发明名称 |
Small molecule inhibitors targeted at Bcl-2 |
摘要 |
The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-X<SUB>L</SUB>. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-X<SUB>L </SUB>that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-X<SUB>L</SUB>, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.
|
申请公布号 |
US7354928(B2) |
申请公布日期 |
2008.04.08 |
申请号 |
US20020286085 |
申请日期 |
2002.11.01 |
申请人 |
THE REGENTS OF THE UNIVERSITY OF MICHIGAN |
发明人 |
WANG SHAOMENG;YANG DAJUN;ENYEDY ISTVAN J. |
分类号 |
A61K31/44;A61K31/00;A61K31/122;A61K31/135;A61K31/335;A61K31/395;A61K31/404;A61K31/4184;A61K31/444;A61K31/452;A61K31/473;A61K31/4745;A61K31/505;A61K31/519;A61K31/65;A61K31/655;A61K45/06 |
主分类号 |
A61K31/44 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|