公开(公告)号：US20130296556A1

公开(公告)日：2013-11-07

申请号：US13938659

申请日：2013-07-10

申请人： Martin James Drysdale ,  Brian William Dyrnock ,  Christoph Krell ,  Michael Mutz ,  Holger Petersen ,  Weijia Zheng

发明人： Martin James Drysdale ,  Brian William Dyrnock ,  Christoph Krell ,  Michael Mutz ,  Holger Petersen ,  Weijia Zheng

IPC分类号： C07D295/155

CPC分类号： C07D295/155 ,  A61K31/5377 ,  C07D261/18

摘要： 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, lartrate, phosphate and hemi fumarate slat thereof; to crystalline forms of such salts; to polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-4-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.

摘要翻译： 本发明涉及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-甲酸乙酰胺的新盐形式，特别是 甲磺酸盐，盐酸盐，酒石酸盐，磷酸盐和半富马酸盐盐; 到这种盐的结晶形式; 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-4-甲酸乙酰胺的多晶型物; 到上述新盐形式的水合物和多晶型物; 使用上述新的盐形式来制备用于治疗由Hsp90介导的病症的药物; 涉及使用新的盐形式治疗由Hsp90介导的病症的方法; 包括这种盐形式的制剂，特别是适于静脉内施用的水溶液; 以及填充这种制剂的琥珀色玻璃容器。