Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl) -phenylamino]-pyrimidin-4-yl}-1-methyl-urea and salts thereof

US9067896B2 · kind B2 · utility

Assignee

• Novartis AG · CH

Inventors

• Joerg Berghausen · Vilsbiburg, DE
• Prasad Koteswara Kapa · Parsippany, US
• Joseph McKenna · London, GB
• Joel Slade · Flanders, US
• Raeann Wu · Montville, US
• Zhengming Du · Beijing, CN
• Frank Stowasswer · Murg, DE

Key dates

• Filing date: Dec 6, 2010
• Grant date: Jun 30, 2015
• Expiry date: Feb 24, 2031

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present technology provides novel anhydrous and hydrated crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea, amorphous and anhydrous crystalline polymorphs of its monophosphoric acid salt, and the hydrochloride salt, including its dihydrate. The present technology further provides methods for preparing the various forms, compositions containing them, and methods of treatment employing them.