30 results about "Cholane" patented technology

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.

The invention relates to a preparation method of 3-beta-peanut amide-7alpha, 12alpha, 5beta-cholane-24-carboxylic acid. The method adopts a two-step reaction route for preparation, which avoids the utilization of protecting groups, reduces reaction steps, decreases unnecessary raw material consumption, increases production efficiency, reduces environment pollution, and has the advantages of high yield and low cost.

The invention relates to a method for preparing 3α-hydroxy-7-oxo-5β-cholanic acid by using biological enzyme catalysis technology and 7α-steroid dehydrogenase for preparation thereof. The method uses chenodeoxycholic acid as a substrate, and in the presence of NAD, lactate dehydrogenase, sodium pyruvate and buffer solution, uses 7α-steroid dehydrogenase to catalyze chenodeoxycholic acid to prepare 3α-hydroxy-7 Oxo-5β-cholanic acid with 7α-steroid dehydrogenase from Halomonas Halomonas jeotgali sp. 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 over 99.7%, and the obtained product content is over 97.5%.

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.

A method for preparing 3α-hydroxy-7oxo-5β-cholanic acid catalyzed by biological enzymes and 7α-steroid dehydrogenase for its preparation. The method uses chenodeoxycholic acid as a substrate, and in the presence of NAD, lactate dehydrogenase, sodium pyruvate and buffer solution, uses 7α-steroid dehydrogenase to catalyze chenodeoxycholic acid to prepare 3α-hydroxy-7 Oxo-5β-cholanic acid with 7α-steroid dehydrogenase from Cyanobacteria Cyanothece sp.ATCC 29155.

The present invention relates to a cholanic acid compound for preventing or treating FXR-mediated diseases. Specifically, disclosed are a cholanic acid compound represented by formula (I) and a pharmaceutical composition containing the compound, or a crystalline form, a pharmaceutically-acceptable salt, a prodrug, a tautomer, a stereoisomer, an enantiomer, and a hydrate or a solvate thereof. The compound in the present invention can be used as a farnesol X receptor agonist and can therefore be applied to the preparation of drugs for treating FXR-related diseases (for example, fatty liver).

The present invention relates to a kind of long-acting rasagiline prodrug and its preparation method and application, the structure of described long-acting rasagiline prodrug is as shown in formula I: wherein, T is selected from or does not have; R 1 and R 2 are independently selected from hydrogen, deuterium and methyl; W is selected from (CH 2 ) n Or not, n is selected from integers from 1 to 15; X is selected from (CH 2 ) m Or not, m is selected from an integer of 1 to 10; Y is selected from -C(=O)NH-, -NHC(=O)- or none; R 3 selected from substituted or unsubstituted C 1 -C 30 Alkyl, substituted or unsubstituted C 2 -C 30 Alkenyl, substituted or unsubstituted C 2 -C 30 Alkynyl, substituted or unsubstituted C 3 -C 30 Cycloalkyl, cholane fatty chain, ‑R 3a -C(=O)O-R 3b ,-R 3a -OC(=O)-R 3b ,-R 3a -C(=O)NH-R 3b ,-R 3a -NHC(=O)-R 3b , or -R 3a -S(=O) 1‑2 O‑R 3b and-R 3a -OS (=O) 1‑2 -R 3b The rasagiline prodrug of the present invention has a high melting point and low solubility, and can form a drug storehouse in the body after being administered as an injection, prolonging the release rate of the drug in the body and achieving long-acting treatment. Purpose.

The present invention relates to a preparation method of obeticholic acid dimer. The carboxyl group and hydroxyl group of obeticholic acid are protected to obtain benzyl 3α,7α-dihydroxy-6α-ethyl-5β-cholanoate ( Ⅵ) and 3α, 7α-bis-(4-methoxytriphenylmethyl)-6α-ethyl-5β-cholanic acid (IV), and then esterify compounds Ⅳ and Ⅵ under alkaline conditions , and finally remove the protective groups of the hydroxyl group and the carboxyl group in turn to obtain the obeticholic acid dimer (I). The obeticholic acid dimer prepared in the present invention has high purity and can be well used for the research on impurities of obeticholic acid without further purification.

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.