25 results about "Androstane" patented technology

The invention provides a method for identifying crude oil types based on comprehensive two-dimensional gas chromatography-time-of-flight mass spectrometry, which comprises the following steps: dissolving a crude oil sample to be identified by using a diluent, and adding a 5alpha-androstane standard substance into the system to obtain a crude oil sample; the method comprises the following steps: carrying out chromatographic analysis on a crude oil sample by using comprehensive two-dimensional gas chromatography-time-of-flight mass spectrometry, and marking the ratio of the weight sum of n-alkane, isoparaffin, monocycloalkane, bicycloalkane, tricycloalkane, tetracycloalkane and pentacycloalkane in the crude oil sample to the weight of the crude oil sample to be identified as S; marking the ratio of the weight sum of monocycloalkane, bicycloalkane, tricycloalkane, tetracycloalkane and pentacycloalkane in the crude oil sample to the weight of the crude oil sample to be identified as N, and identifying the type of the crude oil sample according to the ratio of S to N. The identification method provided by the invention provides a new way for finely identifying the naphthenic crude oil and estimating the reserves of the naphthenic crude oil.

The invention relates to a rigid spiro compound and a preparation method and application thereof.The preparation method comprises the steps that 6-methylene-androstane-4-ene-3, 17-diketone (V) is dissolved in a mixed solution of dichloromethane and trifluoroacetic acid, reaction and reduced pressure distillation are conducted at the temperature of 20-25 DEG C, then extraction washing and distillation are conducted, a rigid spiro compound crude product can be obtained, and the rigid spiro compound is obtained. The crude product can be subjected to column chromatography separation and purification to obtain a refined rigid spiro compound (I). By adopting the preparation method, the friction and wear properties of the base oil are remarkably improved, and the base oil has lower friction coefficient and wear scar diameter, and has good application prospect as an antifriction and wear-resistant additive.

The invention discloses a 3-ketosteroid-delta1-dehydrogenase mutant and application of the 3-ketosteroid-delta1-dehydrogenase mutant in catalyzing dehydrogenation of a steroid compound, the mutant with high catalytic activity is obtained through screening, and the solubility of a substrate is increased by adding a cosolvent Tween-80, so that the biological catalytic efficiency is improved. Under the optimal condition, the mutant disclosed by the invention can improve the feeding amount conversion rate of 15g / L of (16 alpha)-methyl androstane-4, 9-diene-3, 17-diketone to 99.9%.

The invention discloses a negative ion metabolism marker for thyroid-associated ophthalmopathy, a product and application of the negative ion metabolism marker. The metabolic marker is prepared from any one or more of 7alpha, 17alpha-dimethyl-5beta-androstane-3 alpha, 17beta-diol, N, N-dimethyl phosphatidyl ethanolamine, 15 (S)-hydroxy eicosatrienoic acid and 1-myristoyl-2-[(9Z)-octadecenoyl]-sn-glycerol-3-phosphatidylcholine, and the metabolic marker is prepared from any one or more of the following raw materials: 1-myristoyl-2-[(9Z)-octadecenoyl]-sn-glycerol-3-phosphatidylcholine. The invention provides a kit which comprises a detection reagent for detecting the negative ion metabolism marker. The invention provides a computer program product for thyroid-related eye diseases. The product provided by the invention has good feasibility and accuracy, can effectively evaluate the risk of thyroid-related eye diseases, and provides a new tool for clinical diagnosis.

The invention relates to the technical field of organic synthesis of steroid compounds, in particular to a preparation method of androstane-4-ene-3, 6, 17-triketone. Dehydroepiandrosterone acetate is used as an initial raw material to prepare androstane-4-ene-3, 6, 17-triketone through four steps of reactions including chlorohydrination, hydrolysis, oxidation and elimination, the yield and purity of androstane-4-ene-3, 6, 17-triketone are improved, 4-AD impurities are not generated, the total yield of a route reaches 80%, and the purity is larger than or equal to 98.0%; and the preparation process does not involve the use of dangerous chemicals and environment-polluting chromium oxidants, and is suitable for industrial production.

Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na+ / K+ ATPase. In general, the disclosed compounds are derivatives of androstane having the formula (I). Also disclosed herein are pharmaceutical compositions comprising one or more of the compounds of formula (I) for use for the treatment of heart failure.

Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na+ / K+ ATPase. In general, the disclosed compounds are derivatives of androstane having the formula (I)Also disclosed herein are pharmaceutical compositions comprising one or more of the compounds of formula (I) for use for the treatment of heart failure.

The invention relates to the technical field of biological medicines, in particular to a preparation method of an intermediate androstane-17alpha-methyl-17beta-hydroxy-3-ketone of steanoconazole, and belongs to the technical field of biological medicines. The method comprises the following steps: by taking 4-androstenedione as a raw material and p-toluenesulfonic acid as a catalyst, carrying out 3-position ketene etherification protection on the 4-androstenedione and triethyl orthoformate to obtain a compound shown in a formula III; then carrying out Grignard addition on the compound shown in the formula IV and methyl magnesium bromide and carrying out in-situ silyl ether protection to obtain a compound shown in the formula IV; carrying out normal-pressure hydrogenation to obtain a compound as shown in a formula V; and carrying out acid hydrolysis, neutralization, devitrification and recrystallization through a one-pot method to obtain a high-purity target product shown in the formula I. The method is characterized in that the problems of unstable key intermediate, complex process, low yield and the like are successfully solved through in-situ silyl ether protection and one-pot method operation, and the method has the outstanding advantages of short route, safety in operation, high yield, good product purity and suitability for industrial production.

The invention discloses a synthesis method of 5 [alpha]-androstane-2-ene-17-ketone. The 5 [alpha]-androstane-2-ene-17-ketone is used as a The invention provides a preparation method of 5 alpha-androstane-2-ene-17-ketone as shown in a formula I. The preparation method is characterized by comprising the following step: in a solvent, in the presence of proton base, triphenylphosphine and dimethyl azodicarboxylate (DEAD), epiandrosterone is subjected to an elimination reaction, and the 5 alpha-androstane-2-ene-17-ketone as shown in the formula I is obtained. The isomer produced by the preparation method provided by the invention is few in impurities, simple in post-treatment, low in price, mild in reaction condition and less in environmental damage, and the preparation method can be used for industrial production, and the used raw materials are bulk commodities. # imgabs0 #

Provided are androstane and dihydrotestosterone compounds functionalized with carbocyclic groups or heterocyclic groups that may be saturated or unsaturated. The compounds may be used in methods of inhibiting cell growth of malignant cells and / or hyperplastic cells and / or treating individuals having diseases associated with malignant cell growth (e.g., cancer, such as, for example, prostate cancer) and / or hyperplastic cell growth and / or molecular imaging of malignant cells and / or hyperplastic cells and / or inducing degradation of a target protein. Also provided are compositions.

The invention discloses a preparation method of a steroid compound 4, 5-position epoxy compound, and relates to the technical field of organic matter synthesis methods, 17beta-hydroxy-2, 4-ene-androstane [2, 3-d] isoxazole, a medium polar solvent, hydrogen peroxide and an anhydride reagent are used as raw materials for reaction, then alcohol recrystallization is carried out, and the compound 4, 5-position epoxy compound is obtained. Finally, a target product, namely the 4 alpha, 5 alpha-epoxy-17 beta-hydroxyl-2-ene-androstane [2, 3-d] isoxazole, is obtained. The medium polar solvent comprises dichloromethane and chloroform; the anhydride reagents are acetic anhydride and acetic acid. The preparation method provided by the invention has the advantages of short process reaction time and few byproducts, is favorable for improving the purity of the product, and has important guiding significance for the synthesis of subsequent derivative products.

A composition for treating hypogonadism comprises testosterone androstane steroid derivative (TASD), an aromatase inhibitor, and a delivery portion (DP). The TASD, aromatase inhibitor, and DP are combined to form a solution adapted to be administered transdermally. The method comprises the steps of administering a therapeutically effective amount of TASD sufficient to maintain a total serum testosterone level within a therapeutic / stabilized range; administering a therapeutically effective amount of an aromatase inhibitor, sufficient to maintain an estradiol level at or below 35 pg / mL, the TASD and aromatase inhibitor administered simultaneously, via spray. Aspirin is administered if the patient is determined to have an elevated hemoglobin level. In certain embodiments, the hemoglobin level is determined to be elevated if the hemoglobin level is greater than or equal to 17 g / dL and, if elevated, blood is removed from the patient, in therapeutic amounts.

This invention provides a method for preparing androstane-3,6,17-trione (E,Z)-3-[O-(2-aminoethyl)]oxime hydrochloride, comprising the following steps: benzophenone oxime reacts with 2-chloroethylamine hydrochloride in dimethyl sulfoxide, followed by acid-base adjustment, toluene extraction, hydrolysis with concentrated hydrochloric acid to remove the protecting group, and crystallization to obtain high-purity 2-aminoethylamine hydrochloride; androstane-3,6,17-triol is used as a raw material and oxidized under the catalysis of sodium bromate and ruthenium oxide (IV), quenched, separated, washed with water, and crystallized by solvent replacement with isopropanol to obtain androstane-3,6,17-trione; the 2-aminoethylamine hydrochloride solution is mixed and reacted with the trione in tetrahydrofuran solution at low temperature, followed by salting out, filtration, separation, washing with saturated brine and drying with magnesium sulfate, and purification by solvent replacement, water dissolution and concentration, and cooling crystallization to obtain the high-purity target product. This invention significantly improves the yield of the target product by optimizing reaction conditions, while achieving readily available raw materials, low cost, and industrialized production through traditional chemical reaction pathways.

The present disclosure relates to the use of neuroactive steroids, including alfaxalone, alfadolone, alfadolone acetate, pregnanediol, pregnanolone, ent-pregnanolone, pregnanedione, allopregnanediol, allopregnanedione, acebrochol, ganaxolone, hydroxydione, minaxolone, renanolone, (2β,3α,5β)-21-chloro-3-hydroxy-2-morpholin-4-ylpregnan-20-one (Org-20599), 2β-(2,2-dimethyl-4-morpholinyl)-3α-hydroxy-11,20-dioxo-5α-pregnan-21-yl methanesulfonate (Org-21465), 20-(hydroxyimino)pregn-4-en-3-one (EIDD-036), posovolone (Co 134444), zuranolone (SAGE-217), 3α-hydroxy-3β- methyl-21-(pyrazolo[3',4'-c]pyridin-2'-yl)-19-nor-5β-pregnan-20-one (SGE-872), alfaxalone / alfadolone (CT1341), (3β,5β,17β)-3-hydroxyandrostane-17-carbonitrile (3β- OH), (3α,5α)-3-hydroxy-13,24-cyclo-18,21-dinorchol-22-en-24-ol (CDNC24), 3α- dihydroprogesterone (3α-DHP), ent-progesterone, dihydrodeoxycorticosterone (DHDOC), tetrahydrodeoxycorticosterone (THDOC), and betaxalone, for treating or at least partially inhibiting the development or progression of an infection caused by a neurotropic virus in a subject. This disclosure also relates to the use of neuroactive steroids for treating or at least partially inhibiting the development or progression of a condition associated with an infection caused by a neurotropic virus, such as encephalopathy or acute encephalitis.

The invention belongs to the technical field of chemical medicines, and particularly relates to a full-continuous chemical synthesis method of cyproterone acetate. According to the method, 4-androstane-3, 17-diketone is taken as a starting raw material, and a full-continuous device consisting of a plurality of sequentially connected micro-mixers, micro-reactors, an online gravity separation device, an online solvent switching device, an online solvent concentration device, a solvent recovery device and the like is used; the cyproterone acetate product is synthesized through one-step enzyme catalysis reaction, nine-step chemical reaction and continuous operation, dichloromethane, dichloroethane and ethyl alcohol are recycled, and emission of three wastes is obviously reduced. According to the invention, the production efficiency and the process control accuracy can be greatly improved, and the stable product quality is ensured. And decoloring, recrystallizing, filtering and drying the obtained crude cyproterone acetate product to obtain a pure cyproterone acetate product with the purity of more than 99%.

Provided are androstane and dihydrotestosterone compounds functionalized with carbocyclic groups or heterocyclic groups that may be saturated or unsaturated. The compounds may be used in methods of inhibiting cell growth of malignant cells and / or hyperplastic cells and / or treating individuals having diseases associated with malignant cell growth (e.g., cancer, such as, for example, prostate cancer) and / or hyperplastic cell growth and / or molecular imaging of malignant cells and / or hyperplastic cells and / or inducing degradation of a target protein. Also provided are compositions.

The invention provides an improved method for preparing an exemestane intermediate 6-hydroxymethyl-androstane-1, 4-diene-3, 17-diketone, and particularly relates to a method for preparing the 6-hydroxymethyl-androstane-1, 4-diene-3, 17-diketone through a reaction of 1, 3-ditetrahydropyrrolyl-androstane-3, 5-diene-17-ketone under the action of phenol and a formaldehyde aqueous solution, and particularly relates to a method for preparing the 6-hydroxymethyl-androstane-1, 4-diene-3, 17-diketone through the reaction of 1, 3-ditetrahydropyrrolyl-androstane-3, 5-diene-17-ketone. Compared with the prior art, the method has the advantages that the generation of a large amount of bis-hydroxymethylation impurities is avoided, the purity and the yield are improved, the cost is reduced, the stability of the process is improved, and industrialization is facilitated.

A method of treating hypogonadism in a human male patient comprises the steps of administering a therapeutically effective amount of a testosterone androstane steroid derivative (TASD) such as testosterone cypionate sufficient to maintain a total serum testosterone level within a therapeutic / stabilized range. A therapeutically effective amount of an aromatase inhibitor, such as anastrozole, sufficient to maintain an estradiol level at or below 35 pg / mL and an estrogen level above a predetermined level may be administered. A therapeutically effective amount of aspirin is administered if the patient is determined to have an elevated hemoglobin level. In certain embodiments, the hemoglobin level is determined to be elevated if the hemoglobin level is greater than about 16 g / dL and blood is removed from the patient, in therapeutic amounts, if the hemoglobin level is greater than 17 g / dL. In certain embodiments, the serum total testosterone level therapeutic / stabilized range is between about 605-1051 ng / dL.

The application discloses a negative ion metabolic marker of thyroid-associated ophthalmopathy, a product and application thereof. The metabolic marker comprises any one or several of 7alpha, 17alpha-dimethyl-5beta-androstane-3alpha, 17beta-diol, N, N-dimethylphosphatidyl ethanolamine, 15(S)-hydroxyeicosatrienoic acid and 1-tetradecanoyl-2-[(9Z)-octadecenoyl]-sn-glycero-3-phosphatidylcholine. The application provides a kit comprising detection reagents for detecting the negative ion metabolic marker. The application provides a computer program product for thyroid-associated ophthalmopathy. The product provided by the application has good feasibility and accuracy, can effectively evaluate the risk of thyroid-associated ophthalmopathy, and provides a new tool for clinical diagnosis.

This invention provides a method for identifying crude oil types based on two-dimensional gas chromatography-time-of-flight mass spectrometry (GC-TOF-MS). The method includes: dissolving the crude oil sample to be identified using a diluent, then adding a 5α-androstane standard to the system to obtain the crude oil sample; performing chromatographic analysis of the crude oil sample using GC-TOF-MS; denoting the ratio of the sum of the weights of n-alkanes, isoalkanes, monocyclic alkanes, bicyclic alkanes, tricyclic alkanes, tetracyclic alkanes, and pentacyclic alkanes in the crude oil sample to the weight of the crude oil sample to be identified as S; denoting the ratio of the sum of the weights of monocyclic alkanes, bicyclic alkanes, tricyclic alkanes, tetracyclic alkanes, and pentacyclic alkanes in the crude oil sample to the weight of the crude oil sample to be identified as N; and identifying the type of crude oil sample based on the ratio of S to N. This method provides a new approach for the precise identification of naphthenic crude oil and the estimation of naphthenic crude oil reserves.

The application provides a method for improving androstane content based on methyl jasmonate and ApMYC2-ApHSFB2b module, and belongs to the field of plant biotechnology. The application constructs an overexpression vector of ApMYC2 gene and an overexpression vector of ApHSFB2b gene respectively, and transforms the two overexpression vectors into andrographis plants; after transformation, the andrographis plants are treated with methyl jasmonate again. Through the transformation of the overexpression vectors and the treatment of methyl jasmonate, the two work together to directly activate the expression of ApCPS1, a gene in the andrographolide biosynthesis pathway, and then promote the expression of other genes downstream of the synthesis pathway, so as to improve the androstane content, and provide an effective technical means for the planting and development of andrographis.

The invention discloses a metabolic marker combination, a detection kit and application thereof, an establishment method of an arteriosclerosis level prediction model and an arteriosclerosis level evaluation method. The metabolic marker combination comprises 2-hydroxybutyric acid, hydrocinnamic acid, 2-phenylpropionic acid, 5 [beta]-androstane-3 [beta]-ol-17 [beta]-carboxylic acid methyl ester, C18: 1 ceramide, vanillic mandelic acid, menadione, piperine, hippuric acid, carnitine, propionyl glycine, myristic acid, urocanic acid, alpha-linolenic acid, methionine and 5-hydroxymethyl-2-furancarboxylic acid. The arteriosclerosis level evaluation can be efficiently and accurately carried out.

Compounds and compositions for the activation of SERCA2a are disclosed. + / K + Provided are compounds that only moderately inhibit ATPase, but act as near-pure or pure SERCA2a activators.Generally, the disclosed compounds are derivatives of androstane represented by formula (I).Also disclosed herein are pharmaceutical compositions comprising one or more compounds of formula (I) for use in treating heart failure. TIFF2022551165000145.tif4261

The present invention belongs to the field of medicine, and particularly relates to the application of an aromatase inhibitor in the preparation of a medicament for treating melanoma. Experiments have shown that the metabolite Androstane-3β,4β,17β-triol (Triol) produced by formestane in cells can activate ERβ-positive melanoma cells, resulting in cell cycle arrest and inhibited cell growth; moreover, the formestane ointment is convenient to use. Since it is a topical drug, patients have a high acceptance level, can directly reach the tumor site, does not pass through the systemic circulation, and has little side effect after long-term use. It provides a new direction for the treatment of melanoma.

The invention provides a combined marker combination as well as a detection method and a kit thereof. The combined marker combination comprises a plasma protein marker and a blood metabolism marker, the plasma protein marker comprises an adaptor protein PH-containing structural domain, enolase 3, a proline 4-hydroxylase alpha1 chain and ethanol dehydrogenase 1C, and the adaptor protein comprises an adaptor protein PH-containing structural domain, a proline 4-hydroxylase alpha1 chain and a proline 4-hydroxylase alpha2 chain. The blood metabolism marker is prepared from diosgenin, eicosapentaenoic acid, folinic acid, hydroxyprogesterone hexanoate, testosterone, perfluorooctane sulfonic acid, prasterone sulfate, androstane dienone, long pine needle ketone and 1-(22 carbon 4 enoyl) lysophosphatidylcholine. Through cooperative detection of protein-metabolism markers and combined application of a machine learning model, accurate prediction of the age-related disease risk is achieved, the cognitive decline risk can be pre-judged in advance, meanwhile, efficient synchronous detection of multiple markers is achieved by means of a liquid chromatography-tandem mass spectrometry synchronous detection technology, the sample dosage is small, the detection process is standardized, and the detection efficiency is high. The large-scale queue research requirement is met, and multi-center clinical application and popularization are facilitated.