TGF-beta inhibitors

US9884868B2 · kind B2 · utility

Assignees

• Rigel Pharmaceuticals, Inc. · US
• Bristol-Myers Squibb Company · US

Inventors

• Todd Kinsella · Redwood City, US
• Marina Gelman · San Francisco, US
• Hui Hong · Palo Alto, US
• Ihab Darwish · Redwood City, US
• Rajinder Singh · Belmont, US
• Jiaxin Yu · Redwood City, US
• Robert M. Borzilleri · Haneys Mill, US
• Upender Velaparthi · Princeton Junction, US
• Peiying Liu · Madison, US
• Chetan Padmakar Darne · Orange, US
• Hasibur Rahaman · Bengaluru, IN
• Jayakumar Sankara Warrier · Bengaluru, IN

Key dates

• Filing date: Feb 26, 2016
• Grant date: Feb 6, 2018
• Expiry date: Mar 17, 2036

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structureand pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.