C07J41/0094

BILE ACID DERIVATIVES AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF

The present invention provides compounds of Formula I,

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pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.

METHOD FOR PREPARING CHOLIC ACID COMPOUND

The present application belongs to the field of pharmaceutical chemistry, and relates to a method for preparing a cholic acid compound. Specifically, the present application provides a process for preparing a compound as shown in formula I, comprising subjecting a compound of formula 2 to an oxidization reaction to obtain a compound of formula 3; attaching a trimethylsilyl group to the compound of formula 3 to obtain a compound of formula 4; reacting the compound of formula 4 with acetaldehyde to obtain a compound of formula 5; subjecting the compound of formula 5 to a catalytic hydrogenation reaction to obtain a compound of formula 6; and converting a cyano group of the compound of formula 6 to a carboxyl group to give the compound of formula I. The preparation method has high yield, requires less purification operations, and is suitable for industrial application.

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PROCESS FOR PREPARING HIGH PURITIY ALLOPREGNANOLONE AND INTERMEDIATES THEREOF

The invention relates to an efficient and industrially applicable process for the preparation and purification of allopregnanolone and intermediates thereof without the assistance of column chromatography.

Process and intermediates for the 6,7-alpha-epoxidation of steroid 4,6-dienes

The invention relates to a process for preparing a compound of general formula (Ia): wherein R.sup.2, Y, R.sup.4 and R.sup.5 are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.

PREPARATION OF DEOXYCHOLIC ACID

The present invention relates to new and improved processes for the preparation of deoxycholic acid (DCA) and pharmaceutically acceptable salts thereof, as well as to DCA and pharmaceutically acceptable salts thereof, the carbon atoms of which are derived partially or solely from plant sources.

COMPOSITIONS AND METHODS FOR TREATING CLOSTRIDIUM ASSOCIATED DISEASES

The present disclosure provides compounds for preventing, treating, and/or reducing the risk of developing a Clostridium-associated disease in a mammalian subject. Also provided are pharmaceutically acceptable salts of such compounds and compositions that include such compounds and/or pharmaceutically acceptable salts thereof.

Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof

The present invention provides compounds of Formula I, ##STR00001##
pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.

SCROLL COMPOSITE HAVING AMPHIPHILIC SUBSTANCE INSIDE AND METHOD FOR PREPARATION OF THE SAME
20200165136 · 2020-05-28 ·

Provided are a scroll preparing method using a two-dimensional material and a scroll prepared thereby. The scroll preparing method comprises preparing a two-dimensional material. The two-dimensional material is scrolled by providing an amphiphilic substance having a hydrophilic portion and a hydrophobic portion on the two-dimensional material. As a result, a scroll composite including the amphiphilic substance disposed inside a scroll structure is formed.

ISOTOPICALLY LABELED BILE ACID DERIVATIVES
20200165290 · 2020-05-28 ·

The present application relates to isotopically labeled compounds of Formula I and methods of preparation and use thereof.

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COMPOUND FOR TREATING METABOLIC DISEASES AND PREPARATION METHOD AND USE THEREOF
20200131212 · 2020-04-30 ·

Provided are a compound for treating metabolic diseases having the structure as shown in formula (I) or formula (II), or a racemate, stereoisomer, geometric isomer, tautomer, solvate, hydrate, metabolite, pharmaceutically acceptable salt or prodrug thereof. The compound is an activator of FXR and/or a TGR5 receptor, and thus has the activity of activating FXR and/or a TGR5 receptor, and can be used in the preparation of drugs for treating chronic liver diseases, metabolic diseases or portal hypertension.