发明名称 一种稳定的阿西替尼化合物
摘要 本发明属于医药技术领域,具体涉及阿西替尼晶体及其制备方法,本发明得到的阿西替尼晶体具有的优点:纯度高;稳定性好,即使在高湿度条件下吸湿增重也不明显。本发明还涉及使用阿西替尼晶体的组合物治疗晚期肾细胞癌的应用。
申请公布号 CN104650034A 申请公布日期 2015.05.27
申请号 CN201310591197.6 申请日期 2013.11.22
申请人 天津市汉康医药生物技术有限公司 发明人 严洁;李轩
分类号 C07D401/06(2006.01)I;A61K31/4439(2006.01)I;A61P35/00(2006.01)I 主分类号 C07D401/06(2006.01)I
代理机构 代理人
主权项 阿西替尼(化合物I),<img file="473503dest_path_image001.GIF" wi="293" he="193" />                         (Ⅰ)所述阿西替尼的晶体,用CuKa射线作为特征X射线粉末测定中,其图谱具有下列2θ衍射角,晶面间距(d值)和相对强度(I/I<sub>0</sub>),<tables num="0001" id="ctbl0001"><table><tgroup cols="4"><colspec colname="c001" colwidth="23%" /><colspec colname="c002" colwidth="27%" /><colspec colname="c003" colwidth="24%" /><colspec colname="c004" colwidth="24%" /><tbody><row><entry morerows="1">No.</entry><entry morerows="1">d(Å)</entry><entry morerows="1">2θ</entry><entry morerows="1">I/I<sub>0</sub></entry></row><row><entry morerows="1">1</entry><entry morerows="1">15.221</entry><entry morerows="1">9.13</entry><entry morerows="1">11</entry></row><row><entry morerows="1">2</entry><entry morerows="1">14.362</entry><entry morerows="1">10.01</entry><entry morerows="1">35</entry></row><row><entry morerows="1">3</entry><entry morerows="1">13.921</entry><entry morerows="1">10.96</entry><entry morerows="1">24</entry></row><row><entry morerows="1">4</entry><entry morerows="1">13.012</entry><entry morerows="1">11.88</entry><entry morerows="1">67</entry></row><row><entry morerows="1">5</entry><entry morerows="1">12.214</entry><entry morerows="1">12.43</entry><entry morerows="1">82</entry></row><row><entry morerows="1">6</entry><entry morerows="1">11.541</entry><entry morerows="1">12.97</entry><entry morerows="1">69</entry></row><row><entry morerows="1">7</entry><entry morerows="1">10.689</entry><entry morerows="1">13.65</entry><entry morerows="1">54</entry></row><row><entry morerows="1">8</entry><entry morerows="1">9.978</entry><entry morerows="1">14.23</entry><entry morerows="1">35</entry></row><row><entry morerows="1">9</entry><entry morerows="1">9.158</entry><entry morerows="1">15.11</entry><entry morerows="1">95</entry></row><row><entry morerows="1">10</entry><entry morerows="1">8.574</entry><entry morerows="1">15.94</entry><entry morerows="1">41</entry></row><row><entry morerows="1">11</entry><entry morerows="1">7.632</entry><entry morerows="1">16.51</entry><entry morerows="1">84</entry></row><row><entry morerows="1">12</entry><entry morerows="1">6.588</entry><entry morerows="1">16.97</entry><entry morerows="1">61</entry></row><row><entry morerows="1">13</entry><entry morerows="1">6.102</entry><entry morerows="1">18.32</entry><entry morerows="1">71</entry></row><row><entry morerows="1">14</entry><entry morerows="1">5.543</entry><entry morerows="1">19.64</entry><entry morerows="1">39</entry></row><row><entry morerows="1">15</entry><entry morerows="1">4.832</entry><entry morerows="1">20.77</entry><entry morerows="1">42</entry></row></tbody></tgroup></table></tables> 2θ衍射角的误差为±0.2。
地址 300409 天津市北辰区北辰科技园区华实道88号
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