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