6382 results about "Acyl group" patented technology

A compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof wherein X-Y is -NHSO2- or -SO2NH-; R1 is H, CN or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, Cl and alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, optionally substituted heteroaryl, SO2NR14R15, CONR10R11 and alkyl; R8 is selected from H, alkyl, haloalkyl and halo; R9 is H or halo; and R10, R11, R12, R14, and R15 are H or alkyl; R13 is selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; and m is 0-3. The compounds of formula (I) modulate ERAP1 (endoplasmic reticulum aminopeptidase 1) and are for use in treating proliferative, immune or inflammatory disorders, particularly cancer or leukemia. The compounds of formula (I) stimulate a neo-antigen directed immune response in the subject. A method for producing an antigen-presenting cell which presents a neo-antigen using compounds of formula (I) is disclosed. An immunogenic composition comprising an antigen-presenting cell is also disclosed. Exemplified compounds include 4-cyclopropyl-3-(N-(2-(morpholin-3-yl)-5-(trifluoromethyl)phenyl)sulfamoyl)benzoic acid.

The present invention belongs to the technical field of membrane-based water treatment and relates to a novel guanidine-based composite nanofiltration (NF) flat-sheet membrane, and a preparation method and application thereof. The present invention provides a method for preparing a guanidine-based composite NF flat-sheet membrane, where a dense separation layer is formed on the surface of a polyethersulfone ultrafiltration membrane through polymerization reaction between the amino group of 1,3-diaminoguanidine and the acyl chloride group of trimesoyl chloride. Under suitable reaction conditions, the guanidine-based composite NF membrane obtained according to the present invention enables effective separation of multivalent ions over a wide pH range, with a rejection rate of over 96% for 1000 ppm of MgSO4 solution, and can operate continuously and stably in a mixed ions solution with a wide pH.

The present application provides tricyclic triazolo compounds that modulate the activity of diacylglycerol kinase (DGK), which are useful in the treatment of various diseases, including cancer.

The invention belongs to the technical field of medicines, and particularly relates to a disulfide cyclic peptide compound of a melanocortin receptor agonist based on polypeptide small molecules, and the disulfide cyclic peptide compound has the following structure: R2-R1-c (Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-R3-R4, wherein R2 and R4 are respectively and independently selected from an amino group, an acetyl group or a palmitoyl group; r1 and R3 are independently selected from Ile, Arg, D-Phe, Pro or deletion, R1 and R3 are not deleted at the same time, and when R1 or R3 is deleted, at least one of R2 and R4 is a palmitoyl group. The disulfide cyclopeptide compound provided by the invention has relatively good selectivity on melanocortin receptors (MCR1, MCR3, MCR4 and MCR5).

The invention discloses a fine circuit pattern anti-diffusion agent as well as a preparation method and a use method thereof, and relates to the technical field of printed circuit board manufacturing. The fine circuit pattern anti-diffusion agent is prepared from the following components in percentage by mass: 0.05 to 0.3 percent of an oleophobic agent, 0.1 to 0.6 percent of a bonding agent, 0.2 to 1.5 percent of an adhesion promoter, 0.5 to 4.0 percent of a wetting agent, 0.5 to 5.0 percent of a cosolvent and the balance of water, the oleophobic agent is a fluorophenylethylamine derivative, the bonding agent is a carbonyl chloride derivative, the adhesion promoter is a sulfur heterocyclic alkane derivative, the wetting agent is a methylsiloxane silane derivative, and the cosolvent is a sulfonyl ketone derivative. According to the fine circuit pattern anti-diffusion agent, an organic layer can be formed on the copper surface of a circuit board, the binding force between the copper surface and printing ink is enhanced, jet printing printing ink is prevented from diffusing on the copper surface, and the product percent of pass of a jet printing solder mask process is improved.

The present invention relates to crystal modifications of 1,1-dioxo-3,3-dibutyl-5-phenyl-7-methylthio-8-(N-{(R)-α-[N-((S)-1-carboxypropyl)carbamoyl]-4-hydroxybenzyl}carbamoylmethoxy)-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepine (odevixibat), more specifically crystal modifications 1 and 2 of odevixibat. The invention also relates to a process for the preparation of crystal modification 1 of odevixibat, to a pharmaceutical composition comprising crystal modification 1, and to the use of this crystal modification in the treatment of various conditions as described herein.

The invention discloses a preparation method of antistatic modified chinlon filaments, and relates to the field of chinlon filaments. When the antistatic modified chinlon filament is prepared, (formylmethyl) diethyl phosphate and 1-aminopyrrole react to prepare pyrrole diethyl phosphate; reacting the hydroxylated multi-walled carbon nanotube with pyrrole diethyl phosphate to obtain a modified multi-walled carbon nanotube; the preparation method comprises the following steps: reacting 2, 2 '-bipyridine-5, 5'-dicarboxylic acid with 2-amino-5-nitrophenol, and then reducing to obtain a benzoxazole diamine monomer; then, adipic acid, 1, 5-diaminopentane and a benzoxazole diamine monomer are subjected to a reaction, and modified polyamide is prepared; uniformly mixing the modified polyamide, the modified multi-walled carbon nanotubes, pyrrole, ferric trichloride and copper chloride, and performing melt spinning to obtain the antistatic modified polyamide filament. The antistatic modified chinlon filament prepared by the invention has excellent antistatic, flame-retardant, anti-aging and mechanical properties.

The invention discloses a preparation method of a dual PDE3 / 4 inhibitor Encephaline. The preparation method comprises the following steps: carrying out a sizuki coupling reaction on initial raw materials of a compound shown as a formula 1 and a compound shown as a formula 2 to obtain a compound shown as a formula 3, carrying out intramolecular cyclization to obtain a compound shown as a formula 4, converting carbonyl into a compound shown as a formula 5 by using POCl3, and carrying out an alkylation reaction on the compound shown as a formula 5 and a compound shown as a formula 6 to obtain a compound shown as a formula 7. Wherein the acyl imine of the compound as shown in the formula 7 and a compound as shown in a formula 8 are subjected to substitution reaction to obtain the product Encephaline. The selected raw materials are easy to obtain, the operation method is simple and convenient, the product yield is high, and the method is suitable for batch production.

The invention relates to a construction method of a multi-class lipid retention time general prediction model and a prediction system. The method comprises the following steps: by taking experimental retention time tRE of a lipid compound in a training set as a dependent variable and characteristic structure parameters of the lipid compound as an independent variable, carrying out quantitative processing on the independent variable and then carrying out regression modeling analysis, the characteristic structure parameters comprise the total carbon number c and the total carbon-carbon double bond number d of a fatty acyl chain, an ether chain, an alkenyl ether chain or / and a sphingosine skeleton, the types of skeletons contained in the lipid compound and the number of corresponding skeletons, and the types of characteristic groups and residues in the lipid compound and the number of corresponding residues; carrying out numerical quantization on parameters according to the number of skeletons, characteristic groups or residues of the corresponding types; the QSRR general prediction model of the retention time of the multi-class lipid compounds is obtained by adopting regression modeling, a more accurate MRM data acquisition window can be set for the lipid compounds, and the sensitivity, stability and coverage can be improved.

The invention discloses a crosslinked polyethylene reinforced high-strength insulating aerial cable, and belongs to the technical field of crosslinked polyethylene cable materials.The crosslinked polyethylene reinforced high-strength insulating aerial cable is prepared by the steps that hydroxyl is introduced to nano boron nitride powder, then amino is grafted through KH-550, nano alpha-Al2O3 powder is modified through gamma-glycidyl ether oxypropyl trimethoxy silane, and the cross-linked polyethylene reinforced high-strength insulating aerial cable is obtained; the preparation method comprises the following steps: preparing low-density polyethylene, compounding the low-density polyethylene with aminated nano boron nitride powder to form nano composite powder, improving the interface bonding force between the low-density polyethylene and the nano composite powder, carrying out melt blending on the low-density polyethylene and the nano composite powder to improve the dispersity of the nano composite powder in the low-density polyethylene, and carrying out nucleophilic acyl substitution reaction to obtain a fluorine-containing modified monomer. The nano boron nitride powder and the nano alpha-Al2O3 powder are subjected to a cross-linking reaction under the initiation action of an initiator and then coat the exterior of the thermal insulation layer, and the nano boron nitride powder and the nano alpha-Al2O3 powder are bridged through siloxane bonds to form a three-dimensional heat-conducting network, so that the heat resistance of the outer insulating layer is improved.

Disclosed is a printing ink for heat-sensitive recording media, which is (A) or (B) below: (A) a heat-sensitive color-developing printing ink containing a leuco dye, a color developer, a vinylpyrrolidone-vinyl acetate copolymer, and a solvent, wherein the color developer is at least one selected from the group consisting of an N,N'-diaryl urea-based compound represented by general formula (1) (in the formula, R0 represents a C1-12 alkyl group, a C7-12 aralkyl group, or a C6-12 aryl group. The aralkyl group and the aryl group may be substituted with a C1-12 alkyl group, a C1-12 alkoxy group, a C6-12 aryl group, or a halogen atom. A plurality of R0s may be the same or different. A1 represents a hydrogen atom or a C1-4 alkyl group. A plurality of A1s may be the same or different.), a compound represented by general formula (2) (in the formula, R1 to R5 are the same or different, and represent a hydrogen atom, a halogen atom, a nitro group, an amino group, an alkyl group, an alkoxy group, an aryloxy group, an alkylcarbonyloxy group, an arylcarbonyloxy group, an alkylcarbonylamino group, an arylcarbonylamino group, an alkylsulfonylamino group, an arylsulfonylamino group, a monoalkylamino group, a dialkylamino group, or an arylamino group.), and 5-(N-3-methylphenyl-sulfonamide)-N',N''-bis-(3-methylphenyl)-isophthalic acid diamide; and (B) a protective layer printing ink for heat-sensitive recording media, the protective layer printing ink containing an adhesive, a slipperiness imparting agent, and a solvent, wherein the adhesive is a polyvinyl acetal resin, and the slipperiness imparting agent is an alkyl phosphate ester and / or a salt thereof.

The invention discloses a graphene nanometer heavy anti-corrosion coating and a preparation method thereof, and belongs to the technical field of anti-corrosion coatings. The coating is prepared from the following components in parts by mass: 50 to 70 parts of diallyl bisphenol A type epoxy resin, 8 to 15 parts of histidine modifier, 12 to 20 parts of graphene nano composite modified filler, 5 to 10 parts of curing agent, 0.5 to 2 parts of flatting agent and 0.3 to 1 part of defoaming agent. The preparation method of the histidine modifier comprises the following steps: carrying out a Schiff base reaction on 1-palmitoyl-2-oleoyl ethanolamine and N-formyl-L-histidine to generate an intermediate A; reacting with a spiro quaternization reagent to form a quaternary ammonium salt intermediate B; and then compounding with aminopropyltriethoxysilane and silicotungstic heteropoly acid salt to obtain the product. The graphene nano-composite modified filler is prepared by modifying the surface of a graphene oxide / bentonite mutual intercalation layer structure through allyl trimethoxy silane. The graphene nano heavy anti-corrosion coating prepared by the invention forms a high-density cross-linked network, and has excellent barrier property, strong adhesive force, impact resistance and long-acting anti-corrosion performance.

The invention relates to an effective amount of novel acyl phenylalanine derivative as shown in a general formula (I), a preparation method thereof and application of a pharmaceutical composition containing the derivative as a medicine, and compared with the prior art, the novel acyl phenylalanine derivative has a wider application prospect. # imgabs0 #

The invention belongs to the field of enzymatic preparation of structural phospholipids, and particularly relates to a method for preparing phosphatidylserine through interfacial enzyme catalysis. A series of high-activity immobilized phospholipase are prepared by innovatively adopting bifunctional group modified hollow mesoporous silica microspheres as a carrier and adsorbing immobilized phospholipase D. The catalyst has the functions of a catalyst and an emulsifier, and a Pickering emulsion interfacial enzyme catalysis system can be efficiently constructed. In the system, the phosphatidylcholine and the serine are efficiently converted into the phosphatidylserine through a phosphatidyl transfer reaction, the conversion rate of the phosphatidylserine within 20 minutes can reach 85%-95%, and the catalytic efficiency reaches up to 372 mmol / (g.h). In addition, after the catalyst is recycled for 10 times, the conversion rate is still kept at 70.9%, and the catalyst shows excellent stability and reusability. The method has the remarkable advantages of being mild in reaction condition, high in catalytic efficiency, capable of being repeatedly used and the like, and a new technical approach is provided for industrial production of phosphatidylserine.

The invention relates to a bionic exosome for anti-inflammation and repair as well as a preparation method and application thereof, and belongs to the field of cosmetics. The bionic exosome provided by the invention comprises a membrane structure and an internal load phase, the membrane structure comprises a phospholipid bilayer, a stabilizer and a targeting ligand; the internal load phase comprises a solvent and an active component; the phospholipid bilayer is composed of phospholipid compounds; preferably, at least one of the distearoyl phosphatidyl ethanolamine-polyethylene glycol 2000 and the 1, 2-dioleoyl-sn-glycerol-3-phosphoethanolamine is adopted as the phospholipid compound, and at least one of the distearoyl phosphatidyl ethanolamine-polyethylene glycol 2000 and the 1, 2-dioleoyl-sn-glycerol-3-phosphoethanolamine is adopted as the phospholipid compound; at least one of cholesterol, phytosphingosine and sodium stearoyl glutamate is preferably adopted as a stabilizer, so that the stabilizer of the obtained bionic exosome is improved, and the bionic exosome has the advantages of high encapsulation efficiency, good encapsulation efficiency stability, simplicity in operation, excellent anti-inflammatory and repairing effects and the like.

The invention is applicable to the technical field of intelligent response materials, and provides a three-dimensional azobenzene functionalized covalent organic framework intelligent response material and a preparation method thereof. The three-dimensional azobenzene functionalized covalent organic framework intelligent response material is prepared by uniformly grinding 3, 3 ', 5'-tetra [(3 ', 5'-diformylphenyl)]-hexamethyl biphenyl and azobenzene-4, 4 '-diaminotriphenylamine, adding an organic solvent, adding a catalyst acetic acid aqueous solution, quickly freezing, emptying air, sealing with flame, heating after recovering to room temperature, and obtaining the three-dimensional azobenzene functionalized covalent organic framework intelligent response material. According to the invention, the azobenzene functionalized covalent organic framework material with a bcu topological structure is synthesized; the material has excellent photostimulation response CO2 adsorption performance; reversible control of CO2 adsorption capacity can be realized through ultraviolet light and heating conditions, at least five times of circulation can be maintained, and good circulation stability is achieved.

The invention belongs to the technical field of pesticides, and particularly relates to a pyridyl alkoxy pyrimidine compound and application thereof. The compound is shown as a formula I: # imgabs0 #, wherein X and Y respectively and independently represent hydrogen, hydroxyl, alkyl, alkoxy, alkenyloxy, alkynyloxy and the like; z represents hydrogen, halogen, a cyano group, an amino group, a nitro group, a formyl group, a cyano alkyl group, a hydroxyalkyl group, an alkyl group, an alkenyl group, an alkynyl group and the like. The compound or the salt thereof has an excellent effect as an agricultural and horticultural insecticide.

The invention belongs to the technical field of photocuring, and relates to an allyl carbazole ketoxime ester compound, a product containing the allyl carbazole ketoxime ester compound and application of the allyl carbazole ketoxime ester compound. Specifically, the structure of the compound disclosed by the invention is shown as a formula (I), not only is the relative low activity of carbazole acyl free radicals overcome, but also the problems of toxicity, odor and the like in a photocuring system are solved, and the compound has the advantages of wide applicable wavelength range, high photolysis efficiency, good compatibility with monomers or resins and the like. # imgabs0 #

The invention discloses a preparation method of a self-humidifying membrane electrode of a proton exchange membrane fuel cell, relates to a preparation method of a membrane electrode, and aims to solve the technical problem of poor performance of the conventional self-humidifying membrane electrode. The method comprises the following steps: 1, synthesizing a COFs material by using 2, 4, 6-triformyl phloroglucinol and 2, 5-diaminobenzene sulfonic acid through a two-phase method; 2, preparing slurry a by using a Pt / C catalyst and a perfluorosulfonic acid ionomer solution; preparing self-humidifying catalyst layer slurry b from a COFs material, a Pt / C catalyst and a perfluorosulfonic acid ionomer solution; and 3, coating the slurry a on the anode surface of the proton exchange membrane, and coating the slurry b on the cathode surface to obtain the self-humidifying membrane electrode. According to the electrode, H2 / O2 is used as fuel, and the power density is 756.3 mW / cm < 2 > under the relative humidity of 20%; h2 / air is used as fuel, the power density is 437.8-879.7 mW / cm < 2 > under the relative humidity of 50%, and the material can be applied to the field of fuel cells.

The invention discloses a hydrogel patch for gastric perforation repair and a preparation method thereof, and belongs to the technical field of biomedical materials. The preparation method comprises the following steps: dissolving acryloyl valine, acrylic acid, methylene bisacrylamide, a compound A and a photoinitiator in an alcohol solvent, and defoaming to obtain a precursor solution; and placing the precursor solution in a mold, carrying out ultraviolet-induced curing, soaking the obtained hydrogel in a hydrochloric acid solution, and replacing the alcohol solvent to obtain the hydrogel patch for gastric perforation repair. The hydrogel patch provided by the invention has the advantages of strong acid corrosion resistance, good biocompatibility, low swelling ratio, stable adhesion performance in a fluctuating pH environment and the like. The tough and stable adhesion performance ensures that the hydrogel can be permanently and reliably adhered to a gastric perforation part in a dynamic gastric acid environment, and a stable platform is provided for drug delivery, so that the surgical operation time is expected to be shortened, and wound healing is promoted.

The invention discloses an all-solid-state composite dry conductive agent and a preparation method thereof, and belongs to the technical field of batteries. The all-solid-state composite dry conductive agent is prepared by the following steps: uniformly mixing carbon nanotubes, high-dispersion carbon black and graphene to obtain a primary mixture; then preparing a uniformly dispersed glue solution from the composite dispersant and water; and then adding the primary mixture into the glue solution, uniformly mixing, sanding, homogenizing, drying and crushing to obtain the product, the high-dispersion carbon black is obtained by oxidizing carbon black to form active groups such as carboxyl and hydroxyl on the surface of the carbon black, halogenating acyl and then reacting with lithium 2, 5-diaminobenzene sulfonate. The preparation method comprises the following steps: grafting histidine ester into carboxymethyl cellulose by using propylene glycol diglycidyl ester as a cross-linking agent, then introducing allyl-1, 3-sultone, then copolymerizing with lithium 2-acrylamido-2-methylpropanesulfonate and 3-aminobenzoic acid allyl ester protected by fluorenylmethoxycarbonyl, and then deprotecting to obtain the composite dispersant.

Provided herein is a process for preparing compound A comprising (a) admixing 2-isopropyl-4-methylpyridin-3-amine (Compound B), or a salt thereof, a first base, and a reactive compound comprising phosgene or a phosgene equivalent in an organic solvent to form 3-isocyanato-2-isopropyl-4-methylpyridine (Compound C); (b) admixing Compound C and 2,6-dichloro-5-fluoronicotinamide (Compound D) to form 2,6-dichloro-5-fluoro-N-((2-isopropyl-4-methylpyridin-3-yl)carbamoyl)nicotinamide (Compound E); and (c) admixing Compound E and a second base to form a product mixture comprising Compound A and the second base. Also provided herein is a process for synthesizing AMG 510 comprising using Compound A prepared according to the disclosed processes

The invention discloses an implantable absorbable PLA composite material and a preparation method thereof, and relates to the technical field of medical materials. The implantable absorbable PLA composite material is prepared from the following raw materials in parts by weight: 60 to 70 parts of PLA, 5 to 10 parts of poly (lactic-co-glycolic acid), 8 to 12 parts of polycaprolactone, 5 to 8 parts of modified hydroxyapatite, 2 to 3 parts of a toughening agent and 0.2 to 0.6 part of an antioxidant, the toughening agent is prepared by the following steps: reacting hydroxyethyl methylacrylate with ethylenediamine to prepare a four-arm compound, reacting the four-arm compound with 1-chloro-4-isocyanatobutane to prepare an isocyanate compound, and finally reacting the isocyanate compound with polyethylene glycol. The implantable absorbable PLA composite material prepared by the invention has excellent tensile property and impact resistance, and can meet the application requirements of clinical medical treatment.

The invention relates to the field of medicine synthesis, and particularly discloses a preparation method of abesilib and an intermediate thereof. The invention relates to an abesiril intermediate, which is 4-chloro-5-fluoro-2-(methylsulfonyl) pyrimidine (IV) and 4-fluoro-6-(5-fluoro-2-(methylsulfonyl) pyrimidine-4-yl)-1-isopropyl-2-methyl-1H-benzo [d] imidazole (V). The invention further provides a preparation method of the abesiril intermediate. And carrying out nucleophilic substitution reaction on the abesilib intermediate V and 5-[(4-ethyl piperazine-1-yl) methyl] pyridine-2-amine to prepare the abesilib. According to the preparation method, the raw materials are cheap and easy to obtain, the reaction selectivity of functional groups is high, ectopic impurities generated by a halogen atom competition reaction are effectively avoided, meanwhile, introduction of heavy metal palladium can be reduced, and therefore the cost is reduced. The synthetic route is simple, the atom economy is high, the controllability in production is high, and the method is suitable for industrial production.

The invention provides a preparation method of a Janus material for simultaneous screening of protein phosphorylation and palmitoylation modification, and belongs to the technical field of magnetic material synthesis. The method comprises the following steps: firstly, preparing MCeO2; the preparation method comprises the following steps: mixing MCeO2, hexadecyl trimethyl ammonium bromide and ammonia water to obtain a mixed solution, adding 1, 2-bis (triethoxysilane) ethane into the mixed solution for reaction to obtain a product, and dispersing the product into an NH4NO3 solution for reflux reaction to obtain Janus MCP; the preparation method comprises the following steps: reacting Janus MCP with a silane coupling agent, dissolving aminated Janus MCP and 4-ethylene sulfonyl benzoic acid in a buffer solution containing EDC and NHS, and reacting to obtain the Janus material. The preparation method is reliable, the material performance is stable, and the enrichment efficiency of the magnetic Janus on target peptide fragments (phosphorylated peptide fragments and palmitoylated peptide fragments) is remarkably improved.

The invention relates to an alkynyl-modified acyl covalent organic framework (COF) material and application thereof, and relates to the field of preparation of crystalline porous materials and fuel cells. The material is a covalent organic framework material which is synthesized by taking 1, 3, 5-triformyl phloroglucinol and 2, 5-bis (2-propynyloxy) terephthaloyl hydrazine as raw materials through solvothermal reaction under specific conditions, and has relatively high crystallinity. The material has good performance in the aspect of proton conductivity, the highest proton conductivity can reach 6.16163 * 10 <-4 > S / cm, and the mechanical property is enhanced due to introduction of alkynyl. Alkynyl is used as an active functional group, and various chemical reactions can be derived, so that the potential application value of the material is greatly improved.

The invention belongs to the field of preparation of medical intermediates, and particularly relates to a preparation method of an On-DNA sulfinic acid structure compound. The method for preparing the On-DNA sulfinic acid structure compound comprises a step of oxidizing On-DNA thiol (phenol) into the On-DNA sulfinic acid structure compound under alkaline and heating or illumination conditions, a solvent used in the reaction step is a mixed solution of water, dimethyl sulfoxide, N, N-dimethylformamide, acetonitrile, ethanol or tetrahydrofuran, the reaction temperature is not more than 80 DEG C, and the reaction time is not more than 2 hours. And the illumination wavelength ranges from 365 nanometers to 535 nanometers. The On-DNA sulfinic acid structure compound obtained in the invention can be directly used for constructing a structure compound with a sulfonyl group, the reaction condition is mild and convenient, a new method and a new idea are provided for construction of a DNA coding compound library, and the On-DNA sulfinic acid structure compound has a very good application prospect in lead drug development.