| 发明名称 | 托拉塞米化合物 | ||
| 摘要 | 本发明属于医药技术领域，具体涉及托拉塞米及其制备方法，本发明得到的新晶型的托拉塞米，具有的优点：纯度高，最大杂质小于0.5‰；稳定性好；方法重现性好，放大到中试规模，纯度和晶型均能很好重现。本发明还涉及使用新晶型的托拉塞米制造治疗心衰、肾衰、肝硬化腹水、脑水肿等原因引起的中、重度水肿的药物中的应用。 | ||
| 申请公布号 | CN104370805B | 申请公布日期 | 2016.09.07 |
| 申请号 | CN201310349193.7 | 申请日期 | 2013.08.13 |
| 申请人 | 天津汉瑞药业有限公司 | 发明人 | 严洁;李轩 |
| 分类号 | C07D213/74(2006.01)I;A61K31/44(2006.01)I;A61P7/10(2006.01)I | 主分类号 | C07D213/74(2006.01)I |
| 代理机构 | 代理人 | ||
| 主权项 | 式（Ⅰ）的托拉塞米化合物，<img file="dest_path_image001.GIF" wi="363" he="143" />（Ⅰ）其特征在于：用CuKa射线作为特征X射线粉末测定中，其图谱具有下列2θ衍射角和相对强度，其中相对强度(I/I<sub>0</sub>)大于或等于20的如下，<tables num="0001" wi="165"><table><tgroup cols="4"><colspec colname="c001" colwidth="24%" /><colspec colname="c002" colwidth="24%" /><colspec colname="c003" colwidth="31%" /><colspec colname="c004" colwidth="21%" /><tbody><row><entry morerows="1">谱线号</entry><entry morerows="1">2θ（度）</entry><entry morerows="1">晶面间距（d）</entry><entry morerows="1">I/I<sub>0</sub></entry></row><row><entry morerows="1">1</entry><entry morerows="1">10.260</entry><entry morerows="1">8.6146</entry><entry morerows="1">47</entry></row><row><entry morerows="1">2</entry><entry morerows="1">12.840</entry><entry morerows="1">6.8888</entry><entry morerows="1">23</entry></row><row><entry morerows="1">3</entry><entry morerows="1">13.960</entry><entry morerows="1">6.3386</entry><entry morerows="1">51</entry></row><row><entry morerows="1">4</entry><entry morerows="1">19.820</entry><entry morerows="1">4.4757</entry><entry morerows="1">100</entry></row><row><entry morerows="1">5</entry><entry morerows="1">20.560</entry><entry morerows="1">4.3163</entry><entry morerows="1">68</entry></row><row><entry morerows="1">6</entry><entry morerows="1">22.680</entry><entry morerows="1">3.9174</entry><entry morerows="1">30</entry></row><row><entry morerows="1">7</entry><entry morerows="1">25.820</entry><entry morerows="1">3.4477</entry><entry morerows="1">32</entry></row><row><entry morerows="1">8</entry><entry morerows="1">28.120</entry><entry morerows="1">3.1707</entry><entry morerows="1">40</entry></row><row><entry morerows="1">9</entry><entry morerows="1">29.720</entry><entry morerows="1">3.0035</entry><entry morerows="1">34</entry></row><row><entry morerows="1">10</entry><entry morerows="1">30.780</entry><entry morerows="1">2.9025</entry><entry morerows="1">21</entry></row><row><entry morerows="1">11</entry><entry morerows="1">32.180</entry><entry morerows="1">2.7793</entry><entry morerows="1">63</entry></row><row><entry morerows="1">12</entry><entry morerows="1">32.380</entry><entry morerows="1">2.7626</entry><entry morerows="1">61</entry></row><row><entry morerows="1">13</entry><entry morerows="1">32.680</entry><entry morerows="1">2.7379</entry><entry morerows="1">69</entry></row><row><entry morerows="1">14</entry><entry morerows="1">38.680</entry><entry morerows="1">2.3259</entry><entry morerows="1">20</entry></row><row><entry morerows="1">15</entry><entry morerows="1">41.360</entry><entry morerows="1">2.1812</entry><entry morerows="1">24</entry></row></tbody></tgroup></table></tables>2θ衍射角的误差为0.2°,其特征还在于：熔点148.5℃‑149.6℃。 | ||
| 地址 | 300409 天津市北辰区北辰科技园区华实道88号 | ||