发明名称 |
一种(4-取代苯甲酰)氟苯水杨酰胺类化合物及应用 |
摘要 |
本发明公开了一种如式(II)所示的(4-取代苯甲酰)氟苯水杨酰胺类化合物,并公开了所述(4-取代苯甲酰)氟苯水杨酰胺类化合物在制备抗肿瘤药物中、特别是在制备抗子宫内膜癌药物中的应用。本发明的有益效果主要体现在:(1)提供了一种(4-取代苯甲酰)氟苯水杨酰胺类化合物的制备方法;(2)提供了一种新的、有明显抗肿瘤活性的抗子宫内膜癌药物,为新药筛选提供研究基础,具有重大应用前景;(3)制备流程简单,利于产业化生产。<img file="DDA0000140620370000011.GIF" wi="891" he="311" />。 |
申请公布号 |
CN102557983B |
申请公布日期 |
2014.06.11 |
申请号 |
CN201210055432.3 |
申请日期 |
2012.03.05 |
申请人 |
浙江工业大学 |
发明人 |
钟光祥;王妮妮;吕亚萍;夏春年;全勇;曾方;胡汪焱;李凌云 |
分类号 |
C07C235/64(2006.01)I;A61K31/616(2006.01)I;A61P35/00(2006.01)I |
主分类号 |
C07C235/64(2006.01)I |
代理机构 |
杭州天正专利事务所有限公司 33201 |
代理人 |
黄美娟;王兵 |
主权项 |
1.一种如式(Ⅱ)所示的(4-取代苯甲酰)氟苯水杨酰胺类化合物在制备抗子宫内膜癌药物中的应用:<img file="FDA0000411634600000011.GIF" wi="915" he="333" />式(Ⅱ)中,R<sub>6</sub>为H,R<sub>7</sub>为环己基或苄基,为表2化合物之一:表2:<tables num="0001"><table><tgroup cols="4"><colspec colname="c001" colwidth="22%" /><colspec colname="c002" colwidth="20%" /><colspec colname="c003" colwidth="27%" /><colspec colname="c004" colwidth="31%" /><tbody><row><entry morerows="1">化合物</entry><entry morerows="1">R</entry><entry morerows="1">R<sub>6</sub></entry><entry morerows="1">R<sub>7</sub></entry></row><row><entry morerows="1">Ⅱ-1</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">苄基</entry></row><row><entry morerows="1">Ⅱ-2</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">环己基</entry></row></tbody></tgroup></table></tables>或者R<sub>7</sub>为或结构如式(A)所示的取代苯基:<img file="FDA0000411634600000012.GIF" wi="297" he="273" />(A)所述(4-取代苯甲酰)氟苯水杨酰胺类化合物如式(Ⅰ)所示,为表1化合物之一:<img file="FDA0000411634600000013.GIF" wi="905" he="493" />表1:<tables num="0002"><table><tgroup cols="7"><colspec colname="c001" colwidth="17%" /><colspec colname="c002" colwidth="13%" /><colspec colname="c003" colwidth="13%" /><colspec colname="c004" colwidth="13%" /><colspec colname="c005" colwidth="13%" /><colspec colname="c006" colwidth="13%" /><colspec colname="c007" colwidth="18%" /><tbody><row><entry morerows="1">化合物</entry><entry morerows="1">R</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><entry morerows="1">R<sub>4</sub></entry><entry morerows="1">R<sub>5</sub></entry></row><row><entry morerows="1">Ⅰ-1</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-2</entry><entry morerows="1">F</entry><entry morerows="1">CH<sub>3</sub></entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-3</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">CH<sub>3</sub></entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-5</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-6</entry><entry morerows="1">F</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-7</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-8</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-12</entry><entry morerows="1">F</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-13</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-15</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">CH<sub>3</sub></entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-17</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-20</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-23</entry><entry morerows="1">Cl</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-24</entry><entry morerows="1">Cl</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-26</entry><entry morerows="1">-NO<sub>2</sub></entry><entry morerows="1">CH<sub>3</sub></entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-29</entry><entry morerows="1">-NO<sub>2</sub></entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">F</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-31</entry><entry morerows="1">-NO<sub>2</sub></entry><entry morerows="1">H</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">H</entry></row><row><entry morerows="1">Ⅰ-36</entry><entry morerows="1">-NO<sub>2</sub></entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry><entry morerows="1">H</entry><entry morerows="1">Cl</entry><entry morerows="1">H</entry></row></tbody></tgroup></table></tables>。 |
地址 |
310014 浙江省杭州市下城区朝晖六区潮王路18号 |