Process for preparing AG-10, its intermediates, and salts thereof

US10513497B2 · kind B2 · utility

Assignee

• EIDOS THERAPEUTICS, INC. · US

Inventors

• Pooran Chand · Birmingham, US
• Yogesh Gupta · Port Jefferson, US
• Rakesh Kumar Kumawat · San Francisco, US
• Mamoun M. Alhamadsheh · Stockton, US
• Robert Zamboni · Rue du Bois des Loges, CA

Key dates

• Filing date: Feb 16, 2018
• Grant date: Dec 24, 2019
• Expiry date: Feb 16, 2038

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/13
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib as well as crystalline types of Formula IX (AG-10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.