Invention Grant
US08163747B2 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
有权
5-(2,4-二羟基-5-异丙基 - 苯基)-4-(4-吗啉-4-基甲基 - 苯基) - 异恶唑-3-甲酸乙酰胺的酸加成盐,水合物和多晶型物和包含这些形式的制剂
- Patent Title: 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
- Patent Title (中): 5-(2,4-二羟基-5-异丙基 - 苯基)-4-(4-吗啉-4-基甲基 - 苯基) - 异恶唑-3-甲酸乙酰胺的酸加成盐,水合物和多晶型物和包含这些形式的制剂
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Application No.: US12529090Application Date: 2008-02-28
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Publication No.: US08163747B2Publication Date: 2012-04-24
- Inventor: Martin James Drysdale , Brian William Dymock , Christoph Krell , Michael Mutz , Holger Petersen , Weijia Zheng
- Applicant: Martin James Drysdale , Brian William Dymock , Christoph Krell , Michael Mutz , Holger Petersen , Weijia Zheng
- Applicant Address: CH Basel GB Winnersh, Berkshire
- Assignee: Novartis AG,Vernalis (R&D) Ltd.
- Current Assignee: Novartis AG,Vernalis (R&D) Ltd.
- Current Assignee Address: CH Basel GB Winnersh, Berkshire
- Agent Gregory Houghton
- Priority: EP07103346 20070301
- International Application: PCT/EP2008/052443 WO 20080228
- International Announcement: WO2008/104595 WO 20080904
- Main IPC: A61K31/535
- IPC: A61K31/535 ; C07D413/10

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.
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