发明名称 (4-取代苯甲酰)氟苯水杨酰胺类化合物在制备抗乳腺癌药物中的应用
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在制备抗乳腺癌药物中的应用。本发明的有益效果主要体现在:提供了一种具有抗人乳腺癌作用的(4-取代苯甲酰)氟苯水杨酰胺类化合物,为新药筛选提供研究基础,具有较大应用前景。<img file="DDA0000140618850000011.GIF" wi="891" he="311" />
申请公布号 CN102614200B 申请公布日期 2013.09.11
申请号 CN201210055345.8 申请日期 2012.03.05
申请人 浙江工业大学 发明人 夏春年;曾方;钟光祥;王妮妮;全勇
分类号 A61K31/616(2006.01)I;A61K31/625(2006.01)I;A61P35/00(2006.01)I 主分类号 A61K31/616(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乳腺癌药物中的应用: <img file="FDA00003253716900011.GIF" wi="920" he="338" />式(Ⅱ)中,R为氟、氯或硝基;R<sub>6</sub>为H,R<sub>7</sub>为丙基、环己基或苄基;或者R<sub>6</sub>、R<sub>7</sub>连接成环、与同R<sub>6</sub>、R<sub>7</sub>相连的N构成哌嗪基或取代哌嗪基,所述取代哌嗪基上的取代基为4-甲基或4-乙基; 所述的(4-取代苯甲酰)氟苯水杨酰胺类化合物如式(Ⅱ)所示,为表2化合物之一: 表2: <img file="FDA00003253716900012.GIF" wi="1042" he="1308" />或R<sub>6</sub>为H,R<sub>7</sub>为结构如式(A)所示的取代苯基, <img file="FDA00003253716900021.GIF" wi="477" he="268" />所述(4-取代苯甲酰)氟苯水杨酰胺类化合物如式(Ⅰ)所示,所述(4-取代苯甲酰)氟苯水杨酰胺类化合物为表1化合物之一: <img file="FDA00003253716900022.GIF" wi="888" he="476" />表1: <tables num="0001"><table><tgroup cols="7"><colspec colname="c001" colwidth="14%" /><colspec colname="c002" colwidth="14%" /><colspec colname="c003" colwidth="14%" /><colspec colname="c004" colwidth="14%" /><colspec colname="c005" colwidth="14%" /><colspec colname="c006" colwidth="14%" /><colspec colname="c007" colwidth="14%" /><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-4 </entry><entry morerows="1">F </entry><entry morerows="1">H </entry><entry morerows="1">H </entry><entry morerows="1">CH<sub>3</sub></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-9 </entry><entry morerows="1">F </entry><entry morerows="1">-OCH<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-10 </entry><entry morerows="1">F </entry><entry morerows="1">H </entry><entry morerows="1">H </entry><entry morerows="1">-OCH<sub>3</sub></entry><entry morerows="1">H </entry><entry morerows="1">H </entry></row><row><entry morerows="1">Ⅰ-11 </entry><entry morerows="1">F </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></tbody></tgroup></table></tables><tables num="0002"><table><tgroup cols="7"><colspec colname="c001" colwidth="14%" /><colspec colname="c002" colwidth="14%" /><colspec colname="c003" colwidth="14%" /><colspec colname="c004" colwidth="14%" /><colspec colname="c005" colwidth="14%" /><colspec colname="c006" colwidth="14%" /><colspec colname="c007" colwidth="14%" /><tbody><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-14 </entry><entry morerows="1">Cl </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-16 </entry><entry morerows="1">Cl </entry><entry morerows="1">H </entry><entry morerows="1">H </entry><entry morerows="1">CH<sub>3</sub></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-19 </entry><entry morerows="1">Cl </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-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-22 </entry><entry morerows="1">Cl </entry><entry morerows="1">H </entry><entry morerows="1">H </entry><entry morerows="1">-OCH<sub>3</sub></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-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-32 </entry><entry morerows="1">-NO<sub>2</sub></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-34 </entry><entry morerows="1">-NO<sub>2</sub></entry><entry morerows="1">H </entry><entry morerows="1">H </entry><entry morerows="1">-OCH<sub>3</sub></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>。 
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