| 发明名称 | 曲氟沙星的两性离子形式 | ||
| 摘要 | 本发明涉及有式(Ⅰ)的曲氟沙星的两性离子形式,选自于其结晶的收湿的或非收湿的多晶型物和五水合物以及它们的制备方法。本发明还涉及本发明化合物的使用方法和包含本发明化合物的药物组合物,用于治疗哺乳动物的细菌感染。 | ||
| 申请公布号 | CN1190889A | 申请公布日期 | 1998.08.19 |
| 申请号 | CN96195624.0 | 申请日期 | 1996.07.29 |
| 申请人 | 美国辉瑞有限公司 | 发明人 | 道格拉斯·J·M·艾伦;戴维·B·约瑟夫;蒂莫西·诺里斯 |
| 分类号 | A61K31/435;C07D471/04 | 主分类号 | A61K31/435 |
| 代理机构 | 柳沈知识产权律师事务所 | 代理人 | 巫肖南 |
| 主权项 | 1.一种式I的曲氟沙星两性离子晶体形式：<img file="A9619562400021.GIF" wi="887" he="617" />选自；a)表现为如下特征X-射线粉末衍射图案的非收湿第一多晶型物PI <tables id="table1" num="001"><table width="602"><tgroup cols="10"><colspec colname="c001" colwidth="19%" /><colspec colname="c002" colwidth="9%" /><colspec colname="c003" colwidth="9%" /><colspec colname="c004" colwidth="9%" /><colspec colname="c005" colwidth="9%" /><colspec colname="c006" colwidth="9%" /><colspec colname="c007" colwidth="9%" /><colspec colname="c008" colwidth="8%" /><colspec colname="c009" colwidth="9%" /><colspec colname="c010" colwidth="10%" /><thead><row><entry morerows="1"> 峰数 </entry><entry morerows="1"> 1 </entry><entry morerows="1"> 2 </entry><entry morerows="1"> 3 </entry><entry morerows="1"> 4 </entry><entry morerows="1"> 5 </entry><entry morerows="1"> 6 </entry><entry morerows="1"> 7 </entry><entry morerows="1"> 8 </entry><entry morerows="1"> 9 </entry></row></thead><tbody><row><entry morerows="1"> 2_θ_(°)Cu </entry><entry morerows="1"> 6.9 </entry><entry morerows="1"> 9.8 </entry><entry morerows="1"> 11.3 </entry><entry morerows="1"> 12.0 </entry><entry morerows="1"> 13.9 </entry><entry morerows="1"> 16.1 </entry><entry morerows="1"> 16.6 </entry><entry morerows="1"> 17.1 </entry><entry morerows="1"> 17.4 </entry></row><row><entry morerows="1"> d距离 </entry><entry morerows="1"> 12.7 </entry><entry morerows="1"> 9.0 </entry><entry morerows="1"> 7.9 </entry><entry morerows="1"> 7.4 </entry><entry morerows="1"> 6.4 </entry><entry morerows="1"> 5.5 </entry><entry morerows="1"> 5.4 </entry><entry morerows="1"> 5.2 </entry><entry morerows="1"> 5.1 </entry></row><row><entry morerows="1"> 峰数 </entry><entry morerows="1"> 10 </entry><entry morerows="1"> 11 </entry><entry morerows="1"> 12 </entry><entry morerows="1"> 13 </entry><entry morerows="1"> 14 </entry><entry morerows="1"> 15 </entry><entry morerows="1"></entry><entry morerows="1"></entry><entry morerows="1"></entry></row><row><entry morerows="1"> 2_θ_(°)Cu </entry><entry morerows="1"> 19.7 </entry><entry morerows="1"> 20.3 </entry><entry morerows="1"> 21.2 </entry><entry morerows="1"> 22.8 </entry><entry morerows="1"> 23.8 </entry><entry morerows="1"> 26.3 </entry><entry morerows="1"></entry><entry morerows="1"></entry><entry morerows="1"></entry></row><row><entry morerows="1"> d距离 </entry><entry morerows="1"> 4.5 </entry><entry morerows="1"> 4.4 </entry><entry morerows="1"> 4.2 </entry><entry morerows="1"> 3.9 </entry><entry morerows="1"> 3.7 </entry><entry morerows="1"> 3.4 </entry><entry morerows="1"></entry><entry morerows="1"></entry><entry morerows="1"></entry></row></tbody></tgroup></table></tables>b)表现为如下特性X-射线粉末衍射图案的收湿第二多晶型物PII <tables id="table2" num="002"><table width="554"><tgroup cols="9"><colspec colname="c001" colwidth="19%" /><colspec colname="c002" colwidth="11%" /><colspec colname="c003" colwidth="10%" /><colspec colname="c004" colwidth="10%" /><colspec colname="c005" colwidth="10%" /><colspec colname="c006" colwidth="10%" /><colspec colname="c007" colwidth="10%" /><colspec colname="c008" colwidth="10%" /><colspec colname="c009" colwidth="10%" /><thead><row><entry morerows="1"> 峰数 </entry><entry morerows="1"> 1 </entry><entry morerows="1"> 2 </entry><entry morerows="1"> 3 </entry><entry morerows="1"> 4 </entry><entry morerows="1"> 5 </entry><entry morerows="1"> 6 </entry><entry morerows="1"> 7 </entry><entry morerows="1"> 8 </entry></row></thead><tbody><row><entry morerows="1"> 2_θ_(°)Cu </entry><entry morerows="1"> 8.4 </entry><entry morerows="1"> 9.5 </entry><entry morerows="1"> 10.2 </entry><entry morerows="1"> 14.7 </entry><entry morerows="1"> 16.8 </entry><entry morerows="1"> 17.9 </entry><entry morerows="1"> 22.6 </entry><entry morerows="1"> 26.1 </entry></row><row><entry morerows="1"> d距离 </entry><entry morerows="1"> 10.6 </entry><entry morerows="1"> 9.3 </entry><entry morerows="1"> 8.7 </entry><entry morerows="1"> 6.0 </entry><entry morerows="1"> 5.3 </entry><entry morerows="1"> 5.0 </entry><entry morerows="1"> 3.9 </entry><entry morerows="1"> 3.4 </entry></row></tbody></tgroup></table></tables>和c)五水合物，表现为如下特性X-射线粉末衍射图案的曲氟沙星两 性离子五水合物。 <tables id="table3" num="003"><table width="592"><tgroup cols="10"><colspec colname="c001" colwidth="16%" /><colspec colname="c002" colwidth="9%" /><colspec colname="c003" colwidth="9%" /><colspec colname="c004" colwidth="9%" /><colspec colname="c005" colwidth="9%" /><colspec colname="c006" colwidth="9%" /><colspec colname="c007" colwidth="9%" /><colspec colname="c008" colwidth="9%" /><colspec colname="c009" colwidth="9%" /><colspec colname="c010" colwidth="11%" /><thead><row><entry morerows="1"> 峰数 </entry><entry morerows="1"> 1 </entry><entry morerows="1"> 2 </entry><entry morerows="1"> 3 </entry><entry morerows="1"> 4 </entry><entry morerows="1"> 5 </entry><entry morerows="1"> 6 </entry><entry morerows="1"> 7 </entry><entry morerows="1"> 8 </entry><entry morerows="1"> 9 </entry></row></thead><tbody><row><entry morerows="1"> 2_θ_(°) Cu </entry><entry morerows="1"> 6.6 </entry><entry morerows="1"> 8.6 </entry><entry morerows="1"> 12.7 </entry><entry morerows="1"> 13.3 </entry><entry morerows="1"> 15.9 </entry><entry morerows="1"> 18.6 </entry><entry morerows="1"> 19.2 </entry><entry morerows="1"> 20.1 </entry><entry morerows="1"> 21.0 </entry></row><row><entry morerows="1"> d距离 </entry><entry morerows="1"> 13.3 </entry><entry morerows="1"> 10.3 </entry><entry morerows="1"> 7.0 </entry><entry morerows="1"> 6.6 </entry><entry morerows="1"> 5.5 </entry><entry morerows="1"> 4.8 </entry><entry morerows="1"> 4.6 </entry><entry morerows="1"> 4.4 </entry><entry morerows="1"> 4.2 </entry></row><row><entry morerows="1"> 峰数 </entry><entry morerows="1"></entry><entry morerows="1"> 10 </entry><entry morerows="1"> 11 </entry><entry morerows="1"> 12 </entry><entry morerows="1"> 13 </entry><entry morerows="1"> 14 </entry><entry morerows="1"> 15 </entry><entry morerows="1"> 16 </entry><entry morerows="1"> 17 </entry></row><row><entry morerows="1"> 2_θ_(°) Cu </entry><entry morerows="1"></entry><entry morerows="1"> 22.6 </entry><entry morerows="1"> 22.9 </entry><entry morerows="1"> 23.6 </entry><entry morerows="1"> 24.9 </entry><entry morerows="1"> 25.4 </entry><entry morerows="1"> 25.9 </entry><entry morerows="1"> 27.7 </entry><entry morerows="1"> 29.5 </entry></row><row><entry morerows="1"> d距离 </entry><entry morerows="1"></entry><entry morerows="1"></entry><entry morerows="1"> 3.9 </entry><entry morerows="1"> 3.8 </entry><entry morerows="1"> 3.6 </entry><entry morerows="1"> 3.5 </entry><entry morerows="1"> 3.4 </entry><entry morerows="1"> 3.2 </entry><entry morerows="1"> 3.0 </entry></row></tbody></tgroup></table></tables> | ||
| 地址 | 美国纽约州 | ||