Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: The present application relates to novel alkylcarboxylic acids having an oxo-substituted azaheterocyclic partial structure, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.

Abstract: The present application relates to novel alkylcarboxylic acids having an oxo-substituted azaheterocyclic partial structure, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: The present invention relates to a process for modifying diisocyanates for preparing polyisocyanates, where the diisocyanate is reacted using a catalyst, wherein the diisocyanate used is obtained by quenching a gaseous reaction mixture in the phosgenation of diamines in the gas phase, wherein the gaseous reaction mixture comprises at least a diisocyanate, phosgene and hydrogen chloride, wherein a quenching liquid is sprayed into the gas mixture which flows continuously from a reaction zone into a downstream quenching zone, and wherein the quenching liquid is sprayed in by at least two spray nozzles which are arranged at the inlet of the quenching zone at equal intervals along the circumference of the quenching zone.

Abstract: Provided is a novel prophylactic or therapeutic agent for a chorioretinal degenerative disease. The compound of formula (1) or its salt has inhibitory effects on photoreceptor cell death or visual cell death in a mouse model of light damage. Therefore, the compound or its salt is useful as a prophylactic or therapeutic agent for a chorioretinal degenerative disease such as age-related macular degeneration, retinitis pigmentosa. In the formula (1), A is a group (p1), (p2) or (p3); R1 is H, alkyl, aralkyl or OH or its ester; R2 is H or alkyl; R3 is halogen, H, alkyl or OH or its ester; R4 is halogen, H, OH, alkoxy, amino, alkylamino or cycloalkylamino, R3 and R4 may be joined to each other through N to form an unsaturated [1,2,4]oxadiazine ring; R5 is H, alkyl or cycloalkyl; m is 0 or 1; and n is 0 or 1.

Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: The invention relates to compounds of formula wherein Het, A1, A2, A3, A4, D, W, T, Q, Y, X1, X2, R1, R2, R3, R4, k and m are as defined hereinabove, and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, to a process for the preparation of and to the use of those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, to pesticidal compositions in which the active ingredient has been selected from those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in agrochemically usable salt form, to a process for the preparation of and to the use of those compositions, to plant propagation material treated with those compositions, to a method of controlling pests, to intermediates and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, for the preparation of those compounds, E/Z isomers, m

Abstract: A method of dimerizing isocyanates using sulphonamide anions as a dimerization catalyst for the isocyanates and also to a process for preparing oligomeric isocyanates using such catalysts.

Abstract: The present invention provides immunogens for generating anti-neonicotinoid antibodies as well as antibodies, methods, reagents and kits for determining the presence of one or more neonicotinoid insecticides in a sample by immunoassay. The present invention has particular application to determination of the concentration of neonicotinoid insecticides applied to a plant propagation materials such as seed.

Abstract: The present invention relates to the use of sulphonamide salts as catalysts for oligomerizing isocyanates and also to a process for NCO oligomerization using the catalysts of the invention.

Abstract: The invention pertains, at least in part, to new intermediates and synthetic methods for the stereospecific synthesis of oxazinone compounds, which are useful, for example, as antibiotics. The invention also pertains to novel olefinic oxazinone compounds, methods for their synthesis, and methods of using these compounds for the synthesis of oxazinones. The invention also pertains to methods for using the compounds to treat bacterial associated states in subjects.

Abstract: The present invention provides a hetrodiazinon compound having 2-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor antagonistic action, which is represented by the following formula (I), a pharmacologically acceptable salt thereof or hydrates thereof. Wherein A represents O, S or a group represented by the formula NR3 (wherein R3 represents hydrogen atom or a lower alkyl group); R1 and R2 are the same as or different from each other and each represents an optionally substituted (hetero)aryl group etc.; and R4 and R5 are the same as or different from each other and each represents hydrogen atom, hydroxy, a halogen atom, nitrile group, nitro group, a lower alkyl group, a (hetero)aryl group etc.

Abstract: Pyrrolo[1,2-b][1,2,4]oxadiazine-2,3(6H)-diones having the formula: or pharmaceutically acceptable salts thereof, useful as nitric oxide synthase inhibitors wherein each substituent is defined herein.

Abstract: The end-blocked isocyanate prepolymer having an oxadiazine ring according to the present invention is characterized in that at least one of isocyanate groups of a NCO-terminated isocyanate prepolymer, which has NCO groups at the ends and comprises units derived from an oxadiazinetrione compound (A) represented by the following formula (1) and units derived from an active hydrogen compound (B) represented by the following formula (2), is blocked with a unit derived from an end-blocking agent (C) having at least one active hydrogen in one molecule, and that the end-blocked isocyanate prepolymer has a softening point of not lower than 50° C.

Abstract: The invention relates to novel oxazinones designed to bind to the penicillin receptor, methods of synthesizing the compounds, and the use of the compounds as antibacterial agents. The compounds have the general formula (I) Preferably the compounds have a carboxyethyl or a substituted carboxymethyl substituent at the 2-position and a hydroxyl group at the 5-position and have a molecular shape suitable for binding to and reacting with the active site of a pencillin-recognizing enzyme. The compounds are synthesized by condensing a carboxyl-protected N-hydroxy amino acid with a 3-hydroxyprotected-4-bromobutanoic acid to form a a doubly protected N-hydroxy N-acylamino acid, which is cyclized with an organic base to yield a: doubly protected 1,2-oxazin-3-one. The protecting groups are then removed to provide an antibacterial agent.

Abstract: N-substituted perhydro-2,3-diazines of the formula I in which the variables Z, R, m and RA are as defined in claim 1, a process for their preparation and the use of the compounds of the formula I as starting materials for preparing herbicides of the formula V in which R, RA, Z and m are as defined above, X is O or S and Q is a C6-C14-aromatic radical are described.

Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.

Abstract: The present invention relates to polyisocyanate mixtures prepared from aliphatic and/or cycloaliphatic diisocyanates and having a) an average isocyanate functionality of at least 2.0, b) a content of isocyanate groups (calculated as NCO; molecular weight=42) of 4.0 to 28.0 wt. % and c) a content of alkoxy groups having up to 36 carbon atoms of 2.0 to 37.5 wt. %, wherein the alkoxy groups are constituents of allophanate groups or optionally urethane groups, provided that >50 mol % of the alkoxy groups are a constituent of allophanate groups that are connected to at least two polyisocyanate molecules which are each prepared from at least two diisocyanates. The present invention also relates to a process for preparing these polyisocyanate mixtures and to coating compositions, which are highly diluted or dilutable with non-polar solvents and contain these polyisocyanate mixtures and lacquer binders or binder components optionally containing isocyanate-reactive groups.

Abstract: The invention relates to novel oxazinones designed to bind to the penicillin receptor, methods of synthesizing the compounds, and the use of the compounds as antibacterial agents. The compounds have the general formula (I) Preferably the compounds have a carboxyethyl or a substituted carboxymethyl substituent at the 2-position and a hydroxyl group at the 5-position and have a molecular shape suitable for binding to and reacting with the active site of a pencillin-recognizing enzyme. The compounds are synthesized by condensing a carboxyl-protected N-hydroxy amino acid with a 3-hydroxyprotected-4-bromobutanoic acid to form a a doubly protected N-hydroxy N-acylamino acid, which is cyclized with an organic base to yield a doubly protected 1,2-oxazin-3-one. The protecting groups are then removed to provide an antibacterial agent.

Abstract: The present invention relates to compounds containing modified hydrazide groups and corresponding to formula I wherein R represents the residue obtained by removing the isocyanate groups from a monomeric polyisocyanate, a polyisocyanate adduct or an NCO prepolymer, X represents OR′ or NHR′ and R′ represents a group which is inert to isocyanate groups under the conditions used to form the compound of formula I, R″ represents a divalent, linear or branched aliphatic group containing 2 to 10 carbon atoms, provided that there are at least two carbons between the oxygen atoms wherein the aliphatic group may optionally be substituted by heteroatoms to form ether or ester groups, and n is 2 to 6.

Abstract: The invention relates to a novel process of preparing (1,3,4)-oxadiazine derivatives of formula (I) and to their usefulness as pesticides in particular as anthelminticides, insecticides, acaricides, and nematicides.

Abstract: Non-crystallizing N,N′-disubstituted N-(2-hydroxyalkyl)-ureas are used as hydrolysis protection agents in plastics containing ester groups. These disubstituted hydroxy-alkylureas impart excellent protection from hydrolysis to plastics containing ester groups and can be added directly to the plastics to be stabilized without the addition of special solvents.

Abstract: The present invention relates to compounds containing modified hydrazide groups and corresponding to formula I ##STR1## wherein R represents the residue obtained by removing the isocyanate groups from a monomeric polyisocyanate, a polyisocyanate adduct or an NCO prepolymer,X represents OR' or NHR' andR' represents a group which is inert to isocyanate groups under the conditions used to form the compound of formula I andn has a value of 2 to 6.The present invention also relates to one-component, thermoset coating compositions containing the compounds of formula I and a cross-linking component that is reactive with these compounds. Finally, the present invention relates coatings, sealants and adhesives prepared from these thermoset compositions.

Abstract: The invention relates to novel (1,3,4)-oxadiazine derivatives of formula (I), to a process and intermediates for their preparation, and to their usefulness as pesticides, in particular as anthelminthics, insecticides, acaricides, and nematicides.

Abstract: The present invention relates to a process for the preparation of trimerized polyisocyanates that contain at least 30 mole % of iminooxadiazinedione groups (asymmetric trimers) in the trimer mixture, by catalytically trimerizing a starting isocyanate selected from organic di- or polyisocyanates having a number average molecular weight of 140 to 600 and containing aliphatically, cycloaliphatically and/or araliphatically bound isocyanate groups in the presence of a quaternary phosphonium polyfluoride trimerization catalyst corresponding to the formulaR.sub.4 P.sup.+ F.sup.- n(HF)whereinR represents identical or different, optionally branched aliphatic, aromatic and/or araliphatic C.sub.1 -C.sub.20 groups, or two or more R groups may also form, with one another and with the phosphorus atom, saturated or unsaturated rings andn has a value of 0.1 to 20.

Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).

Abstract: Compounds of formula (I), wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a group ##STR2## R.sub.1 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.3 is hydrogen, an unsubstituted or substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group, or C(.dbd.O)--R.sub.5, R.sub.5 is C.sub.1 -C.sub.4 alkyl C.sub.1 -C.sub.4 alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R.sub.6).sub.2, each R.sub.6, independently of the other, is hydrogen, C.sub.1 -C.sub.4 alkyl or unsubstituted or substituted phenyl, X is CH--NO.sub.2, N--CN or N--NO.sub.2 and n is from 1 to 3, in free form or in salt form, and, where appropriate, tautomers of those compounds and the salts thereof, can be used as agrochemical active ingredients and can be prepared in a manner known per se.

Abstract: Insecticidal dihydrooxadiazine compounds having the formula: ##STR1## wherein X is O or S; R is a substituted or unsubstituted phenyl or heterocyclic group; R.sup.1 is halogen, haloalkyl or haloalkoxy; R.sup.2, R.sup.3 , and R.sup.4 are, independently, hydrogen, alkyl or alkoxy; R.sup.5 is nitro, cyano, alkoxy, alkyl, haloalkoxy, dialkylamino, alkylthio, phenoxy, phenylthio, or alkoxycarbonyl; R.sup.6 is hydrogen, alkyl, alkylthio, alkoxyalkyl, alkoxycarbonyl, acyl, or benzyl, wherein R.sup.3 and R.sup.5 together can form a ring.

Abstract: 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.

Abstract: 1,2,4-oxa-diazolino and 1,2,4-oxa-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.

Abstract: The present invention relates to polycyclic iminooxadiazinediones A corresponding to formula I ##STR1## The present invention also relates to mixtures of these polycyclic iminooxadiazinediones with other isocyanate derivatives and to their use for the production of optionally foamed polyurethane plastics, for the production of paints and coatings and for the production or formulation of active ingredients, pharmaceutical products, etc.

Abstract: N-alkyl polyhydroxy alkyl amines such as N-methyl glucamine having a Gardner Color of less than 1 are reacted with sources of fatty acyl groups such as methyl esters, anhydrides, and/or fatty acids that have greater than 98% transmittance at 460 nm in organic hydroxy solvents such as methanol to prepare N-alkyl polyhydroxy amine amides with good color. The N-alkyl polyhydroxyamines can be purified by crystallization, and/or subjected to reductive bleaching, to provide superior color. The reaction is preferably carried out at low temperature for short periods of time and with low catalyst levels to minimize formation of cyclic products. The resulting amide product can be further purified by treatment with anionic and cationic exchange resins to remove soap and amine impurities. The anionic ion exchange resin can be readily regenerated by acidifying it followed by washing with an organic solvent.

Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.

Abstract: Arthropodicidal compounds, compositions and use of compounds having the formula ##STR1##

Abstract: Phthalazinedione compounds and pharmaceutical compositions are described. The compositions are useful in treating human or animal patients to alleviate or cure disease or disease symptoms caused by nuclear ADP-ribosyl and similar transferases.

Abstract: Disclosed are novel anellated triazole compounds of formula, in which R.sup.A, m, n, X--X, V, W and Q have the meaning stated in the specification; a method of their preapartion; and their use as herbicides.

Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R.sup.1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.

Abstract: A method for handling and stabilizing a (2-alkyl)-acryloyl isocyanate represented by the formula (1) ##STR1## is disclosed, which comprises the steps of: reacting an azomethine compound represented by formula (2) ##STR2## with the (2-alkyl)-acryloyl isocyanate of formula (1) to obtain the reaction product of formula (3) ##STR3## and dissolving said reaction product into a solvent to regenerate the (2-alkyl)-acryloyl isocyanate of formula (1); the identity of said solvent and R-groups being defined herein.

Abstract: Arthropodicidal carboxanilides of Formula I and II ##STR1## wherein Q is selected from the group ##STR2## A, E, G, X, X.sup.1, Y, Z, Z.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and n are as defined in the text, arthropodicidal compositions containing said compounds and a method for using the compounds to control arthropods.

Abstract: A solvent soluble heterocyclic o-hydroxy thione carrying a lipophilic group and the process for the selective extraction of gallium, and certain other related metals, especially from solutions containing excess aluminium.

Abstract: The invention provides novel 2,3,6 substituted quinazolinones having the formula: ##STR1## wherein R.sup.6, R and X are as described in the specification, which have activity as angiotensin II (AII) antagonists.

Abstract: The invention concerns an aryl derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a heterocyclic moiety, and X.sup.1 is oxy, thio, sulphinyl, sulphonyl, difluoromethylene, imino, (1-4C)alkylimino or optionally substituted (1-4C)alkylene, or X.sup.1 is a group of the formula--X.sup.4 --CR.sub.2 -- or --CR.sub.2 --X.sup.4 --whereinX.sup.4 is oxy, thio, sulphinyl, sulphonyl or carbonyl and each R is hydrogen, methyl or ethyl;each of Ar.sup.2 and Ar.sup.3 is optionally substituted phenylene;X.sup.2 is oxy, thio, sulphinyl or sulphonyl;R.sup.1 is (1-4C)alkyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X.sup.3 --A.sup.2 -- which together with the carbon atom to which A.sup.1 and A.sup.2 are attached define a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X.sup.

Abstract: A process for the preparation of 1,3-disubstituted 2-nitroguanidines of the formula I ##STR1## in which R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or a radical --CH.sub.2 B; A is an unsubstituted or mono- to tetrasubstituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, which may contain one or two substituents from the group comprising C.sub.1 -C.sub.3 haloalkyl having 1 to 7 halogen atoms, cyclopropyl, halocyclopropyl having 1 to 3 halogen atoms, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, C.sub.2 -C.sub.3 haloalkenyl and C.sub.2 -C.sub.3 haloalkynyl having 1 to 4 halogen atoms, C.sub.1 -C.sub.3 haloalkoxy having 1 to 7 halogen atoms, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkylthio having 1 to 7 halogen atoms, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro and one to four substituents from the group comprising C.sub.1 -C.sub.3 alkyl, C.sub.

Abstract: Novel compounds having the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.

Abstract: Angiotension II inhibition is exhibited by ##STR1## wherein: R.sup.1 and R.sup.2 are each independently hydrogen, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, thiophenalkyl, pyridylalkyl, or --R.sup.8 CO.sub.2 R.sup.9 ;R.sup.3 is a single bond, --S--, or --O--;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, aralkyl, cycloalkylalkyl, or thiophenalkyl;R.sup.7 --(CH.sub.2).sub.n --CO.sub.2 R.sup.9, ##STR2## --NHSO.sub.2 CF.sub.3, --SO.sub.3 H, --C(CF.sub.3).sub.2 OH, ##STR3## --PO.sub.3 H, ##STR4## --CONHOR.sup.12, --CONHNHSO.sub.2 CF.sub.3, --(CH.sub.2).sub.n --5--tetrazolyl (optionally substituted with R.sup.9), and the remaining symbols are as defined in the specification.

Abstract: Pyridazinone, triazinone and oxapyridazinone compounds which are useful in inhibiting lipoxygenase enzymes, particularly 5-lipoxygenase.

Abstract: There is provided a pest control composition containing a compound represented by the formula, ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and independently mean a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted and X means an electron attracting group or a salt thereof.The compounds are of minimal toxicity to man, domestic animals and fish and selectively display remarkable control effect on pests.

Abstract: Organophosphorus-substituted oxadiazines are disclosed which exhibit insecticidal, acaricidal and nematicidal activity, as well as compositions including such compounds, and methods for controlling insects, acarids or nematodes employing such compounds and/or compositions. Also disclosed are novel intermediates useful in the preparation of such compounds.