| 发明名称 | Gain-of-function Bcl-2 inhibitors | ||
| 摘要 | Compounds are described that are useful for treating an apoptosis-associated disease, which are specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Also described is a method for treating an apoptosis-associated disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of an active compound that is specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Several scaffolds of active compounds are described. | ||
| 申请公布号 | US8865901(B2) | 申请公布日期 | 2014.10.21 |
| 申请号 | US201213437795 | 申请日期 | 2012.04.02 |
| 申请人 | Fred Hutchinson Cancer Research Center | 发明人 | Hockenbery David;Simon Julian |
| 分类号 | A61K31/47;C07D217/22;C07D401/12;C07C251/86;C07D271/08;C07D213/77;C07C323/20;C07C235/60 | 主分类号 | A61K31/47 |
| 代理机构 | Baker & Hostetler LLP | 代理人 | Baker & Hostetler LLP |
| 主权项 | 1. An isolated compound consisting of Formula I wherein: R1 is OH, Cl, or methoxy;R2 is NO2, t-butyl or methoxy;R3 is H, methyl, or t-butyl;R4 is H, Cl, Br, t-butyl, or methylR5 is H, Cl, or OH; andR6 is wherein A is CH or N;R7 is H, NO2, or CF3; andR8 is H or Cl;or a salt, or a hydrate, or a solvate of any of the foregoing. | ||
| 地址 | Seattle WA US | ||