Acid addition salts, hydrates and polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide and formulations comprising these forms

US8163747B2 · kind B2 · utility

Assignees

• Novartis AG · CH
• VERNALIS (R&D) LTD · GB

Inventors

• Martin James Drysdale · Winnersh, GB
• Brian William Dymock · Singapore, SG
• Christoph Max Krell · Basel, CH
• Michael Mutz · Glückstadt, DE
• Holger Petersen · Pastetten, DE
• Weijia Zheng · Cambridge, US

Key dates

• Filing date: Feb 28, 2008
• Grant date: Apr 24, 2012
• Expiry date: Feb 24, 2029

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D261/18
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to new salt forms of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide, in particular the mesylate, hydrochloride, tartrate, phosphate and hemi fumarate salt thereof; to crystalline forms of such salts; to polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide; to hydrates and polymorphs of the new salt forms mentioned above; to the use of the new salt forms mentioned above for the manufacture of a medicament for the treatment of a disorder mediated by Hsp90; to a method for treating a disorder mediated by Hsp90 using the new salt forms; to formulations comprising such salt forms, in particular aqueous solutions suitable for intravenous administration; and to amber glass containers being filled with such formulations.