Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.

Abstract: A composition comprising an isothiazolone compound mixed with a branched cyclodextrine, wherein the isothiazolone compound can be stabilized to water, so that it is possible to provide an aqueous solution comprising an isothiazolone compound which is excellent in storage stability and aqueous solution stability.

Abstract: Stable composition of 1,2-benzisothiazolin-3-one (BIT) in dipropylene glycol having lower pH and lower viscosity than known compositions. The BIT is present as an alkali metal salt obtained by reacting 0.75 to 1.07 moles alkali metal hydroxide with one mole BIT.

Abstract: This invention is directed to certain 2-(alkoxycarbonylamino)- and 2-(alkoxycarbonylimino)benzlmidazole derivatives which are useful in the topical, oral or parenteral treatment of animals suffering from helminth infections.

Abstract: N-acyldipeptides of formula I ##STR1## wherein R represents a rest of formula ##STR2## and R.sub.4, Y, m, n and Z have the meaning as defined in the description, R.sub.1 represents hydrogen, a 1-10 C. alkyl, an optionally substituted methyl or benzyl,R.sub.2 represents a --CO--A group,wherein A has the meanings as defined in the description,R.sub.3 represents a --(CH.sub.2).sub.p --CO--W group,wherein p and W have the meaning as defined in the description.

Abstract: A method for producing an alkylthiobenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of an alkylthiobenzamide with a halogen in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent and a subsequent reaction with a halogen; and a method for producing a 1,2-benzisothiazol-3-one by carrying out a reaction of a 2-(alkylthio)benzamide with a halogenating agent.

Abstract: A method of treating depression or stroke in a patient suffering therefrom by administering a substituted aminomethylchroman of the formula ##STR1## in which Z--denotes a group of the formula ##STR2## and R.sup.1, E and F can be hydrogen or other radicals, or salts thereof.

Abstract: There are provided substituted benzisoxazole and benzisothiazole compounds having the structural formula I ##STR1## Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.

Abstract: Benzimidazole anthelmintic agents of the formula (I) and their non-toxic salts, wherein R.sup.1, which is in the 5(6)-position, is either H or certain stated substituents, "alk" is a methylene or ethylene group; R.sup.2 is cyano, C.sub.1 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, C.sub.2 -C.sub.4 alkanoyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenoxy, aryl, heteroaryl, aryl-(C.sub.1 -C.sub.4 alkoxy) or heteroaryl-(C.sub.1 -C.sub.4 alkoxy), in which "aryl" means phenyl optionally substituted by 1 to 3 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphinyl, and C.sub.1 C.sub.4 alkylsulphonyl in which "heteroaryl" means thienyl, furyl or pyridininyl all optionally substituted by 1 to 3 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphinyl and C.sub.1 -C.sub.4 alkylsulphonyl; and R.sub.3 is a C.

Abstract: Compounds of the general formula ##STR1## are cyclized to the corresponding isothiazolinone using a carbonyl halide of the formula RCOX where R is halogen or alkyl and X is halogen. R.sup.3 and R.sup.4 are preferably such as to form a 5 or 6 membered ring. Useful carbonyl halides are phosgene and propionyl chloride. Using acyl halides such as propionyl chloride, a mixture of the isothiazolinone and a salt of the carboxylic acid can be obtained, for example an essentially equimolar mixture of 2-methyl-4,5-trimethyl-4-isothiazolin-3-one and sodium propionate.

Abstract: Composition as a highly useful concentrated biocide, said composition being solid at 20.degree. C., easily meltable and solidifyable, capable of undergoing remelt and resolidification without loss of homogeneity and method.

Abstract: Novel bleach catalysts, a method for bleaching substrates using these catalysts and bleach compositions containing the catalysts are reported. These catalysts are magnesium salts of sulfonimines. Substrates such as fabrics and dishware may be bleached in an aqueous solution containing the magnesium sulfonimine salts and a peroxygen compound.

Abstract: Colorless precursors of preformed image dyes are provided which are useful as the color image-forming materials in thermal imaging systems. These colorless precursors possess at least one thermal protecting group that undergoes fragmentation upon heating and at least one leaving group that undergoes irreversible elimination upon heating, said protecting and leaving groups maintaining the precursor in its colorless form until heat is applied to effect removal of these groups whereby the precursor is converted to an image dye.

Abstract: Girondalones of the formula I useful as microbicides ##STR1## wherein A is a residue of a dialdehyde;R.sub.1 is independently selected from the group consisting of R.sub.2 and (C.sub.1 -C.sub.18)alkyl and;R.sub.2 is ##STR2## wherein (i) X.sub.1 and X.sub.2 can be joined to form a 5 or 6 membered fused carbocyclic ring, said ring being saturated, unsaturated, or aromatic; or(ii) X.sub.1 =Cl, H, methyl, or Br; andX.sub.2 =H, Cl, or Br.

Abstract: Biocidal isothiazolinone or isothiazolothione compounds are stabilized with an effective amount of a free-radical scavenger compound. Exemplary of the biocidal isothiazolones are 1,2-benzisothiazolin-3-one, 2-methyl-4-5-trimethylene-4-isothiazolin-3-one, 5-chloro-2-methyl-4-isothiazolin-3-one and 2-methyl-4-isothiazolin-3-one. Effective free-radical scavengers include 3,3-thiodipropionic acid.

Abstract: Compounds of the general formula ##STR1## are cyclised to the corresponding isothiazolinone using a carbonyl halide of the formula RCOX where R is halogen or alkyl and X is halogen. R.sup.3 and R.sup.4 are preferably such as to form a 5 or 6 membered ring. Useful carbonyl halides are phosgene and propionyl chloride.

Abstract: Process for preparing enantiomers of general formula (I): ##STR1## where Z, R.sub.1, R.sub.2, R.sub.3 and n are defined in the description. The compounds obtained according to the invention are useful as medicinal products.

Abstract: Antimicrobial compounds of the formula ##STR1## wherein R is hydrogen, halogen, or (C.sub.1 -C.sub.4)alkyl group;R.sub.1 is hydrogen or halogen; alternatively, R and R1 may be taken together with the carbons to which they are attached to form a 5- to 7-membered carbocyclic ring, said ring optionally being aromatic;R.sub.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl group; andR3 is hydrogen, substituted or unsubstituted (C.sub.1 -C.sub.18)alkyl, substituted or unsubstituted (C.sub.2 -C.sub.18)alkenyl, substituted or unsubstituted (C.sub.2 -C.sub.18)alkynyl, substituted or unsubstituted (C.sub.4 -C.sub.8)cycloalkyl or cycloalkenyl, substituted or unsubstituted (C.sub.6 -C.sub.10)aryl or arylalkyl group are disclosed.

Abstract: A compound of the formula ##STR1## in which R.sup.1 and R.sup.2 taken together, and R.sup.3 and R.sup.4 taken together, independently represent a polymethylene chain leaving 3 or 4 carbon atoms, or a polymethylene chain having 3 or 4 carbon atoms substituted by at least one lower alkyl radical having from 1 to 4 carbon atoms and R.sup.5 to R.sup.8 are independently hydrogen, hydrocarbyl or substituted hydrocarbyl. Typically R.sup.1 and R.sup.2 and also R.sup.3 and R.sup.4 complete a trimethylene ring, R.sup.5 and R.sup.7 are each hydrogen and R.sup.6 and R.sup.8 are alkyl such as methyl. The compounds have microbiological activity.

Abstract: For binding 5-HT.sub.

Abstract: Antimicrobial compounds of the formula ##STR1## wherein R is hydrogen, halogen or (C.sub.1 -C.sub.4)alkyl group;R.sub.1 is hydrogen or halogen; alternatively, R and R1 may be taken together with the carbons to which they are attached to form a 5- to 7-membered carbocyclic ring, said ring optionally being aromatic;R.sub.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl group; andR3 is hydrogen, substituted or unsubstituted (C.sub.1 -C.sub.18)alkyl, substituted or unsubstituted (C.sub.2 -C.sub.18)alkenyl, substituted or unsubstituted (C.sub.2 -C.sub.18)alkynyl, substituted or unsubstituted (C.sub.4 -C.sub.8)cycloalkyl or cycloalkenyl, substituted or unsubstituted (C.sub.6 -C.sub.10)aryl or arylalkyl group are disclosed.

Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.

Abstract: Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described.A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.

Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.

Abstract: The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives.The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton.The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.

Abstract: Novel benzisothiazole- and benzisoxazole-3-carboxamides, processes and intermediates for the preparation thereof, and methods of treating psychoses utilizing compounds and compositions thereof are disclosed.

Abstract: A compound of the formula ##STR1## in which R.sup.1 and R.sup.2 taken together, and R.sup.3 and R.sup.4 taken together, independently represent a polymethylene chain having 3 or 4 carbon atoms, or a polymethylene chain having 3 or 4 carbon atoms substituted by at least one lower alkyl radical having from 1 to 4 carbon atoms, and R.sup.5 to R.sup.8 are independently hydrogen, hydrocarbyl or substituted hydrocarbyl. Typically R.sup.1 and R.sup.2 and also R.sup.3 and R.sup.4 complete a trimethylene ring, R.sup.5 and R.sup.7 are each hydrogen and R.sup.6 and R.sup.8 are alkyl such as methyl. The compounds have microbiological activity.

Abstract: Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.

Abstract: A particulate composition comprising an isothiazolinone or isothiazolothione or a salt or complex thereof and a water soluble metal salt. The salt is typically a metal salt, for example the sodium salt of 1,2-benzisothiazolin-3-one and the water soluble metal salt is particularly an alkali metal salt such as disodium hydrogen phosphate. A preferred composition can be obtained by stirring together an isothiazolinone or isothiazolothione, a base and an alkali metal phosphate in the presence of water until a dry particulate product is obtained. The particulate product is typically highly and rapidly soluble in water and may be stored in a container formed from a water soluble material, for example a bag formed from polyvinyl alcohol.

Abstract: There are provided o-carboxy-(5-oxo-2-imidazolin-2-yl)benzo-(5-membered)-heterocyclic compounds and derivatives thereof and a method for the use therewith to control monocotyledenous and dicotyledenous plant species.

Abstract: Nematicidal compositions which comprise as active ingredient compounds of formula I ##STR1## wherein R is nitro or halogen, and also processes for the preparation of the compounds of formula I, novel intermediates of the preparation process and methods of using the compounds and the compositions in the control of nematodes are described.

Abstract: There are described new benzoisothiazoles of general formula I ##STR1## wherein X and R have meanings given in the description, a process for their preparation and their use as pesticides, especially against nematodes.

Abstract: A method of stabilizing a 3-isothiazolone compound against chemical decomposition comprising introducing a sufficient amount of an alkene to stabilize said 3-isothiazolone compound and a composition comprising 3-isothiazolone and an amount of an alkene sufficient to stabilize said isothiazolone.

Abstract: 2-adamantyl-4-isothiazoline-3-one has the formula ##STR1## wherein R.sub.1 and R.sub.2, each independently, represent hydrogen or halogen,or R.sub.1 and R.sub.2, taken together, form a polymethylene chain having 3-4 carbon atoms, optionally substituted by lower alkyl or halogen,or R.sub.1 and R.sub.2, taken together, form a pyridine ring with the double bond of the 4-isothiazoline-3-one ring andAda represents 1'-adamantyl, 2'-adamantyl or 1'-adamantyl methyl, and its mineral or organic acid salt.The compound is useful as an antibacteria, antialgae or antifungus agent in various industrial fields.

Abstract: A composition comprising(a) a 3-isothiazolone compound of the formula ##STR1## wherein R and R.sup.1 are independently selected from hydrogen, halogen or R is a (C.sub.1 -C.sub.4) alkyl group and R.sup.1 is a halogen or R and R.sup.1 may be joined to form an unsaturated 5- or 6-membered carbocyclic ring; Y is hydrogen, a (C.sub.1 -C.sub.18) alkyl group, an unsubstituted or halo-substituted alkenyl or alkynyl of 2 to 8 carbon atoms, a cycloalkyl or substituted cycloalkyl of 3 to 12 carbon atoms, an aralkyl or halo-, (C.sub.1 -C.sub.4) alkyl-, or (C.sub.1 -C.sub.4) alkoxy-substituted aralkyl of up to 10 carbon atoms, or an aryl or halo-, (C.sub.1 -C.sub.4) alkyl-, or (C.sub.1 -C.sub.4) alkoxy-substituted aryl group of up to 10 carbon atoms; and(b) an amount of a metal bromate salt sufficient to stabilize said composition;wherein said composition if free of metal nitrate salt is disclosed. Methods of use of the above compositions are also disclosed.

Abstract: Newly synthesized chromogenic thiol-indicating benzoisothiazolone derivatives having the structure: ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, are useful in the detection of thiols, particularly in an aqueous system. This process comprises contacting the aqueous system with a chromogenic thiol-indicating benzoisothiazolone derivative as described herein. Chromophoric changes due to thiol-mediated reduction of the benzothiazolone derivative then occur. Such changes can be in a solution or on an indicator surface in contact or having been in contact with the aqueous system. The chromophoric changes, due to a bathochromic shift in characteristic light absorption upon reduction of the benzoisothiazolone derivative, are proportional to the amount or rate of appearance of thiols in the aqueous system.

Abstract: Nitro-substituted heterocyclic compounds of the formula (I) ##STR1## wherein R is hydrogen or alkyl, Z is an optionally substituted aryl or optionally substituted heterocyclic group containing at least one atom selected from N, O and S,A is optionally substituted ethylene or optionally substituted trimethylene, andB stands for 2 or 3 members of a heterocyclic ring which is formed, together with the adjacent C-atom and N-atom and at least one of said members may represent a hetero atom and may be optionally substituted, provided that when B stands for 3 members, two of which are carbon atoms and the other one is a nitrogen atom which is located in the middle of the three members, then at least one of said two carbon atoms must be substituted by a keto group. Such compounds being useful as insecticides.

Abstract: Novel compounds having an affinity for 5-hydroxytryptamine receptors of the formula ##STR1## in which R.sup.1 stands for H, alkyl, aralkyl or heteroarylalkyl,X stands for H, OCH.sub.3, OH, SCH.sub.3, halogen, CN or CONH.sub.2,Y stands for a straight-chain or branched, saturated or unsaturated alkylene chain having up to 6 carbon atomsandZ stands for a group of the formula ##STR2## --OR.sup.4, --SO.sub.m R.sup.5, --COOR.sup.6 or CONR.sup.7 R.sup.8 or salts thereof.

Abstract: Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.

Abstract: Retinal is prepared by condensing a C.sub.15 sulphide of formula: ##STR1## in which R.sub.1 denotes aryl, aralkyl, pyridyl, 2-thiazolyl, 2-benzothiazolyl, 2-benzimidazolyl or 2-benzoxazolyl, with a haloacetal of formula: ##STR2## in which X denotes a halogen atom and R denotes an alkyl radical containing 1 to 4 carbon atoms, to give a C.sub.20 sulphide acetal of formula: ##STR3## in which R.sub.1 and R are defined as above, hydrolysing the said sulphide acetal to give a C.sub.20 sulphide aldehyde of formula: ##STR4## in which R.sub.1 is defined as above, desulphurizing the said sulphide aldehyde to give retinal, and isolating the retinal obtained.

Abstract: The present invention concerns new 5-alkylbenzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl ring of the formula: ##STR2## or R.sub.1 is naphthyl, heterocycle or a bicyclic heterocycle and R.sub.1 -R.sub.7 are described in claim 1.These compounds are useful for prophylaxis or treatment of heart and circulatory disease especially to increase contractility of the heart, lower blood pressure and/or influence the thrombocyte function and improve the microcirculation.

Abstract: Fungicidally effective aminomethyl heterocyclic compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents hydrogen or alkyl, or represents in each case optionally substituted cyclohexyl or phenyl andR.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, dialkoxyalkyl, hydroalkyl, hydroxyalkoxyalkyl, alkoxycarbonylalkyl, dioxolanylalkyl, dioxanylalkyl or oxolanylalkyl, or represent in each case optionally substituted cycloalkylalkyl, cycloalkyl, aralkyl, aralkenyl or aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can optionally contain further hetero atoms,or acid addition salts thereof.

Abstract: A process for preparing a 4,5-tri or tetramethylene-4-isothiazoline-3-one comprises cyclizing a 2-alkyl or aralkyl thio-1-cycloalkene-1-carboxamide in the form of its sulfoxide in an organic solvent in the presence of a acid chloride and adding to the resulting 4,5-tri or tetramethylene-4-isothiazoline-3-one hydrochloride a mineral or organic base or water so as to free the 4,5-tri or tetramethylene-4-isothiazoline-3-one in the form of a free base.

Abstract: The invention relates to new thieno-1,2-thiazole derivatives of the formula ##STR1## wherein A, with the two carbon atoms of the thiazole ring, forms a group of the formula ##STR2## and the broken line indicates the double bond present in the thieno structures of the formulae IIa and IIb, n denotes the integer 2, 3 or 4, R denotes hydrogen or lower alkyl, R.sub.1 denotes hydrogen, lower alkyl, halogen, trifluoromethyl, lower alkoxy or lower alkylthio and R.sub.2 denotes hydrogen, lower alkyl or halogen; and the pharmaceutically acceptable salts of compounds of the formula I wherein R denotes hydrogen, a process for their preparation, pharmaceutical products containing these compounds, and their use in medicaments. The compounds of the formula I and salts thereof have a lipid-lowering action.

Abstract: The invention relates to a novel 3-acylaminobenzisothiazole-S,S-dioxide of formula I ##STR1## to the preparation thereof, to insecticidal compositions containing said compound and to the use thereof for controlling insects, in particular plant-destructive sucking insects.

Abstract: The invention relates to N-indolylethyl-sulphonic acid amides of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are defined in the specification and X is carboxyl, alkoxycarbonyl, cyano or carboxamido. These active compounds are useful in medicaments in combating thromboses, thromboembolisms, allergies or asthmatic disorders.

Abstract: Derivatives of 4-hydroxy-methyl-piperidine having general formula: ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be alkyl or may form, with the carbon they are bound to, a cycloalkyl group or the group ##STR2## with R.sub.6, R.sub.7, R.sub.8 and R.sub.9 being hydrogen or alkyl; R.sub.5 may be H, alkyl, aryl, alkenyl, etc.; Y may be an organic or inorganic group or atom having a valence from 1 to 4 and n is an integer from 1 to 4.The use of the derivatives of the alkyl-substituted 4-hydroxy-methyl-piperidine of formula (I) as stabilizers of polymeric substances, and polymeric compositions stabilized with said piperdine derivatives.This invention relates to new derivatives of alkyl-substituted 4-hydroxy-methyl-piperidine, to the use thereof as stabilizers of polymeric substances usually subject to worsening owing to thermal and/or photo-oxidation, and to the polymeric compositions stabilized with said derivatives.

Abstract: Microbicidal substituted pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represent in each case optionally substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl andHet represents an optionally substituted heterocyclic radical.Intermediates therefor of the formula ##STR2## in which R is alkyl, are also disclosed.

Abstract: The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives.The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton.The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.