93 results about "Epiandrosterone" patented technology

A composition and various formulations comprise preventative or therapeutic amounts of an epiandrosterone, analogue thereof or salt thereof, and / or a ubiquinone or salt thereof, and a pharmaceutically or veterinarily acceptable carrier or diluent. The composition and formulations are useful for treating bronchoconstriction, respiratory tract inflammation and allergies, asthma, and cancer. A method of treating diseases associated with low adenosine levels or adenosine depletion comprises administering folinic acid or a pharmaceutically acceptable salt hereof in a preventative or therapeutic amount, or an amount effective to treat adenosine depletion.

A pharmaceutical or veterinary composition, comprises a first active agent selected from a dehydroepiandrosterone and / or dehydroepiandrosterone-sulfate, or a salt thereof, and a second active agent comprising a tyrosine kinase inhibitor, delta opioid receptor antagonist, neurokinin receptor antagonist, or VCAM inhibitor for the treatment of asthma, chronic obstructive pulmonary disease, or other respiratory diseases. The composition is provided in various formulations and in the form of a kit. The products of this patent are applied to the prophylaxis and treatment of asthma, chronic obstructive pulmonary disease, or other respiratory diseases.

The invention discloses a synthesis process of vecuronium bromide. The synthesis process comprises the following steps: generating epiandrosterone sulfonyl ester (III) by carrying out esterification reaction between epiandrosterone (II) and paratoluensulfonylchloride; generating 5Alpha-androst-2-alkene-17-ketone (IV) by carrying out elimination and dehydration reaction between the (III) and 2,6-lutidines; generating 17-acetoxyl-5Alpha-androstane-2,16-diene (V) by carrying out enolization and esterification reaction between the (IV) and isopropenyl acetate; generating (2Alpha, 3Alpha, 16Alpha,17Alpha)-diepoxy-17Beta-acetyl-5Alpha-androstane (VI) by epoxy reaction of the (V) under the effect of hydrogen peroxide; generating 2Beta, 16Beta-di(1-piperidyl)-5Alpha-androstane-3Alpha-hydroxyl-17-ketone (VII) by ring-opening and addition reaction of the (VI) under the effect of hexahydropyridine; generating 2Beta, 16Beta-di(1-piperidyl)-5Alpha-androstane-3Alpha,17Beta-diol (VIII) by the (VII)under the reduction of potassium borohydride; generating 2Beta, 16Beta-di(1-piperidyl)-3Alpha, 17Beta- acetoxyl-5Alpha-androstane (IX) by carrying out esterification reaction of the (VIII) under the acetylation of acetic anhydride; and generating vecuronium bromide (I) by carrying out quaternary ammonium salt reaction between the (IX) and bromomethane. The invention has the advantages of low cost,less pollution and high yield.

Novel methods for treating or reducing the likelihood of acquiring symptoms or diseases due to the menopause, in postmenopausal women, particularly osteoporosis, vaginal atrophy and dryness, hypogonadism, diminished libido, skin atrophy, connective tissue disease, urinary incontinence, breast, endometrial, ovarian and uterine cancers, hot flashes, loss of muscle mass, insulin resistance, fatigue, loss of energy, aging, physical symptoms of menopause, in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor are disclosed. Said method comprising novel ways of administering and dosing dehydroepiandrosterone (DHEA) in order to take advantage of positive androgenic effects in the vaginal layers lamina propia and / or the layer muscularis, without undesirably causing systemic estrogenic effects in order to avoid the risk of breast and uterine cancer. Pharmaceutical compositions for delivery of active ingredient(s) useful to the invention are also disclosed.

The invention discloses a making method of 2 alpha, 3 alpha-epoxy-16 alpha-bromine-5 alpha-androstane-17-ketone as intermediate of steroidal muscular relaxation drug, which comprises the following steps: dissolving epiandrosterone in the benzene; adding catalyst; stirring; heating; refluxing 8-12h; preparing 5 alpha-androst-2-olefin-17-ketone; reacting the 5 alpha-androst-2-olefin-17-ketone and copper bromide in the carbinol to produce 16 alpha-bromine-5 alpha-androst-2-olefin-17-ketone; reacting the 16 alpha-bromine-5 alpha-androst-2-olefin-17-ketone and m-perbenzoic acid in the composite solvent of water and dichloromethane; producing the product through eliminating, bromizing and epoxidising.

The invention discloses a composition for resisting ageing and improving male energy. The composition is prepared from a raw material and an auxiliary material; the raw material is prepared from the following components in parts by weight: 1-15 parts of nicotinamide mononucleotide, 1-10 parts of protopanoxadiol, 1-9 parts of icarisid I, 2-8 parts of baohuoside I, 3-7 parts of dehydroepiandrosterone and 2-10 parts of ursodesoxycholic acid. The composition is reasonable in composing prescription and proper in compatibility; in the composition, the four of the nicotinamide mononucleotide (NMN), the icarisid I, the baohuoside I and protopanoxadiol are used as monarch drugs together, the composition is capable of comprehensively regulating gonad axis and invigorating kidney-yang and liver, candelay ageing period of the gonad axis and improve the sexual function after being taken for a long time; through intercoordination and synergistic effect of various components, the composition is comprehensive in nutrition, has very good palatability, is particularly suitable for males to take and thus relieving the symptoms of male ageing syndrome and improving the male energy. The invention alsoprovides a preparation containing the composition and a preparation method of the preparation. The preparation method is simple, is moderate in condition and is suitable for industrial batch production.

A preparation method for dehydroepiandrosterone, comprising: in a protective atmosphere, adding potassium tert-butoxide to tert-butanol, stirring evenly, adding 4-androstenedione to obtain a mixture,and adding the mixture dropwise to a sodium ascorbate-containing acetic acid solution for a reaction to obtain 5-androstenedione; dissolving the 5-androstenedione in an organic solvent, adding a ketone reductase, a glucose dehydrogenase, glucose and a redox coenzyme to obtain a mixture, controlling the pH of the mixture to be 6.0-6.3, stirring and reacting for 1-6 hours at 22-26 DEG C to obtain areaction solution, and performing separation and purification on the reaction solution to obtain dehydroepiandrosterone, the ketone reductase and the glucose dehydrogenase being coexpressed by a microbial strain and added in the form of a crude enzyme solution. The synthesis process of the preparation method has few steps, simple operations, high yields and low costs, and may be widely applied toindustrial scale production. Also provided is an enzyme for preparation.

The invention belongs to the field of medicinal chemistry and in particular relates to dehydroepiandrosterone D cyclobenzo-aminothiazole ring imine and imine reducing compounds as well as a preparation method and application thereof. The compounds are shown in a formula I in the specification. An in-vitro antineoplastic activity experiment indicates that the compounds have better broad-spectrum antineoplastic activity, have a favorable inhibition effect on multiple human cancer cells, such as EC109 and EC9706 and are suitable for research of antineoplastic lead compounds or preparation of novel antineoplastic medicaments. The preparation method is simple and convenient and suitable for industrial production.

The present invention discloses a dehydroepiandrosterone (DHEA) enzyme-linked immunosorbent assay kit development method, which comprises: adopting dehydroepiandrosterone and succinic anhydride as raw materials, and adopting an anhydride mixing method to respectively prepare dehydroepiandrosterone artificial antigen (DHEA-BSA and DHEA-OVA) and anti-dehydroepiandrosterone (DHEA) monoclonal antibody so as to prepare an enzyme-linked immunosorbent assay (ELISA) kit. Compared with the high performance liquid chromatography (HPLC) method, the method of the present invention has the following advantages that: operation steps are simple, a plurality of samples can be detected in one time, expensive instrument is not required, and detection sensitivity, the required time and other aspects are better than the HPLC method. Compared to the HPLC method, the ELISA method has the following characteristics that: uses of organic reagents such as n-hexane, acetonitrile, methanol and the like are not required, poison on experimenters and environment can be reduced, and an environmental protection characteristic is provided.

The invention discloses a method for preparing epiandrosterone. 4-androstenedione (I) is used as a raw material to prepare the epiandrosterone. The reaction formula is shown in the description. The low-cost 4-androstenedione is used as the raw material for the first time, and the epiandrosterone is obtained through synthesis on the mild reaction conditions, so that the production cost is greatly lowered, and the method is suitable for large-scale industrial production.

The invention relates to a method for hydroxylating dehydroisoandrosterone (DHEA) by using colletotrichumlini ST-1. The method for hydroxylating the dehydroisoandrosterone by using the colletotrichumlini ST-1 is characterized in that: in a conversion process, a way of pre-including the DHEA and methyl-beta-cyclodextrin with an equimolar ratio first and then feeding is adopted, so that the water solubility and the conversion efficiency of the DHEA are significantly improved. Under a condition that a substrate feeding amount is 10g / L, the conversion rate is as high as 95% and the total yield of products 7 alpha-OH-dehydroepiandrosterone and 7,15 alpha-OH-dehydroepiandrosterone is 80.94%.

The invention discloses a preparation method of androst-2-en-17-one. The method comprises the steps that 4-androstenedione is adopted as a raw material, three-step reactions of a protective reaction,a reduction reaction and a deprotection reaction are adopted for synthesizing epiandrosterone, in an organic solvent, a carrier solid phase acid catalyst soaked with acid is used for catalyzing, epiandrosterone dehydration is performed to eliminate 3-bit hydroxyls in molecules, and a target product is obtained. 4-androstenedione obtained by phytosterol extracted from a soybean oil deodorization distillate through the modern fermentation technology is adopted as a raw material; 4-androstenedione is subjected to the three-step reactions to synthesize a key intermediate epiandrosterone, and raw materials are abundant in source and low in price. The epiandrosterone is used for preparing a target product, compared with a traditional method, a synthetic route is cut into a one-step reaction fromtwo-step reactions, the method is economical and environmentally friendly, and production and operation are easier. By adopting the carrier solid phase acid catalyst soaked with acid for catalyzing,an oligomer makes indirect contact with the acid catalyst, the reactions are mild and stable, the dehydration elimination reactions are performed in the thermodynamics stable 2,3-bit directions, and the reaction selectivity is good.

The invention discloses a preparation method of 5 alpha-androstane-2-ethylene-17-ketone. The preparation method comprises the steps of taking epiandrosterone (formula I as shown in the specification)as a raw material to give a dehydration reaction by joint catalysis of protonic acid and trifluoromethanesulfonate, and performing post-treatment, recrystallization and separation on a reaction product to form 5 alpha-androstane-2-ethylene-17-ketone (formula II as shown in the specification). The preparation method avoids the use of much organic base compound in the traditional method, has the advantages of high reaction yield, short procedure, good selectivity, low cost, less waste gas, waste water and industrial residue and the like and is a synthesis method suitable for industrial production.

The invention relates to a preparation method of 1alpha-dehydroepiandrosterone, belonging to a preparation method of steroide compounds. The preparation method is characterized by comprising the following steps of: carrying out a dehydrogenated oxidizing reaction on glycol-condensed dehydroepiandrosterone as a raw material under the action of a metallic palladium catalyst, an allyl phosphodiester ligand and alkali to generate conjugated ketene; and carrying out epoxidation and liquid ammonia-metal reduction and deprotecting reaction to obtain the 1alpha-dehydroepiandrosterone. The invention has the advantages of simple process flow, short production cycle, high product yield, low production cost, low price and easy accessibility of the raw material and a reagent, simple operation, no need of column chromatography and other operations and suitability for large-scale preparation and production. In addition, the invention solves the problems of complicated process, long production cycle, low yield and high production cost existing in the method for fermenting microorganisms in the prior art.

Novel methods for reduction or elimination the incidence of hot flushes, vasomotor symptoms, and night sweats while decreasing the risk of acquiring breast, uterine or endometrial cancer and furthermore having beneficial effect by inhibiting the development of osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, diabetes type 2, loss of muscle mass, adiposity, Alzheimer's disease, loss of cognition, loss of memory, or vaginal dryness in susceptible warm-blooded animals including humans involving administration of an amount of a sex steroid precursor, particularly dehydroepiandrosterone (DHEA) and an antiestrogen or a selective estrogen receptor modulator, particularly compounds having the general structure:Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

The invention discloses an industrial production method of 5 alpha-androst-2-ene-17-one. The method comprises the following steps of: dissolving epiandrosterone p-toluenesulfonates into a monomethylpyridine solvent, carrying out beta-elimination reaction within a certain temperature range, and removing p-toluenesulfonates to obtain the 5 alpha-androst-2-ene-17-one. The industrial production method has the advantages of simple and easily-obtained raw materials, simplicity and convenience in operation, no 3,4-double bond isomerization impurities in the finally-obtained product, safety in production, high yield and little pollution from three wastes so as to be suitable for industrial production.

The invention belongs to the field of pharmaceutical chemistry, and discloses a novel synthesis method of Istaroxime. The method comprises the following steps: by using dehydrogenated epiandrosterone as an initial raw material, carrying out epoxidation, ring opening, reduction, oxidation and other reactions to prepare an intermediate M-06; by using ethyl benzoate as an initial raw material, reacting the ethyl benzoate with hydroxylamine hydrochloride to obtain phenyl hydroximic acid, carrying out hydrochlorination and chlorination by using ethanolamine as a raw material to obtain dichloroacetate, and carrying out substitution, hydrolysis and other reactions on the dichloroacetate and the phenyl hydroximic acid to obtain an intermediate M-11; and finally, reacting the M-06 with the M-11 to obtain the end product Istaroxime. According to the method, in the intermediate M-06 synthesis process, the polarity of all the intermediates has great differences from that of the impurities and reaction reagents; and in the intermediate 11 synthesis process, the active spots capable of participating in the chemical reaction in the reaction substrate are simple. Therefore, the method can achieve the requirements without carrying out column chromatography purification, thereby simplifying the synthesis after-treatment process.

The invention provides a novel method for preparing dehydroepiandrosterone, discloses a preparation method of dehydroepiandrosterone, and belongs to the technical field of preparation and processing of compounds. The method comprises the following steps of: taking 4-androstenedione (I) as a starting raw material, carrying out an acetylation reaction to obtain 3-acetoxyl-delta 3, 5-androstadiene-17-ketone (II), and then carrying out a biological enzyme method reaction on the obtained intermediate compound (II) to obtain the product dehydroepiandrosterone. The compound II in the invention is used as a key intermediate, the property of the compound II is more stable than that of 5-AD, and the purity is high, so that the stability of entering the next step of the biological enzyme method is effectively ensured; the biological enzyme method of the reaction route adopts a composite biological enzyme with a specific ratio, and the composite biological enzyme with the specific ratio acts on the compound II and has a better and more stable conversion effect; and the single-batch yield of the route is larger than 90%, the purity of the product compound III is high, the purity is larger than 99%, and the industrial application value is higher.

Belonging to the field of biotechnology, the invention relates to a method of utilizing a coenzyme regeneration and resin in-situ extraction integrated strategy to promote hydroxylation of DHEA (dehydroepiandrosterone) by Colletotrichum lini ST-1. The method is characterized in that in the conversion process, a 10g / L cosubstrate is added to conduct NADPH regeneration, and simultaneously D101 type macroporous adsorption resin is employed for in-situ extraction of the product, thus significantly enhancing the conversion rate of C. lini ST-1 on DHEA. Under the condition of a substrate feeding amount of 10g / L, the conversion rate of the substrate DHEA is 93%, and the yield of 7 alpha, 15 alpha-diOH-DHEA can reach 7.12 g / L.

The invention provides a production method for synthetizing epiandrosterone from single enol ketone acetate. The production method comprises the steps of: taking single enol ketone acetate as a material, and obtaining epiandrosterone by oximating, rearrangement and hydrolysis reaction, wherein the purity can be up to over 98.5%; and the yield achieves over 68%. Hydrogenation is saved; the problem of high industrial cost due to the fact that palladium chloride-calcium carbonate is taken as a catalyst in the traditional method is solved; the product yield is improved; and the process has the characteristics of being simple to operate, small in pollution, high in yield and the like, and is suitable for industrial production.

The invention discloses a steroid hormone detection method that comprises the following steps: adding an internal standard substance into a sample to be detected; carrying out a derivatization reaction; detecting an analyte by using chromatography tandem mass spectrometry; the analyte comprises a first steroid hormone and a second steroid hormone at the same time; the first steroid hormone is selected from at least one of the following steroid hormones: estradiol and estriol; and the second steroid hormone is selected from at least one of the following steroid hormones: dehydroepiandrosterone,dehydroepiandrosterone sulfate, testosterone, dihydrotestosterone, androstenedione, cortisol, cortisone, 11-deoxycortisol, 17alpha-hydroxyprogesterone, 17alpha-hydroxypregnenolone, aldosterone, cortisol, deoxycortisol, progesterone and pregnenolone. The detecting method has the advantages of few operation steps and short detection time, and can specifically, sensitively, accurately and quantitatively analyze the analyte substance.

Kits for treating or preventing chronic obstructive pulmonary disease (COPD) by using as active agent a non-glucorticoid steroid, analogue thereof, such as dehydroepiandrosterone (DHEA) and dehydroepiandrosterone sulfate (DHEA-S), or their salts, in an amount effective for preventing or treating COPD.

The invention provides a method for preparing an intermediate of eplerenone 3 Beta, 5- dihydroxy-15 Beta, 16 Beta-methylene-5 Beta-androstane-6-alkene-17-ketone (q10) from dehydroepiandrosterone acetate.

The invention discloses a method for detecting the content of DHEA in human body fluid. The method comprises the steps of detecting dehydroepiandrosterone in saliva by using a high performance liquid chromatography-tandem mass spectrometry technology, specifically, S1, adding the following reagents into a kit: a mobile phase I, a mobile phase II, a standard substance mother solution, an internal standard solution, a diluent, an extracting solution, a quality control substance and a redissolving solvent; S2, detecting the dehydroepiandrosterone in the pretreated saliva by adopting the high performance liquid chromatography-tandem mass spectrometry technology; S3, separating the dehydroepiandrosterone from the interferent by using high performance liquid chromatography; S4, quantifying by using an isotope internal standard method; S5, taking the concentration ratio of the standard substance to the internal standard substance as an X axis and the peak area ratio of the standard substance to the internal standard substance as a Y axis; and S6, establishing a standard curve, and calculating the content of the dehydroepiandrosterone in the sample to be detected. The method is high in sensitivity and good in specificity, saliva sample treatment is simple, methodology verification meets requirements, and it is indicated that the method is reliable and capable of being applied to quantitative detection of dehydroepiandrosterone in human saliva.

A pharmaceutical or veterinary composition, comprises a first active agent selected from a dehydroepiandrosterone and / or dehydroepiandrosterone-sulfate, or a salt thereof, and a second active agent comprising a phosphodiesterase-4 inhibitor for the treatment of asthma, chronic obstructive pulmonary disease, or any other respiratory disease. The composition is provided in various formulations and in the form of a kit. The products of this patent are applied to the prophylaxis and treatment of asthma, chronic obstructive pulmonary disease, or any other respiratory disease.

The invention relates to a method for producing a steroidal drug intermediate, in particular to a method for preparing dehydroepiandrosterone through conversion of plant sterols by resting cells. Themethod includes the steps of 3-position hydroxyl protective reaction, bioconversion of the resting cells, hydrolysis and purification. According to the method, the plant sterols are used as raw materials to produce dehydroepiandrosterone, the raw materials are easily available, the production cost is reduced, the yield is higher, the reaction route is shorter, and reaction steps and post-treatmentsteps required by most traditional preparation methods are eliminated; and a resting cell conversion method is adopted, the conversion system is single in nutrition and low in risk of infection and has an adjustable bacterial volume, and good conversion ability can be ensured.

The invention provides a novel technology for synthesizing epiandrosterone by adopting 4-androstenedione through selective hydrogenation reducing.Epiandrosterone is synthesized by adopting 4-androstenedione through selective hydrogenation reducing, therefore, the reaction path is greatly shortened, generation of an intermediate reaction by-product is prevented, and the product purity and yield are high; in addition, the reaction raw material consumption is lower, the cost is reduced, and the concept requirement for green production is met.