3948results about "Steroids" patented technology

The invention discloses a compound with anti-tumor activity. The compound has a chemical structural formula as shown in a formula (I). The compound belongs to a novel tetracyclic triterpenoid natural product, has good fat solubility and chemical stability, and can be conveniently extracted from the rhizome of a herbal medicine Polygala fallax Hemsl. And prepared into an oral or injection form. The invention also provides a preparation method and application of the compound. The compound provided by the invention can obviously inhibit the growth of mouse lung cancer and reduce the volume and weight of tumor, and can be used for treating tumor diseases.

The invention relates to a decarboxylation coupling method catalyzed by N-heterocyclic carbene. Small organic molecule N-heterocyclic carbene is used as an organic catalyst, manganese is used as a reducing agent, aromatic acid or derivatives thereof and an electrophilic reagent are subjected to cross coupling, and multi-structure ketone is prepared. Small organic molecule N-heterocyclic carbene is used as an organic catalyst, manganese is combined as a reducing agent, cross coupling of aromatic acid or derivatives thereof and some cheap and easily available electrophilic reagents can be promoted, ketones with various structures can be provided at high yield, and the method is especially suitable for preparation of high-steric-hindrance ketone compounds and has wide application prospects. The method has the advantages of high yield, convenience in separation, high efficiency, mildness, low-cost economy and high industrial application value, and the requirement on transition metal catalysis can be reduced.

The present application provides compounds that are proteolysis targeting chimeras containing a celastrol-based ubiquitin ligase targeting moiety. Methods of using these compounds for treating various diseases, such as neurodegenerative diseases and cancer, are also provided.

The invention provides a method for synchronously extracting tea seed oil and tea saponin from tea seeds, and belongs to the technical field of active substance extraction. According to the method, the extraction rate and the purity are remarkably improved by finely regulating and controlling the extraction conditions. The specific composite oil extraction auxiliary agent and the ultrasonic-assisted extraction technology are adopted, and the power, time and solvent ratio are optimized, so that the extraction efficiency and the product quality of the tea seed oil and the tea saponin are superior to those of the tea seed oil and the tea saponin prepared by a traditional method. Experimental data prove that the extraction rate of the tea seed oil reaches 27.22%, and the purity of the tea seed oil reaches 99.66%; the extraction rate of the tea saponin is 21.85%, and the purity of the tea saponin reaches 96.50%. By increasing the utilization rate of the raw materials and reducing the production cost, the market competitiveness of the product is improved, the high-quality tea seed oil and tea saponin meet the requirements of the market for natural products, and the tea seed oil and tea saponin have wide application prospects.

25HC3S choline and crystalline 25HC3S choline are described herein. Pharmaceutical formulations of 25HC3S choline such as with crystalline 25HC3S choline and methods of treating or preventing disease with same such as hypercholesterolemia, hypertriglyceridemia, and conditions related to fat accumulation and inflammation (e.g., non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), alcoholic hepatitis, acute kidney injury (AKI), psoriasis, and atherosclerosis) are further disclosed herein. Methods for preparing 25HC3S, including crystalline 25HC3S choline, are also provided.

The invention discloses a steroid compound as well as a preparation method and application thereof. The invention specifically discloses a steroid compound with a structure as shown in a formula I and the like or a pharmaceutically acceptable salt of the steroid compound. The compound provided by the invention has SREBP pathway inhibitory activity, and can be used for preventing and / or treating obesity, hyperlipidemia, fatty liver, diabetes, atherosclerosis, cardiovascular and cerebrovascular diseases, liver cancer, skin injury and other diseases. # imgabs0 #

To provide a method for producing an oleanolic acid-containing extract which enables easy production of an oleanolic acid-containing extract from grape pomace without the need of using high-concentration organic solvents.SOLUTION: This method includes: a first step of preparing a mixed solution containing a natural deep eutectic solvent with sugar beet-derived betaine as the hydrogen bond acceptor and grape pomace; and a second step of deriving an extract containing an oleanolic acid from the mixed solution prepared in the first step.SELECTED DRAWING: None

The invention provides heterobifunctional compounds comprising an effector protein binding moiety selected from mTor, PLK1, CDKI, CDK2, CDK9, BRD4, AURKA, AURKB, MEK, Src, c-KIT, KIF11, HSP90, tubulin, proteasome, topoisomerase or HD AC which is linked to a moiety that binds to a target protein selected from KRAS, HER2 or EGFR. Pharmaceutical compositions and their use in treating disease, such as cancer, are also disclosed.

The invention provides a crystal form of a neuroactive steroid derivative and application thereof, and belongs to the technical field of medicines. The crystal form of the neuroactive steroid derivative (with the structure as shown in the formula I) provided by the invention is radiated by Cu-K alpha, and characteristic diffraction peaks of an X-ray powder diffraction pattern expressed by a 2 theta angle comprise 11.450 + / -0.200 degrees, 15.724 + / -0.200 degrees, 19.040 + / -0.200 degrees, 22.955 + / -0.200 degrees and 24.975 + / -0.200 degrees. The crystal form provided by the invention has the advantages of good fluidity, no electrostatic phenomenon, high stability and almost no hygroscopicity, and can stably exist under the conditions of high temperature, high humidity and illumination; the compound has a relatively strong positive regulation effect on a GABAA receptor, has relatively good pharmacokinetic properties and oral absorption rate, and can be applied to preparation of oral and other dosage form medicines for efficiently resisting diseases such as postpartum depression. # imgabs0 #

The invention relates to a ligand-effector moiety provided with at least one saponin and antibody-effector moiety provided with at least one saponin. An aspect of the invention is a composition comprising the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention. The invention also relates to an antibody-drug conjugate comprising covalently linked saponin and to an antibody-oligonucleotide conjugate comprising covalently linked saponin. An aspect of the invention relates to a pharmaceutical composition comprising the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention, and optionally further comprising a pharmaceutically acceptable excipient. The invention also relates to the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin, for use as a medicament. The invention also relates to the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention for use in the treatment or prophylaxis of a cancer.

This invention relates to a crystalline 19-nor C3,3-disubstituted C21-pyrazolyl steroid of Formula (I),and compositions thereof. Also disclosed herein are methods of making the same and methods of using the same.

The present invention relates to the electrochemical oxidation of allylic C- H bonds in specific compounds to obtain specific α,β unsaturated ketones in the presence of t-butyl hydroperoxide. This process is particularly suitable for the electrochemical oxidation of cholesterol, stigmasterol, campesterol, β-sitosterol, brassicasterol, 25-hydroxycholesterol, 24-hydroxycholesterol, lanosterol, pregnenolone, and the esters thereof.

The invention discloses a synthesis method of 7-dehydrocholesterol and derivatives thereof, which comprises the following steps: cooling a compound (I), cuprous bromide and dimethyl sulfide compound under the protection of inert gas to obtain a reaction system, adding a Grignard reagent (II) or a Grignard reagent (III), stirring, reacting at room temperature, carrying out heating reaction, and cooling to obtain the 7-dehydrocholesterol. Performing post-treatment to obtain a product; if the product is the Grignard reagent (II), the product is 7-dehydrocholesterol and the derivative thereof; if the reagent is the Grignard reagent (III), the product is 25-hydroxy-7-dehydrocholesterol and the derivative thereof. The method is high in total yield, mild in reaction condition, simple in process route, high in product purity, low in three-waste generation amount, simple in post-treatment, environment-friendly and low in equipment requirement, the purity of 95% or above can be obtained through simple recrystallization, and conventional chemical equipment can be used for production.

The invention provides a culture method for improving immunity of fishes. The culture method comprises the following steps: S1, selection of culture points; S2, specification and layout of net cages; S3, selection and throwing of fish fries; according to the fry disinfection method disclosed by the invention, the fry are soaked and disinfected by using a compound disinfectant prepared from povidone iodine, polysorbate, citric acid and vitamin C in a specific proportion, so that pathogenic microorganisms on the surfaces and gill parts of fish bodies are effectively killed. According to the breeding management, the immunity of the fish body is comprehensively enhanced by feeding the fish with an immune conditioner composed of campesterol palmitate, immunomodulatory peptide, beta-glucan and astaxanthin in a specific proportion. According to the bottom mud management, the content of harmful substances is reduced by putting a bottom mud modifier composed of sodium molybdate, nitrifying bacteria, photosynthetic bacteria, tetrandrine and sodium alginate in a specific proportion, growth of pathogenic bacteria is inhibited, nutrient substance circulation is promoted, the water quality environment is optimized, and healthy growth of fry is promoted.

The present application provides a variety of salts of 25HC3S, including crystalline salts of 25HC3S. Provided herein are pharmaceutical formulations of the salts of the invention, and methods of treating or preventing diseases therewith, the diseases such as non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), alcoholic hepatitis, acute kidney injury (AKI), psoriasis, atherosclerosis, hypercholesterolemia, hypertriglyceridemia, alcoholic fatty liver disease (AFLD), alcoholic steatohepatitis (ASH), leptin resistance, leptin deficiency, diabetic conditions, autoimmune conditions, inflammatory conditions, and the like. Nervous system disorders, EB virus related growth, and disorders associated with fat accumulation and inflammation. Methods of making the salts of the present application are also provided.

The invention provides a co-amorphous substance co-loaded with trilobatin and glycyrrhizic acid as natural sweeteners, which does not need to add any auxiliary materials, does not relate to special processes and equipment, and is simple, convenient and efficient in preparation method, easy to industrialize and low in cost. According to the double-drug-loading co-amorphous substance prepared by the invention, the water solubility of the two components can be remarkably improved at the same time, the sweetness of the double-drug-loading co-amorphous substance is superior to that of the original components, and the double-drug-loading co-amorphous substance can be used for improving the solubility of other insoluble components; the compound can be used as a multifunctional flavoring agent and has a wide application prospect.

The invention discloses a compound derivative represented by a formula I or an isotope labeled compound thereof, or an optical isomer, a geometric isomer, a tautomer or an isomer mixture thereof, or a pharmaceutically acceptable salt thereof. According to the application of a double protection strategy, diversified carrier fragments are introduced to 5-hydroxyl and hydroxylamine in N4-hydroxycytidine molecules, the N4-hydroxycytidine prodrug is invented, the affinity of lung cell membranes (phospholipid membranes) is improved, and the physicochemical properties of the drug are made to meet the requirements of the physiological environment of lung tissue. Therefore, the compound disclosed by the invention has a wide application prospect in the aspect of broad-spectrum respiratory virus resistance. # imgabs0 #

The invention discloses a preparation method of epiandrosterone, which comprises the following step: in a closed reactor and in a hydrogen atmosphere, reacting a mixture containing dehydroepiandrosterone, a catalyst and a solvent to obtain the epiandrosterone. The method for preparing the Pd-based catalyst comprises the following steps: soaking the carrier in an alkaline solution of which the pH value is adjusted to 8-9, stirring for a certain time, carrying out suction filtration after stirring, and drying in a drying oven. Stirring for a period of time, dispersing the carrier in ultrapure water, slowly dropwise adding a mixed solution of a precursor and auxiliary metal ions, stirring for a certain period of time, carrying out suction filtration on the catalyst, drying in a drying oven, and reducing palladium metal; and washing the catalyst after reduction, and drying in a drying oven for a certain time to obtain the catalyst. The catalyst disclosed by the invention is used for preparing epiandrosterone, the conversion rate of a dehydroepiandrosterone raw material is greater than 99.9%, the selectivity of a target product epiandrosterone is greater than 96%, and the selectivity of a byproduct dienedione is less than 4%.

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 preparation method of tanshinone, salvianolic acid and a salvia miltiorrhiza extract, which comprises the following steps: performing percolation extraction on crushed salvia miltiorrhiza by using an ethanol solution, and collecting percolate; recovering ethanol from the percolate, precipitating and carrying out solid-liquid separation to obtain a water solution and a precipitate, adding a solid dispersant into the precipitate, crushing, and extracting with ethanol to obtain a tanshinone ethanol solution; recovering and concentrating the water solution, adjusting the pH value to be greater than 1 and less than 3 under stirring, carrying out alcohol precipitation to remove impurities, and collecting the supernatant to obtain a salvianolic acid ethanol solution; or adjusting the pH value of the water solution to be greater than 2 and less than 4, then recovering, concentrating, carrying out alcohol precipitation to remove impurities, and collecting the supernate to obtain the salvianolic acid ethanol solution; salvianolic acid ethanol liquid and tanshinone ethanol liquid are respectively used for preparing tanshinone and salvianolic acid or preparing a radix salviae miltiorrhizae extract containing tanshinone and salvianolic acid. The method is simple to operate, free of special equipment, high in production efficiency and low in cost; the yield of the salvianolic acid extract is about 12%, the content of salvianolic acid B is about 30%, and the extraction transfer rate is greater than 80%.

Disclosed are a steroid compound having a structure represented by formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a use thereof. The compound has SREBP pathway inhibitory activity, and can be used for preventing and / or treating diseases such as obesity, hyperlipidemia, fatty liver, diabetes, atherosclerosis, cardiovascular and cerebrovascular diseases, liver cancer, and skin injury.

Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6 and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and / or anesthesia.

The invention discloses a limonin compound and application thereof in preparation of a medicine for preventing and / or treating cancers. The structure of the limonin compound is shown as a formula I or II. The cancer is at least one of breast cancer, liver cancer, gastric cancer, esophageal cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, prostatic cancer, nasopharynx cancer, cervical cancer, ovarian cancer, kidney cancer and skin cancer. According to the invention, activity screening is carried out on various natural product extracts, it is found for the first time that limonin compounds with structural formulas I and II have excellent inhibitory activity on various different types of human cancer cells, and an optional scheme is provided for broad-spectrum anti-cancer drugs. Related results also show that the compound provided by the invention can inhibit migration and invasion ability of breast cancer cells, promote cell apoptosis and retard a cell cycle. The limonin compound applied in the invention is derived from mallotus oblongifolius, the source is wide, and the production cost is low.

The invention discloses a ginsenoside hydrogen sulfide donor derivative as well as a preparation method and application thereof, and belongs to the technical field of natural medicines and medicinal chemistry. According to the invention, a series of ginsengenin hydrogen sulfide donor derivatives are designed and synthesized by taking ginsengenin as a lead compound, and the myocardial protection activity of the synthesized derivatives is tested; results show that the ginsenoside hydrogen sulfide donor derivative prepared by the invention has relatively good heart protection activity for treating myocardial ischemia, arrhythmia and myocardial infarction, and has the potential of serving as a heart protection medicine.

The invention discloses a ganoderma lucidum extraction method based on a reusable magnetic enzyme. The ganoderma lucidum extraction method comprises the following steps: S1, preparing a nanoscale amination modified Fe3O4-SiO2 magnetic composite carrier; s2, on the basis of the amination modified Fe3O4-SiO2 magnetic composite carrier, cellulase is added, and a magnetic immobilized enzyme buffer solution is obtained; s3, the ganoderma lucidum sporocarp is put into a magnetic immobilized enzyme buffer solution to be subjected to enzymolysis, extraction and filtration, effective components of ganoderma lucidum are obtained, and magnetic immobilized enzyme is recycled for repeated utilization; according to the method, the magnetic nanoparticles are modified, so that the surfaces of the magnetic nanoparticles have specific active groups, meanwhile, the magnetic response advantage of an inorganic magnetic material is reserved, the nanoscale amination-modified Fe3O4-SiO2 magnetic composite carrier is prepared, enzyme molecules can be directly anchored on the surfaces of the magnetic nanoparticles, and enzyme activity is improved. The immobilized enzyme can be conveniently recycled from a reaction system, so that the cost of an enzyme preparation can be reduced, and the enzyme activity stability can be improved.

The invention discloses a preparation method of 1alpha-hydroxyl dinorhydrin, the structural formula of the 1alpha-hydroxyl dinorhydrin is shown as a formula (1), the method comprises the following steps: by taking dinorhydrin shown as a formula (2) as a raw material, preparing the 1alpha-hydroxyl dinorhydrin through five steps of acylation, bromination, debromination, epoxidation / hydrolysis and ring opening, and the reaction formula is as follows: # imgabs0 #. All reactions are carried out under normal pressure, reagents with high toxicity are not used in the reaction process, the reaction yield is high, the total yield of the five-step reaction can reach 48.46%, and the method is suitable for industrial production.

The invention discloses a method for preparing plant-derived cholesterol through chemical catalysis, which is characterized in that plant-derived BA is used as a raw material, chemical catalytic reduction is carried out through an intermediate compound 3, compared with an enzyme method, a large number of proper enzymes do not need to be screened, the cost is low, the stability is good, in addition, the influence of reaction sites on the Grignard addition yield is avoided through hydroxyl protection, and the yield of the plant-derived cholesterol is improved. Finished product isomer impurities can be reduced, the product yield is improved, and purification treatment is facilitated. The whole preparation route does not need an expensive catalyst, the reaction condition is mild, the specificity is high, the high-purity cholesterol can be obtained only through simple aftertreatment in each step, the method is suitable for industrial production, and the quality can meet the standards of medical injection and pharmaceutic adjuvants.

A steroidal compound and its conjugate, specifically the compound and its conjugate or its tautomer, mesomer, racemate, enantiomer, diastereoisomer, or mixture thereof, or its pharmaceutically acceptable salt; and the preparation method and application of the compound and its conjugate.