R3 and R4 are independently selected from benzyl, alkyl group containing up to 6 carbon atoms; n is an integer from 1 to 6; m is an integer from 1 to 10; X− is a counter anion of quaternary centres selected from halides including chloride, bromide, iodide and methane sulphonate and its derivatives such as trifluoro methane sulphonate, benzene sulphonates including its p-bromo, nitro and methyl derivative.

Abstract: The present invention discloses an improved process for the N-acylation of amino alcohols employing an organic acid in the form of an acid halogenide, wherein the acylation occurs in an organic solvent in the additional presence of water.

Abstract: A method for enhancing the purity of a desired compound comprising: Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents; Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: and Step (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.

Abstract: The present invention generally relates to the individual stereoisomers of the drug valnoctamide (a mixture of four stereoisomer kinds, VCD-valmethamide or 2-ethyl-3-methyl pentanamide) useful in treatment of neurological and psychotic disorders such as different kinds of epilepsy and affective disorders, and useful as tranquilizers and to treat pain, and to pharmaceutical compositions containing, as an active ingredient, these stereoisomers. The present invention further relates to a method for stereoselective separation and quantification of the four stereoisomers from a racemic mixture of VCD or plasma of patients treated with the racemic drug. The present invention further relates to a unique method for the synthesis of the individual stereoisomers.

Abstract: A new composition of matter for a diamidodiol and a method for preparing the diamidodiol. The exemplary diamidodiol has the formula C15H30N2O4 and is prepared by reacting a first quantity of 2-amino-2-methyl-1-propanol with a second quantity of a di-substituted malonyl dichloride (i.e., diethylmalonyl dichloride), preferably in ethyl acetate as solvent. A tetraamido macrocycle is prepared from the diamidodiol in two steps by oxidizing the diamidodiol to form a diacid followed by coupling using a known procedure of the diacid with an aryl diamine (e.g., 1,2-diaminobenzene) to yield the tetraamido macrocycle.

Abstract: The present invention provides an inexpensive one-step method for preparing an aromatic carboxamide, such as a phenyl substituted carboxamide) by reacting an aromatic amine (e.g. a phenylamine) and a carboxylic acid (e.g. an alkanoic acid or ester thereof) in the presence of a boron containing compound (e.g. boronic acid or boric acid) and, optionally, a chelating agent (e.g. a 2-pyridinylamine).

Abstract: A novel Claisen rearrangement reaction is provided. An allylic reactant such as an allylic amine, an allylic ether or an allylic thioether is reacted with an acid chloride in the presence of a Lewis acid catalyst composition composed of a Lewis acid and a base selected from the group consisting of tertiary amines and non-nitrogenous bases. The stereochemistry of the reaction product is readily controlled by the positioning and size of substituents on the allylic reactant. The reaction may be carried out on a solid support, i.e., on the surface of a substrate suitable for conducting solid phase chemical reactions.

Abstract: A process for the preparation of S-N,N′-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzenedicarboxamide, comprising the reaction of S-(−)-5-[[2-(acetyloxy)-1-oxopropyl]amino]-2,4,6-triiodo-1,3-benzenedicarboxylic acid dichloride (III) with 2-amino-1,3-propanediol (serinol) without a solvent, followed by hydrolysis of the acetate group.

Abstract: The invention relates to new imides, to a plurality of processes for their preparation and to their use as fungicides.

Abstract: Oxime ethers of formula (I) in which a) X is an N atom and Y is an oxygen atom or NH, or b) X is CH and Y is an oxygen atom, in which furthermore R1 is C1-C4alkyl; R2 is hydrogen, C1-C4alkyl or cyclopropyl; and in which R3 and R4 are as defined herein, are fungicidal, acaricidal and insecticidal active ingredients for agriculture. They can be employed as formulated crop protection compositions.

Abstract: The present invention relates to hydroxymandelic acid amides of phenolic amines which can be used as antioxidants or as free-radical scavengers, particularly in the cosmetic or dermatological field, in foods and in cosmetic and dermatological compositions.

Abstract: A process for the preparation of S-N,N′-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzenedicarboxamide, comprising the formation of S-N,N′-bis[2-hydro-xy-1-(hydroxymethyl)ethyl]-5-[(2-(acetyloxy)-1-oxopro-pyl)amino]-2,4,6-triiodo-1,3-benzenedicarboxamide star-ting from S-(−)-5-[[2-(acetyloxy)-1-oxopropyl]amino]-2,4,6-triiodo-1,3-benzenedicarboxylic acid dichloride and 2-amino-1,3-propanediol in a solvent, characterized in that the solvent is selected from the group consisting of: lower alcohols, monoalkyl ether glycols and straight or branched cyclic alkyl ethers.

Abstract: A process for the preparation of a racemic or optically active compound of the formula where the group R1 is an unsubstituted or a halogen substituted C1-4-alkyl, a C1-4-alkoxy, an aryl, an arylalkyl, an aryloxy, or arylalkylloxy.

Abstract: Method for the acylation of amines are disclosed in which includes reacting a first reactant containing an amine group with a second reactant containing an acyl halide group, wherein the reaction takes place in the presence of secondary carboxylic acid salt form, of formula I: R4R5CHCOOH  I wherein R4 is an alkyl group having 1 to 10 carbon atoms; and R5 is an alkyl group having 1 to 10 carbon atoms.

Abstract: A novel process for the preparation of (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9H-purin-9-yl)-2-cyclo-pentene-1-methanol of the formulae ##STR1## is described. This entails in the first stage (.+-.)-2-aza-bicyclo[2.2.1]hept-5-en-3-one of the formula ##STR2## being acylated to give a (.+-.)-2-azabicyclo[2.2.1]hept-5-en-3-one derivative of the general formula ##STR3## in which R.sup.1 denotes C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, aryl or aryloxy, the latter being reduced in the second stage to give a cyclopentene derivative of the general formula ##STR4## in which R.sup.

Abstract: Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them.Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction and for the treatment of angina pectoris. They also inhibit, in a preventive manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the triggering of ischemically induced cardiac arrhythmias.

Abstract: A method for enhancing the purity of a desired compound comprising:Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents;Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: andStep (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.

Abstract: Compounds which are useful as a tachykinin antagonist are substituted alkyltetraamine derivatives which are represented by the following formula (I) or a pharmaceutically acceptable salt, a complex compound or a solvate thereof. ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each is a phenyl group which may be substituted with one or more hydroxyl, lower alkoxy and/or acyloxy group(s). The compounds are useful as an anti-inflammatory agent, anti-allergic agent, analgesic, antiemetic, agent for irritable colon syndrome, agent for dermal disease, agent for vasospastic disease, agent for cerebral ischemic disease, antidepressant, antianxiety agent, agent for autoimmune disease, antispasmodic, and as a muscle relaxant, etc.

Abstract: The present invention relates to serinamide, glycinamide, alaninamide and phenylalaninamide derivatives of formula (I) wherein R, R', R.sub.1 and R.sub.2 are as defined in the disclosure. The compounds (I) are useful for the treatment of neurological diseases.

Abstract: This invention provides perfluoro(alkoxycycloalkane) carbonyl fluoride compounds wherein, pendant from the fluorinated ring, are from 2 to 5 perfluoroalkoxy groups having from 1 to 4, preferably 1 to 2, carbon atoms with the proviso that when one or more of the perfluoroalkoxy groups contain from 3 to 4 carbon atoms, there are no more than 3 pendant groups. Also described are amidoamine intermediates prepared from the carbonyl fluoride compounds as precursors for surfactants used in aqueous film-forming foam (AFFF) compositions.

Abstract: Carboxamides of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 is unsubstituted or substituted bicycloalkyl, tricycloalkyl or bicycloalkenyl;R.sup.2,R.sup.3 and R.sup.4 are each, independently of one another, hydrogen, or unsubstituted or substituted: alkyl, cycloalkyl, cycloalkenyl or heterocyclyl;Ar is unsubstituted or substituted aryl or hetaryl,but excluding 2-cyano-N-[1-(1-naphthyl)ethyl]-3-phenyl-bicyclo[2.2.1]hept-5-ene-2-carbox amide, a process for their preparation, compositions comprising compounds I and the use of compounds I for preparing the compositions, and further a process for controlling harmful fungi and the use of the compounds I for this purpose.

Abstract: Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.

Abstract: Azinooxime ethers of the formula I ##STR1## (X=NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 ; Y=O, NZ, where Z=H, alkyl; R.sup.1 =H, alkyl; R.sup.2 =cyano, nitro, trifluoromethyl, halogen, alkyl, alkoxy; m=0, 1, 2, it being possible for the radicals R.sup.2 to be different if m=2; R.sup.3 =H, cyano, alkyl, haloalkyl, alkoxy, cycloalkyl; R.sup.4, R.sup.5, R.sup.6 =indepedently of one another H, unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl), and their salts, processes and intermediates for their preparation and their use for controlling harmful fungi and animal pests.

Abstract: N-long-chain acyl acidic amino acids or salts thereof are prepared by condensing an acidic amino acid or a salt thereof and a C.sub.8 -C.sub.22 long-chain fatty acid chloride in an aqueous solvent with stirring at a stirring power of not less than 0.2 kW/m.sup.3 while keeping the pH in the range of 10-13.

Abstract: Benzoylguanidines of the formula I ##STR1## in which: R(1) to R(4) have the meanings given in the claims, are antiarrhythmic pharmaceuticals, having a cardioprotective component, which are also valuable for the prevention of ischemically induced damage, in particular in association with the triggering of ischemically induced cardiac arrhythmias. As a consequence of inhibiting the cellular Na.sup.+ /H.sup.+ exchange mechanism, they are used for treating acute or chronic damage triggered by ischemia. In addition to this, they are notable for their strong inhibitory effect on the proliferation of cells. They are suitable for preventing the genesis of high blood pressure.

Abstract: There are described benzoylguanidines of the formula I ##STR1## having the definitions of R(1) to R(4) indicated in the text, and their pharmaceutically tolerable salts. They are obtained by reaction of a compound II ##STR2## with guanidine. They are outstanding agents for the treatment of disorders of the cardiovascular system.

Abstract: The invention concerns hydrazonoacetic acid amides of general formula (I), a process for producing them, and the use of the said amides as pesticides. In the formula shown, the following meanings apply: A stands for a simple bond or optionally substituted alkylene; Q stands for oxygen or sulphur, R.sup.1 stands for optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclyl; R.sup.2 stands for hydrogen or optionally substituted alkyl, cycloalkyl, cycloalkenyl, aryl or heterocyclyl; R.sup.3 and R.sup.4 are identical or different and each stand for hydrogen or optionally substituted alkyl or cycloalkyl; R.sup.2 and R.sup.3 together with the nitrogen atom to which they are bound form an optionally substituted heterocyclyl ring; R.sup.5 stands for optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclyl.

Abstract: Disclosed are A N-[(fluoroalkoxy)phenoxyalkyl]benzamide compound represented by the formula (1): ##STR1## wherein R.sup.1 and R.sup.3 may be the same or different and represent a hydrogen atom, a halogen atom, a C.sub.1-4 alkyl group, a C.sub.1-4 alkoxy group, a C.sub.1-4 haloalkyl group, a C.sub.1-4 haloalkoxy group, a cyano group, a nitro group, or a hydroxy group; R.sup.2 represents a hydrogen atom, a halogen atom, a C.sub.1-4 alkyl group, or a C.sub.1-4 alkoxy group; A represents an oxygen atom, or a sulfur atom; n is an integer of 1 to 6; x is 1 to 4; y is 0 to 6; z is 2 to 9; m is 0 to 2; provided that 2x+1=y+z+m, an intermediate thereof, processes thereof and an agricultural and horticultural chemical for controlling noxious organisms containing the above-mentioned compound as an effective ingredient which is available as a nematocide, an acaricide, a fungicide, etc.

Abstract: A group of benzamide compounds are disclosed which are useful for treating neurodegenerative disorders. Methods for making these compounds are provided. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease which can exhibit themselves as progressive loss of central nervous system function. The compounds can arrest or slow the progressive loss of function.

Abstract: Substituted Indanylidineacetylguanidines, process for their preparation, their use as medicaments or diagnostic and medicaments containing them:Indanylidineacetylguanidines I ##STR1## and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and X have the meanings given in the claims, are effective inhibitors of the cellular sodium/proton antiport (Na.sup.+ /H.sup.+ exchanger), which, in numerous diseases (essential hypertension, atherosclerosis, diabetes and the like) is also increased in those cells which are readily accessible for measurements, such as, for example, in erythrocytes, platelets or leukocytes. They are also advantageous for the preparation of a medicament for the treatment or prophylaxis of disorders of lipid metabolism.

Abstract: Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them Benzoylguanidines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4) are as defined in the specification, and pharmaceutically tolerated salts thereof.

Abstract: Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.

Abstract: A process is provided for the production of nitrobenzamides or aminobenzamides having the formula: ##STR1## in which n is 1 or 2, preferably 1, X is an amino or nitro group and R is hydrogen, unsubstituted alkyl or alkyl substituted by halogen, C.sub.1 -C.sub.4 -alkoxy, phenyl, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, a mono- or di-C.sub.1 -C.sub.4 alkylated amino group or by --SO.sub.3 M in which M is hydrogen, an alkali metal atom, ammonium or a cation formed from an amine, which process comprises reacting a nitrobenzoyl chloride having the formula: ##STR2## in which n has its previous significance, with an aqueous solution of an amine having the formula NH.sub.2 --R in which R has its previous significance, in the presence of an inert organic solvent, to produce a compound having the formula: ##STR3## in which n and R have their previous significance; and finally optionally reducing the nitro group(s) to amino group(s).

Abstract: This invention refers to a new process for the synthesis of (S)-N,N'-bis?(2-hydroxy-1-(hydroxymethyl)ethyl!-5-?(2-hydroxy-1-oxopropyl! amino!-2,4,6-triiodo-1,3-benzendicarboxamide, of formula (III), ##STR1## starting from 5-amino-2,4,6-triiodo-1,3-benzendicarboxylic acid dichloride characterized by a new step of chromatographic purification through resins of (S)-5-??2-(acetyloxy)-1-oxopropyl!amino!-2,4,6-triiodo-1,3-benzendicarboxy lic acid dichloride, which enables the direct conversion to the compound of formula (III), without preventive isolation.

Abstract: Benzoylguaridines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4), R(5) are as defined in the specification, and pharmaceutically tolerated salts thereof.

Abstract: Alkylbenzoylguanidines of the formula I ##STR1## in which A, R.sup.1, R.sup.2 and R.sup.3 have the given meanings, and their physiologically harmless salts exhibit antiarrhythmic properties and act as inhibitor of the cellular Na.sup.+ /H.sup.+ antiporter.

Abstract: A process for the preparation of (S)-N,N'-bis?2-hydroxy-1-(hydroxymethyl)ethyl!-5-(2-acetoxy-propionylamino )-2,4,6-triiodo-isophthalamide, an intermediate useful for the synthesis of iopamidol, by reaction between L-5-(2-acetoxy-propionylamino)-2,4,6-triiiodoisophthaloyl dichloride and 2-amino-1 ,3-propanediol in N-methylpyrrolidone and in the presence of a base, is described.

Abstract: Novel monoamine oxidase B inhibitors of formula (I), wherein R.sub.1 .dbd.H, an optionally substituted benzyloxy or phenylethoxy group; p=0-3; R.sub.3 .dbd.H, a CN, OH, CCH group, a C.sub.1 -C.sub.3 alkoxy-carbonyl group, or a C.sub.1 -C.sub.3 alkylated cyanomethyl group; R.sub.2 .dbd.H or a C.sub.1 -C.sub.3 alkyl group; n=0 or 1; if n=0, R.sub.4 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 alkoxy group, while if n=1, y=1 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.3 alkoxy group or a phenyl group. The invention also concerns processes for the preparation of said novel inhibitors and the therapeutic use thereof.

Abstract: A method of preparing acylated .alpha.-amino carboxylic acid amides directly from amino nitriles in high yield and purity. The method involves acylating the amino nitrile with an acyl halide under Schotten-Baumann conditions, and hydrolyzing the resulting nitrile to the amide. The resulting acylated amino carboxylic acid amide precipitates and can be isolated by filtration in high purity.

Abstract: This invention provides perfluoro(alkoxycycloalkane) carbonyl fluoride compounds wherein, pendant from the fluorinated ring, are from 2 to 5 perfluoroalkoxy groups having from 1 to 4, preferably 1 to 2, carbon atoms with the proviso that when one or more of the perfluoroalkoxy groups contain from 3 to 4 carbon atoms, there are no more than 3 pendant groups.In yet another aspect, this invention provides aqueous film-forming foam (AFFF) compositions comprising one or more perfluoro(alkoxycycloalkane) carbonyl group-containing surfactants and one or more water-soluble fluorine-free surfactants selected from the group consisting of nonionic hydrocarbon-containing surfactants with a hydrophilic-lipophilic balance (HLB) value greater than or equal to about 10 and ionic hydrocarbon-containing surfactants having a carbon chain length containing inclusively from about 6 to about 10 carbon atoms.

Abstract: The present invention relates to substituted benzoylguanidines, a process for their preparation, their use as medicament or diagnostic agent, and medicament comprising them.

Abstract: An aminoarylaminoarazole can be prepared by a process comprising the steps of condensing a condensable nitroarylcarbonyl compound with an aminonitroarylol, an aminonitroarylthiol, or a triaminonitroarene to form a dinitroanilide, then reducing and cyclizing the dinitroanilide under such conditions to form the aminoarylaminoarazole. The aminoarylaminoarazole is useful in making PIBX polymers.

Abstract: Alkyl-benzoylguanidines of the formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 have the meanings given, and physiologically acceptable salts thereof show antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

Abstract: A process for producing an ethenyl amide compound, which comprises reacting a Schiff base compound having a carbon atom adjacent to a carbon atom constituting an imino group and at least one hydrogen atom on the carbon atom with an acylhalide at a reduced pressure while removing by-produced hydrogen halide by distillation to produce an ethenyl amide compound having an amide bond in the molecule and a double bond between carbons at .alpha.-position and .beta.-position with respect to the nitrogen atom of the amide bond.

Abstract: A compound of formula (I), wherein R.sup.1 and R.sup.2 are independently selected from chloro, fluoro, bromo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 haloalkyl provided that both R.sup.1 and R.sup.2 are not fluoro; R.sup.3 and R.sup.4 are independently selected from hydrogen and C.sub.1-6 alkyl, and pharmaceutically acceptable salts, solvates or physiologically functional derivatives thereof, their use in medicine, particularly the phrophylaxis or treatment of conditions associated with inflammation, arthritis, or pain, pharmaceutical compositions comprising them, and processes for their preparation are disclosed.