1209results about "Steroids" patented technology

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 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 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 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 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.

This invention relates to the field of biotechnology, and more particularly to a swelling-promoting seahorse oil and its application in the preparation of anti-sarcopenia products. Obtained using a supercritical carbon dioxide extraction process, the swelling-promoting seahorse oil of this invention has been experimentally verified to inhibit muscle degradation, promote muscle cell activation and differentiation, increase muscle mass, and enhance muscle strength and endurance. Furthermore, it exerts its effects through dietary supplementation with no significant adverse reactions, and can be used to prepare anti-sarcopenia related foods, health products, or pharmaceuticals to meet the muscle health maintenance needs of the elderly.

The present disclosure provides compounds containing modified saponin compounds, pharmaceutical compositions containing modified saponin compounds, methods of using modified saponin compounds and pharmaceutical compositions, and methods of manufacturing modified saponin compounds. The compounds and pharmaceutical compositions of the present disclosure can be used in combination with one or more other therapeutic agents for treating viral infections and other diseases.

Provided herein are 19-nor C3, 3-disubstituted steroids of Formula (I); and pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined herein, and A is a heteroaryl ring system comprising 3 or 4 nitrogens as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, and tinnitus.

This invention belongs to the field of organic synthesis technology, specifically relating to 1,4-silicon-nitrogen heterocyclic compounds, their synthesis methods, and applications. The synthesis method includes the following steps: using diethyleneamine and disiloxane as substrates and B(C6F5)3 as catalyst, the 1,4-silicon-nitrogen heterocyclic compound is synthesized in solvent one. The reaction formula is as follows: The synthesis method of this invention has advantages over existing technologies, such as safety and environmental friendliness, wide substrate adaptability, low reaction temperature, short reaction time, high yield, fewer by-products, and fewer reaction reagents.

The invention discloses a preparation method of fluorohydrocortisone acetate, and belongs to the technical field of medicine synthesis. According to the method, the fluorine hydrocortisone acetate is obtained through one-step reaction by taking the Anecortisone acetate as an initial raw material and taking a mixture of an organic solvent and water as a solvent under the condition of a Fe (III) reagent and a fluorine reagent. The preparation method disclosed by the invention is simple and convenient to operate, high in safety, mild in reaction condition, low in cost, high in yield, small in corrosivity and suitable for industrial mass production; meanwhile, the problems that in the prior art, operation is inconvenient, corrosivity is high, toxicity is large, dangerousness is high, the requirement for equipment is high, and the yield is low are solved, and a new technical scheme more suitable for industrial production is provided.

We provide lipid prodrugs of neurosteroids. [Solution] The present invention provides lymphoid-directed lipid prodrugs, their pharmaceutically acceptable compositions, methods for producing such prodrugs and compositions, and methods for improving the bioavailability or other properties of therapeutic agents comprising a portion of a lipid prodrug. The present invention also provides methods for treating diseases, disorders, or pathological conditions, the methods comprising administering the disclosed lipid prodrug or its pharmaceutically acceptable composition to a patient in need thereof.

The application discloses a method for extracting soybean saponins and soybean oligosaccharides, and belongs to the technical field of natural product extraction. The method comprises the following steps: puffing treatment of soybean meal, wall breaking treatment in a high-voltage electric field; acid precipitation, collection of supernatant; after ultrasonic oscillation of the supernatant, a composite enzyme is added for enzymolysis, and a material liquid after enzymolysis is obtained; after filtration of the material liquid, the material liquid is loaded onto a macroporous resin column for adsorption, and after completion of the adsorption, effluent is collected; the effluent is purified and concentrated to obtain soybean oligosaccharides; an ethanol solution is used to elute the resin column, and eluate is collected; the eluate is recovered by ethanol and dried to obtain soybean saponins; the composite enzyme comprises amylase and beta-glucosidase. The method can significantly improve the extraction rate and purity of soybean saponins and soybean oligosaccharides, the whole process uses water as the main solvent, the consumption of organic solvents and the pollution to the environment are reduced, and the unit process water consumption, unit energy consumption and unit cost are reduced.