C07J41/0094

Cholane derivatives for use in the treatment and/or prevention of FXR and TGR5/GPBAR1 mediated diseases

The present invention relates to compounds having cholane scaffolds of formula (I), ##STR00001##
said compounds for use in the treatment and/or prevention of FXR and TGR5/GPBARI mediated diseases.

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.

Inhibitors of glucocorticoid receptor

The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism.

Method for preparing cholic acid compound

The present application relates to a method for preparing a cholic acid compound. Specifically, the method prepares a compound as shown in formula I, including 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. ##STR00001## ##STR00002##

3-(4'-SUBSTITUTED)-BENZYL-ETHER DERIVATIVES OF PREGNENOLONE

The invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 is C1-8 alkyl, C1-8 alkoxy, CN, NO.sub.2, amino, COOH, COOCH.sub.3, OH, N.sub.3, or halogen and R2 is H, OH, C1-8 alkyl, C1-8 alkoxy, C2-C6 alkenyl, halogen, Bn-O—, Bn- optionally substituted, or Ph- optionally substituted.

##STR00001##

Neuroactive steroids, compositions, and uses thereof

Described herein are neuroactive steroids of the Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof; wherein R.sup.1a and R.sup.1b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

Intermediates for the Synthesis of Bile Acid Derivatives, in Particular of Obeticholic Acid

The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):

##STR00001##

wherein: custom-character, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Y are as defined herein.

The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

Inhibitors of glucocorticoid receptor

The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism.

NEUROACTIVE STEROIDS AND COMPOSITIONS AND METHODS THEREOF
20210188897 · 2021-06-24 ·

The invention provides novel neuroactive steroids and pharmaceutical compositions thereof, as well as methods of their preparation and use, in therapy of various diseases and conditions, for example, various neurological or brain diseases.

Compound for treating metabolic diseases and preparation method and use thereof

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.