发明名称 |
氮杂二环己烷衍生物的用途 |
摘要 |
本发明涉及1-[2-氟-4-(三氟甲基)苯基]-3-(3-{[4-甲基-5-(4-甲基-1,3-噁唑-5-基)-4H-1,2,4-三唑-3-基]硫基}丙基)-3-氮杂二环[3.1.0]己烷的酒石酸盐及其溶剂合物、药物制剂、它们的制备方法以及它们在药物中的用途。 |
申请公布号 |
CN101528221B |
申请公布日期 |
2013.05.08 |
申请号 |
CN200780039208.2 |
申请日期 |
2007.08.20 |
申请人 |
葛兰素集团有限公司 |
发明人 |
克莱尔·L·安德顿;瑟吉奥·巴奇;斯蒂芬尼亚·比托;佛朗哥·萨托 |
分类号 |
A61K31/403(2006.01)I;A61P25/30(2006.01)I |
主分类号 |
A61K31/403(2006.01)I |
代理机构 |
北京市柳沈律师事务所 11105 |
代理人 |
孔宪静 |
主权项 |
1.结晶化合物,其为(1S,5R)-1-[2-氟-4-(三氟甲基)苯基]-3-(3-{[4-甲基-5-(4-甲基-1,3-<img file="FSB00000861183000011.GIF" wi="60" he="53" />唑-5-基)-4H-1,2,4-三唑-3-基]硫基}丙基)-3-氮杂二环[3.1.0]己烷(2R,3R)酒石酸盐且为倍半水合物,其具有如图1所示的X-射线粉末衍射光谱,其中所述XRD图以2θ角表示,且采用利用铜Kα辐射的衍射仪获得:<tables num="0001"><table><tgroup cols="2"><colspec colname="c001" colwidth="49%" /><colspec colname="c002" colwidth="50%" /><tbody><row><entry morerows="1"> 角度</entry><entry morerows="1"> d值</entry></row><row><entry morerows="1"> 2θ°</entry><entry morerows="1"> 埃</entry></row><row><entry morerows="1"> 5.9</entry><entry morerows="1"> 15.0</entry></row><row><entry morerows="1"> 6.9</entry><entry morerows="1"> 12.9</entry></row><row><entry morerows="1"> 7.7</entry><entry morerows="1"> 11.4</entry></row><row><entry morerows="1"> 10.2</entry><entry morerows="1"> 8.7</entry></row><row><entry morerows="1"> 11.8</entry><entry morerows="1"> 7.5</entry></row><row><entry morerows="1"> 11.9</entry><entry morerows="1"> 7.4</entry></row><row><entry morerows="1"> 13.4</entry><entry morerows="1"> 6.6</entry></row><row><entry morerows="1"> 14.6</entry><entry morerows="1"> 6.1</entry></row><row><entry morerows="1"> 15.1</entry><entry morerows="1"> 5.8</entry></row><row><entry morerows="1"> 15.5</entry><entry morerows="1"> 5.7</entry></row><row><entry morerows="1"> 15.7</entry><entry morerows="1"> 5.7</entry></row><row><entry morerows="1"> 16.4</entry><entry morerows="1"> 5.4</entry></row><row><entry morerows="1"> 17.1</entry><entry morerows="1"> 5.2</entry></row><row><entry morerows="1"> 17.6</entry><entry morerows="1"> 5.0</entry></row><row><entry morerows="1"> 18.4</entry><entry morerows="1"> 4.8</entry></row><row><entry morerows="1"> 19.3</entry><entry morerows="1"> 4.6</entry></row><row><entry morerows="1"> 19.5</entry><entry morerows="1"> 4.5</entry></row><row><entry morerows="1"> 19.9</entry><entry morerows="1"> 4.5</entry></row><row><entry morerows="1"> 20.4</entry><entry morerows="1"> 4.3</entry></row><row><entry morerows="1"> 20.6</entry><entry morerows="1"> 4.3</entry></row><row><entry morerows="1"> 22.7</entry><entry morerows="1"> 3.9</entry></row><row><entry morerows="1"> 23.6</entry><entry morerows="1"> 3.8</entry></row><row><entry morerows="1"> 24.5</entry><entry morerows="1"> 3.6</entry></row><row><entry morerows="1"> 24.7</entry><entry morerows="1"> 3.6</entry></row><row><entry morerows="1"> 24.9</entry><entry morerows="1"> 3.6</entry></row><row><entry morerows="1"> 25.2</entry><entry morerows="1"> 3.5</entry></row><row><entry morerows="1"> 26.3</entry><entry morerows="1"> 3.4</entry></row><row><entry morerows="1"> 26.5</entry><entry morerows="1"> 3.4</entry></row><row><entry morerows="1"> 27.0</entry><entry morerows="1"> 3.3</entry></row><row><entry morerows="1"> 27.3</entry><entry morerows="1"> 3.3</entry></row><row><entry morerows="1"> 27.5</entry><entry morerows="1"> 3.2</entry></row><row><entry morerows="1"> 27.9</entry><entry morerows="1"> 3.2</entry></row><row><entry morerows="1"> 28.5</entry><entry morerows="1"> 3.1</entry></row><row><entry morerows="1"> 29.8</entry><entry morerows="1"> 3.0</entry></row><row><entry morerows="1"> 30.5</entry><entry morerows="1"> 2.9</entry></row><row><entry morerows="1"> 31.3</entry><entry morerows="1"> 2.9</entry></row><row><entry morerows="1"> 32.3</entry><entry morerows="1"> 2.8</entry></row><row><entry morerows="1"> 34.1</entry><entry morerows="1"> 2.6</entry></row><row><entry morerows="1"> 35.7</entry><entry morerows="1"> 2.5</entry></row><row><entry morerows="1"> 36.1</entry><entry morerows="1"> 2.5</entry></row><row><entry morerows="1"> 36.9</entry><entry morerows="1"> 2.4</entry></row><row><entry morerows="1"> 39.0</entry><entry morerows="1"> 2.3</entry></row><row><entry morerows="1"> 39.2</entry><entry morerows="1"> 2.3</entry></row><row><entry morerows="1"> 39.9</entry><entry morerows="1"> 2.3</entry></row></tbody></tgroup></table></tables> |
地址 |
英国米德尔塞克斯 |