Stable polymorph on N-(3-ethynylphenyl)-6, 7-bis (2methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof

US6900221B1 · kind B1 · utility

Assignee

• OSI Pharmaceuticals, LLC · US

Inventors

• Timothy Norris · Gales Ferry, US
• Jeffrey W. Raggon · Uncasville, US
• Richard Connell · Trumbull, US
• James D. Moyer · Downingtown, US
• Michael John MORIN · Waterford, US
• Shama Kajiji · Mystic, US
• Barbara Foster · San Leandro, US
• Karen Ferrante · East Greenwich, US
• Sandra Leta Silberman · Dover, US

Key dates

• Filing date: Nov 9, 2000
• Grant date: May 31, 2005
• Expiry date: Nov 9, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D239/94
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to a stable crystalline form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride designated the B polymorph, its production in essentially pure form, and its use. The invention also relates to the pharmaceutical compositions containing the stable polymorph B form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine as hydrochloride, as well other forms of the compound, and to methods of treating hyperproliferative disorders, such as cancer, by administering the compound.