1449results about "Steroids" patented technology

The invention relates to the technical field of extraction and separation of compounds in traditional Chinese medicinal materials, in particular to a method for simultaneously separating and purifying three pentacyclic triterpenoids from a tripterygium hypoglaucum root medicinal material. Three pentacyclic triterpenoid monomers are obtained through the steps of smashing, reflux extraction, normal-phase silica gel chromatography, reversed-phase high-pressure column chromatography, recrystallization and the like, the method is high in extraction efficiency and small in reagent dosage, the three pentacyclic triterpenoid compounds can be obtained at the same time, and the obtained compounds are high in purity and yield, have high social and economic value and are suitable for industrial production. The purity of the obtained plasmin, tripterine and demethylzeylasteral is high, and a foundation is laid for the preparation and production of reference substances of triterpenoid components in the roots of pyracantha fortunei, the subsequent pharmacological activity and the development of new immune drugs.

The invention discloses a synthesis method of oxyalkyl isourea and application of the oxyalkyl isourea as a free radical alkylation reagent. According to the synthesis method, cheap and rich alcohol compounds and carbodiimide are used as raw materials, oxygen alkyl isourea is synthesized in one step under the mild condition of metal catalysis, the synthesis process is simple and convenient, the yield is high, and hectogram-level large-scale preparation can be achieved. The synthesized oxyalkyl isourea can be used as a free radical alkylation reagent to be applied to a coupling reaction of metal catalysis, so that different alkylate products rich in saturated carbon sequence structures are prepared, and the method has a good application prospect.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a dammarane sapogenin-isatin derivative and application thereof in anti-tumor treatment. The dammarane sapogenin-isatin conjugate is constructed by taking dammarane sapogenin as a mother nucleus, deriving the dammarane sapogenin and chloroacetic acid and then introducing an indolone structural unit, and R1, R2 and R3 are as described in the claims and the specification. According to the invention, isatin fragments and ginsenoside are coupled for the first time, the anti-tumor activity of the compounds is systematically evaluated, and the action mechanism research of the compounds in colorectal cancer and other tumors is further developed. Results show that the obtained compound has relatively good anti-tumor efficacy, tumor cell selectivity, relatively low toxicity and relatively high bioavailability, and shows good patent medicine potential and wide market prospects.

The invention belongs to the field of organic synthetic chemistry, and relates to a preparation method of melatonin and meerythrine indole derivatives and compounds. Specifically, the indole derivative is efficiently synthesized by taking arylamine and carboxylic acid as raw materials through a one-pot two-step reaction in the presence of catalysis of ferric chloride hexahydrate (FeCl3. 6H2O), a ligand, a diazotization reagent, an additive and a solvent under the conditions of visible light irradiation, inert atmosphere and room temperature. According to the method, visible light induced iron-based LMCT catalysis and iron lewis acid catalysis functions are integrated, and efficient integration of diazotization, decarboxylation, free radical coupling and cyclization reaction is achieved. The method has the advantages that raw materials are cheap and easy to obtain, reaction conditions are mild, substrate applicability is wide, functional group compatibility is good, operation is easy, convenient and safe, and environment friendliness is achieved, gram-level scale preparation can be achieved, and a green and efficient synthesis path is provided for indole compounds with biological activity such as melatonin and meerythrine.

The invention discloses design and synthesis of a series of brain-targeted ginsenoside Rg1 derivatives and application of the brain-targeted ginsenoside Rg1 derivatives in treatment of Alzheimer's disease. According to the invention, ginsenoside Rg1 and polyethylene glycol with a specific chain length are covalently linked to successfully construct the derivative capable of enhancing the penetrating power of the blood-brain barrier. The series of derivatives provided by the invention not only solve the problems of poor brain targeting and insufficient stability of natural Rg1, but also can inhibit neuroinflammation by regulating and controlling an NLRP3 / caspase-1 signal channel in an LPS-induced neuroinflammation model, and finally, the learning and memory ability is remarkably improved. The product is simple and convenient in preparation process and good in biological safety, and a new candidate compound is provided for developing a new generation of Alzheimer disease treatment medicines.

The invention relates to equipment for preparing clobetasol propionate liniment and a preparation method of the clobetasol propionate liniment. The equipment comprises a material mixing mechanism, a barrel, a stirring shaft rotationally arranged on the barrel, stirring blades for stirring substances, a partition plate for separating the interior of the barrel, a crystallization rod for cooling materials and a drying mechanism for drying the substances. Wherein the stirring blades are fixedly arranged around the stirring shaft, and the stirring blades at the bottom are arranged around the stirring shaft in a swinging manner; the partition plate is movably arranged in the barrel around the stirring shaft; the crystallization rod is movably arranged at the bottom of the barrel; the drying mechanism communicates with the bottom of the barrel; the drying mechanism is communicated with the mixing mechanism; the partition plate is arranged between the fixed first ring frame and the rotary second ring frame; the partition plate is connected with the first ring frame and the second ring frame. The second ring frame rotates to drive the partition plate to open or separate the cylinder. The preparation method solves the problem that the preparation efficiency of clobetasol propionate is affected due to more preparation equipment caused by complex process steps in the clobetasol propionate liniment preparation process in the existing scheme.

The invention discloses a method for extracting ginsenoside based on a supercritical extraction method, and relates to the technical field of traditional Chinese medicine extraction. The ginsenoside is extracted through a supercritical extraction method, the extraction process is convenient and efficient, the purity of the ginsenoside is high, organic solvent residues are avoided, the method is green and environmentally friendly, carbon dioxide can be recycled, and the operation cost is low; through degreasing pretreatment, fat-soluble components in ginseng powder are removed, the extraction purity of saponin is increased, the solid loading capacity of supercritical extraction is reduced, the mass transfer resistance is reduced, and the extraction efficiency is improved; the ginsenoside is purified in a post-treatment mode of resin adsorption and elution, polar impurities can be further removed, glutamine is adopted for surface functionalization of the resin, acylamino and carboxyl are introduced to the surface of the resin and can form hydrogen bonds with phenolic hydroxyl groups in the ginsenoside, functional adsorption is achieved, meanwhile, impurities are removed, and the content of the ginsenoside is increased. Reaction conditions are simple and mild, and adsorption efficiency is high.

The invention discloses a method for extracting ecdysterone from cyanotis arachnoidea by using a deep-eutectic solvent, and belongs to the technical field of ecdysterone extraction. The method comprises the following steps: mixing a deep-eutectic solvent which takes choline chloride and a hydrogen bond donor material as raw materials with water, extracting ecdysterone in roots and stems of Cyanotis arachnoidea to obtain an ecdysterone crude extract, precipitating the ecdysterone crude extract by adding water, filtering, and adsorbing ecdysterone by using macroporous resin. Adding water for elution to obtain a deep-eutectic solvent-water mixed solution, and recovering under reduced pressure to obtain an extraction solvent for cyclic utilization; and eluting by using alcohol with different concentrations to obtain an ecdysterone crude extract, and purifying the crude extract to obtain high-purity ecdysterone. Compared with a conventional extraction method, the process method adopted by the invention has the advantages that the process is simple, efficient, green and environment-friendly, the used eutectic solvent can be recycled, the loss caused by heating volatilization in the extraction process is avoided, the ecdysterone extracted by the method is pure white, the content of ecdysterone can reach 90% or above after simple purification, and the method is suitable for industrial production. After re-purification, the purity of ecdysterone detected by high performance liquid chromatography is up to 98% or above.

The invention belongs to the technical field of organic synthesis, and particularly relates to an alkyl pentafluorosulfenyl compound and a preparation method and application thereof.The preparation method comprises the following steps that in the protective gas atmosphere, in a solvent, SF5Cl serves as a pentafluorosulfenyl source, an olefin compound serves as a reaction substrate and a free radical trapping agent, a thiol compound serves as a hydrogen source, and the alkyl pentafluorosulfenyl compound is obtained through a one-step reaction; under the action of an olefin additive, the alkyl pentafluorothio compound is constructed by a one-step method through a visible light-induced free radical process, and the olefin additive is used for inhibiting generation of a pentafluorothio chloride byproduct from a pentafluorothio source and an olefin compound. According to the method disclosed by the invention, a series of alkyl pentafluorosulfenyl compounds can be prepared by only needing olefin double bonds in substrates and selecting more substrates through the reaction, the reaction is simple, the reaction condition is mild, the reaction can be completed under visible light, the reaction time is short, the implementation is easy, and the method is suitable for industrial production. And a method support is provided for further screening the alkyl pentafluorosulfenyl compound with excellent biological activity.

The invention relates to a vitamin D3 and 7-dehydrocholesterol eutectic as well as a preparation method and application thereof. The eutectic is prepared from the following raw materials: vitamin D3 and 7-dehydrocholesterol in a molar ratio of (1-1.2): (1-1.2). The yield of the obtained eutectic substance is high, the preparation method is easy to operate, high-toxicity raw materials and waste residues difficult to treat do not exist, and the vitamin D3 eutectic method is more environmentally friendly and high in eutectic efficiency.

The invention relates to the technical field of pharmaceutical chemicals, in particular to a preparation method of 11beta, 17alpha-dyhydroxyl-6 alpha-methylpregna-4-ene-3, 20-diketone, and discloses a preparation method of 11beta, 17alpha-dyhydroxyl-6 alpha-methylpregna-4-ene-3, 20-diketone. The method comprises the following steps: S1, adding a 11beta, 17alpha-dyhydroxyl-6 alpha-methylpregna-4-ene-3, 20-diketone crude product into a mixed solution of a solvent A and a solvent B, heating to 25-35 DEG C, and stirring for dissolving until the solution is clear, so as to obtain a 11beta, 17alpha-dyhydroxyl-6 alpha-methylpregna-4-ene-3, 20-diketone crude product; s2, carrying out transposition elimination reaction; s3, carrying out acidification deprotection reaction; s4, adjusting the pH value; s5, standing and layering; s6, decoloring; s7, performing concentration; s8, cooling and crystallizing; s9, carrying out solid-liquid separation; and S10, carrying out vacuum drying, so as to obtain a finished product of the 11beta, 17alpha-dyhydroxyl-6 alpha-methyl pregna-4-ene-3, 20-diketone. The method has the characteristics of high yield and good product quality, is stable and is easy to realize industrial production.

The application relates to a preparation method of a fritillaria cirrhosa bulbus extract. Step one: drying and crushing fritillaria cirrhosa bulbus to obtain fritillaria cirrhosa bulbus powder, taking the fritillaria cirrhosa bulbus powder and a cyclodextrin powder to stir-fry a mixture one; step two: adopting ethanol normal-temperature reflux extraction on the mixture one to separate supernatant one and filter residue; step three: recovering and drying the filter residue in step two, taking the dried filter residue and the cyclodextrin powder to stir-fry a mixture two; step four: adopting ethanol and organic acid normal-temperature reflux extraction on the mixture two; step five: combining the supernatant one and supernatant two, adding into a macroporous adsorption resin impurity removal device, then adding ethanol into the macroporous adsorption resin impurity removal device until the eluent is colorless; concentrating and drying to obtain the fritillaria cirrhosa bulbus extract. The application can obviously improve the extraction efficiency of total alkaloids of fritillaria cirrhosa bulbus and has a good application prospect.

The invention belongs to the technical field of medical chemistry, and particularly relates to a targeted protein degradation compound containing an SYVN1 binding compound and application of the targeted protein degradation compound. According to the invention, a series of compounds interacting with SYVN1 are found, and the compounds can be used as'warheads' to participate in ERAD and effectively degrade transmembrane protein targets. Based on the SYVN1 binding compound, a new TPD technology for hijacking ERAD is established, and a brand new platform is provided for processing TMSPs and other proteins which are difficult to target by the current TPD technology. A SYVN1 interaction compound is further connected with a known ligand interacting with a protein target through a chemical linker, a series of ERADEC molecules are generated, the molecules can significantly degrade target protein, and a new possibility is provided for targeted degradation of drugs.

Disclosed is a class of antibody-hormone drug conjugates having novel structures, or pharmaceutically acceptable salts thereof. Specifically, provided are an antibody-drug conjugate having the general structural formula Ab-(L-D)n or a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition containing the conjugate, and a use thereof in the treatment of autoimmune diseases.

To provide an onium salt for use in a chemically amplified resist composition that exhibits high solvent solubility, high sensitivity, and high contrast in photolithography using high-energy radiation, while also offering superior lithography properties such as exposure latitude (EL) and line width roughness (LWR); a chemically amplified resist composition comprising the onium salt as a photoacid generator; and a pattern forming process using the chemically amplified resist composition.SOLUTION: The present invention provides an onium salt represented by formula (1).SELECTED DRAWING: None

The present invention relates to a saponin-based saponin derivative comprising a triterpene aglycone and a first and / or second sugar chain, the saponin derivative comprising: an aglycone core structure containing a derivatized aldehyde group; and / or the first sugar chain containing a derivatized carboxyl group; and / or the second sugar chain containing at least one derivatized acetoxy group. The present invention also relates to a first pharmaceutical composition comprising the saponin derivative of the present invention. In addition, the present invention relates to a pharmaceutical combination comprising the first pharmaceutical composition of the present invention and a second pharmaceutical composition comprising any one or more of an antibody-toxin conjugate, a receptor-ligand-toxin conjugate, an antibody-drug conjugate, a receptor-ligand-drug conjugate, an antibody-oligonucleotide conjugate, or a receptor-ligand-oligonucleotide conjugate. The present invention also relates to the first pharmaceutical composition or the pharmaceutical combination of the present invention for use as a medicament or in the treatment or prevention of cancer, an infectious disease, a viral infection, hypercholesterolemia, primary hyperoxaluria, hemophilia A, hemophilia B, alpha-1 antitrypsin-associated liver disease, acute hepatic porphyria, transthyretin-mediated amyloidosis, or an autoimmune disease. Furthermore, the present invention relates to an in vitro or ex vivo method for translocating a molecule from outside a cell into the cell, which method comprises contacting the cell with the molecule and with a saponin derivative of the present invention.

The invention belongs to the technical field of medical analysis, and particularly relates to a method for separating chemical components in hemsley rockvine root. According to the present invention, various chromatography methods are adopted to carry out separation and purification, such that sitroside (I), vanillyl glycolII (II), 5-hydroxymaltol (III), vanillic acid (IV), afzelin (V), 2, 3-dihydroxypyrazole (9E, 11E)-13-hydroxypyrazole (9, 11-dienoate), and 2, 3-dihydroxypyrazole (10E, 12E)-9-hydroxypyrazole (10, 12-dienoate) are obtained from hemsley rockvine root. Wherein the compounds II, III, VI and VII are separated from the hemsley rockvine root for the first time, and development and quality control of the hemsley rockvine root medicinal material are facilitated.

To provide antisense oligonucleotide sequences and methods of using the same for treating neurological diseases.SOLUTION: Provided is an oligonucleotide comprising linked nucleosides having a sequence of at least 19 contiguous nucleobases, wherein the sequence of nucleobases comprises a portion of at least 10 contiguous nucleobases that is at least 90% complementary to an equal length portion of nucleobases contained at a specified position of a specified sequence.SELECTED DRAWING: Figure 1A

The invention discloses a derivative of a rice bran extract as well as a preparation method and application of the derivative. A C-3 benzoate prodrug system is constructed, the transmembrane absorption efficiency is remarkably improved by optimizing the oil-water partition coefficient, fixed-point slow release of active ingredients is achieved through inflammatory tissue esterase, and high bioavailability and low irritation are both considered. Meanwhile, C-25 fluorine atoms are introduced to serve as biological electron isosteres, and target affinity is enhanced by means of the unique electronic effect and polar hydrophobicity of the C-25 fluorine atoms; spatial conformation is locked through side chain saturation, so that the compound shows anti-inflammatory and tissue repair activity which is obviously superior to that of natural cycloartanol under the same dosage.

Potent soft corticosteroid pharmaceutical compositions comprising them and method for use as anti-inflammatory agents. Also, a method for softening fluticasone propionate and similar corticosteroids to arrive at potent but safer alternatives. The compound S-fluoromethyl 17α-dichloroacetoxy-6α,9α-difluoro-11β-hydroxy-16a- methyl-3-oxoandrosta-1,4-diene-17β-carbothioate, which is equally potent to but safer than fluticasone, is among those provided. Another compound of particular interest is 2-hydroxyethyl 17α-dichloroacetoxy-6α,9α-difluoro-11β-hydroxy-16β- methyl-3-oxoandrosta-1,4-diene-17β-carboxylate.

To provide a process for forming drug crystals of narrow size distribution and desire dimensions and morphology.SOLUTION: The present invention relates to a process for providing corticosteroid crystals of desired size distribution and morphology, the process comprising the steps of: providing recrystallized ultra-large columnar crystals having aspect ratios of more than 1 and less than 20, the aspect ratio of a given columnar crystal being the ratio of a longest dimension along a lengthwise axis relative to a shortest dimension of a transverse plane perpendicular to the lengthwise axis; and sizing the recrystallized ultra-large columnar crystals to provide a collection of sized crystals having target dimensions, wherein the sizing includes segmenting at least a part of the recrystallized ultra-large columnar crystals along the respective lengthwise axes while retaining the dimensions of the transverse plane perpendicular to the lengthwise axis.SELECTED DRAWING: None

The invention discloses a multifunctional water-soluble fertilizer containing S-propionyl lactone and a wetting penetrant and a preparation method of the multifunctional water-soluble fertilizer, and relates to the technical field of agricultural fertilizers. The invention relates to a multifunctional water-soluble fertilizer containing S-propionyl brassinolide and a wetting penetrant. The multifunctional water-soluble fertilizer is prepared from the following components in parts by mass: 0.01 to 0.05 part of S-propionyl brassinolide, 0.5 to 3 parts of wetting penetrant, 30 to 35 parts of macroelement fertilizer, 1 to 5 parts of medium element fertilizer, 0.05 to 0.1 part of microelement fertilizer, 5 to 10 parts of dispersing agent, 0.5 to 1 part of antioxidant and 40 to 50 parts of water. Through the synergistic effect of the S-propionyl lactone and the wetting penetrant, the resistance of plants to diseases is enhanced, the disease infection rate is reduced, and the overall health level of the plants is improved. The special antioxidant is adopted, and the optimized preparation process is matched, so that the fertilizer is not easy to precipitate, layer and the like in the storage process, and the long-term stability of the fertilizer is ensured.

The application provides a method for synthesizing an eplerenone intermediate N-1 by one-pot method, and belongs to the technical field of organic synthesis. The method is characterized in that: the eplerenone intermediate N-4 is dissolved in dichloromethane, a potassium carbonate aqueous solution and dibromohydantoin are added to perform an opening ring reaction; after the reaction is completed, hydrochloric acid is directly added to perform a rearrangement reaction; then water is separated and methanol is added in the organic layer to perform an ozonation reaction; then sodium sulfite is added to perform a reduction reaction; then hydrochloric acid is added to perform a methyl esterification reaction, so as to obtain the eplerenone intermediate N-1 crude product, and finally the eplerenone intermediate N-1 fine product is obtained through refining. The method realizes the one-pot synthesis of the eplerenone intermediate N-1 from the eplerenone intermediate N-4 through the continuous reactions of opening ring, rearrangement, ozonation, reduction and methyl esterification, and can avoid column chromatography purification, so that the method becomes a green chemical process route with greatly reduced organic solvent consumption and wastewater.

The present application relates to the technical field of microbial medicine, and particularly to a preparation method and application of indole diterpenoid compounds. Specifically, the extract of plant endophytic fungus F4a after solid fermentation culture is separated and purified to obtain indole diterpenoid compounds; the plant endophytic fungus F4a is a strain with the preservation number CCTCC NO: M 2012531. The indole diterpenoid compounds provided by the present application have significant antifeedant, insecticidal and hypotensive activities, and they can be used as ideal candidate compounds of antifeedants, insecticides or hypoglycemic drugs. The compounds can be produced through fungal fermentation, and the preparation method is simple, efficient and high in product purity. The present application has good application prospect.

The application belongs to the technical field of organic synthesis, and particularly relates to a preparation method of alpha soludex. The preparation method takes 11-ketoprogesterone as raw material, firstly acetylates the ketone group at the 3 position, then obtains 3beta-hydroxyl through a composite biological enzyme method, and finally obtains alpha soludex through hydrogenation and translocation reaction. The composite biological enzyme method is used to obtain 3beta-hydroxyl, has good specificity, mild reaction conditions, does not need special equipment, and has high conversion efficiency. The preparation method of the application is easy to purify the reaction products of each step, the total mass yield of the final alpha soludex product is greater than 85%, and the HPLC purity is greater than 99.5%. The preparation method of the application has low cost and is suitable for industrial large-scale production.

The invention provides a steroid hormone double-bond selective hydrogenation catalyst as well as a preparation process and application thereof, and belongs to the technical field of catalysts. The preparation process of the hydrogenation catalyst comprises the following steps: (1) preparing a carrier loaded with an active metal: dispersing the carrier in a cerium-containing metal salt ethanol solution, stirring, and carrying out suction filtration, drying and temperature programming roasting after stirring to prepare the carrier loaded with the active metal; (2) loading a bimetal carrier: dipping the active metal-loaded carrier in the precursor solution, carrying out ultrasonic-assisted dipping, and then dropwise adding an alkali solution to adjust the pH value of the solution so as to obtain a bimetal-loaded carrier solution; and (3) reduction: slowly dropwise adding a reducing agent solution into the solution, and after reduction is completed, separating, washing and carrying out vacuum drying to obtain the catalyst. The preparation process is green and safe, and the prepared catalyst can be used for selective hydrogenation reaction of steroid hormone double bonds and has relatively high selectivity and conversion rate.

The invention belongs to the field of radioactive chemical synthesis, and particularly relates to carbon-14 labeled tetrahydroprogesterone as well as a preparation method and application thereof. The carbon-14 labeled tetrahydroprogesterone provided by the invention has a structure as shown in a formula I; the carbon-14 labeled tetrahydroprogesterone provided by the invention has the advantages that the labeled sites are determined, the radiochemical purity and the chemical purity are relatively high, the nuclide carbon-14 is firmly labeled in tetrahydroprogesterone molecules and is not easy to fall off, and the requirements of tracer experiments in pharmacokinetics can be met.

The invention provides a green synthesis method of a benzocyclic ketone compound, which comprises the following steps: mixing a compound with a structure shown as a formula (I), a compound with a structure shown as a formula (II), a catalyst, alkali and a solvent, and reacting under a blue light shining condition to obtain a compound with a structure shown as a formula (III), namely the benzocyclic ketone compound. Experiments show that the method provided by the invention can construct the benzocyclic ketone compound through a one-step reaction, is wide in substrate adaptability and mild in reaction condition, and has good application prospects and research values for synthesis of benzocyclic ketone compound derivatives.