129 results about "Nitrone" patented technology

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.

Disclosed are aryl, heteroaromatic and bicyclic aryl nitrone compounds and pharmaceutical compositions containing such derivatives. The disclosed compositions are useful for preventing and/or treating pain, neurodegenerative, autoimmune and inflammatory diseases or conditions in mammals.

Disclosed are aryl, heteroaromatic and bicyclic aryl nitrone compounds and pharmaceutical compositions containing such derivatives. The disclosed compositions are useful for preventing and/or treating pain, neurodegenerative, autoimmune and inflammatory diseases or conditions in mammals.

The present invention provides a method for storing holographic data comprising providing a holographic storage medium comprising an optically transparent substrate including a photochemically active dye having at least two nitrone groups; and irradiating the optically transparent substrate with a holographic interference pattern, wherein the pattern has a first wavelength and an intensity both sufficient to convert, within a volume element of the substrate, at least some of the photochemically active dye into a photo-product, and producing within the irradiated volume element concentration variations of the photo-product corresponding to the holographic interference pattern, thereby producing a first optically readable datum corresponding to the volume element.

The present invention involves the use of nitrone free radical trapping agents in the treatment and prevention of gliomas. The agents may be used alone or combined with other traditional chemo- and radiotherapies and surgery, to treat or prevent glioma occurrence, recurrence, spread, growth, metastasis, or vascularization.

The invention discloses a surface self-assembly gold nanoprobe with the free radical capture performance and a preparing method and the application thereof. The surface self-assembly gold nanoprobe with the high free radical capture performance is prepared by the following steps: the surface of a gold nano-particle is connected with nitrone free radical probe ligand with the structure of formula II by a connexon of the structure of formula I. The nitrone free radical probe ligand is connected with R3 radical group end. The gold nano-particle is connected with sulfhydryl end of the connexon. In formula Ia and formula Ib, R3 is -OH, -NH2 or -COOH, n is equal to 2-11, and n1 is equal to 1-4. In formula IIc, R1 is -P(O)(OC2H5)2, and R2 is OH, COOH or CH2OH. The surface self-assembly gold nanoprobe with the high free radical capture performance can capture free radicals under low concentration and can be applied as an antioxidant.

The present application discloses compositions and methods of synthesis and use involving click chemistry reactions for in vivo or in vitro formation of therapeutic and/or diagnostic complexes. Preferably, the diagnostic complex is of use for 18F imaging, while the therapeutic complex is of use for targeted delivery of chemotherapeutic drugs or toxins. More preferably, a chelating moiety or targetable construct may be conjugated to a targeting molecule, such as an antibody or antibody fragment, using a click chemistry reaction involving cyclooctyne, nitrone or azide reactive moieties. In most preferred embodiments, the click chemistry reaction occurs in vivo. In vivo click chemistry is not limited to 18F labeling but can be used for delivering a variety of therapeutic and/or diagnostic agents.

Certain simple chemical agents, referred to herein as nitrone related therapeutics or "NRTs", when administered to a patient susceptible to neovascularization (angiogenesis), can intervene and inhibit the disease's progress. Methods for therapeutically and prophylactically inhibiting angiogenesis by administering one or more NRTs are disclosed as are pharmaceutical compositions for use in such methods of treating. NRTs useful in these compositions and therapeutic methods are also disclosed.

Compositions containing unsaturated fatty esters may be stabilized against atmospheric oxidation by the addition of an antioxidant package containing a phenolic oxidant and a nonphenolic oxygen scavenger, which may be a hydroxylamine, an amine N-oxide, an oxime, or a nitrone. If an amine N-oxide is used, it may be used with or without a phenolic antioxidant. Compositions treated in this manner show good resistance to atmospheric oxidation and resultant viscosity increase.

The invention is the use of nitronyl substituted hindered phenols as antioxidants in therapeutic applications. In the preferred embodiment the compositions have the general formula: Wherein R1 is hydrogen, an alkyl or an aryl and R2 is an alkyl or an aryl; R3 is an alkyl; and R4 is an alkyl. Further, the invention relates to novel compositions useful as antioxidants. The novel compounds include: 2,6-di-tert-butyl-4-(N-tert-octyl)nitronyl phenol (DBONP); 2,6-dimethyl-4-(N-tert-octyl)nitronyl phenol (DMONP); N-tert-octyl-C-phenyl nitrone (OPN).

The invention provides an O-glycoside nitrone compound which is a novel nitrone glycoside and a synthetic method thereof, belonging to the field of chemical synthesis. The compound is synthesized by the following steps of: firstly catalyzing sugar and acetic anhydride with acid to produce totally acetylated sugar; then reacting the totally acetylated sugar with red phosphorus and liquid bromine under an acidic condition to generate brominated sugar; then reacting the brominated sugar with hydroxyl-contained aromatic aldehyde under the action of a phase transfer catalyst to produce O-benzaldehyde glycoside; and finally reacting the O-benzaldehyde glycoside with N-substituted hydroxylamine to obtain a target product. The O-glycoside nitrone compound has single beta-form configuration and simultaneously has the advantages of natural chirality, structural diversity and the like. The synthetic method has the advantages of low price and easy obtained raw materials, environmental protection, reproducibility and the like and creates a good condition for industrialization.

A process for preparing the superfine gel of raw Chinese-medicinal materials includes such steps as pulverizing to obtain superfine powder, sterilizing, adding propanediol, grinding, dissolving carbomer, EDTA-2Na and mycosten in water, swelling to become gel matrix, mixing with the superfine medicine dispersed liquid, adding nitrone and distilled water and stirring. Its advantages are no loss of active components and quick release.

The invention relates to a polysubstituted isoxazolidine derivative and a preparation method thereof. The structural formula of the polysubstituted isoxazolidine derivative is as shown in a Formula (I) in the specification, wherein R1 and R2 are substituted aryl or alkyl; a substituent group on Ar can be alkoxy, halogen or alkyl; the substituted aryl is phenyl or naphthyl; and the alkyl generally comprises methyl, ethyl and cyclohexyl. The preparation method comprises the following steps: at room temperature, in an air or nitrogen atmosphere, dissolving a nitrone derivative as shown in a Formula (II), an olefin structure-containing compound as shown in a Formula (III) and a photocatalyst as shown in a Formula (IV) in an organic solvent, performing uniform mixing, performing illumination under blue LED lamps or filament lamps for hours; and after the reaction is completed, performing rotary evaporation on the solvent, and performing separation and purification through silica gel column chromatography to obtain the polysubstituted isoxazolidine derivative. The method solves the problems of need of a high temperature heating system, high energy consumption, strict conditions and high equipment requirements in the existing isoxazolidine derivative synthesis process; and the method is mild in conditions, simple, convenient to operate and high in yield.

The invention discloses an alpha-xenyl-N-alkyl nitro ketones compound of which the structural formula is as shown in formula (I). The synthetic method is: first adding the benzene boric acid and the bromo benzaldehyde into the toluene which carry on the Suzuki coupling reaction to produce biphenyl formaldehyde under the existence of the potassium phosphate hydrate and the palladium catalyst. Then mixing the biphenyl formaldehyde, 2-nitryl-2- alkyl propane and zinc powder together in the ethyl alcohol, adding ethanoic acid, and put into the refrigerator for refrigeration, then separated for depuration. The alpha-xenyl-N-alkyl niter ketones compound connects aromatic group on the PBN benzene ring, and can increase the steric hindrance of the free radical addition atom and weaken the disproportionation extinguishment of the free radical addition compound or the enzyme catalyzed extinguishment inside the organism thus to increase the life of the free radical addition compound. The nitro alkone compound can be effective reagent for examining the free radicals in the lipin system like cell membrane.

The present invention discloses a method of synthesizing multi-hydroxy pyrrolidine alkaloid. The present invention comprises the following steps: 1) the multi-hydroxy ring-shaped nitrone of the structure in formula II reacts to prepare Cbz-protected amide of the structure in formula III; 2) the amide of the structure in formula III is changed into an alpha, beta-unsaturated ketone of the structure IV; 3) the alpha, beta-unsaturated ketone of the structure IV and ketone do the dual-hydroxylation reaction with the influence of osmium tetroxide and NMO system to get a structure in formula V; 4) the formula V is catalyzed and hydrogenated to get the multi-hydroxy pyrrolidine alkaloid of the structure in formula I. The present invention startes from the low-cost and easily accessible raw materials; the sugar derived multi-hydroxy chiral nitrone is used as a key chiral intermediate; a set of simple, effective and practical methods of highly three-dimensional selectivity and high production rate to synthesize the multi-hydroxy pyrrolidine alkaloid of hyacinthacine C₁ category is formed through the pro-nuclear addition, Wittig reaction, double-hydroxylation and reductive amination and other reactions.

The invention provides a method for synthesizing N-benzylhydroxylamine hydrochloride in industrial production. The method comprises the following steps: mixing an oxidant, diphenylamine and an organic solvent under the action of tungstate, so as to obtain C-phenyl-N-benzyl nitrone; mixing the C-phenyl-N-benzyl nitrone, MTBE and hydroxylamine hydrochloride methyl alcohol, so as to obtain a product, namely N-benzylhydroxylamine hydrochloride. The overall synthesis process disclosed by the invention is simple and convenient to operate, and stable in condition, the reaction yield is high and the product purity is high. According to the technique disclosed by the invention, the effectiveness of the method is confirmed by multiple batches of kilo-scale verification; and the large-scale production of N-benzyl hydroxylamine is smoothly achieved.

Disclosed are aryl, heteroaromatic and bicyclic aryl nitrone compounds and pharmaceutical compositions containing such derivatives. The disclosed compositions are useful for preventing and/or treating pain, neurodegenerative, autoimmune and inflammatory diseases or conditions in mammals.

This invention relates to a double hydroxy, high proline ramification and the preparation method and application. The invention utilize 5 - nitrine - 5 - deoxypentose chirality structure to prepare 5 - nitrine methyl - 3, 4 -double shield hydroxy nitrone, furthermore utilize addition reaction of nitrone and ester enol siloxane type nucleophilic reagent, to prepare double hydroxy high proline ramification. This invention has good regioselectivity, high stereoselectivity, be able to proceeding bulk preparation.