Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists

US10392413B2 · kind B2 · utility

Assignee

• ARDELYX, INC. · US

Inventors

• Jason G. Lewis · Castro Valley, US
• Michael R. Leadbetter · Fremont, US
• Jeremy Caldwell · Village of La Jolla, US
• Dean R. Dragoli · Los Altos, US
• Noah Bell · Fremont, US
• Jeffrey W. Jacobs · Fremont, US
• Patricia Finn · Fremont, US
• Rakesh K. Jain · Penfield, US
• Tao Chen · 安丰镇, CN
• Matthew Siegel · Menlo Park, US

Key dates

• Filing date: Dec 19, 2016
• Grant date: Aug 27, 2019
• Expiry date: Dec 19, 2036

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/05
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, diabetes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula: where R1, R2, R2′, R3, R4, X1, X2, X3, X4, Q, and n are described herein.