Patent AU-2020213376-B2 (AU)
Title: Compounds and methods for the targeted degradation of the androgen receptor
Inventor: JIN MEIZHONG
IPC: C07D403/06
Filed: 2020-08-07
Granted: 2021-07-29
Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) 
Androgen Receptor. In particular, the present invention is directed to compounds, which contain on 
one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds 
Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to 
effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad 
range of pharmacological activities associated with compounds according to the present invention, 
consistent with the degradation/inhibition of Androgen Receptor.
WO 2016/118666 PCT/US2016/014187 
1/7 
UIGIOJd lGbJei PGPeJbGCI 
(1) 
E 
0 
0 ,- 11 
...... .....  ....... ......  ....... ......  ........ .......  ........ .......  ......... ........  ......... ........  ......... ........  ......... .........  .......... .........  ......... .  ........... .........  ..........  ........... ..........  .. .... ...........  ...............................................  .. ........................................  ................................................  ... ........................................  ................................................  ... ..........................................  .................................................  ... ..........................................  ..................................................  .... ..........................................  ..................................................  .... ...........................................  ..................................................  .... .............................................  ...................................................  .... ............................................  ..................................................  .............................................  ...................................................  ...................I ............................  .................................................  ..............................................  .................................................  ................................................  ................................................  ..................... .....................  ................................................  ...............................................  ................................................  ................... .....................  ................................................  ..............................................  .............................................  ................... .......................  .................................................  ...................I .........................  ................................................  ..................................................  ..................................................  ......................... ..................  ...................... .......................  ...................................................  ............................................  ...........................................  ..............................................  .............................................  ......................I ...................  ................... ...........................  ..............................................  .............................................  ................... ...................  ................................................  ..............................................  ............................................  .............................................  .............................................  ........................................  ............................................  .......................................  ..........................................  ..........................................  .....................................  ................... ...............  ...........................................  ..........................................  ........................................  ........................................  .............................. .........  .......................................  ...................................... .  .....................................  ...................................  ..................................  .................................  ...............................  ..............................  .............................  ............................  ...........................  .........................  .......................  ......................  ....................  ..................  ...............  ............  
..............  ........................  ........................ .  ........................  ........................ .  ........................  ........................ .  ...............  ............................. .  
......................................  ....................................  .....................................  .....................................  .....................................  A .....................................  .....................................  .................................... .  .....................................  ................... ................ .  .................. ..................  ................ .................. .  ................ ................  .................................... .  ..................................  ................ ................ .  ................ ................  .................................... .  ................  ... ...... . . ....... .  ...........  .............................................  ................................................  .................................................  ..................................................  .................................................  ..................................................  ...................................................  ................................................  ...................................................  ..................................................  .................................................  ................................................  ................................................  ................................................  ..................................................  ...............................................  ........................ ....................  ................................................  ..................................................  ...............................................  ...................... ......................  .................................................  .................................................  ..................... ... ....................  ..................................................  .................................................  ...................... .....................  .............................................  ...................... ..................  ....................................................  ...................................................  ..............................................  .....................  .............................  ................... ....................  ..............................................  ....................... ....................  ................................................  ...............................................  ..............................................  ....................I ......I ....................  .............................................  .................... ...................  ..........................................  .............................................  ............................................  .................. ..................  ..........................................  .................. ................  ..........................................  ...........................................  ..........................................  .........................................  ........................................  .......................................  .......................................  ......................................  ......................................  ....................................  ....................................  ..................................  ..................................  ...............................  ...........................  ..........................  ........................  ......................  ....................