Abstract: The invention provides pharmaceutical compositions comprising primary N-hydroxylamines and related therapeutic, prophylactic, diagnostic and screening methods. The pharmaceutical compositions generally comprise a pharmaceutical composition comprising an orally administrable effective unit solid dosage of a primary N-hydroxylamine or a pharmaceutically acceptable salt thereof and substantially free of a nitrone corresponding to the hydroxylamine.

Abstract: The present invention provides a polyimide having the formula (II) formed by reacting a dianhydride with the diamine having the formula (I). The polyimide provided by the present invention serves as a material for preparing the liquid crystal aligning film, wherein the liquid crystal aligning film could achieve the pre-tilt angle of 88-90° by containing only less than 5% of the diamine having the formula (I), which could highly lower down the manufacturing cost.

Abstract: Alkanolamine compositions are disclosed. The composition comprises an alkanolamine and hydroxylamine or hydrazine. Preferred alkanolamine includes diethanolamine, triethanolamine, and mixtures thereof. The composition of the invention has significantly reduced discoloration.

Abstract: A method for preparing hydroxylamine is provided that includes the steps of (i) pretreating an acidic buffer solution; and (ii) reducing nitrate ions in the acidic buffer solution with hydrogen to give hydroxylamine in the presence of catalysts, wherein the pretreatment is performed by adding a precipitant represented by formula (I) to the acidic buffer solution, [(A)aM(CN)6.xH2O]??(I) allowing the metal impurities in the acidic buffer solution to react with the precipitant to form metal complex, and then to remove the metal complex. The metal complex is formed and separated by pretreating the acidic buffer solution with a specific precipitant without adjusting pH and changing the composition of the acidic buffer solution prior to hydroxylamine synthesis, thus enhancing the selectivity of the hydroxylamine production.

Abstract: Compounds of formula wherein A0, A1 and A2 are each independently of the others a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge which is unsubstituted or substituted by from one to six identical or different substituents selected from halogen and C3-C8cycloalkyl; Y is, for example, O, S, SO or SO2; M is O or NOR6, X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylcarbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C2-C6alkynyl; Q is, for example, O, S, SO or SO2; W is, for example, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; D is CH or N; R4 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R5 is, for example, C1-C12alkyl, C3-C8cycloalkyl or —N(R7)2; R7 is H, C1-C6alkyl, C1-C3haloalkyl, C1-C6alkylcarbonyl, C1-C3haloalkylcarbonyl, C1-C6alkoxycarbonyl, C3-C8cycloalkyl, C3-C8 cycloalkyl

Abstract: A method for preparing hydroxylamine, comprising the steps of: (i) pretreating the acidic buffer solution with the compounds having a functional group represented by formula (I), thereby removing metal impurities from the acidic buffer solution; and (ii) reducing nitrate ions in the acidic buffer solution with hydrogen to give hydroxylamine in the presence of catalysts, According to the present invention the selectivity for reducing nitrate ions to give hydroxylamine can be significantly enhanced.

Abstract: A process for preparing N,N-dihydrocarbylhydroxylamines of the general formula (I) where R1, R2, R3 and R4 are selected independently from among hydrogen, aliphatic, cycloaliphatic, heteroaromatic and aromatic radicals, or R1 and R2 and/or R3 and R4 are joined to form a ring, and not more than one radical among R1, R2, R3 and R4 is hydrogen, which comprises the steps a) reaction of hydroxylamine H2NOH or a salt of hydroxylamine with a compound of the general formula (II) or (III) where R1, R2, R3 and R4 are as defined in formula (I), b) hydrogenation of the compound formed in step a) in the presence of a catalyst, c) further reaction of the compound formed in step b) with a compound of the general formula (II) or (III) and hydrogenation of the reaction mixture in the presence of a catalyst and d), if appropriate, reaction of the salt of the dihydrocarbylhydroxylamine formed in step c) with a base.

Abstract: To provide a novel compound which inhibits the generation of AGE and an AGE generation inhibitor containing the compound. A compound represented by the following formula or a pharmaceutically acceptable salt thereof, a medicinal composition containing the compound or such a salt thereof, and an additive composition containing the compound.

Abstract: A method for preparing hydroxylamine by reducing nitric acid or its salt with hydrogen gas in an aqueous medium in the presence of a catalyst, wherein reduction of nitric acid or its salt is performed in a reactor comprising a reaction section, a cooler disposed at the lower portion of the reactor, and a middle gas distributor and a lower gas distributor respectively disposed above and below the cooler for introducing hydrogen gas into the reaction section. According to the present invention, gas distribution become more uniform by disposing the gas distributors at different positions of the reactor, which results in higher yield of hydroxylamine.

Abstract: This invention pertains to a novel process for preparing sterically hindered N-substituted alkyloxyamines from alkenes by the transition-metal-catalyzed reaction of a intermediate alkylborane with a sterically hindered nitroxyl radical.

Abstract: Compounds of formula (I) and (IA) have antibacterial or antiprotozoal activity: formula (1) formula (2) wherein: Z represents a radical of formula N(OH)CH(?O) or of formula C(?O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl, or, except when Z is a radical of formula N(OH)CH(?O), a hydroxy or amino group; R2 represents a radical of formula R10—(X)n-(ALK)m- wherein R10 represents hydrogen, or an optionally substituted c1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 ?alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent NH—, —O— or S— linkages, X represents NH—, —O— or S—, and m and n are independently 0 or 1; R3 represents hydrogen, C1-C6alkyl, or benzyl; and R4 is as defined in the specification.

Abstract: A process is described for preparing isoxazoles of the formula I where the substituents are as defined below: R1 is hydrogen, C1-C6-alkyl, R2 is C1-C6-alkyl, R3, R4, R5 are hydrogen, C1-C6-alkyl, or R4 and R5 together form a bond, R6 is a heterocyclic ring, n is 0, 1 or 2; which comprises preparing an intermediate of the formula VI where R1, R3, R4 and R5 are as defined above, followed by halogenation, thiomethylation, oxidation and acylation to give compounds of the formula I. Also novel intermediates for preparing the compounds of the formula I and novel processes for preparing the intermediates are described.

Abstract: The present invention relates to open chain alkoxyamine compounds, a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) at least one open chain alkoxyamine compound. Further aspects of the present invention are a process for polymerizing ethylenically unsaturated monomers, and the use of open chain alkoxyamine compounds for controlled polymerization. The intermediate N-oxyl derivatives, a composition of the N-oxyl derivatives with ethylenically unsaturated monomers and a free radical initiator X, as well as a process and their use for polymerization are also subjects of the present invention.

Abstract: The corresponding ?-aminooxy ketone is manufactured with a high yield and a high enantioselectivity. A manufacturing method for an optically active ?-aminooxy ketone derivative expressed by formula (1), wherein a ketone expressed by formula (2) is caused to react with a nitroso compound expressed by formula (3) in the presence of a proline derivative expressed by formula (4). In the formula, R1 and R2 respectively denote an alkyl, alkenyl or alkynyl group, and R1 and R2 may be linked to form a ring. R3 denotes an aryl, heterocyclic, alkyl, alkenyl or alkynyl group. A denotes a hydrogen atom, alkoxy group, aryloxy group, acyloxy group or silyloxy group which may have a substituent.

Abstract: An O-substituted hydroxylamine having the following general formula: R1—CHX—O—NH2 wherein X is hydrogen or an alkyl; and R1 is an unsubstituted or substituted phenyl, thienyl, furanyl, pyrrolyl or —CR2?CR3R4; wherein R2, R3 and R4 are hydrogen, halogen or alkyl. The O-substituted hydroxylamine exhibits at least one property selected from the group consisting of: essentially free of hydroxylamine; essentially free of any solvent; a water content of between about 0% to 90% by weight; and a high strength (as measured by mole of the O-substituted hydroxylamine per gram of sample) of between about 0.5 to 3.3-fold as much as a 40% O-substituted hydroxylamine salt solution, by weight. The O-substituted hydroxylamine further comprising at least one additional property selected from the group consisting of: a purity of between about 98% to 100%, based on gas chromatographic area; and a purity drop of less than about 1.2% after 78 days at 40° C.

Abstract: A polymer adapted for the Shrink resist treatment of textile materials imparting water, stain and/or oil repellency. The polymer includes a fluorinated polyether.

Abstract: Disclosed are compounds of the formula wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of beta-secretase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.

Abstract: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.

Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compoundsd and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R1–R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.

Abstract: An initiator system for radical polymerization, which comprises a combination of compounds of the formulae:

Abstract: Alkoxyamines containing a vinyl group as represented by the following general formula (1) are produced in a method which comprises a process of heating divinyl benzene, nitroxide compound and organic peroxide up to a temperature at which the organic peroxide decomposes thermally: (In the formula, R1 represents an aryl group or an R2O group, wherein R2 represents a linear or branched alkyl group having 1-12 carbon atoms or a cycloalkyl group. R3 and R4 are each tertiary alkyl group having 4-6 carbon atoms or of cyclic structure where R3 and R4 are connected with each other having a total carbon number of 8-16. In case of cyclic structure, they are optionally substituted either by an alkyl group, an oxo group, a hydroxyl group, an acyloxy group or an alkoxy group.) Furthermore, graft polymers can be produced by the use of high molecular radical polymerization initiators from which an alkoxyamine group suspends.

Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: The invention pertains to a compound of formula (I), (II) or (III) wherein R1 and R2 are independently of each other hydrogen, C1-C18alkyl, C3-C18alkenyl, C3-C18alkinyl or phenyl which are unsubstituted or substituted by NO2, halogen, amino, hydroxy, cyano, carboxy, C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylamino or di(C1-C4alkyl)amino; A is a group capable of forming a stable free nitroxyl radical A*, which is bound via its oxygen atom to the carbon atom; Y is O, NR3 or CHR3—Xa, wherein Xa is O, S or NR3; R3 is hydrogen, C1-C18alkyl, C3-C18alkenyl, C3-C18alkinyl or phenyl which are unsubstituted or substituted by NO2, halogen, amino, hydroxy, cyano, carboxy, C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylamino or di(C1-C4alkyl)amino; Q1 is an organic or inorganic radical, derived from a compound having at least one functional group being capable of reacting with a hydroxy group; Q2 is an organic radical derived from a mono or polyfunctional alcohol, mono or polyfunctional aminoalcohol, mono or polyfunctional amine

Abstract: Sterically hindered N-substituted aryloxyamines are prepared by the Keggin polyoxometalate or the transition metal substituted polyoxometalate (TMS-POM) catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitoxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.

Abstract: The invention relates to a compound of formula Ia, Ib or Ic The open chain alkoxyamine compounds are useful for the polymerization of ethylenically unsaturated monomers. The compounds of the present invention provide polymeric resin products having low polydispersity. The polymerization process proceeds with enhanced monomer to polymer conversion efficiency. In particular, this invention relates to stable free radical-mediated polymerization processes which provide homopolymers, random copolymers, block copolymers, multiblock copolymers, graft copolymers and the like, at enhanced rates of polymerization and enhanced monomer to polymer conversions.

Abstract: The present invention relates to a method for easily producing a tertiary amine with high yield. A tertiary amine represented by general formula (1) is produced by adding a metal-containing reagent represented by general formula (6) into a reaction system consisting of thioamide represented by general formula (4), a methylating agent represented by general formula (5) and a solvent, and then adding thereto a Grignard reagent represented by general formula (7).

Abstract: The present invention relates to the use of certain resorcinol derivatives as skin lightening agents.

Abstract: A nueroprotectant composition wherein the active ingredient is pGLU-GLU-PRO-NH2 or a combination of pGLU-GLU-PRO-NH2 (EEP) and N-tert-Butyl-&agr;-(2-sulfophenyl)nitrone (SPBN) or other nitrone. A method of treating and preventing diseases and injuries of the brain, spinal cord and retina is also presented by administering the endogenous tripeptide EEP to a subject as a neuroprotectant or by administering EEP in combination with SPBN or other nitrone.

Abstract: The invention relates to substituted N-Alkyl/Alkenyl/Cycloalkyl/Heterocycyl N-Aryl/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 disease. Preferred tertiary-heteroalkylamine compounds are substituted N-cycloalkyl N-benzyl aminoalcohols.

Abstract: The invention provides novel adamantane compounds having one of the following formulas: wherein: R1 and R3 are H, OH, alkyl, cycloalkyl, amino or aryl, and can be the same or different; R2 is H, NH2, alkyl, OH, COOH, amino, amide, or carbamate; R4-R8 are H, OH, NH2, alkyl, OH, COOH, ester, amino, amide, or alkyloxy, and can be the same or different; R9-R14 are H, alkyl, or phenyl, and can be the same or different; and wherein when any of R1-R8 is amino, the compounds are the free bases and their acid addition salts. The present invention also relates to compositions and methods for treating and/or preventing neurological and inflammatory disorders in a patient by administering a therapeutically effective amount of the compounds of formula (I), (II) or (III) and a pharmaceutically acceptable carrier.

Abstract: Compounds of formula (I) are antibacterial agents: wherein Z represents a radical of formula —N(OH)CH(═O) or of formula —C(═O)NH(OH), and R1-R4 are as defined in the specification. A method for the treatment of bacterial or protozoal infections in humans and non-human mammals, which comprises administering to a subject suffering such infection an antibacterially or antiprotozoally effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof.

Abstract: A process for preparing alkoxyamines in a biphasic medium comprises mixing an ionic liquid, an organic solvent, a metal salt, a ligand for the metal, a halocarbon compound ZX and a nitroxide, keeping the reaction medium stirring at a temperature of between 20° C. and 90° C. until the nitroxide has disappeared, separating the mixture by decantation, recovering the organic phase, and optionally washing it with water and then isolating the alkoxyamine by evaporating the organic solvent under reduced pressure.

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-phenoxy-N-phenyl aminoalcohols.

Abstract: A one-pot process for the preparation of functional alkoxyamines of the general formula (I), is disclosed. The process entails (1) reacting an oxidizing agent with a sterically hindered secondary amine to produce an aqueous phase and a nitroxyl radical (2) removing the aqueous phase and adding to the nitroxyl radical one or more vinyl monomer(s) conforming to a formula and a system which produces free radicals. Also disclosed is a process of polymerizing monomers using the functional alkoxyamine.

Abstract: Novel methods, processes and metal complexes attached to a hypoxia-localizing moiety comprising

Abstract: The invention relates to substituted polycyclic aryl and heteroary 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 diamines.

Abstract: A one-pot process for the preparation of alkoxyamines conforming to formulae (I) or (II), preferably (I) 1

Abstract: A one-pot process for the preparation of functional alkoxyamines of the general formula (I), 1

Abstract: For the preparation of a multimodal polymer at least one monomer is subjected to free radical polymerization in the presence of several alkoxyamines comprising the sequence of formula: in which RL is a monovalent radical exhibiting a molar mass of greater than 15, A represents the core of the alkoxyamine and n is a non-zero integer, the alkoxyamines exhibiting different values of n.

Abstract: The invention relates to a new process for the preparation of functionalized alkoxyamine initiators, new alkoxyamine initiators based on (meth)acrylate which are prepared by this process, and their use for the preparation of polymers.

Abstract: Sterically hindered N-substituted aryloxyamines are prepared by the transition-metal-catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitroxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.

Abstract: The invention relates to 2-benzoylcyclohexane-1,3-diones of the formula I where R1, R2 are each hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR5, —OCOR6, —OSO2R6, —SH, —S(O)nR7, —SO2OR5, —SO2NR5R8, —NR8SO2R6 or —NR8COR6; R3 is hydrogen, cyano, alkyl, haloalkyl, —OR7, —SR7 or —NR7R10; R4 is hydrogen, substituted or unsubstituted alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, —COR9, —CO2R9, —COSR9 or —CONR8R9; X is oxygen or NR8; n is 0, 1 or 2; R5 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R6 is alkyl or haloalkyl; R7 is alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R8 is hydrogen or alkyl; R9 is alkyl, alkenyl, alkynyl, phenyl or benzyl; R10 is alkyl, haloalkyl, alkenyl or alkynyl; Q is a cyclohexane-1,3-dione ring with or without substitution attached in position 2; and agriculturally useful salts thereo

Abstract: Hypericin, helianthrone and derivatives thereof of general formula (I) 1

Abstract: PBN (&agr;-phenyl-tert-butylnitrone), and its derivatives nitrone-based free radical traps, significantly reduce preneoplastic nodule development as well as inhibit hepatocellular carcinoma (HCC) formation at very low levels. The involvement of reactive oxygen species (ROS) in cancer development has been strongly implicated for many years. The involvement of ROS has been strongly implicated in cancer development is a model system where feeding a choline deficiency (CD) diet to rats leads to hepatocellular carcinoma (HCC) development. Administering PBN in the drinking water inhibits HCC formation. Preneoplastic nodule growth in the liver is significantly suppressed by administering PBN, or some of its natural metabolites, in the diet. The effectiveness of PBN in preventing HCC development in the CD liver model is considered due to its prevention of tumor development after the target cells have already been initiated, i.e. genetically changed into tumor cells.

Abstract: This invention relates to a process for preparing N-substituted hydroxylamines from N-substituted aryl- or heteroaryloxaziridines by acid hydrolysis and isolation of the N-substituted hydroxylamines in the form of their salts.

Abstract: Sterically hindered N-substituted alkoxyamines are prepared by the transition-metal-catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitroxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.

Abstract: The invention concerns a method for preparing alkoxyamines in a biphasic medium. Said method consists in mixing an ionic liquid, an organic solvent, a metal salt, a metal ligand, a halogeno-carbonaceous ZX compound and a nitroxide, maintaining the reaction medium under agitation at a temperature between 20° C. and 90° C., until the nitroxide is eliminated, decanting, recuperating the organic phase, optionally washing it with water and then in isolating the alkoxyamine by evaporating the organic solvent under reduced pressure.

Abstract: This invention provides a process for the preparation of a benzimidazole derivative (I) or a pharmaceutically acceptable salt thereof, wherein R1 is C1-C6 alkyl, C1-C6 alkoxyl, etc., R2 is C1-C6 alkyl, and R3 is hydrogen or a protecting group, which exhibits excellent hyopoglycemic action, said process comprising condensation of an amine derivative (III) with a carboxylic acid derivatives (II) to afford a compound (IV), followed by cyclization of compound (IV) in the presence of an acid.

Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol 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. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Subsbitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N-phenoxy N-phenyl aminoalcohols.

Abstract: The invention relates to open chain alkoxyamine compounds useful as polymerization regulators. The open chain alkoxyamine compounds are useful for the polymerization of ethylenically unsaturated monomers. The compounds of the present invention provide polymeric resin products having low polydispersity. The polymerization process proceeds with enhanced monomer to polymer conversion efficiency. In particular, this invention relates to stable free radical-mediated polymerization processes which provide homopolymers, random copolymer, block copolymers, multiblock copolymers, graft copolymers and the like, at enhanced rates of polymerization and enhanced monomer to polymer conversions.