Abstract: The present invention relates to isoindole derivatives, and more particularly to 5-(hydroxymethyl)oxazolidine-2-one derivatives which are substituted at the 3 position by an indazole, benzisoxazole or benzisothiazole ring system, to a process for their preparation and to their application in therapy.

Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.

Abstract: Arthropodicidal compounds, compositions and arthropodicidal use of compounds having the formula ##STR1## wherein A, X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, m and n are as defined in the text.

Abstract: [5(6)-(benzisoxa-, benzisothia- or indazol-3-yl)-1H-benzimidazol-2-yl]carbamates of formula (I) wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, halo, hydroxy or C.sub.1-4 alkyloxy; R.sup.2 is C.sub.1-4 alkyl; and X is O, S, SO, SO.sub.2 or NR.sup.3, said R.sup.3 being hydrogen, C.sub.1-4 alkyl, aryl or arylC.sub.1-4 alkyl. The compounds of formula (I) have anthelminthic properties. Compositions containing said compounds as active ingredient, a method of combating helminths, and a process for preparing said compounds and compositions.

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: 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: Organic stabilizers are used to stabilize various materials which are normally unstable neat or in solution. These compositions exhibit bactericidal, fungicidal and algaecidal properties.

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: Naphthotriazolium salts which are chromogenic indicators for reducing substrate, such as NADH or NADPH.

Abstract: Process for the preparation of pure, unsymmetrically disubstituted ureas of the general formula ##STR1## in which R denotes a phenyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy, aryloxy or trifluoromethyl groups, an oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, benzoxazolyl or benzothiazolyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy or trifluoromethyl groups and R.sub.1 and R.sub.2 independently of one another denote a hydrogen atom or an alkyl group, where R.sub.1 and R.sub.2 are not simultaneously hydrogen or R.sub.1 and R.sub.2 together denote a butylene or pentylene group, by reaction of an N-alkyl- or N,N-dialkylurea with an unsubstituted or substituted arylamine or a heterocyclic amine in the presence of that amine which is already present in the starting material, the respective N-alkyl- or N,N-dialkylurea.

Abstract: The invention relates to novel azo dyes of the formula ##STR1## wherein R.sup.1 is an alkyl radical containing 1 to 12 carbon atoms, which is unsubstituted or substituted by hydroxy, alkoxy, cyano or phenyl, or is an aryl radical selected from the group consisting of phenyl, 1-naphthyl, 2-naphthyl, 2-pyridyl, 4-pyridyl, 2-pyrimidinyl and 2-thienyl, these radicals being unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, --NHR.sup.3, --NH--C.sub.2 -C.sub.6 alkanoyl,--NH--benzoyl, phenoxy, COOR.sup.3, --CONHR.sup.3, phenyl, sulfo or C.sub.1 -C.sub.4 alkylsulfone,R.sup.2 is hydrogen or a radical as defined for R.sup.1,R.sup.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, which is unsubstituted or substituted by hydroxy, alkoxy, cyano or phenyl, or phenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, --NH--C.sub.2 -C.sub.6 alkanoyl, --NH--benzoyl, phenoxy, phenyl, sulfo or C.sub.1 -C.sub.

Abstract: A method of controlling plant growth is provided comprising applying to the plants or to a habitat thereof a herbicidally effective amount of a compound having the structure: ##STR1## wherein R.sup.1 is selected from the group consisting of carboxy, cyano, ester ##STR2## or amido ##STR3## wherein R.sup.2 is selected from the group consisting of a straight-chained alkyl group or a branched-chain alkyl group, of about 1 to 8 carbon atoms,R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen, alkyl of about 1 to 8 carbon atoms, cycloalkyl of about 5 to 6 carbon atoms, and heterocyclyl of about 5 to 6 carbon and hetero atoms, or,R.sup.3 and R.sup.4 taken together with the nitrogen atoms to which they are attached form a heterocyclyl group having 5 to 6 carbon and hetero atoms. Also, novel compounds having the above structure are provided.

Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.

Abstract: Dyes of the formula ##STR1## where R and R.sub.1 are independently of the other hydrogen, halogen, nitro, alkyl or alkoxy and KK is the radical of a coupling component, which are particularly suitable for dyeing polyester fibers if no water-solubilizing group is present, and which are particularly suitable for dyeing and printing textile materials made of polyamide fibers when at least one sulfo group is present in the dye.

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: A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hydrogenation catalyst is suspended in a solvent, the nickel concentration is 0.1 to 10% by weight, based on the primary amine. The starting materials are separate from each other, brought to 80.degree. to 150.degree. C. and 1 to 15 MPa and fed into the catalyst suspension simultaneously with stirring and reacted in one step to form the tertiary N,N-dimethylamines.

Abstract: Inhibiting HMG-CoA reductase, as in treating hyperlipopproteinaemia, lipoproteinaemia and arteriosclerosis, with the new N-substituted N-amino-pyrroles of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2 is an aryl or heteroaryl radical,R.sup.3 is a hydrogen or an organic radical,R.sup.4 and R.sup.5 each independently is hydrogen or an organic radical or, together, they complete a heterocylic ring,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.10 is hydrogen or alkyl, and R.sup.11 is hydrogen, an organic radical or a cation.

Abstract: A thermal imaging method is provided which comprises heating imagewise a di- or triarylmethane compound possessing within its di- or triarylmethane structure an aryl group substituted in the ortho position to the meso carbon atom with a moiety ring-closed on the meso carbon atom directly through a nitrogen atom, which nitrogen atom is also bound to a group with a masked acyl substituent that undergoes fragmentation upon heating to liberate the acyl group for effecting intramolecular acylation of said nitrogen atom to form a new group in the ortho position whereby the di- or triarylmethane compound is rendered colored in an imagewise pattern corresponding to said imagewise heating.

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: Novel compounds of the general formula I ##STR1## where X and Y independently of one another are each carboxyl, a carboxylic ester group, cyano or an unsubstituted or substituted carbamyl or carboxylic hydrazide group and X and Y together form a radical of the formula ##STR2## where R.sup.1 is hydrogen or a radical of a primary amine and R.sup.2 and R.sup.3 are each hydrogen or unsubstituted or substituted alkyl, cycloalkyl or aryl, are very useful as diazo components.

Abstract: A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting parmacological activity, including anti-secretory and anti-ulcerogenic activity, pharaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.

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: The invention relates to the use of 3-acylaminobenzisothiazole-S,S-dioxides of the formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl, phenyl, or C.sub.1 -C.sub.10 alkyl which is substituted by halogen or C.sub.1 -C.sub.5 alkoxy, and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, trifluoromethyl, amino or nitro, for controlling insects and representatives of the order Acarina. The invention further relates to novel compounds of the formula I, wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl, phenyl, or C.sub.1 -C.sub.10 alkyl which is substituted by halogen or C.sub.1 -C.sub.5 alkoxy, and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, trifluoromethyl, amino or nitro, with the proviso that R.sub.2, R.sub.3, R.sub.4 and R.sub.

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

Abstract: Novel methods for treatment of neoplastic disease states in animals, which methods comprise administering a therapeutically effective amount of a compound of the formula IIIa, ##STR1## wherein: Y is hydrogen or lower alkyl; and Z is an hydroxy substitited 1-pyrrolidinyl radical, ora lower alkyl substituted piperidyl radical, ora 1-piperazinyl radical or an acetamino, acetyl, carbamido, cyano, carboxy lower alkylamino, di-lower alkoxy, nitro, sulfamyl, or lower alkyl substituted anilino radical, ora radical of the formula, ##STR2## wherein R is hydrogen or lower alkyl and R.sup.1 is a nitrogen containing heterocyclic radical selected from the group consisting of amino substituted triazolyl, lower alkyl substituted isothiazolyl, benzothiazolyl, and nitro and halo substituted derivatives of benzothiazolyl, or R.sup.

Abstract: Pyrazole sulfonamides are found to have utility as preemergent and/or postemergent herbicides or plant growth regulants.

Abstract: A class of bicyclic benzenoid aminoalkylene 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.

Abstract: The use in pest control of 3-acrylaminobenzisothiazoles of the formula I ##STR1## wherein R.sub.1 is unsubstituted or substituted alkyl or phenyl, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, trifluoromethyl, amino or nitro, and R.sub.6 is hydrogen or --COR.sub.1.There are also described the novel compounds of the formula Ia ##STR2## wherein R.sub.1 ' is C.sub.1 -C.sub.10 -alkyl substituted by halogen or by C.sub.1 -C.sub.5 -alkoxy, or is unsubstituted C.sub.2 -C.sub.10 -alkyl or phenyl,R.sub.2 ', R.sub.3 ', R.sub.4 ' and R.sub.5 ' independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, trifluoromethyl, amino or nitro, andR.sub.6 ' is hydrogen or --COR.sub.1 '; orR.sub.1 ' is methyl,R.sub.2 ', R.sub.3 ', R.sub.4 ' and R.sub.5 ' independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.

Abstract: A class of bicyclic benzenoid aminoalkylene 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.

Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which the substituents are defined in the detailed description.The compounds show pharmaceutical activity as selective histamine H.sub.2 -antagonists.

Abstract: A process for the preparation of a 3-hydrazino-1, 2-benzisothiazole 1,1-dioxide of the formula ##STR1## in which R.sup.1 and R.sup.2 each independently is hydrogen, alkyl, halogen, amino, hydroxyl or carboxyl, andR.sup.3 and R.sup.4 each independently is hydrogen, alkyl, cycloalkyl or aryl,comprising reacting a 3-keto-2H,3H-1,2-benzisothiazole 1,1-dioxide of the formula ##STR2## with a hydrazine of the formula ##STR3## in a molar ratio of 1:1 to 1:50, in an inert solvent, at a temperature between 75.degree. C. and 200.degree. C. and for a reaction time of 15 to 40 hours. The products, some of which are known, are fungicidally active and can also be used as intermediates.

Abstract: A process for preparing certain thieno-fused heterocyclic compounds having H.sub.2 -receptor antagonist and antisecretory activity, which involves the reaction of a mercaptan, obtained by reduction of a thienoisothiazole amino alkyl disulfide, with a 5-substituted-2-furanylmethanol; and said thienoisothiazole amino alkyl disulfide intermediates.

Abstract: A process for preparing certain benzo- and thieno-fused heterocyclic compounds having H.sub.2 -receptor antagonist and antisecretory activity, which comprises the amide reduction of N-substituted carbamoyl-containing benzo- or thieno-fused heterocyclic intermediates; and said N-substituted carbamoyl-containing benzo- or thieno-fused heterocyclic intermediates.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, quaternized derivative, N-oxide or solvate thereof:R.sub.1 --Ar--(CH.sub.2).sub.a --X--(CH.sub.2).sub.b --NH--Het (I)wherein: the substituents are defined in the specification.The compounds are useful in treating excess gastric acid secretions such as peptic ulcers.

Abstract: A process for preparing certain thieno-fused heterocyclic compounds having H.sub.2 -receptor antagonist and antisecretory activity, which comprises reacting a suitable thienoisothiazole derivative with an appropriate (furanylmethylthio)ethanamine derivative to yield an intermediate, which is subjected to cyclization to yield the desired final product.

Abstract: Aniline derivatives of the formula ##STR1## wherein X=alkyl,Z=H or alkyl, andY=S-alkyl, SO.sub.2 -alkyl, CO.sub.2 -R (R=alkyl, cycloalkyl, or H) or--if Z=H--Br,are diazo components for preparing valuable azo dyestuffs and starting materials for preparing compounds of the formula ##STR2## and new azo dyestuffs derived therefrom and which--in their nonionic form--are highly suitable for dyeing polyester fibres in blue shades having high tinctorial strength and high fastness levels.

Abstract: 3-Amidino-benzisothiazole-1,1-dioxides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each C.sub.1 -C.sub.5 -alkyl or C.sub.2 -C.sub.5 -alkenyl,R.sub.3 is hydrogen or methyl, orR.sub.1 and R.sub.2 together form a C.sub.3 -C.sub.6 -alkylene chain which can be interrupted by O, S or NH, orR.sub.1 and R.sub.3 together are --CH.sub.2 --CH.sub.2 --CH.sub.2 --, andX.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, halo-C.sub.1 -C.sub.5 -alkyl or C.sub.1 -C.sub.5 -alkoxy.A process for producing these 3-amidino-benzisothiazole-1,1-dioxides and their use for controlling pests are described.

Abstract: Compounds of the formula: ##STR1## wherein B is a moiety having the formula: ##STR2## R is mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, cycloalkyl of 4-7 carbon atoms, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, lower alkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro.X is SO.sub.2, SO, S or C.dbd.O; andA is amine selected from the group ##STR3## , wherein R.sup.1 is hydrogen or R.sup.2 CH.sub.2 wherein R.sup.2 is mono- or diloweralkylamino, mono- or di-N-lower alkylaminoloweralkyl, (2-furyl)methylamino, benzylamino, lowercycloalkylamino, 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-thiazolidinyl, 4-morpholinyl or 4-thiomorpholinyl; R.sup.3 is hydrogen or (1-piperidinyl)methyl with the proviso that when R.sup.

Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof have been found to show pharmacological activity as selective histamine H.sub.2 -antagonists. The substituents in the compounds of formula (I) are defined in the main body of the disclosure.

Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof have been found to show pharmacological activity as selective histamine H.sub.2 -antagonists.The substituents in Formula (I) are defined in the specification.

Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which one of R.sub.1 and R.sub.2 represents hydrogen, halogen or a C.sub.1-4 alkyl group which may be optionally substituted by hydroxy or C.sub.1-4 alkoxy, and the other represents the group R.sub.4 R.sub.5 NAlk-- in which R.sub.4 represents hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, heteroaralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkylamino or cycloalkyl, and R.sub.5 represents hydrogen or a C.sub.1-4 alkyl group or R.sub.4 and R.sub.5 may, together with the nitrogen atom to which they are attached, form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.

Abstract: Acyl cyanides of the formula ##STR1## in which R represents alkyl or substituted alkyl of from 1 to 8 carbon atoms, cycloalkyl or substituted cycloalkyl of from 3 to 12 carbon atoms, aryl or substituted aryl; or an optionally substituted 5-membered or 6-membered heterocyclic radical which can also be fused with a benzene ringare prepared by reacting the corresponding carboxylic acid anhydride in the presence of a carboxylic acid halide with an alkali metal cyanide or anhydrous acid, at a temperature of between 50.degree. and 300.degree. C.

Abstract: The disclosure herein relates to a novel process for producing tertiary 2-haloacetamides by reacting primary or secondary 2-haloacetamides with an agent capable of generating an anion of the primary or secondary 2-haloacetamide under base conditions and alkylating the anion of the 2-haloamide with an alkylating agent; said anion is generated, for example, by electrolysis or by metals, metal hydrides, fluorides, oxides, hydroxides, carbonates, phosphates, or alkoxides.

Abstract: Compounds which have the general formula ##STR1## and those which can be obtained from them with a Vilsmeier type reagent and have the formula ##STR2## as well as salts thereof, are useful as anti-inflammatory agents.

Abstract: Benzisothiazolines having the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, alkoxy, halogen or nitro;R.sub.2 is alkyl; and R.sub.3 is (i) ##STR2## wherein X is oxygen, sulfur or imino or (ii) ##STR3## wherein Y is alkoxy, alkyl, or arylalkyl, have useful pharmacological activity.

Abstract: Compounds which have the general formula ##STR1## and those which can be obtained from them with a Vilsmeier type reagent and have the formula ##STR2## as well as salts thereof, are useful as anti-inflammatory agents.