发明名称 |
Emetine derivatives, prodrugs containing same, and methods of treating conditions using same |
摘要 |
Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2′-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia. |
申请公布号 |
US9492560(B2) |
申请公布日期 |
2016.11.15 |
申请号 |
US201313828877 |
申请日期 |
2013.03.14 |
申请人 |
Bakare Oladapo;Denmeade Samuel Ray;Akinboye Emmanuel S. |
发明人 |
Bakare Oladapo;Denmeade Samuel Ray;Akinboye Emmanuel S. |
分类号 |
A61K47/48;C07D455/08;C07D401/06 |
主分类号 |
A61K47/48 |
代理机构 |
Fitch, Even, Tabin & Flannery LLP |
代理人 |
Fitch, Even, Tabin & Flannery LLP |
主权项 |
1. A compound comprising formula (I): where M is selected from the group consisting of: and where: X1=H, —NO2, —CO2X2, —OX3, halogen, or C1-C4 alkyl, X2=C1-C4 alkyl or H, X3=C1-C4 alkyl or H, Q=OH, V+O−, V=metal ion, Y=H or C1-C6 alkyl, Z=H, C1-C4 alkyl, or halogen, p=0 to 8, and t=1 to 4, and wherein when M is the compound is selected from the group consisting of |
地址 |
Beltsville MD US |