Abstract: This invention is directed to substituted aryl compounds, which are linked to a substituted indole moiety by various linkers, and the kynurenine/kynuramine-like metabolites of these agents, their preparation and pharmaceutical compositions containing these compounds. This invention further is directed to the pharmaceutical use of the compounds for inhibiting GSK3? kinase and/or modulating N-methyl-D-aspartate (NMDA) channel activities for the treatment of neurodegenerative and other disorders.

Abstract: The present invention provides the diaminophenyladamantane derivatives with antitumor activities and the preparation method therefore. The method includes a step of reacting an aromatic diol with at least one 5-halo-2-nitrophenol in the presence of at least one inorganic base in an organic solvent with a relatively high boiling point.

Abstract: Novel metal-chelate complexes comprising aminocarboxylate ligands including substituted aromatic amide moieties, such as those having the formula wherein R13, A1, R1 and R2 are as defined herein, are disclosed.

Abstract: The present disclosure relates to a novel family of sulfur-containing secondary para-phenylenediamines, to processes for preparing them, to compositions for dyeing keratin fibers, for example keratin fibers such as the hair, comprising, in a suitable dyeing medium, at least such one sulfur-containing secondary para-phenylenediamine. The present disclosure also relates to processes for dyeing keratin fibers with the compositions according to the present disclosure and to multi-compartment dyeing kits containing such compositions.

Abstract: This invention relates to pyrimidine derivatives of general formula I in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases.

Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: The invention relates to benzoylcyclohexenone derivatives of general formula (I) wherein the variables R1 to R10 and n have the designation cited in claim 1.

Abstract: A process is described for the synthesis of an aryl sulfur pentafluoride compound. In one embodiment of the present invention, there is provided a process for preparing an aryl sulfurpentafluoride compound comprising: combining an at least one aryl sulfur compound with a fluorinating agent to at least partially react and form an intermediate aryl sulfurtrifluoride product; and exposing the intermediate aryl sulfurtrifluoride product to the fluorinating agent and optionally a fluoride source to at least partially react and form the aryl sulfurpentafluoride compound.

Abstract: The present invention relates to novel reactive dyes of the formula (I) where R1 to R4 are independently hydrogen, C1–C8-alkyl, C2–C8-alkyl, wherein nonadjacent CH2 groups may be replaced by oxygen atoms or imino or C1–C4-alkylimino groups and/or CH2 groups by carbonyl groups, C2–C8-alkenyl, aryl, arylalkylene or a moiety containing a reactive group or the precursor of a reactive group, with the proviso that at least one of R1 to R4 is a moiety which contains a reactive group or the precursor of a reactive group. The present invention further relates to the use of the reactive dyes of the formula (I) for dyeing substrates containing nucleophilic groups and to preparations containing at least one reactive dye of the formula (I).

Abstract: Disclosed are colorant compounds of the formula 1

Abstract: Disclosed are colorant precursor compounds of the formula 1

Abstract: The invention provides polyfluorinated aromatic or heterocyclic compounds comprising at least three ring substituents, at least one of which comprises a sulfurpentafluoride group and at least one of which comprises a labile group; methods for their preparation are also disclosed. Preferably, the compounds comprise either two sulfurpentafluoride groups or one sulfurpentafluoride group and one other polyfluorinated group, such as a trifluoromethyl group. Said labile group preferably comprises an amino, bromo or nitro group. Said compounds are useful in the preparation of medicaments.

Abstract: Compounds of formula I are effective in treating disorders modulated by opiate receptor activity and/or monoamine activity. In formula I, R1 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl; R2 is selected from hydrogen, hydroxy, cyano, haloalkyl, glycosyl, SO2R5, and OR5; R3 and R4 are independently selected from hydrogen and lower alkyl, or R3 and R4 taken together with nitrogen form a five- or six-membered heterocyclic or substituted heterocyclic ring; and R5 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl.

Abstract: A class of substituted biphenyl compounds is described for use in treating inflammation and inflammation-related disorders.

Abstract: The object of the present patent application are 3-aminophenol derivatives of formula (I) or the physiologically compatible, water-soluble salts thereof 1

Abstract: Substituted (Z)-styrylbenzyl sulfones of the formulae (I, II, III, IV), pharmaceutically acceptable salts thereof, and compositions thereof are provided as cell antiproliferative agents, including, for example, anticancer agents.

Abstract: N-Substituted glucamine compounds of formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections the compounds of formular I may be used alone, or in combinatioin with another antiviral agent selected from among nucleosides, nucleotides, immunomodulators, immunostimulants or various combination of such other agents.

Abstract: A process for the preparation of thiophenols of formula (I) wherein n is an integer from 1 to 5 and R is hydrogen, alkyl, hydroxyalkyl, alkylamino, dialkylamino, alkenyl, alkynyl, alkoxy, alkylthio, phenyl, naphthyl, phenoxy, phenylthio, halogen, hydroxy, mercapto, carboxyl, sulfo or heterocyclyl, by reacting phenyldiazonium salts of formula (II) wherein n and R are as defined and X is halogen or hydrogen sulfate, with sulfur at elevated temperature in the presence of an aqueous base and isolating the compounds of formula (I).

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted mercapto amines.

Abstract: The present invention provides an aniline derivative represented by the formula (I) 1

Abstract: The present invention is directed to labeled compounds, [2H1, 13C], [2H2, 13C] and [2H3, 13C]methyl aryl sulfides wherein the 13C methyl group attached to the sulfur of the sulfide includes exactly one, two or three deuterium atoms and the aryl group is selected from the group consisting of 1-naphthyl, substituted 1-naphthyl, 2-naphthyl, substituted 2-naphthyl, and phenyl groups with the structure 1

Abstract: Organic dye molecular materials prepared by coupling existing organic chromophore molecules to benzene or carbazole derivatives and nonlinear optical polymeric compounds having polyimide repeating units coupled with the organic dye molecular material are provided.

Abstract: New ligands having a backbone comprised of NCCX can be combined with a metal or metal precursor compound or formed into a metal-ligand complex to catalyze a number of different chemical transformations, including polymerization.

Abstract: Disclosed is a process for forming an azomethine compound, comprising: (a) reacting a compound “A” having an active methylene group or methine group with an arylprimaryamine compound “B”; (b) in the presence of a base and an oxidizing agent and in a solvent medium containing a ketone compound having the formula R1C(O)R2 wherein R1 and R2 are independently C1-C4 alkyl groups; (c) at a temperature low enough to provide a yield of the azomethine product of at least 50 mole % based on compound A.

Abstract: The invention concerns a method for the condensation of aromatic derivative(s) or a sulphinic derivative by a perhalogenated, advantageously perfluorinated, carbon atom. Said method is characterized in that it consists in subjecting said sulphinic derivative and said aromatic derivative to the action of a strong acid whereof the pKa is not more that 0. The invention is applicable to organic synthesis.

Abstract: A method for the preparation of hydroxythiol compounds by reacting a hydroxyl-protected halide compound having the structure: X—R—OPg with magnesium in a Grignard-suitable solvent to form a hydroxyl-protected magnesium halide compound, wherein R is selected from substituted or unsubstituted aliphatic radicals, substituted or unsubstituted cyclic aliphatic radicals, substituted or unsubstituted aromatic radicals, substituted or unsubstituted araliphatic radicals and substituted or unsubstituted heterocyclic radicals; Pg is a protecting group; and X is selected from the group consisting of F, Cl, Br and I; then reacting said hydroxyl-protected magnesium halide compound with sulfur in the Grignard-suitable solvent to form a hydroxyl-protected thiomagnesium halide compound; and hydrolyzing the protected hydroxyl group to form a hydroxythiomagnesium halide compound and converting the thiomagnesium halide to a thiol; wherein the protecting group is selected so that species formed by the de-protection

Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkyamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted mercapto amines.

Abstract: Indane compounds of general formulae (1) to (4) and their pharmaceutical use, particularly to achieve mast cell stabilising activity and/or anti-inflammatory activity are described.

Abstract: The present invention is directed to a new process for the synthesis of vinyl sulfoxides, in particular diarylvinyl sulfoxides

Abstract: Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.

Abstract: Disclosed is a process for selectively reducing a nitrile containing organic compound that also contains a sulfone moiety, the nitrile being reduced to a primary amine.

Abstract: A process for preparing S-(&ohgr;-aminoalkylamino) alkyl aryl sulfide dihydrochlorides includes the steps of (a) reacting aryl mercaptan and (&ohgr;-aminoalkylamino) alkylbromide dihydrobromide to cause condensation thereof in the presence of an organic base in an organic solvent and provide a condensation product; (b) converting the condensation product to a dihydrochloride salt; and (c) precipitating the dihydrochloride salt. Preferably the precipitated dihydrochloride salt is recrystallized. These dihydrochlorides are new and effective antidotes for sulfur mustard toxicity.

Abstract: The invention provides novel crosslinking aromatic diamines useful in preparing polyamic acids and polyimides for optical alignment layers. The novel compositions comprise crosslinking diamines containing a C3-C20 linear or branched hydrocarbon chains containing 1 to 4 carbon-carbon double bonds.

Abstract: The present invention relates to a new method for the synthesis of 2-hydroxyalkyl-para-phenylenediamines which are substituted or unsubstituted at the 5-position of the benzene ring, new 2-hydroxyalkyl-para-phenylenediamines which are substituted or unsubstituted at the 5-position of the benzene ring, their use for the oxidation dyeing of keratinous fibers, the dyeing compositions containing them, as well as the methods of dyeing using them.

Abstract: A compound of Formula I, providing tetrapartate prodrugs is provided 1

Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be colorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.

Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.

Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be calorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.

Abstract: This invention relates to a process for preparing perfluoroalkyl aryl sulfides by reaction of disulfides with alkali metal salts of aliphatic perfluorocarboxylic acids in the presence of a high-boiling aprotic solvent at elevated temperature and reduced pressure, wherein the product formed is distilled off at the rate at which it is formed. This invention further relates to the novel compounds 2-nitrophenyl pentafluoroethyl sulfide and 2-aminophenyl pentafluoroethyl sulfide.

Abstract: 4-(N,N-Dialkylamino)aniline compounds of the following general formula (I): wherein R1 represents an alkyl group, an aryl group or a heterocyclic group, R2 to R5 each represent a hydrogen atom or a substituent, and R2 and R3, R1 and R2, or R4 and R5 may form a ring together; a processing composition for color photography, which contains at least one of these compounds; and a color image-forming method wherein at least one of these aniline compounds is used.

Abstract: A compound of the formula: ##STR1## wherein: A is hydrogen, a substituted or unsubstituted C.sub.1 to C.sub.4 alkyl, a substituted or unsubstituted C.sub.1 to C.sub.4 alkoxy or a substituted or unsubstituted phenyl;W is a substituted or unsubstituted phenylene or a substituted or unsubstituted naphthylene;Y is--CH.sub.2 --CH.sub.2 --Z wherein Z is selected from --OSO.sub.3 H, --SSO.sub.3 H, --OPO.sub.3 H, --OCOCH.sub.2 --Cll.sub.3, Cl, Br or F; andm is 1 or 2, e is 0 or 1,with the sum of e+m=2.

Abstract: N-arylsulfilimine compounds, such as S,S-dimethyl-N-(2,6-dichlorophenyl)sulfilimine, were prepared and found to catalyze the reaction of aromatic sulfonyl chloride compounds, such as 2-chlorosulfonyl-7-fluoro-5-ethoxy[1,2,4]triazolo[1,5-c]pyrimidine, with aromatic amine compounds, such as 2,6-dichloroaniline, to form N-arylarylsulfonamide compounds, such as N-(2,6-dichlorophenyl)-7-fluoro-5-ethoxy[1,2,4]triazolo[1,5-c]-pyrimidine- 2-sulfonamide. The aryl moiety of the N-arylsulfilimine catalyst and the aryl moiety of the aromatic amine compound were generally chosen to be identical.

Abstract: A novel substituted benzenedithiol metal complex represented by the general formula (1) is provided. The substituted benzenedithiol metal complex is useful as a singlet oxygen quencher and as an optical data recording medium per se. ##STR1## wherein M is a transition metal; A.sup.+ is a quaternary ammonium group; and R is an organic group selected from the group consisting of organic groups represented by the formulae (i), (ii), (iii) and (iv): ##STR2## (wherein R.sup.1 is an alkyl group having 1 to 4 carbon atoms) ##STR3## (wherein n is 3, 4 or 5), ##STR4## (wherein R.sup.2 is one of a hydrogen atom and a substitutent having 1 to 4 carbon atoms).

Abstract: Novel nitrobenzene compounds of the nitroparaphenylene-diamine type substituted by sulphur in the 5-position are disclosed. These compounds are intended especially for the dyeing of keratin fibers and in particular human hair. A process for their preparation, dyeing compositions in which these compounds are present and a dyeing process in which these compositions are used are also disclosed.

Abstract: 2-Amino-6-chlorophenyl-alkylsulfanes are prepared in a particularly advantageous manner by hydrogenating 2-chloro-6-nitrophenyl-alkylsulfanes catalytically in the presence of a solvent without the addition of a further sulfur compound, and the novel compound 2-amino-6-chlorophenyl-isopropylsulfane is provided.

Abstract: Reagents and methods for multi-step labeling of nucleic acids allow the addition of relatively insoluble or unstable labels to nucleic acid in the final step. Nucleic acids can be stored as a stable intermediate capable of reacting with a label conjugated to a thiol-reactive group.

Abstract: Odor formation during storage of (hydrocarbylthio)aromatic amines due to formation and release of odoriferous sulfur-containing species such as dihydrocarbyldisulfides, is suppressed. To accomplish this, a small amount of N,N-dihydrocarbylhydroxylamine odor-inhibitor (e.g., N,N-diethylhydroxylamine) is blended with the (hydrocarbylthio)aromatic amine. This enables products such as a mixture of 3,5-di(methylthio)-2,4-diaminotoluene and 3,5-di(methylthio)-2,6-diaminotoluene) to be stored for long periods of time with significantly reduced formation and release of odoriferous sulfur-containing species.

Abstract: 1-phenyl-2-dimethylaminomethyl-cyclohexan-1-ol compounds, methods of preparing them and the use of these compounds in drugs are described.

Abstract: 4-Mercaptobenzoylguanidines of the formula I ##STR1## in which A, R.sub.1, R.sub.2 and R.sub.3 have the meanings given, and the physiologically unobjectionable salts thereof exhibit antiarrhythmic properties and are active as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.