Abstract: The application relates to compounds of formula A: or a salt, solvate, ester, tautomer, amino acide conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

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

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

Abstract: The present invention provides an NASH therapeutic agent including: an FXR agonist, preferably obeticholic acid or a pharmaceutically acceptable salt thereof; and an ARB or a pharmaceutically acceptable salt thereof.

Abstract: The present invention pertains to an oral preparation having exceptional elutability, the oral preparation containing obeticholic acid or a pharmacologically acceptable salt thereof, a water-soluble excipient, a disintegrating agent, and a water-soluble polymer binder, wherein the oral preparation is a quick-release tablet.

Abstract: The present invention relates to a pharmaceutical composition comprising a combination of an FXR agonist and a fibrate. Also disclosed is use of the combination for the treatment, amelioration or prevention of an FXR mediated disease or condition, such as primary biliary cholangitis (PBC).

Abstract: The application relates to compounds of formula A: or a salt, solvate, ester, tautomer, amino acid conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

Abstract: The present application provides Compound 1: or a pharmaceutically acceptable salt or amino acid conjugate thereof. The present invention relates to an FXR activator and to methods of making and using said compound.

Abstract: The present invention relates to a pharmaceutical composition comprising a combination of an FXR agonist and at least one lipid lowering agent (e.g., PPAR-alpha agonist, PPAR-delta agonist, PPAR-alpha and delta dual agonist, and/or statin). Also disclosed is use of the combination for the treatment or prevention of a FXR mediated disease or condition, such as primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), portal hypertension, bile acid diarrhea, NAFLD (nonalcoholic fatty liver disease), NASH (non-alcohol-induced steatohepatitis), and other chronic liver diseases. The combination of the present invention is useful for the treatment or prevention of conditions related to elevated lipid and liver enzyme levels. The present invention also relates to packs or kits including the pharmaceutical combination.

Abstract: The present invention relates to methods and novel intermediates useful in the preparation of a compound of formula (A) or a pharmaceutically acceptable salt thereof, comprising converting the aldehyde of a compound of formula (B) with a reducing agent to prepare a compound of formula (C) and converting the compound of formula (C) with a sulfating reagent to prepare a compound of formula (A). An objective of the present invention is to provide methods of preparing bile acid derivatives and novel intermediates. A use of the methods and intermediates described relates to the synthesis of bile acid derivatives which activate both FXR and TGR5.

Abstract: The present disclosure relates to methods and novel intermediates useful in the preparation of a compound of formula I or pharmaceutically acceptable salt, hydrate, solvate or amino acid, sulfate or glucuronide conjugate, or prodrug thereof, comprising the step of reacting a compound of formula I-4 with a halogenating reagent to provide a compound of formula I-5a

Abstract: The present application provides a compound of formula I: or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1-R10, m, n, p, and are as described herein. The present invention relates generally to FXR modulators and to methods of making and using said compounds.

Abstract: The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1, R2, R3, R4, R5, and R6 are as described herein. The present invention relates generally to selective FXR agonists and to methods of making and using them.

Abstract: The present invention relates to a method for inhibiting fibrosis that occurs in an organ where the farnesoid X receptor (FXR) is expressed. This method involves the step of administering a high potency, activating ligand of FXR in an effective amount to a patient who is not suffering from a cholestatic condition. The invention also provides pharmaceutical compositions containing an effective amount of an FXR ligand and kits for dispensing the pharmaceutical compositions.

Abstract: The present application relates to a pharmaceutical composition comprising a combination of an FXR agonist and at least one additional therapeutic agent that lowers the glucose level in the blood, stimulates insulin secretion, and/or increases insulin sensitivity. The present application relates to use of the pharmaceutical composition for the treatment or prevention of a FXR mediated disease or condition, such as NAFLD and NASH, a disease or condition related to an elevated level of glucose in the blood, decreased secretion of insulin, and/or decreased insulin sensitivity such as hyperglycemia, diabetes, obesity, and insulin resistance, or for lowering the glucose level in the blood, stimulating insulin secretion, and/or increasing insulin sensitivity.

Abstract: The present application provides Compound 1: or a pharmaceutically acceptable salt or amino acid conjugate thereof. The present invention relates to an FXR activator and to methods of making and using said compound.

Abstract: The application relates to compounds of formula A: or a salt, solvate, ester, tautomer, amino acid conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

Abstract: The disclosure relates to obeticholic acid formulations with improved stability, dissolution, and/or solubility, methods of preparing the same for use and methods of treating various diseases and conditions.

Abstract: The disclosure relates to obeticholic acid formulations with improved stability, dissolution, and/or solubility, methods of preparing the same for use and methods of treating various diseases and conditions.

Abstract: The invention relates to compounds of formula (I): wherein R is ethyl and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.