- 专利标题: PROTEOLYSIS TARGETING CHIMERA (PROTAC) FOR DEGRADATION OF AURORA A-KINASE
-
申请号: US17906184申请日: 2021-03-10
-
公开(公告)号: US20230118911A1公开(公告)日: 2023-04-20
- 发明人: Elmar WOLF , Martin EILERS
- 申请人: Julius-Maximilians-Universitaet Wuerzburg
- 申请人地址: DE Wuerzburg
- 专利权人: Julius-Maximilians-Universitaet Wuerzburg
- 当前专利权人: Julius-Maximilians-Universitaet Wuerzburg
- 当前专利权人地址: DE Wuerzburg
- 优先权: EP20162690.0 20200312
- 国际申请: PCT/EP2021/056048 WO 20210310
- 主分类号: A61K47/55
- IPC分类号: A61K47/55 ; A61K47/54 ; A61P35/00
摘要:
The invention concerns a Proteolysis Targeting Chimera (PROTAC) or a pharmaceutically acceptable salt thereof for degradation of Aurora A-kinase in cells of a mammal which PROTAC has the chemical structure AAB-L-E3B, wherein AAB is a binding unit for Aurora A-kinase, L is a linker and E3B is a binding unit for E3-ubiquitin ligase Cereblon, wherein E3B comprises the structure of thalidomide or of one of its analogs lenalidomide, pomalidomide, and apremilast, wherein L comprises or consists of an alkyl ether residue or a polyalkyl ether residue or an alkyl ether residue or a polyalkyl ether residue in which at least one C—C bond is replaced by a C═C double bond, which polyalkyl ether residue has at least two ether groups or at least two ether groups in which one O-atom is replaced by an S-atom or a part of the O-atoms is replaced by S-atoms or wherein L comprises or consists of an alkyl thioether residue or a polyalkyl thioether residue or an alkyl thioether residue or a polyalkyl thioether residue in which at least one C—C bond is replaced by a C═C double bond, which polyalkyl thioether residue has at least two thioether groups, wherein L connects AAB and E3B via a chain of atoms having five to thirteen subsequently arranged atoms, wherein atoms of functional groups connecting the linker with AAB and E3B are not considered as part of said chain.
信息查询
IPC分类: