Intercept Pharmaceuticals, Inc.

Ardea Biosciences, Inc

Gabriel Galvin

Jean-Luc Girardet

Irina Zamansky

Mathew Yanik

Roberto Pellicciari

Esmir Gunic

Antimo Gioiello

Laszlo R Treiber

Kevin Schaab

Myoung Goo Kim

Ronald D Lewis, Ii

Bartjan Koning

Thomas Hensel

Frederik Ronald Leusink

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

Isotopically labeled bile acid derivatives

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 

Methods and intermediates for the preparation of bile acid derivatives

The present application relates to a method of preparing compounds of Formula (A) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof. 

Methods for preparation of bile acids and derivatives thereof

The present application relates to a method of preparing a bile acid derivative or a pharmaceutical acceptable salt, solvate, or amino acid conjugate thereof, comprising direct alkylation of a carbon atom at the C-6 position of 7 keto lithocholic acid (KLCA) with an alkylating agent and reduction of a keto group at the C-7 position.

Methods for the preparation of obeticholic acid and derivatives thereof

Described herein are certain processes for the synthesis of compounds of Formula (I): 

Manufacture of 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid

Crystalline polymorph forms of 2-(5-bromo-4-(4-cyclopropyl naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented.

[object Object]

Crystalline polymorphs and solid mesophase forms of sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate are described. In addition, pharmaceutical compositions and uses of such compositions for the treatment of a variety of diseases and conditions are provided.

Growing community of inventors

San Diego, CA, United States of America

Gabriel Galvin