30 results about "Cholane" patented technology

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 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.