30 results about "Cholane" patented technology

The invention discloses an antigen antibody complex dissociation liquid kit, which is prepared by blending reagents of 0.3 volume percent of Triton-X100, 1.5 volume percent of lauryl sodium sulfate and 1.5 volume percent of 3-[(3-cholane amidopropyl)-dimethylammonium]propanesulfonic acid in equal amount. The invention also discloses application of the kit in separating a pathogenic antigen antibody complex. The kit of the invention effectively realizes rapid dissociation of the pathogenic antigen antibody complex in a serum or blood plasma sample to be detected, increases the absolute concentration value of an antigen and an antibody, and greatly improves the detection sensitivity of the sample to be detected.

The invention relates to an ursodeoxycholic acid compound for preventing or treating an FXR (farnesol X receptor)-mediated disease. Specially, the invention discloses the ursodeoxycholic acid compound shown in formula (I) and a drug combination containing the compound or the crystalline pharmaceutically-acceptably salt of the compound, a produg, tautomer, stereisomer, enantiomer, aquo-complex or solvate. The compound can serve as FXR stimulant and then is applicable to preparation of drugs for treating FXR related diseases such as fatty liver.

The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a 19-nor cholane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.

This invention provides a new method for preparing obeticholic acid which belongs to the technical field of medicine. Its raw material is E/2 -3alpha-hydroxy-b-ethylidene-keto-5beta-cholane-24-acid methyl ester(OB-4)which can be gained easily. First, OB-3 can be produced through hydroxy-protection with tetra hydropyrane protecting group. Then, OB-2 can be produced through hydrogenation-reduction in alkaline aqueous solution. Then, OB-1 can be produced through reducing again. At last, the target product--obeticholic acid can be got through catalyzing and removing tetrahydropyrane. The method is simple in production process, the content of isomer impurity is low, and the method is a new synthetic method of obeticholic acid suitable for industrial production.

The invention discloses a method for preparing obeticholic acid type 1. The method comprises the steps that firstly, (E)-3 alpha,7 alpha-dyhydroxyl-6-ethylidene-5 beta-cholane-24-acid or (E)-3 alpha,7 alpha-dyhydroxyl-6-ethylidene-5 beta-cholane-24-acid ester (a compound II), alkali, a solvent and 5% palladium on carbon are loaded into a reactor, the mixture reacts under the pressure of 1-3 atmospheres, a hydrogenation reaction is carried out at the preserved temperature until it is indicated that hydrogen does not conduct absorption any more; reaction liquid is cooled to 40-50 DEG C and filtered, filter liquid is added with water and heated to 40-50 DEG C, and a solution is obtained; secondly, the obtained solution is dipped with a thin acid solution to regulate the pH value to be 1-6, the solution is cooled, stirred for crystallization and filtered, and obeticholic acid type 1 is obtained through vacuum drying. By means of the preparing method, crystallized obeticholic acid type C does not need to be obtained, and obeticholic acid type 1 is obtained in one step, so that production steps are reduced, operation is simplified, aftertreatment is easy, and cost is reduced.

The present invention provides a cyclic cholane carboxylate derivative and a preparation method thereof, and uses of the cyclic cholane carboxylate derivative in industrial preparation of 25-hydroxycholesterol (1), wherein R1 in the cyclic cholane carboxylate derivative represented by a formula I is straight chain or branched chain C1-C12 alkyl, R2 is methyl or ethyl, and the formula (I) is defined in the specification. According to the present invention, the starting raw material stigmasterol of the 25-hydroxycholesterol (1) synthesis process route has characteristics of low price, easy obtaining and reliable commercial source; and particularly during the constructing of the 17-position side chain of 25-hydroxycholesterol (1), the reaction conditions are mild, the reaction steps are simple, the special and dangerous reagents are not required, the harsh reaction conditions are not required, the redundant reaction steps are not required, the chromatographic separation and purification is not required, the industrial production is easily achieved, and the significant progress is achieved compared to the prior art.

The invention relates to a synthesis method of three impurities of obeticholic acid. The method has important significance in synthesizing high-quality obeticholic acid. The method mainly studies 3 alpha,7 beta-dyhydroxyl-6-ethyl-5 beta-cholane-24-acid (V), 3 alpha,7 beta-dyhydroxyl-6 alpha-ethyl-5 beta-cholane-24-alcohol (VI) and 3,7-dicarbonyl-6 alpha-ethyl-5 beta-cholane-24-acid (VII). The synthesis route is shown in the description.

The invention discloses a preparation method of OCA (obeticholic acid). (E)-3 alpha-hydroxy-6-ethylidene-7-one-5 beta-cholane-24-acid or (E)-3 alpha-hydroxy-6-ethylidene-7-one-5 beta-cholane-24-acid ester, a solvent and a reducing agent are placed in a reactor to react to produce (E)-3 alpha, 7 alpha-dihydroxy-6-ethylidene-5 beta-cholane-24-acid or (E)-3 alpha, 7 alpha-dihydroxy-6-ethylidene-5 beta-cholane-24-acid ester. (E)-3 alpha, 7 alpha-dihydroxy-6-ethylidene-5 beta-cholane-24-acid or (E)-3 alpha, 7 alpha-dihydroxy-6-ethylidene-5 beta-cholane-24-acid ester, alkali, a solvent and a catalyst are placed in the reactor for hydrogenation to produce OCA. OCA with the purity of 99.5% or above can be obtained with the preparation method, the process is simple and good in reproducibility, thesolvent is safe, non-toxic, conventional and easy to obtain, post-treatment is simple, and the production cycle is short.

The invention relates to a preparation method of 3 alpha, 7 alpha-dihydroxy-6 alpha-ethyl-5 beta-cholane-24-aldehyde. The method is simple, convenient and high in yield and content. The3 alpha, 7 alpha-dihydroxy-6 alpha-ethyl-5 beta-cholane-24-aldehyde can be conveniently used as a reference substance of related substances for quality control of obeticholic acid or derivatives of obeticholic acid,or used for impurity identification of obeticholic acid or diffracted substances of obeticholic acid, and is beneficial to detection control in the production process of obeticholic acid or derivatives of obeticholic acid and quality control of drugs containing obeticholic acid or derivatives of obeticholic acid.

The invention discloses a method for extracting (20R)-22E-24-ethyl cholane-4,22-diene-3-ketone from stems and leaves of Coix lacryma-jobi. The method comprises the following steps: dried stems and leaves of Coix lacryma-jobi are crushed, ethanol is added and heated, reflux extraction is carried out, and an extracting solution is condensed in order to obtain an extract A; water is added into the extract A and the extract A is dispersed, petroleum ether is used for extraction, and petroleum ether is partially condensed in order to obtain an extract B; silica gel column chromatography is carried out for the extract B firstly, petroleum ether-ethyl acetate gradient elution is carried out, separated and purified components are collected, chromatography is carried out, pure dichloromethane is used for elution, separated and purified components are separated and purified by preparation type high performance liquid chromatography, a tR=31 min component is collected, condensation and crystallization are carried out, and the product is obtained. (20R)-22E-24-ethyl cholane-4,22-diene-3-ketone is extracted from waste stems and leaves of Coix lachrymal-jobi, environmental pollution is reduced, utilization rate of stems and leaves of Coix lacryma-jobi is improved, an industry chain of Coix lacryma-jobi is prolonged, income of Coix lacryma-jobi industry is increased, and the method has good economic benefits and ecological benefits.

The invention discloses a type-1 obeticholic acid preparation method. The type-1 obeticholic acid preparation method comprises the following steps that firstly, the mixture of 3 alpha-hydroxyl-6 alpha-ethyl-7-ketone-5 beta-cholane-24-acid ester, alkali and a solvent is heated to reach the temperature of 75-105 DEG C, a reducing agent is added for reaction, TLC tracking is performed till raw materials react completely, the reaction solution is cooled to reach the temperature of 30-50 DEG C, an organic solvent and water are added, a pH value of the solution is regulated to be 3-5 by using hydrochloric acid, solution separation is performed, and organic phase reduced-pressure drying by distillation is performed to obtain a colorless light yellow oily residue; secondly, water and alkali are added into the obtained residue, heating is performed for dissolution, and a solution is obtained; finally, a dilute hydrochloric acid is slowly and dropwise added into the obtained solution to regulate the pH value to be 3-4, and cooling, stirring for crystallization, filtering and vacuum drying are performed to obtain a type-1 obeticholic acid.

The invention relates to a method for preparing ursodeoxycholic acid by using biological enzyme catalysis technology and 7β-steroid dehydrogenase for preparation thereof. The method uses 3α-hydroxy-7 oxo-5β-cholanic acid as a substrate, and in the presence of NADP, glucose, glucose dehydrogenase and buffer solution, 3α-hydroxy-7 Preparation of ursodeoxycholic acid from oxo-5β-cholanic acid with 7β-steroid dehydrogenase from Ruminococcus twistersensis Ruminococcus torques ATCC 27756. The method has the advantages of simple operation, mild and easy-to-control reaction conditions, short reaction time, a substrate conversion rate as high as 99.7%, and the obtained product content is above 98.5%.

The invention discloses an isomer of cholanic acid as well as a detection method and application thereof, a novel isomer 3 beta type cholanic acid of cholanic acid is found in a pig gall substance serving as a Naoliqing preparation raw material, and the byproduct widely exists in pig gall powder and pig bile paste medicinal materials and is transferred into a Naoliqing preparation along with the production feeding process, and the substance is used as an index for detecting the quality of the pig gall raw material, so that the quality risk caused by component change can be avoided.