83 results about "Succinamopine" patented technology

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001" / >(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup

The invention relates to a quantum dot fluorescent probe and application thereof. The invention is characterized in that the quantum dot fluorescent probe utilizes a difunctional cross-linking agent long-chain succinimidyl-4-[N-maieimidomethyl]cyclohexane-1-carboxy-[6-amidocaproate] (SMCC) to undergo a cross-linking reaction with an amino group on the surface of an amino quantum dot; a maleimide group is produced on the surface of the quantum dot; a to-be-labeled antibody is reduced by a reducing agent dithiothreitol (DTT) so as to reduce a disulfide bond into a mercapto group; and the mercapto group and the maleimide group form a covalent bond so as to realize labeling of the quantum dot with the antibody. The quantum dot fluorescent probe is applied to (1) detection of one protein oncofetal antigen or (2) detection of a plurality of protein CEA, euron-specific enolase (NSA) and a cytokerain fragment 19CYFRA21-1, wherein the detection limit of detection (1) is 38 pg / ml, and the detection limit of detection (2) is 0.9 ng / ml.

The invention discloses a carbon nano tube immobilized laccase, which is prepared by the following steps of carrying out grafting of succinimido and grafting of a nitrilotriacetic acid functional group on a carbon nano tube; carrying out surface functionalization treatment through copper ion chelating and modifying, and carrying out immobilized reaction with the laccase with copper ion removal. The laccase active center is directly connected with the copper ions of the carbon nano tube surface functional group, so that the real meaning direct electron transfer can be realized, and the shielding effect produced by a laccase protein shell on the direct electron transfer process from the active center to the carbon nano tube is overcome. The carbon nano tube immobilized laccase provided by the invention solves the problem of limitation of the electron transfer rate during the carbon nano tube immobilized laccase catalytic process, the sensitivity of the immobilized laccase in biological detection can be improved, the lowest detection limit during phenol determination is reduced by 85 percent to 96 percent, and the current density in biological fuel cell application is improved by 80 percent to 120 percent.

The invention discloses a fluorescence resonance energy transfer probe, a preparation method and application thereof. According to the invention, the fluorescent group 7-(N, N-diethylamino)coumarin-3-carboxylic acid succinimidyl ester is connected to the quenching group 4-[4-(dimethylamino)benzeneazo]benzoic acid N-succinimidyl ester through a polypeptide chain able to be cut by the matrix metalloproteinase II (MMP-2) to construct the fluorescence resonance energy transfer probe. Human liver cancer 7402 cell and human normal liver cell LO-2 are adopted as the research object, and cell imaging experiments are carried out to detect the MMP-2 expression level of the 7402 cell and LO-2 cell. In vitro experiments (the fluorescence response of MMP-2, MMP-1 and other species to the probe) show the targeting of the probe to MMP-2, and the cell imaging result shows that the MMP-2 expression level of the human liver cancer 7402 cell is higher than the human normal liver cell LO-2.

The invention belongs to the technical field of medical preparations, and discloses nanometer chitosan ultrasonic microbubble targeting prostate cancer cells and preparation and application thereof. A method comprises the following steps of (1) mixing chitosan, methacryloyloxyethyl trimethyl ammonium chloride and N-succinimidyl 3-maleimidopropionate, and heating to react, so as to obtain modified chitosan; adding a prostate antigen, adjusting the pH (potential of hydrogen) value of a system, and continuing to react, so as to obtain a complex; (2) stirring and mixing an inert matter with low boiling point, the complex and water, so as to obtain primary emulsion; (3) adding a dispersant and an additive into an oil-phase solvent, uniformly mixing, adding the primary emulsion, stirring at high speed, adding a crosslinking agent to cure, adding a precipitating agent to precipitate, washing, centrifuging at high speed, and drying particles, so as to obtain the ultrasonic microbubble. The nanometer chitosan ultrasonic microbubble has the advantages that the targeting property is good, the tissue penetration ability is strong, the affinity is high, and the nanometer chitosan ultrasonic microbubble is suitable for the ultrasonic developing of the prostate cancer cells.

The invention discloses a polyasparagine derivative modified oil-water separation stainless steel mesh film and a preparation method thereof. A ring-opening reaction is used for grafting zwitterions,dopamine, long-chain alkyl groups, ethanolamine and other groups on a polysuccinimide polymer; and the dopa / zwitterion functionalized polyasparagine derivative modified oil-water separation stainlesssteel mesh film is obtained by modifying the surface of a stainless steel mesh. The polyasparagine derivative modified oil-water separation stainless steel mesh film provided by the invention has thecharacteristics of a good oil-water separation effect and good stability; the used polyasparagine derivative material has biodegradability and an environmental protection property; and after the polyasparagine derivative material is used, the waste does not cause secondary pollution to environments. The preparation method of the polyasparagine derivative modified oil-water separation stainless steel mesh film is simple and convenient in technology, fast in process, mild in reaction, easy in control, and has high safety.

The invention describes a method for preparing a meningitis polysaccharide conjugate vaccine. The meningitis polysaccharide conjugate vaccine is developed based on the method. The method comprises the following steps: (1) activating meningococcus polysaccharides by cyanogen bromide, then deriving the meningococcus polysaccharides which are activated by the cyanogen bromide by ethanediamine, finally deriving the polysaccharides by a reagent which is of a structure of succinimidyl ester-R-maleimide; (2), sulfhydrylating carrier proteins; (3) combining the derived meningococcus polysaccharides with the sulfhydrylated carrier proteins. As conjugation bridges between the meningococcus polysaccharides and the carrier proteins are very long, the spatial shielding effect of the carrier proteins on the antigenic epitopes of the polysaccharides is reduced, and the original immunization property of the polysaccharide conjugate vaccine is improved.

The present invention discloses phytoagglutinin modified lactic acid-hydroxyacetic acid copolymer with specific adhesion to prolong the retention time or preparation in gastrointestinal tract obviously and raise the bioavailability of orally taken medicine greatly. The polymer consists of biodegradable material lactic acid-hydroxyacetic acid copolymer and bioadhesive material phytoagglutinin. The phytoagglutinin modified lactic acid-hydroxyacetic acid copolymer is prepared through dissolving lactic acid-hydroxyacetic acid copolymer, 1-ethyl-3-carbodimide and N-hydroxy succinimide in non-proton type polar solvent, and reaction at room temperature via stirring for 2-12 hr; adding water, filtering and collecting precipitate to obtain PLGA-NHS; dissolving phytoagglutinin and PLGA-NHS in mixed solvent of water and non-proton type polar solvent, filtering the reacted mixture, taking the dialysate, and freeze drying to obtain the phytoagglutinin modified lactic acid-hydroxyacetic acid copolymer.

Cobalt(II) complexes of the D2-symmetric chiral porphyrins are effective catalysts for asymmetric cyclopropanation reactions with succinimidyl diazoacetate. The Co-catalyzed reaction is suitable for various olefins, providing the corresponding cyclopropane succinimidyl esters in high yields and excellent diastereo- and enantio-selectivity. The resulting enantioenriched cyclopropane succinimidyl esters can serve as convenient synthons for the general synthesis of optically active cyclopropyl carboxamides through mild reactions with a wide range of amine derivatives, including unprotected peptides and amino sugars

A crosslinked polymer particle can be obtained by carrying out a crosslinking reaction between a non-crosslinked polymer particle containing a succinimidoxycarbonyl group and a compound having two or more amino groups.

The invention relates to an immunogen and the preparation method thereof. The preparation method comprises the steps as follows: cross-linking peptide (hCG-CTP37) composed of amino acid molecules of Beta subunit C-terminal 37 of human chorionic gonadotrophin hormone in the presence of heterobifunctional cross-linking agent N-(Epsilon-maleimidocaproyloxy)succinimidyl (EMCS) using diphtheria toxin mutant CRM197 as carrier protein to obtain CTP37CRM197. The carrier protein has the advantages of high recovery rate, easy purification, and suitability for large-scale industrial production. The cross-linked product has the advantages of high cross-linking rate, short preparation time and reduced production cost. The invention also relates to an application of drug adopting appropriate immunoadjuvant as adjuvant in tumor therapy by employing the immunogen prepared by the method as effective component of therapeutic vaccine.

The invention relates to a wormwood extract modified PP spunbond non-woven fabric. The modified PP spunbond non-woven fabric comprises the following effective components of, in percentage by mass, 0.1%-5% of wormwood extract. According to the preparation method, the wormwood extract and porous nano material are subjected to modification treatment, and the wormwood extract is "packaged" in porous channels of the porous material due to the fact that the nano porous material has a large specific surface area, so that components of the wormwood extract cannot be damaged when the non-woven fabric is prepared later, and the performance of the non-woven fabric is improved; soluble chitin, 2-hydroxybenzimidazole, cellulose acetate butyrate, adipic dihydrazide, N-hydroxysuccinimide and polyamine are added, so that the mechanical strength, the wear resistance and the moisture absorption of the non-woven fabric are further effectively improved; the obtained modified nano composite material is added into a fat-soluble solvent to be ground, can be dispersed uniformly, and is mixed and spun with PP slices to obtain the modified PP spunbond non-woven fabric, so that the softness, air permeabilityand water absorption of the non-woven fabric can be improved.

The invention discloses a preparation method and application of magnetic nanoparticles crossing a blood-eye barrier. The preparation method comprises taking purified bacterial magnetosomes BMs, and binding the amino terminals of the bacterial magnetosomes BMs and cysteine in a TAT polypeptide through an N-succinimido-3-(2-pyridinedithio)propionate as a cross-linking agent to obtain magnetic nanoparticles crossing a blood-eye barrier. The magnetic nanoparticles are TAT-BMs composite carriers. The magnetic nanoparticles can cross a blood-eye barrier and expand the application potential of magnetic nanomaterials in treatment on eye diseases.

Provided is a lubricating oil composition for use in internal-combustion engines, containing a base oil (A), an ashless dispersant (B) containing a non-boronated alkenylsuccinic acid imide (B1) and a boronated alkenylsuccinic acid imide (B2), a thiadiazole compound (C), and an aromatic carboxylate (D) having one or more hydroxy groups, wherein the content of the component (C) is 0.2 to 1.2% by mass based on the total amount of the lubricating oil composition, the content of a zinc dithiophosphate is, as calculated in terms of zinc atoms, less than 500 ppm by mass based on the total amount of the lubricating oil composition, and the content of a metal-based detergent is, as calculated in terms of metal atoms, less than 600 ppm by mass based on the total amount of the lubricating oil composition.

The invention discloses an antifogging film material and a preparation method thereof. The method comprises the following steps: S1, adding allyl succinimido carbonate, ethylene glycol dimethacrylate, polyethylene glycol monoallyl ether, N-vinyl carbazole, vinyl beta-cyclodextrin quaternary ammonium salt, 2,3,5,6-tetrafluoroterephthalic acid, an isocyanate-terminated polyurethane prepolymer, an initiator, a catalyst and nano titanium dioxide into an organic solvent, and stirring the components to obtain a mixture, uniformly stirring the mixture and coating the mixture on a polyfluortetraethylene plate or a glass plate; s2, placing the substrate in an inert gas atmosphere, drying to constant weight at 85-95 DEG C, and then removing the film to obtain a polymer film; s3, performing radiation grafting to prepare the anti-fog film material. The anti-fog film material disclosed by the invention is remarkable in anti-fog effect, good in oil and dust pollution resistance and excellent in thermal stability, wear resistance, mechanical property, durability and performance stability.

The invention discloses a preparation method of a fluorescence sensor for Cr (VI) real-time detection and a product produced thereby. The preparation method comprises the steps of: dissolving N,N'- succinimido carbonate in 1, 4-dioxane, adding triethylamine, uniformly stirring, adding a PVA-co-PE nanofiber membrane, heating, and slowly stirring for reaction; after the reaction is finished, fully washing the membrane with 1, 4-dioxane, and drying the membrane at low temperature to obtain an activated PVA-co-PE nanofiber membrane; dissolving carbon dot powder into deionized water, with the concentration being 0.2 g / L-5 g / L; immersing the activated PVA-co-PE nanofiber membrane into the carbon dot solution, and slowly stirring to react for 30-180 minutes at the reaction temperature of 20-100 DEG C; and washing the membrane with ultra-pure water until no fluorescence is detected in the residual liquid to obtain a carbon dot-based nanofiber membrane, namely the fluorescence sensor. The fluorescence sensor has high selectivity and sensitivity, the maximum detection limit can reach 1 ppb or below, and after the fluorescence sensor is repeatedly used for five times, the morphology of the nanofibers is still kept good.

The invention relates to quaternary ammonium salt, which has a cation structural formula shown in a specification, wherein R1 and R2 are respectively and independently expressed as C2-C4 alkyl, and R3 independently expresses amino, hydroxyl, carboxyl, aldehyde group, mercapto group, hydrazino or succinimido. The invention also relates to a preparation method and an application, the cation structure of the quaternary ammonium salt with small molecular weight contains disulfide bond, which can be decomposed under effect of reduced glutathione in cells, cytotoxicity can be reduced, and the release of nucleic acid medicines can be improved.

The invention relates to the technical field of immunodetection, in particular to an optical fiber probe as well as a preparation method and application thereof. The preparation method of the optical fiber probe comprises the following steps: (1) immersing an optical fiber into a solution of 8-aminopyrene-1, 3, 6-trisulfonic acid trisodium salt, and reacting to obtain an optical fiber connected with a silanization group; (2) immersing the optical fiber connected with the silanization group into an N, N'-disuccinimidyl carbonate solution, and reacting to obtain an optical fiber carrying a bifunctional group; and (3) immersing the optical fiber carrying the bifunctional group into an antigen solution, and reacting to obtain the optical fiber probe. When the prepared optical fiber probe is applied to fipronil detection, the linearity is good, and the sensitivity can reach 0.2 microgram / L.

The invention provides a urine microalbumin detection reagent strip and a preparation method thereof, and belongs to the technical field of medical examination. The reagent strip comprises a supporting plate and a filter paper sheet, wherein the filter paper sheet is attached onto the supporting plate; the filter paper sheet is immerged in dyeing liquid; the dyeing liquid is prepared from a reagent I and a reagent II; the reagent I is prepared from cyanine dyes, trolamine buffer solution, Triton X-100, sodium benzoate and PEG-4000; the reagent II is prepared from disodium hydrogen phosphate-monosodium orthophosphate buffer solution, O-(N-succinimido)-N N N'N'-tetramethyl tetrafluorohydrazine carbamide borate, sodium azide and dimethyl acetamide. The cyanine dyes of the prepared urine microalbumin detection reagent strip can fast react with microalbumin in urine; when the concentration of the microalbumin is in a range of 0 to 200mg / L, the test paper is at the obvious color gradation from being achromatic color to dark blue; the visual distinguishing and machine reading are easy; the determination result is accurate; the stability is high.

The invention discloses a large-scale preparation technology for high-purity mesalazine enteric-coated sustained-release tablet preparations. The preparation technology includes the following steps: dissolving polyglutamic acid into water, adding an N-hydroxysuccinimide NHS solution and a 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC solution, and performing reaction for 4-8 h at room temperature so as to obtain an activated polyglutamic acid solution; adding a cross-linking agent and an initiator with the mass ratio being 1:(0.1-0.5) into the activated polyglutamic acid solution, performing reaction for 0.5-1 h at 0-5 DEG C after uniform mixing, then mixing the product and a water-soluble polymer solution, and performing stirring reaction for 1-3 h under 30-40 DEG C to obtain water-soluble polymer-polyglutamic acid copolymer; slowly adding mesalazine and the water-soluble polymer-polyglutamic acid copolymer into a granulating machine under stirring, then adding a thickening agent, and forming a suitable soft material through stirring; and preparing the soft material into dried granules, and obtaining the high-purity mesalazine enteric-coated sustained-release tablet preparations through tablet compressing and coating. The preparation technology is simple and suitable for commercial process.

The invention relates to a preparation method of a starch microsphere and human recombinant tissue factor lipid composite hemostatic material. The preparation method comprises the following steps: dissolving potato starch in deionized water, mixing with emulsified soybean oil according to the mass ratio of water phase to oil phase solution of 1: 2.0-1: 2.5, and forming starch microspheres with mutually condensed hydroxyl groups under the action of an initiator; further dispersing the obtained starch microspheres in anhydrous 1,4-dioxane, modifying with N,N'-disuccinimido carbonate (DSC), adding human recombinant tissue factor lipids, and combining the tissue factors with the starch microspheres in a covalent bonding manner. The starch microsphere and human recombinant tissue factor lipid composite hemostatic material is obtained through centrifugation, cleaning and vacuum drying, and a rapid blood coagulation effect is achieved by utilizing the starting blood coagulation function of tissue factors.

This invention relates to chemistry and biochemistry applied to the field of medicine and is referred to a new method of prevention and therapeutic treatment of conformational diseases (CD), in particular to amyloid origin diseases by administrating an effective amount of one or more compounds, salts, prodrugs or solvates, which are considered herein as chemical chaperonins, of Formula I,Where: R1: -alkylenyl-C(O)NH-alkylenyl-R3, -alkylenyl-C(O)O—R4;R3: —COOH, —OH, —SH, —NH2, —NH-alkyl-, —NH-dithiocarbamate-alkyl, —N-alkyl-dithiocarbamate alkaline earth metal salts.R4: succinimidyl group.R2: —H, -alkyl; wherein the term “alkyl” is characterized by a linear or branched aliphatic chain, hydrogen and saturated carbon atoms, comprising a methyl, ethyl, n-propyl, iso-propyl, n-butyl or iso-butyl groups. Wherein, the term “alkylenyl” refers to a divalent analog of a linear or branched alkyl group, preferably ethylenyl (—CH2CH2—) or butylenyl (—CH2CH2CH2CH2—) radicals. These compounds are neutral, lipophilic, and have low molecular weight. The present invention provides a novel method for CD prevention and therapeutic treatment, by inhibition, reduction and breakdown of prefibril, protofibril, amyloid fiber and plaque structures, all of them characterized by presenting cross-β-toxic structures (e.g. Alzheimer disease (AD), Parkinson's disease (PD), Diabetes Mellitus Type II (DM2), etc.), through the administration of the Formula I compounds, which are considered herein as chemical chaperonins, in any acceptable pharmaceutical composition of one or more compounds or salts thereof, prodrug or solvate, that are capable of inhibiting, reducing, removing, etc., the formation of these structures which cause a protein misfolding, as well as to disaggregate fibers already formed.

The invention belongs to the field of biological technology, and specifically relates to the coupling, preparation method and application of annexin V with the ability to bind to phosphatidylserine and its variant molecules and the anticancer drug doxorubicin. (3-Dimethylaminopropyl) carbodiimide hydrochloride and N-hydroxysulfosuccinimide are used as a crosslinking agent to couple with doxorubicin, and a method for preparing a soluble conjugate. The prepared conjugates have better anti-tumor activity, which lays the foundation for further research on targeted anti-tumor drugs and their applications.

The invention discloses a thermoplastic resin composite material for a bottom shell of a notebook computer and a manufacturing method of the thermoplastic resin composite material. The composite material is characterized by being prepared from the following raw materials in parts by weight: 45-55 parts of fluorine-containing hyperbranched polyethylene copolymer, 25-35 parts of allyl succinimido carbonate / 4-acryloyl hydroxybenzoic acid benzophenone / allyl boronic acid pinacol ester / 4-vinyl-2, 8-bis (trifluoromethyl) quinoline copolymer, 3-5 parts of 3-(diethoxy o-acyloxy)-1, 2, 3-benzotriazine-4-ketone, 3-5 parts of a coupling agent, 6-10 parts of mullite fibers, 5-8 parts of nano boron fibers, 2-4 parts of steel fibers, 1-3 parts of an antioxidant, 1-2 parts of a heat stabilizer, 3-5 parts of a plasticizer and 1-2 parts of a lubricant. The thermoplastic resin composite material has the advantages of good mechanical properties, excellent flame retardance and aging resistance, excellent weather resistance and heat resistance, good performance stability and long service life.