发明名称 博舒替尼一水合物及其制备方法
摘要 本发明属于医药技术领域,具体涉及博舒替尼一水合物及其制备方法,本发明得到的博舒替尼一水合物,含有一个结晶水,具有的优点:稳定性好、制备过程易于工业化,质量重现性良好、能很好的控制产品纯度。本发明还涉及使用这种水合物的组合物治疗慢性粒细胞性白血病的药物中的应用。
申请公布号 CN104447542A 申请公布日期 2015.03.25
申请号 CN201310418354.3 申请日期 2013.09.16
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 C07D215/54(2006.01)I;A61K31/496(2006.01)I;A61P35/02(2006.01)I 主分类号 C07D215/54(2006.01)I
代理机构 代理人
主权项 式Ⅰ所示博舒替尼的一水合物,<img file="2013104183543100001dest_path_image001.GIF" wi="308" he="165" />                         (Ⅰ)   用卡尔费休法测定,所述水合物含有重量百分比3.00%‑4.00%的水分;所述博舒替尼一水合物的晶体,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">17.459</entry><entry morerows="1">8.52</entry><entry morerows="1">36</entry></row><row><entry morerows="1">2</entry><entry morerows="1">16.325</entry><entry morerows="1">9.01</entry><entry morerows="1">19</entry></row><row><entry morerows="1">3</entry><entry morerows="1">14.762</entry><entry morerows="1">11.48</entry><entry morerows="1">58</entry></row><row><entry morerows="1">4</entry><entry morerows="1">13.854</entry><entry morerows="1">12.21</entry><entry morerows="1">87</entry></row><row><entry morerows="1">5</entry><entry morerows="1">12.789</entry><entry morerows="1">13.63</entry><entry morerows="1">98</entry></row><row><entry morerows="1">6</entry><entry morerows="1">10.368</entry><entry morerows="1">14.15</entry><entry morerows="1">121</entry></row><row><entry morerows="1">7</entry><entry morerows="1">9.856</entry><entry morerows="1">14.82</entry><entry morerows="1">16</entry></row><row><entry morerows="1">8</entry><entry morerows="1">8.936</entry><entry morerows="1">16.09</entry><entry morerows="1">18</entry></row><row><entry morerows="1">9</entry><entry morerows="1">8.120</entry><entry morerows="1">17.33</entry><entry morerows="1">19</entry></row><row><entry morerows="1">10</entry><entry morerows="1">7.154</entry><entry morerows="1">18.10</entry><entry morerows="1">78</entry></row><row><entry morerows="1">11</entry><entry morerows="1">6.657</entry><entry morerows="1">18.93</entry><entry morerows="1">56</entry></row><row><entry morerows="1">12</entry><entry morerows="1">5.869</entry><entry morerows="1">20.11</entry><entry morerows="1">68</entry></row><row><entry morerows="1">13</entry><entry morerows="1">5.157</entry><entry morerows="1">21.32</entry><entry morerows="1">17</entry></row><row><entry morerows="1">14</entry><entry morerows="1">4.681</entry><entry morerows="1">23.49</entry><entry morerows="1">69</entry></row><row><entry morerows="1">15</entry><entry morerows="1">4.412</entry><entry morerows="1">24.60</entry><entry morerows="1">85</entry></row><row><entry morerows="1">16</entry><entry morerows="1">2.462</entry><entry morerows="1">25.88</entry><entry morerows="1">49</entry></row><row><entry morerows="1">17</entry><entry morerows="1">1.511</entry><entry morerows="1">26.94</entry><entry morerows="1">76</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