Process for the preparation of apixaban

US9603846B2 · kind B2 · utility

Assignee

• Cadila Healthcare Ltd. · IN

Inventors

• Brij Khera · Ahmedabad, IN
• Kumar Kamlesh SINGH · Sayla, IN
• Santosh Devidas DIWAKAR · Ahmedabad, IN
• Sunil Dnyaneshwar Narode · Sayla, IN
• Hiteshkumar Natwarlal Suthar · Ahmedabad, IN

Key dates

• Filing date: Nov 24, 2015
• Grant date: Mar 28, 2017
• Expiry date: Nov 24, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A crystalline Form N-1 of apixaban substantially free from one or more of: 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid; 7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-1-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide; or methyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate, relative to apixaban by area percentage of HPLC and having a mean particle size equal to or greater than 100 μm.