55 results about "Orthoester" patented technology

The invention discloses organic nano composite hydrogel as well as a preparation method and application of the organic nano composite hydrogel, and belongs to the technical field of biological medicine delivery. The polysaccharide-based nano prodrug in the composite hydrogel can be subjected to surface protonation under the stimulation of a tumor extracellular slightly acidic environment, so that cellular uptake is promoted, low-pH / high-concentration glutathione in tumor cells is responded, intracellular aggregation and controllable release of the nano drug are realized, the retention time of the drug in the cells is prolonged, and the bioavailability of the drug is improved. The technical effect of killing tumor cells through combined chemotherapy is achieved. According to the preparation method disclosed by the invention, the release of the polysaccharide-based nano prodrug from the hydrogel and the tissue infiltration capacity are accelerated by adopting fluorinated orthoester, the infiltration of the polysaccharide-based nano prodrug to cells is increased, and then the drug-loaded compound is encapsulated by using gellan gum, so that the slow-release effect of the polysaccharide-based nano prodrug is enhanced; therefore, the efficient enrichment of the medicine at the tumor part is realized.

The present disclosure provides polymorphs of 3-(2,3,5,6-tetrafluoro-3′-trifluoromethoxy-biphenyl-4-ylcarbamoyl)-thiophene-2-carboxylic acid, and methods of making such polymorphs. The present disclosure further provides pharmaceutical compositions and kits comprising polymorphs of the invention, and methods of treating, preventing, or ameliorating a disease or condition comprising administering a polymorph of the invention.

The invention belongs to the technical field of nano biological medicines, and particularly relates to injectable organic composite hydrogel combined with photo-thermal chemotherapy as well as a preparation method and application thereof. The injectable organic composite hydrogel combined with photo-thermal chemotherapy is composed of an orthoester compound and a water-phase hydrogel, the orthoester compound is emulsified and then uniformly dispersed in the hydrogel, and the hydrogel is formed by crosslinking carboxymethyl chitosan and glutaraldehyde. In the injectable organic composite hydrogel combined with photo-thermal chemotherapy provided by the invention, firstly, oily orthoester is utilized to dissolve a cis-platinum prodrug and indocyanine green to obtain an orthoester compound, then the orthoester compound is uniformly emulsified and loaded in the hydrogel, dynamic imine bonds of the hydrogel respond to tumor slightly acidic environment breakage, and then the dynamic imine bonds of the hydrogel are separated from the dynamic imine bonds of the hydrogel, so that the injectable organic composite hydrogel combined with photo-thermal chemotherapy can be used for preparing the injectable organic composite hydrogel combined with photo-thermal chemotherapy. The orthoester compound successfully escapes, along with degradation of the oily orthoester, the cis-platinum prodrug and the indocyanine green are self-assembled through hydrogen bonds to form nanoparticles, the enrichment and retention capacities of the two drugs at the tumor site are enhanced, and the overall curative effect is improved.

The invention particularly relates to a UV-cured epoxy resin material for 3D printing and a preparation method of the UV-cured epoxy resin material. The epoxy resin material is prepared from the following raw materials in parts by weight: 60 to 65 parts of epoxy acrylate resin, 30 to 35 parts of epoxy resin, 2 to 5 parts of ANFs / graphene / MoS2 composite lubricant, 4 to 6 parts of flexibilizer, 3 to 5 parts of repairing agent, 3 to 5 parts of spiro orthoester, 1 to 3 parts of initiator, 0.6 to 1.5 parts of tetrahydrofuran acrylate and 0.1 to 1 part of rheology modifier. The UV-cured epoxy resin material for 3D printing obtained by the scheme has good toughness, impact resistance and wear resistance, and has good self-recovery capability and high long-term reliability under a heating condition for conditions such as slight scratches and cracks in 3D printing application.

The invention belongs to the technical field of biological medicine, and discloses a bionic nano-particle suspension formulation based on orthoester compounds and a preparation method of the bionic nano-particle suspension formulation. The bionic nanoparticle suspension formulation comprises a liquid auxiliary material, a photosensitizer and bionic nanoparticles, wherein the photosensitizer and the bionic nanoparticles are dispersed in the liquid auxiliary material. According to the present invention, an orthoester compound represented by a formula I is adopted as a liquid auxiliary material, bionic nanoparticles and a photosensitizer are simultaneously introduced into OE to obtain the bionic nanoparticle suspension formulation having multiple antitumor mechanisms, the bionic nanoparticles are cancer cell membrane vesicle-coated nano-drugs, and the cancer cell membrane vesicle-coated nano-drugs can be prepared through a cancer cell membrane biomimetic technology, such that the cancer cell membrane vesicle-coated nano-drugs can be prepared into the bionic nanoparticle suspension formulation having multiple antitumor mechanisms; the homologous targeting function provided by the cancer cell membrane is utilized, and the active targeting property and cellular uptake of the nano-drug are remarkably improved. Formula I: # imgabs0 #

The invention relates to the technical field of preparation of biological materials and pharmaceutical preparations, in particular to organic composite hydrogel as well as a preparation method and application thereof. The specific preparation method comprises the following steps: dissolving a targeted drug in orthoester to obtain a targeted drug-orthoester solution; the preparation method comprises the following steps: mixing an oxidized dextran solution, a targeted drug-orthoester solution and a carboxymethyl chitosan solution, carrying out vortex treatment, and standing to prepare the organic composite hydrogel. The solubility of the targeted drug in the hydrogel is improved by utilizing orthoester, the orthoester can carry the targeted drug to efficiently escape from the hydrogel, and the targeted drug can be self-assembled to form nanoparticles along with degradation of the orthoester in the escape process, so that the retention capacity of the targeted drug at a tumor site is enhanced, and the targeting drug can be used for treating tumor tumors. The drug enrichment capacity is improved, meanwhile, the toxic and side effects of the whole body are reduced, and the problems that nano-drugs are poor in solubility, still prone to being removed after intravenous administration and poor in enrichment effect at tumor sites are solved.

The invention discloses a pH response hydrogel microneedle, which comprises a microneedle substrate, microneedle tips are arranged on the microneedle substrate, the height of the microneedle tips is 100-1600 microns, the diameter of the tip ends of the microneedle tips is 5-15 microns, and the density of the microneedle tips is 200-1000 pieces per square centimeter. The preparation method comprises the following steps: preparing a hyaluronic acid solution for the microneedle substrate, preparing a methacrylated chondroitin sulfate solution for the microneedle tip, preparing methacrylated orthoester, preparing orthoester, preparing a non-steroidal anti-inflammatory drug solution, preparing a microneedle tip solution, preparing the microneedle and demolding the microneedle to prepare the complete soluble microneedle patch. The invention has the advantages of high drug efficiency, high efficiency in dissolving fat / water drugs, and long-acting slow release.

The invention discloses a preparation method of fiazonetin, and belongs to the technical field of medicinal chemistry. According to the route, 2-halo-3-methylpyrazine which is low in price and easy to obtain is used as a raw material and sequentially reacts with hydrazine hydrate and orthoester, and then a hydrogenation reduction reaction is performed to generate a compound 4; carrying out chiral resolution or chiral separation on the compound 4 and carrying out condensation reaction on the compound 4 and p-fluorobenzoyl halide to obtain an intermediate compound 5 or 5'and a new intermediate compound 6; reacting the compound 6 with a halogenating reagent to obtain a compound 7; carrying out Suzuki coupling reaction on the compound 7 and a compound 8 to obtain a compound, namely, the compound of the formula A, namely, non-azonepan; according to the route, the raw materials are simple, easy to obtain and low in cost; the reaction is simple, the preparation efficiency is high, and the reaction yield of each step can be higher than 90%; no harsh reaction conditions exist, and operation is safe; post-treatment is simple and convenient, and environmental pollution is low. The method is suitable for large-scale production; a high-chiral product can be obtained, the chiral purity value of a final product is as high as 99.5%, and the method has relatively good market value and profound practical significance. # imgabs0 #

The invention provides a preparation method and application of a modified PVC adsorbent for gold extraction of carbonaceous gold ore, and belongs to the technical field of organic polymer materials and resource utilization. Based on construction of a hydroxylation-xanthate esterification reaction and bifunctional adsorption sites, a series of chemical modification paths of acetate nucleophilic substitution-hydrolysis-carbon disulfide alkali treatment are established, and xanthate functional groups with high reaction activity are accurately constructed on an inert PVC framework. Sulfur atoms in xanthate groups of the modified PVC are excellent electron donors and can generate strong chemical adsorption with metal impurities or polar sites on the surface of carbon, meanwhile, Van der Waals interaction between a main chain of the modified PVC and the carbon is reserved, and unmodified PVC or single hydroxylated PVC does not have the synergism of chemical adsorption and physical adsorption, so that the modified PVC can be used for preparing the carbon-modified PVC composite material, and the carbon-modified PVC composite material can be used for preparing the carbon-modified PVC composite material. And leap-type improvement of the adsorption capacity and selectivity of organic carbonaceous in minerals is realized.

According to the method, a 2-aminobenzamide compound and orthoester are used as reaction substrates, titanocene dichloride is used as a catalyst, methanol or ethanol is used as a solvent, and the quinazolinone compound is synthesized through cyclization under the catalysis of titanocene dichloride. According to the method, titanocene dichloride generates Lewis acid (Cp2Ti (OCH3) Cl or Cp2Ti (OEt) Cl) and # imgabs0 # acid (HCl) with high catalytic activity in situ under the action of a 2-aminobenzamide compound and methanol or ethanol, and the quinazolinone compound is efficiently and catalytically synthesized under the combined action of the two acids. The method has the advantages that the reaction system is cheap and easy to obtain, the substrate range is wide, the reaction condition is mild, the yield of the target product is high, and the method has a wide application prospect.

The present invention relates to an injectable dermal filler formulation for providing an improved and homogeneous volumizing and filling effect. In particular, the formulation comprises a combination of hyaluronic acid and poly(orthoester) and may be used for cosmetic purposes.

A slow-reaction recyclable epoxy resin system for structural composites and a process of recycling the composites made therefrom are disclosed. The system includes an epoxy resin component including: a high purity epoxy resin selected from a high purity bisphenol A epoxy resin, a high purity bisphenol F epoxy resin, and combinations thereof, where the high purity epoxy resin is in a range of from 20 wt% to 95 wt% of the total weight of the cyclopentene resin component; a standard epoxy resin selected from a standard bisphenol A epoxy resin, a standard bisphenol F epoxy resin, and combinations thereof, where the standard epoxy resin is in the range of from 1 wt% to 50 wt% of the total weight of the epoxy resin component; and a curing agent component including a curing agent having at least one cleavage bond selected from a group including an acetal bond, a ketal bond, a formal bond, an orthoester bond, or a siloxy bond. The pot life of the slow-reaction recyclable epoxy resin system is greater than 540 minutes at 25 DEG C.

A treatment composition comprising at least one fragrance raw material and an esteramine or a salt thereof, which may be obtained by a process using a catalytic amount of at least one orthoester, and a method for treating an article or surface, optionally comprising treating the article or surface with such treatment composition in the presence of water.

To provide an injection chemical composition that can achieve both curability in water and foaming and curability in non-water environments, even after being exposed to high temperature and high humidity environments. [Solution] An injection solution composition comprising a first agent (A) and a second agent (B), wherein the first agent (A) comprises an aqueous solution of sodium silicate (A-1), an organic polyol (A-2), and a tertiary amine catalyst (A-3), and the second agent (B) comprises an organic polyisocyanate containing a mixture of diphenylmethane diisocyanate and polymethylene polyphenyl polyisocyanate having 3 or more isocyanate functional groups (B-1), or a reaction product (B-1') of an active hydrogen group-containing compound and a mixture (B-1), at least one acid component (B-2) selected from the group consisting of phosphate monoesters and phosphate diesters, and at least one hydrolyzable component (B-3) selected from the group consisting of orthoester compounds and acetal compounds.

The present application provides a method for preparing a high-purity key intermediate M2 of dicardipine drugs, belonging to the technical field of drug intermediate preparation. A dehydrating agent is added during the preparation of the intermediate M2, and the dehydrating agent is an orthoester dehydrating agent. Using the method provided in the present application, the yield of the intermediate M2 is 84.3%, the HPLC purity is 99.63%, M2Z3: 0.17%; M2Z4: 0.15%; other impurities <0.10%, and the content of impurities P0Z4 (i.e., M2Z3) and P0Z5 in the further prepared nicardipine is determined to be: P0Z5 <0.02%, P0Z4 <0.02%.

[Question] To provide an alkali-developable curable resin composition that suppresses performance degradation even under relatively harsh storage conditions. [Solution] An alkali-developable curable resin composition characterized by comprising at least (A) an alkali-soluble resin, (B) a photopolymerization initiator having an oxime bond, (C) a reactive diluent, and (D) a thermosetting resin, wherein the composition is at least a two-component system in which the (B) photopolymerization initiator having an oxime bond and the (A) alkali-soluble resin are blended into separate compositions, and at least one (E) orthoester compound is blended with the (B) photopolymerization initiator having an oxime bond.

The present invention aims to provide a radiosensitive linear composition, a hardened film, a method for manufacturing the same, a semiconductor element, a display element, and a polymer that can produce a film with excellent adhesion. A radiosensitive linear composition comprises: a polymer containing a structural unit (I) having a base represented by formula (1), a photoacid generator, and an orthoester compound. In formula (1), R... 1 It can be a hydrogen atom, a halogen atom, a hydroxyl group, or an alkoxy group having 1 to 6 carbon atoms. R 2 and R 3 Each of the following can be independently a hydrogen atom, a halogen atom, a hydroxyl group, an alkoxy group with 1 to 6 carbon atoms, an alkyl group with 1 to 10 carbon atoms, or a phenyl group. "*" indicates a bond.

A composition comprising (a) a therapeutic agent or a pharmaceutically acceptable salt thereof; (b) a PEG-monoorthoester-lipid; (c) an amphiphilic lipid; (d) a cationic lipid and / or a beta-alanyl-prolyl-cysteine methyl ester; and optionally (e) a steroid and / or a ceramide and / or DOPE. The composition for use as a medicament.

The present application relates to the technical field of nickel-based catalyst, and discloses a diimine ligand, a preparation method and application thereof, wherein the raw materials for preparing the diimine ligand contain acenaphthenequinone, a protective agent, substituted aniline and a catalyst, the protective agent is selected from one or more than two of ortho ester, amine, hydrazine and substituted hydrazine; and the molar ratio of the acenaphthenequinone, the protective agent, the substituted aniline and the catalyst is 1:(0.5-3):(1.6-2.4):(0.1-10). In the present application, a certain amount of protective agent is added to the reaction system, the acenaphthenequinone is reacted with the ortho ester or low-molecular-weight amine to generate ketal or imine, the ketal or imine is separated or not separated, and then reacted with the substituted aniline to generate the target product diimine ligand, no water is generated in the synthesis reaction of the diimine ligand, the balance can be effectively promoted to the forward reaction, and the reaction yield is improved.

This invention discloses a cross-linked nanoprodrug, a nano-self-assembled hydrogel precursor tablet prepared therefrom, and its applications. The nano-self-assembled hydrogel precursor tablet of this invention is prepared by direct compression of the cross-linked nanoprodrug or by compression of a cross-linked nanoprodrug mixed with a drug-loaded orthoester compound. It exhibits high nanodrug content, enhanced nanoparticle release, and high storage and transport stability, as well as good patient compliance. This nano-self-assembled hydrogel precursor tablet responds to the pH gradient environment of the gastrointestinal tract. In acidic gastric juice, through protonation of functional groups, it forms a three-dimensional network structure of nano-self-assembled hydrogel mediated by hydrogen bonds. Subsequently, it stably passes through the small intestine into the colon. In the alkaline colonic environment, its functional groups deprotonate, hydrogen bonds break, and the drug is efficiently released under the electrostatic repulsion between nanoparticles and the synergistic repulsion of the orthoester compound. While preferentially adhering to colonic lesions through electrostatic interactions, it significantly improves the targeted and synergistic therapeutic effect on CRC.

The present application relates to a kind of preparation methods of 3,4-dihydroxy-5-methoxybenzoic acid methyl ester, with gallic acid as raw material, it is reacted with trimethyl orthoformate or trimethyl orthoacetate, trimethyl orthoformate or trimethyl orthoacetate can realize the protection of adjacent diphenol hydroxyl on one hand, on the other hand, carboxyl esterification and 5-hydroxyl are methylated, form the methyl ester of 5-phenolic hydroxyl methylation and 3,4-orthoester protection benzoic acid shown in formula 1a or formula 1b, further by acidic solution treatment, deprotection is carried out, and the target product 3,4-dihydroxy-5-methoxybenzoic acid methyl ester is prepared.The preparation method is mild in reaction condition, process is simple, easy to operate, product yield and purity are high, solve the wastewater problem in borax protection method, and avoid using toxic dimethyl sulfate for methylation, process condition is simple, easy to operate, convenient for industrialization, with very high application value.

The invention discloses a preparation method of fiazonetin, and belongs to the technical field of medicinal chemistry. According to the route, a 3-methylpyrazine compound is used as a raw material, a compound 3 is obtained through an amine alkylation reaction or a condensation reaction, the compound 3 reacts with orthoester to obtain a compound 4, the compound 4 is subjected to a hydrogenation reduction reaction to obtain a compound 5, and the compound 5 is subjected to chiral resolution or chiral separation to obtain a compound 6. And carrying out condensation reaction on the compound 6 and p-fluorobenzoyl halide to obtain the non-azonepan. The raw materials are simple and easy to obtain, low in cost and more suitable for large-scale industrial production; according to the present invention, the route reaction is simple, the preparation efficiency is high, the yield of each reaction step can achieve about 90%, the ee value of the final product can achieve more than 99.0%, the chiral purity is high, no harsh reaction condition exists, and the method is suitable for large-scale production, and has good market value and profound practical significance. # imgabs0 #

To provide a polymer for delivery of agents, and a formulation comprising the polymer.SOLUTION: There is provided a polymer including: (1) a polymer skeleton as alkylene; (2) a plurality of first pendant groups including nucleosides; (3) a plurality of first linking moieties that covalently bond the first pendant groups to the polymer skeleton; (4) a plurality of second pendant groups including polyalkyleneoxides; and (5) a plurality of second linking moieties that covalently bond the second pendant groups to the polymer skeleton, wherein the first linking moieties contain a group selected from the group of those in the figure and the second linking moieties contain a hydrolytically labile group selected from the group consisting of an ester group, an ortho ester group, a thioether ester group, an anhydride group, an amide group, and a carbonate group.SELECTED DRAWING: Figure 3A

The invention discloses a pH-responsive supramolecular salicylic acid nanogel and a preparation method and application thereof, and the pH-responsive supramolecular salicylic acid nanogel comprises the following preparation raw materials by mass: 3-30% of salicylic acid; 0.6 to 1.5 percent of orthoester; 30 to 50% of poloxamer; 0.5 to 5.0 percent of polyhydric alcohol; 0.5-1% of a surfactant; and the balance solvent. Through supramolecular design, salicylic acid molecules and a precursor containing a pH sensitive group (orthoester) are integrally constructed into a nanogel network through non-covalent self-assembly, so that the contradiction between solubility and irritation of high-concentration salicylic acid is fundamentally solved; the prepared pH-responsive supramolecular salicylic acid nanogel can realize the synergistic effects of stable loading of high-concentration salicylic acid, targeted response release of an inflammatory site and low skin irritation, and the preparation process is simple, convenient and environment-friendly, is suitable for industrial production, and has a wide application prospect in the field of functional skin care products.

Provided is a method for producing a solvent-free siloxane composition which is solvent-free and has excellent long-term stability. A method for producing a solvent-free siloxane composition, the method including the following steps (1), (2), and (3) in this order. Step (1): A step for preparing a siloxane compound having a silanol group at a terminal by reacting a silane compound. Step (2): After the amide compound has been added, a step for dehydrating with an orthoester and removing the solvent by evaporation is performed. Step (3): A step for obtaining a terminated siloxane compound by dissolving the terminal silanol group-containing siloxane compound in an organic solvent and then adding a blocking agent.

The invention discloses a pH response hydrogel microneedle as well as a preparation method and application thereof. The pH response hydrogel microneedle comprises a hydrogel microneedle main body and colchicine loaded in the hydrogel microneedle main body, the hydrogel microneedle main body is hydrogel with a three-dimensional network structure, which is formed by covalent cross-linking of methacrylated hyaluronic acid and methacrylated orthoester. The hydrogel microneedle prepared by taking the methacrylated hyaluronic acid and the methacrylated orthoester as cross-linking components not only has good mechanical property, swelling property and biocompatibility, but also can respond to the microenvironment pH of an inflammation part by virtue of the pH sensitivity of the methacrylated orthoester, so that the utilization rate of a medicine is improved, and the bioavailability of the medicine is improved. The acute gout arthritis can be quickly and efficiently treated, and the clinical application potential is huge.

The invention discloses an infrared stealth film material of functionalized polystyrene and a preparation method thereof, and belongs to the technical field of functional material preparation. The infrared stealth film material of functionalized polystyrene is composed of the following components in parts by weight: 53-67 parts of a base film material, 8-12 parts of modified polystyrene, and 0.8-1.3 parts of an adhesive, wherein the base film material is prepared from meta-iodoaniline, trimethylsilyl acetylene, diisopropyl xanthate disulfide, tetramethylammonium hydroxide, polyvinylidene fluoride, and polymethyl methacrylate, and the modified polystyrene is prepared from syringaldehyde, n-butyl bromide, 2,2'-dipyrrolyl methane, 2-thiophene boric acid, and polystyrene cross-linked microspheres. The infrared stealth film material of functionalized polystyrene prepared by the method has excellent stealth performance and mechanical properties.

The invention relates to the technical field of medicine preparation, and particularly provides a semaglutide injection and a preparation method thereof.The semaglutide injection comprises semaglutide, a polyorthoester polymer, a cosolvent and a diluent, based on the total mass of the semaglutide injection, the mass ratio of the polyorthoester polymer is 40-80%, and the mass ratio of the cosolvent to the diluent is 40-80%. The mass ratio of the poly orthoester polymer to the cosolvent is (40-80): (2-15). The polyorthoester polymer and the cosolvent are mutually compounded, so that the effect of the polyorthoester polymer serving as a sustained-release skeleton is fully volatilized, the drug release period is remarkably prolonged, meanwhile, the problem of burst release of the drug is avoided, the stable release performance of the drug is improved, the stability of the injection is high, and even if phenol is not added to serve as a preservative, the injection does not have toxic or side effect. And the injection also has a relatively long shelf life.

The invention discloses a preparation method of a cellulose-based radiation cooling material, and belongs to the technical field of cooling materials. Comprising the following steps: adding a tetraethyl orthosilicate solution into absolute ethyl alcohol, stirring, then adding deionized water, adjusting the pH value to be alkaline by using ammonia water, and continuously stirring to obtain a SiO2 spherical prepolymer; continuously adding xanthate cellulose nanofibers, stirring, and centrifuging to obtain a precipitate; finally, adding water into the precipitate to uniformly disperse the precipitate, so as to prepare a SiO2 (at) CNF mixed solution; adding tert-butyl alcohol into the SiO2 (at) CNF mixed solution, and stirring to obtain a dispersion; and pouring the dispersion into a mold, carrying out freezing treatment, and then drying to obtain the SiO2 (at) CNF hybrid aerogel. The aerogel can be applied to the field of radiation cooling.

The present disclosure provides for methods of producing analgesia in a subject. In some cases, methods produce analgesia in a subject undergoing arthroscopic subacromial decompression surgery. The present disclosure also relates to improved sustained release drug delivery systems. In some cases, a composition comprises an active pharmaceutical agent; at least one of sucrose acetate isobutyrate and a polyorthoester; an organic solvent; and 2,6-dimethylaniline, wherein the 2,6-dimethylaniline is present at a level less than 500 ppm. In some cases, a composition comprises bupivacaine N-oxide at a level less than 1 wt %, based on weight of the composition. In some cases, a composition comprises metal present at a level less than 5 ppm. Dosage forms and methods are also provided.