发明名称 Maleate salts of (e)-n-{ 4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl} -4-(dimethylamino)-2-butenamide and crystalline forms thereof
摘要 600349 Disclosed herein is a method of preparing (E)-N-{ 4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl} -4-(dimethylamino)-2-butenamide as a maleate, monohydrate salt, comprising reacting the free base with maleic acid in a water-alcohol solution at a temperature in the range of between 50°C to 60°C Specifically, the crystalline form II characterised by X-ray diffraction peaks at the following angles (±0.20°) of 2theta in its X-ray diffraction pattern comprising 6.53, 8.43, 13.01, 15.17 and 16.76. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.
申请公布号 NZ600349(A) 申请公布日期 2013.12.20
申请号 NZ20080600349 申请日期 2008.10.16
申请人 WYETH LLC 发明人 LU QINGHONG;KU MANNCHING SHERRY;CHEW WARREN;CHEAL GLORIA K.;HADFIELD ANTHONY F.;MIRMEHRABI MAHMOUD
分类号 C07D401/12;A61K31/404;A61P35/00 主分类号 C07D401/12
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