发明名称 紫杉醇衍生物、其制备方法和其药物组合物与用途
摘要 本发明公开了一类侧链含有二级胺基团,水溶性好的新的紫杉醇衍生物,如通式(I)所示,这类化合物其制备方法,含有这类化合物的药物组合物,以及化合物用于制备治疗癌症药物中的应用。<img file="b06178949920060516a000011.GIF" wi="851" he="513" />
申请公布号 CN101062925B 申请公布日期 2012.08.22
申请号 CN200610078949.9 申请日期 2006.04.28
申请人 中国医学科学院药物研究所 发明人 吴克美;叶仙蓉;籍秀娟;张福荣;王凤
分类号 C07D305/14(2006.01)I;C07D417/12(2006.01)I;A61K31/337(2006.01)I;A61P35/00(2006.01)I 主分类号 C07D305/14(2006.01)I
代理机构 北京三高永信知识产权代理有限责任公司 11138 代理人 何文彬
主权项 1.选自下列组群的化合物:<img file="FFW00000057052700011.GIF" wi="914" he="548" /><tables num="0001"><table><tgroup cols="4"><colspec colname="c001" colwidth="20%" /><colspec colname="c002" colwidth="19%" /><colspec colname="c003" colwidth="35%" /><colspec colname="c004" colwidth="25%" /><tbody><row><entry morerows="1">  化合物</entry><entry morerows="1">  R<sub>1</sub></entry><entry morerows="1">  R<sub>2</sub></entry><entry morerows="1">  R<sub>3</sub></entry></row><row><entry morerows="1">  I<sub>1</sub></entry><entry morerows="1">  OH</entry><entry morerows="1">  对甲氧基苄基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>2</sub></entry><entry morerows="1">  OH</entry><entry morerows="1">  间氟苄基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>3</sub></entry><entry morerows="1">  OH</entry><entry morerows="1">  苄基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>4</sub></entry><entry morerows="1">  OH</entry><entry morerows="1">  2-噻唑甲基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>5</sub></entry><entry morerows="1">  OH</entry><entry morerows="1">  对二甲基氨基苄基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>6</sub></entry><entry morerows="1">  OH</entry><entry morerows="1">  对氯苄基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>7</sub></entry><entry morerows="1">  OH</entry><entry morerows="1">  环戊基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>8</sub></entry><entry morerows="1">  OH</entry><entry morerows="1">  环己基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>9</sub></entry><entry morerows="1">  OAc</entry><entry morerows="1">  苄基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>10</sub></entry><entry morerows="1">  OAc</entry><entry morerows="1">  对氯苄基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>11</sub></entry><entry morerows="1">  OAc</entry><entry morerows="1">  间氟苄基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>12</sub></entry><entry morerows="1">  OAc</entry><entry morerows="1">  对甲氧基苄基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>13</sub></entry><entry morerows="1">  OAc</entry><entry morerows="1">  2-噻唑甲基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>14</sub></entry><entry morerows="1">  OAc</entry><entry morerows="1">  环己基</entry><entry morerows="1">  Ph</entry></row><row><entry morerows="1">  I<sub>15</sub>     </entry><entry morerows="1">  OAc</entry><entry morerows="1">  环戊基</entry><entry morerows="1">  Ph</entry></row></tbody></tgroup></table></tables>。
地址 100050 北京市宣武区先农坛街1号