Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

Abstract: Compounds of formula (I) 1

Abstract: The present invention provides a compound of the formula (I) and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. In said formula, X=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Y=O, (CH2)m, S, SO, SO2, NH, NR8; Z=NH, O, NR8, S, SO, SO2. The remaining substituents are described in the specification.

Abstract: An electrochromic device comprising at least one substantially transparent substrate having an electrically conductive material associated therewith, and an electrochromic medium which comprises a solvent, a cathodic material, and an anodic electrochromic material represented by the formula: wherein R1-R10 are the same or different and at least three of R1-R10 are the same or different and comprise a straight or branched alkyl, aryl, alkaryl, or aralkyl group containing approximately 1 to approximately 40 carbon atom(s), and/or a silyl or siloxyl group containing approximately 1 to approximately 40 silicon atom(s), wherein the carbon or silicon atom(s) may be a linking group to, or part of, one or more functional groups comprising nitrites; nitro constituents; sulfoxides; sulfonates; phosphonium constituents; phosphonates; phosphonites; ammonium constituents; viologens, including bipyridinyl constituents; carbonyls, including carbonates, carbamates; ketones; esters; and amides; ethers, inclu

Abstract: This invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof; in which preferably R3, R4 and R6 are each hydrogen; X is C═O or CH2; and R7 and R8 are each independently selected from the group consisting of hydrogen, (C1-C12)alkyl, (C3-C8)cycloalkyl and (C1-C12)alkyl (C6-C14)aryl; or R7 and R8 when taken together form a (C2-C7)alkylene group; or —NR7R8 together forms a (C2-C14)heterocyclic or substituted (C2-C14)heterocyclic. Such compounds modulate the activity of serine hydrolases and can be used in pharmaceutical compositions for the treatment of Alzheimer's disease.

Abstract: A process for synthesizing 2-amino-5-dimethlyaminophenyl thiosulfonic acid comprises the step of oxidizing N,N′-dimethyl-&rgr;-phenylene-diamine in the presence of a source of thiosulfate ions, while maintaining the temperature of the reaction mixture not higher than about 10° C. This compound is useful as an intermediate in the synthesis of toluidine blue O. A process for manufacturing toluidine blue O with improved yield, includes the step of preparing the intermediate 2-amino-5-diethylaminopropyl thiosulfonic acid according to the above described procedure.

Abstract: This invention is directed to certain N,N′-dinitroso phenylenediamines useful as polymerization inhibitors for acrylic acids and esters thereof. Also disclosed are compositions containing such compounds, and methods for inhibiting polymerization using such compounds and compositions.

Abstract: A process for synthesizing 2-amino-5-dimethlyaminophenyl thiosulfonic acid comprises the step of oxidizing N,N′-dimethyl-&rgr;-phenylene-diamine in the presence of a source of thiosulfate ions, while maintaining the temperature of the reaction mixture not higher than about 10° C. This compound is useful as an intermediate in the synthesis of toluidine blue O. A process for manufacturing toluidine blue O with improved yield, includes the step of preparing the intermediate 2-amino-5-diethylaminopropyl thiosulfonic acid according to the above described procedure.

Abstract: A compound of formula (I) ##STR1## its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates, wherein R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are the same or different; R.sup.1 and R.sup.2 together represent along with carbon atoms to which they are attached an aromatic cyclic structure containing 5-6 ring atoms which may optionally be substituted; X represents a heteroatom selected from oxygen or sulfur; R.sup.7 represents hydrogen atom, hydroxy, alkoxy, halogen, lower alkyl group or optionally substituted aralkyl group or forms a bond together with R.sup.8 ; R.sup.8 represents hydrogen atom, hydroxy, alkoxy, halogen, lower alkyl group or optionally substituted aralkyl or R.sup.8 forms a bond together with R.sup.

Abstract: A reagent, kit and method for the quantative determination of ascorbic acid in a sample uses ascorbate oxidase which catalyzes the reaction of reduced ascorbic acid to oxidized ascorbic acid and hydrogen peroxide. Ascorbic acid in the sample is reacted with oxygen in the presence of the ascorbate oxidase, chromogen and peroxidase. Absorbance is determined and compared with a known calibration curve.

Abstract: Thienopyrimidine derivatives are disclosed. Also disclosed are methods for the production and use of these compounds.

Abstract: A process for removing aromatic heterocyclic compounds from a product-containing solution, in particular a protein solution, by bringing the solution into contact with a support material. The process is preferably carried out following a virus inactivation with acridine or acridine derivatives and makes it possible to remove these virus-inactivating agents from the solution without there being any significant product losses or changes in the biological activity of the solution.

Abstract: A diamine compound of the following formula (1): ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl group or a lower alkoxy group, each of A.sub.1, A.sub.2 and A.sub.3 which are independent of one another, is a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, or a group of the following formula (2): ##STR2## wherein R.sub.1 is as defined above, and X is a substituted or unsubstituted arylene group or a substituted or unsubstituted heterocyclic bivalent group.

Abstract: A quinuclidine derivative represented by the following general formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, which has strong squalene synthase inhibiting activity and is useful as a cholesterol lowering agent without causing side effects. ##STR1## (Symbols in the formula represent the following meanings; R.sub.1 : a hydrogen atom, a halogen atom or a lower alkyl group,R.sub.2 : a hydrogen atom, a hydroxyl group or a lower alkoxy group,. . : a single bond or a double bond, with the proviso thatR.sub.2 does not exist when . . . is a double bond,X and Y: the same or different from each other and each represents a bond, an oxygen atom (--O--), a carbonyl group (--CO--), a group represented by the formula --S(O).sub.p -- or a group represented by the formula --NR.sub.3 --,p: 0, 1 or 2,R.sub.3 : a hydrogen atom or a lower alkyl group which may have a substituent,A: a saturated or unsaturated lower alkylene group, a group of the formula --(CH.sub.2).sub.m Z(CH.sub.

Abstract: The present invention involves a method for the preparation of substituted 3-(phenylimino)-3 H-phenothiazines or phenoxazines which method involves reacting phenothiazine or phenoxazine with an aromatic amine in the presence of periodic acid as coupling agent.

Abstract: A biological stain composition contains toluidine blue O and a pharmaceutically acceptable oxidizing agent to convert any leuco toluidine blue O to the chromo form. A dry composition for preparing the stain includes the toluidine blue O, the oxidizing agent and an effervescent agent. These compositions are preferably buffered to improve shelf stability and clinical consistency. Compositions for intra-oral application contain a flavoring agent.

Abstract: There is disclosed a novel phenothiazine derivative of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are a C.sub.1-6 alkyl group and at least one of them has as a substituent a group which can react with amino group, thiol group or carboxyl group, and X.sup.- is a counter ion of the phenazathionium. Their production and the intermediates used in the production are also disclosed. The compound (I) is a derivative of methylene blue and is applicable to photodynamic therapy of cancer or immunoassays utilizing chemiluminescence.

Abstract: The present invention relates to the preparation of antioxidant additives to lubricants and to their use in lubricating compositions. The additives according to the invention have the formula:ArAr'(H)N--(R--X).sub.a --R'Ywhere--Ar and Ar' are identical or different aromatic radicals, R and R', which are identical or different, denote a C.sub.2 -C.sub.18 linear or branched alkylene radical, X denotes an oxygen or sulphur atom or an --NH group, a is an integer between 0 and 5 and Y is chosen from the group consisting of --NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2, which are identical or different, denote a hydrogen atom or a C.sub.1 -C.sub.12 alkyl, alkenyl, cycloalkyl or arylalkyl radical --N.dbd.CH--Ar.sub.1 where Ar.sub.1 is an aryl radical containing at least one phenolic group --NR.sub.1 --CO--Ar.sub.1 and ##STR1## where R.sub.3 denotes a saturated or unsaturated, linear or branched alkyl radical.

Abstract: A novel prolinal derivative of general formula: ##STR1## [wherein A represents a group of the general formula: ##STR2## (wherein one of R.sup.1 and R.sup.2 represents hydrogen atom and the other represents alkyl group of from 2 to 5 carbon atoms, alkoxy group of from 1 to 5 carbon atom(s), phenyl group, benzyl group, cycloalkyl group of from 4 to 6 carbon atoms or (cycloalkyl group of from 4 to 6 carbon atoms)--methyl group or R.sup.1 and R.sup.2 each represents, same or different, alkyl group of from 1 to 4 carbon atom(s).) or a group of the general formula: ##STR3## (wherein m represents an integer of from 3 to 6.) n represents an integer of from 3 to 10.D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, nitro group, trifluoromethyl group, alkyl or alkoxy group of from 1 to 4 carbon atom(s).]possess inhibitory activity on prolyl endopeptidase, and therefore be useful for treating and/or preventing agent for amnesia.

Abstract: The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents.A compound disclosed is 2,4-diallylamino-6-{4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl) methylamino]piperidin-1-yl}-1,3,5-triazine.

Abstract: An optical probe enables the study of enzyme activity by absorbance spectroscopy or by sensitive fluorescence methods. In particular, the probe provides the ability to monitor the activity of cytochrome P-450.sub.scc enzyme, the rate limiting enzyme for steroid biosynthesis. Located on the inner mitochondrial membrane, P-450.sub.scc catalyzes the conversion of cholesterol to pregnenolone and isocapraldehyde by sequential oxidations of the cholesterol side chain. The fluorogenic probe includes a cholesterol-like steroid linked to a chromophore through a linking group. The chromophore is selected to have little optical response when linked to the steroid substrate and an enhanced optical response when cleaved from the substrate and linking group. Thus, a fluorescent anion that can be optically detected is generated by the side-chain cleavage reaction during steroidogenesis.

Abstract: A cationic dye-borate anion compound represented by the formula: ##STR1## where D+ is a cationic dye moiety selected from the group consisting of cationic cyanine, carbocyanine, hemicyanine, rhodamine, and azamethine dyes; R.sup.1 is alkyl; and R.sup.2, R.sup.3, and R.sup.4 are aryl. Such cationic dye-borate anion compounds are useful photoinitiators of free radical addition reactions.

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

Abstract: Diaryl sulphides and diaryl selenides of formula:Ar--X--Arwhere X=S or Se and Ar=aryl are made by the action of sulphur and sulphur dioxide or selenium and selenium dioxide on a compound of formula:Ar--HThe process is especially useful for the preparation of phenothiazines of formula ##STR1## in which X=S or Se and Z and Z.sub.1, which may be identical or different, are each hydrogen, halogen, alkyl or alkoxy.

Abstract: Urea derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently a 4-disubstituted aminoaryl group or the like, and R.sup.3 is a carboxyalkyl group or the like, is soluble in water and effective as a color producing reagent for determining hydrogen peroxide or the like or the activity of peroxidase.

Abstract: Novel adducts of oxazine urea chromophors or thiazine urea chromophors with organic substrates are provided which are useful in analytical techniques for the detection and measurement of biological and clinical compounds of interest.

Abstract: Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.

Abstract: Novel chromophor derivatives of cyclic anhydrides are provided which have the ability to react with a variety of organic substrates forming adducts which are useful in analytical techniques for the detection and measurement of biological compounds.

Abstract: Oxazine, thiazine and diazine leuco dyes are synthesized through a reaction using a dicyclohexylcarbodiimide adduct. The adducts are themselves novel compounds.

Abstract: Novel urea derivatives of oxazine and thiazine chromophors have the structural formula I or II. ##STR1## wherein M is oxygen or sulfur, R.sub.1 and R.sub.2 are aliphatic alkyl groups or hydrogen; R.sub.3 is hydrogen or alkyl group; R.sub.4 is hydrogen, alkyl or amine group; R.sub.5 is hydrogen, amine or alkyl group; X.sup..crclbar. is an anion consisting of an organic (e.g. CH.sub.3 COO.sup..crclbar., CH.sub.3 CH.sub.2 COO.sup..crclbar. and the like) or inorganic specie (e.g. Cl.sup..crclbar., Br.sup..crclbar., I.sup..crclbar., ClO.sub.4.sup..crclbar., SO.sub.4 ", and the like); n is 0 to 20; Z is N.dbd.C.dbd.O, N.dbd.C.dbd.S, carboxylic, primary or secondary amine, and when n=0, Z may be ##STR2## wherein Q is hydroxyl, amino, carboxylic, sulfydryl, isocyanato, or isothiocyanato.The functional oxazine-urea and thiazine-urea derivatives react with compounds of interest to form adducts resulting in the fluorescent labeling of the compound.

Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.

Abstract: Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.

Abstract: 3-(N--R.sup.2 --N-Acylamino)-7-(N--R.sup.3 --N--R.sup.4 -amino)-10-acylphenothiazines and phenoxazines useful as color formers, particularly in electrochromic recording systems, are prepared by the interaction of the corresponding 3-(N--R.sup.2 -amino)-7-(N--R.sup.3 --N--R.sup.4 -amino)phenothiazinium or phenoxazinium halide with a reducing agent to obtain the corresponding leuco compound and subsequently interacting the leuco compound with at least two molecular proportions of an acylating agent.

Abstract: The present invention refers to novel anellated 4H-1,4-benzothiazines, several processes for the synthesis thereof, their use as pharmaceutical agents, in particular their use as lipoxygenase-inhibiting agents, pharmaceutical compositions containing the novel benzothiazines and a process for their manufacture.

Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.

Abstract: Novel phenoxazine and phenothiazine dyes have the formula ##STR1## wherein X can be --S-- or --O--;each R can be the same or different and is independently selected from(1) hydrogen,(2) an unsubstituted aryl or alkyl group or these groups substituted by up to four groups selected from alkyl, alkoxy, cyano, hydroxy, halogen, nitro, mercapto, alkylsulfonyl, arylsulfonyl, and Z, where Z is as defined below, wherein all alkyl and alkoxy groups have 1 to 20 carbon atoms; and(3) Z, wherein Z can be ##STR2## wherein each Q can be the same or different and is independently selected from(1) hydrogen,(2) an unsubstituted aryl or alkyl group or these groups substituted by up to four groups selected from alkyl, alkoxy, cyano, hydroxy, halogen, nitro, mercapto, alkylsulfonyl, arylsulfonyl, and Z, where Z is as defined above, wherein all alkyl and alkoxy groups have 1 to 20 carbon atoms; andR' is the same or different and is independently selected from hydrogen, halogen, alkyl or alkoxy of 1 to 6 carbon atoms or these grou

Abstract: 3-(R-Carbonyloxy)-7-(N-R.sup.1 -N-R.sup.2 -amino)-10-(RCO)-phenothiazines useful as color formers, particularly in electrochromic recording systems, are prepared by the interaction of the corresponding 7-(N-R.sup.1 -N-R.sup.2 -amino)phenothiazin-3-one with a reducing agent to obtain the corresponding leuco compound and subsequently interacting the leuco compound with about two molecular proportions of an acylating agent.

Abstract: Urethanes are made by reacting an organic nitro compound with an organic compound containing at least one hydroxyl group in the presence of carbon monoxide, hydrogen and a catalyst system. The carbon monoxide and hydrogen are used in quantities such that the molar ratio of CO to H.sub.2 is from 0.3:1 to 3:1. The catalyst system is made up of at least one noble metal or compound of a noble metal from Group VIIIB of the Periodic System of Elements, at least one organic nitrogen base and a co-catalyst combination of iron or copper oxidic or hydroxidic compound and a chloride compound. The product urethanes are useful in the production of isocyanates and pesticides.

Abstract: Hydrocarbon processing equipment is protected against fouling during the processing of hydrocarbons at elevated temperatures by adding to the equipment small amounts of the N,N'-dimer of phenothiazine or a substituted phenothiazine.

Abstract: Vinyl aromatic compounds are stabilized against undesired polymerization by adding to the vinyl aromatic compounds small amounts of at least one N,N' dimer of phenothiazine or a substituted phenothiazine and at least one mono- or ditertiary alkylphenol.

Abstract: Vinyl aromatic compounds are stabilized against undesired polymerization by adding to the vinyl aromatic compounds small amounts of at least one N,N' dimer of phenothiazine or a substituted phenothiazine and at least one mono- or ditertiary alkyl catechol and/or at least one mono- or ditertiary alkylhydroquinone.

Abstract: Vinyl aromatic compounds are stabilized against undesired polymerization by adding to the vinyl aromatic compounds small amounts of the N,N'-dimer of phenothiazine or a substituted phenothiazine.

Abstract: Vinyl aromatic compounds are stabilized against undesired polymerization by adding to the vinyl aromatic compounds small amounts of at least one N,N-diarylhydroxylamine and at least one N,N' dimer of phenothiazine or substituted phenothiazine.

Abstract: Recording members having excellent light resistance are obtained by using as a dye precursor specific diarylaminofluoran compounds.

Abstract: Compounds of the formula ##STR1## wherein each X, which may be identical or different from the other X, is oxygen or imino;R.sub.1 is hydrogen, fluorine, chlorine or bromine;R.sub.2 and R.sub.3, which may be identical or different from each other, are each hydrogen; unsubstituted or mono-substituted alkyl of 1 to 6 carbon atoms, where the substituent is phenyl or dialkylamino with 1 to 3 carbon atoms in each alkyl moiety; pyridyl; or cycloalkyl of 5 to 7 carbon atoms;R.sub.2 and R.sub.

Abstract: A urethane is produced by reacting an organic nitro compound with carbon monoxide and an organic compound containing at least one hydroxyl group in the presence of a catalyst and a co-catalyst. This reaction is conducted in the liquid phase at elevated temperature and pressure. The catalyst employed is an element and/or compound of an element from the group of noble metals of the 8th Secondary Group of the Periodic Table. The co-catalyst used is formed from (1) a component taken from the group consisting of iron oxychloride, a mixture of iron compounds containing iron oxychloride and oxide-chloride combinations and (2) metallic iron or an iron alloy in finely divided or high surface form. The oxides which may be used in the oxide-chloride combinations of co-catalyst component (1) are the oxides and/or oxide hydrates of tetravalent tin, trivalent chromium, hexavalent molybdenum, hexavalent tungsten, pentavalent vanadium, divalent iron and trivalent iron.

Abstract: An improved process for preparation of a condensed product of phenothiazine and p-nitrosophenol which contains more than 60% by weight of indophenol S-oxide of the formula ##STR1## by condensing phenothiazine with p-nitrosophenol in sulphuric acid wherein the improvement comprises the phenothiazine being in 60 to 90% strength sulphuric acid at the time of addition of the p-nitrosophenol.

Abstract: Novel dyestuffs containing amino or imino groups and their preparation are provided.These dyestuffs have the general formula ##STR1## wherein R is --N(R.sub.3)CH.sub.2 --Z or --N.dbd.CH--Z, X is N or CR.sub.6 where R.sub.6 is a hydrogen atom or an optionally substituted alkyl or aryl group, Y is S.sup..sym., O.sup..sym., N or N.sup..sym. R.sub.7 where R.sub.7 is a hydrogen atom or an optionally substituted alkyl or aryl group, R.sub.1, R.sub.1 and R.sub.2 each represent a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom complete a heterocyclic ring, or one of R.sub.1 and R.sub.2 can be hydrogen and the other of R.sub.1 and R.sub.2 can be aryl, Z is a group which comprises both an activating group which contains at least one double bond system and also a ballasting group and R.sub.4 and R.sub.5 each represent optional substituents or form an annelated benzene ring.

Abstract: This invention relates to an improved process for the production of urethanes (i.e. carbamic acid esters) by reacting organic nitro compounds with carbon monoxide and organic compounds containing at least one hydroxy group in the presence of a unique catalyst system. The catalyst system consists of palladium or a palladium compound and iron oxychloride or a mixture of iron compounds containing iron oxychloride.

Abstract: Green sulfur dyestuff is produced by reacting phenothiazine in sulfuric acid with an oxidizing agent, condensing the oxidized phenothiazine with p-nitrosophenol and thionating with sulfur and sodium sulfide the condensate in a bake or reflux process.