20 results about "Pregnenolone" patented technology

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, sublingual administration, topical administration, transdermal administration, or combinations thereof and uses thereof.

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, and uses thereof.

Disclosed is a method and a brexanolone containing oral composition for treating CNS disorders such as depression. An embodiment of the invention comprises orally administering a brexanolone containing composition to a subject having a CNS disorder. The composition and methods disclosed herein exhibit effective oral absorption / bioavailability and a predetermined ratio of bioavailability in a fed state administration relative to a fasted state administration.

The application relates to the technical field of organic synthesis, and particularly discloses a synthesis process of high-purity pregnenolone, which comprises the following steps: S1, esterification reaction of progesterone and an acylation reagent to obtain product 1; S2, ketalization reaction of the product 1, diol and a dehydrating agent in the presence of a catalyst to obtain product 2; S3, reduction reaction of the product 2 and a reducing agent to obtain product 3; and hydrolysis reaction of the product 3 and an acidic compound to obtain pregnenolone. The synthesized pregnenolone has high purity and yield.

Microemulsions are described where hydrophobic liquid droplets are distributed in a continuous hydrophilic liquid phase. In relation to conventional oil-in-water (OIW) microemulsions, the described microemulsions may be thought of as modified oil-in-water (MOIW) microemulsions, where both the “oil” and “water” phases of the microemulsion are modified. The oil phase droplets of the MOIW microemulsion are modified with alcohol and can solubilize alcohol-soluble species, including nonderivatized hormones. More preferably, the modified oil phase droplets of the MOIW microemulsion directly solubilize nonderivatized hormones. The oil phase droplets of the MOIW microemulsion include DHEA, pregnenolone, and a polyphenol, where a ratio of DHEA to polyphenol is from 1:1 to 12:1 by weight. Methods of supporting and / or increasing bloodstream hormone levels in perimenopausal and postmenopausal females and improving menopausal symptoms also are disclosed.

This invention discloses sterol side-chain cleaving enzymes and 3β-hydroxysteroid dehydrogenases / Δ from different sources. 4,5 Amino acid sequences, coding sequences, and applications of isomerases. This invention, based on synthetic biology and molecular pharmacognosy, explores sterol side-chain cleaving enzymes and 3β-hydroxysteroid dehydrogenases / Δ from different plant sources. 4,5 Isomerases, which will yield sterol side-chain cleavage enzymes and 3β-hydroxysteroid dehydrogenases / Δ 4,5 The coding sequences of the isomerases were constructed into expression cassettes, and using Saccharomyces cerevisiae as the chassis strain, highly efficient pregnenolone or progesterone synthesizing strains were obtained. The pregnenolone yield of the constructed strains reached as high as 14.46±2.16 mg / L, and the progesterone yield reached as high as 32.78±1.84 mg / L. This achieved high-level synthesis of pregnenolone and progesterone by genetic engineering methods, providing an important foundation for the green synthesis of steroid hormones.

The invention provides a steroid compound containing a 3-methyl allopregnenolone mother nucleus structure as well as a preparation method, a pharmaceutical composition and application of the steroid compound, and belongs to the technical field of medicines. The invention provides a steroid compound containing a 3-methyl pregnenolone mother nucleus structure, and pharmaceutically acceptable salts, stereoisomers, tautomers, prodrugs, solvates or isotope compounds of the steroid compound. The steroid compound containing the 3-methyl pregnenolone mother nucleus structure has a structure as shown in a formula I. The invention further provides a preparation method of the steroid compound containing the 3-methyl pregnenolone mother nucleus structure. The steroid compound containing the 3-methyl allopregnenolone mother nucleus structure has a strong positive regulation effect on a GABAA receptor, and has potential application to treatment of central nervous system related diseases.

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 discloses a directional preparation process of B crystal form dexamethasone. The process comprises the following steps: by taking 16-dehydropregnanone propionate as a starting material, sequentially performing catalytic dehydrogenation by using steroid 1, 4-dehydrogenase from bacillus subtilis, performing catalytic dehydrogenation by using potassium methyltrifluoroborate / copper acetate / 2, 4-dihydroxyprogesterone propionate as a starting material, and performing catalytic hydrogenation by using potassium methyltrifluoroborate / The preparation method comprises the following steps: preparing dexamethasone free alkali by key steps of stereoselective methylation of a 2, 2 '-bipyridine system, catalysis of 11 beta-hydroxylation by immobilized CYP11B1 monooxygenase, epoxidation of peroxybenzoic acid, ring opening of hydrogen fluoride-ethanol and the like, and finally directionally crystallizing in a system solution consisting of 0.5% malic acid and isopropanol-water in a volume ratio of 3: 1 to obtain the high-purity B crystal form dexamethasone.

The invention relates to application of ginsenoside Rg4 as a unique active ingredient in preparation of a medicine for improving male delayed gonad hypofunction, belonging to the field of biological medicine. According to the invention, the action mechanism of the Rg4 for improving LOH is defined for the first time: the Rg4 can specifically up-regulate the mRNA expression quantity of StAR and StARD7 in a testis tissue, and promote the transport of cholesterol to the inner mitochondrial membrane of a testis Leydig cell from the transcriptional level; the Rg4 improves the mRNA expression quantity of P450scc, 3 beta-HSD in testicular tissues by promoting the efficient transport of cholesterol, enhances the conversion of cholesterol to pregnenolone and the catalytic synthesis of subsequent steroids, and improves the endogenous testosterone synthesis capability; the Rg4 can recover the negative feedback regulation function of an HPG axis, regulate secretion of pituitary LH and FSH to physiological steady state, and avoid abnormal fluctuation of hormone level. The invention fills the technical blank of Rg4 in the field of LOH gene regulation and control.

The invention relates to the technical field of cell engineering and biopharmacy, and discloses a method for promoting synthesis of steroids in forest musk gland cells, which comprises the following steps: determining the tolerance range of cholesterol concentration through a pre-experiment, setting an experimental group, culturing cells, collecting and treating a sample, and detecting by LC-MS (Liquid Chromatography-Mass Spectrometry). According to the method for promoting synthesis of the steroids in the lindel gland cells, the synthesis amount of the seven steroids in the lindel gland cells can be up-regulated by regulating the cholesterol concentration of the culture medium to 10-20 mg / L, the content of pregnenolone is up-regulated by 4.12 times (Plt, 0.05), the content of progesterone is up-regulated by 1.46 times (Plt, 0.05), and the method is remarkably superior to that of existing culture without cholesterol regulation; a complete standardized process from pre-experiment, culture, sample treatment to detection is provided, the experiment result repeatability is high, and the method can be directly applied to industrial production.

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, and uses thereof.

Disclosed are: a poultry feed comprising at least one selected from the group consisting of progesterone, pregnenolone, and medroxyprogesterone; and a method for breeding poultry, the method comprising a step for causing poultry to ingest at least one selected from the group consisting of progesterone, pregnenolone, and medroxyprogesterone.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a biological oxidation preparation method of a key intermediate in a chemical synthesis medicine production process. A compound A synthesized by photocatalytic isomerization of pregnenolone is used as a raw material. Under the action of alcohol dehydrogenase, the compound A is oxidized to form a compound B, and then the compound B is shifted in a hydrogen chloride ethanol solvent to form the didrogesterone. Through the preparation technology provided by the invention, the high-purity didrogesterone bulk drug can be obtained with low cost and high efficiency.

The invention discloses a bacterium-derived steroid side chain lyase and application of a mutant of the bacterium-derived steroid side chain lyase. Compared with the amino acid sequence shown in SEQ ID NO: 1, the steroid side chain lyase has amino acid residue difference at one or more sites of the 91st site, the 323rd site and the 324th site; compared with SEQ ID NO: 1, the amino acid sequence has at least 90% of sequence consistency; and the steroid side chain lyase has a steroid side chain splitting effect equivalent to or better than that of the steroid side chain lyase with the amino acid sequence shown as SEQ ID NO: 1. The steroid side chain lyase or the mutant thereof breaks through the limitation that traditional eukaryotic source P450scc is low in expression level, poor in activity and large in transformation difficulty, not only expands the species distribution range of P450scc, but also provides efficient and engineered novel enzyme resources for microbial synthesis of steroid key prodrugs (such as pregnenolone and progesterone), and has broad application prospects. The method has great application potential and economic value.

The invention discloses preparation and application of a CYP87A4 enzyme mutant, and belongs to the technical field of enzyme engineering. According to the present invention, the digitalis lanceolata source CYP87A4 enzyme is adopted as the starting sequence, and the CYP87A4 enzyme mutant capable of improving the pregnenolone yield is obtained through site-specific mutagenesis; compared with the yield (127.6 mg / L) of pregnenolone of a strain expressing WT, the yield of pregnenolone of recombinant strains expressing mutants I206A, I206A / P213S and I206A / P213S / S111L is 153.7 mg / L, 189.7 mg / L and 204.9 mg / L respectively, and the industrial application value and competitiveness of the mutants and genetically engineered bacteria in the field of biological medicine are remarkably improved.

Microemulsions are described where hydrophobic liquid droplets are distributed in a continuous hydrophilic liquid phase. In relation to conventional oil-in-water (OIW) microemulsions, the described microemulsions may be thought of as modified oil-in-water (MOIW) microemulsions, where both the “oil” and “water” phases of the microemulsion are modified. The oil phase droplets of the MOIW microemulsion are modified with alcohol and can solubilize alcohol-soluble species, including nonderivatized hormones. More preferably, the modified oil phase droplets of the MOIW microemulsion directly solubilize nonderivatized hormones. The oil phase droplets of the MOIW microemulsion include DHEA, pregnenolone, and a polyphenol, where a ratio of DHEA to polyphenol is from 1:1 to 12:1 by weight. Methods of supporting and / or increasing bloodstream hormone levels in perimenopausal and postmenopausal females and improving menopausal symptoms also are disclosed.

The present invention generally relates to a specific pregnenolone derivative for its use for the treatment of a cognitive disorders. More particularly, the invention relates to a compound of Formula (I)for its use in the treatment of cognitive disorders. Indeed, the compound of the invention is in vivo very potent in correcting the cognitive impairments observed in cognitive disorders.

The invention belongs to the technical field of biology, and particularly relates to a method for synthesizing a steroid hormone compound by utilizing saccharomyces cerevisiae. The invention finds that overexpression of SPT23 is beneficial to the yield of steroid hormone progesterone in saccharomyces cerevisiae, further overexpression of SPT23, MGA2 and OLE1 is beneficial to the yield of steroid hormone pregnenolone in saccharomyces cerevisiae, and exogenous addition of oleic acid is also beneficial to the yield of steroid hormone pregnenolone in saccharomyces cerevisiae. Therefore, the invention provides a solution for improving the yield of the steroid hormone compound in the saccharomyces cerevisiae, and has practical significance.

This invention relates to compounds of Formula I and their isotopic forms, stereoisomers, tautomers, pharmaceutically acceptable salts, pharmaceutically acceptable solvates, hydrates, prodrugs, and polymorphs. The compounds of Formula I can be used as inhibitors of cytochrome P450 monooxygenase 11A1 (CYP11A1), effectively inhibiting the synthesis of testosterone and pregnenolone, and have good application prospects in the preparation of drugs for diseases such as prostate cancer and breast cancer.