公开(公告)号：WO2023049438A1

公开(公告)日：2023-03-30

申请号：PCT/US2022/044686

申请日：2022-09-26

申请人： SONATA THERAPEUTICS, INC. ,  LANTERMANN, Alexandra ,  CHEKLER, Eugene, L. Piatnitski ,  BLOM, Daniel ,  COUTO, Kiley, Marie ,  LEFKER, Bruce, Allen ,  KITCHEN, Douglas, Bruce

发明人： LANTERMANN, Alexandra ,  CHEKLER, Eugene, L. Piatnitski ,  BLOM, Daniel ,  COUTO, Kiley, Marie ,  LEFKER, Bruce, Allen ,  KITCHEN, Douglas, Bruce

IPC分类号： A61K31/4439 ,  A61K31/4196 ,  C07D401/14 ,  C07D249/08 ,  C07D401/04

摘要： Provided herein are compounds (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, stereoisomers, tautomers, isotopically labeled derivatives, solvates, hydrates, polymorphs, co-crystals, and prodrugs thereof, pharmaceutical compositions thereof, and kits comprising the same. The compounds provided herein are G protein-coupled receptor kinase (e.g., GRK2, GRK3) inhibitors and are therefore useful for, e.g., treating and/or preventing diseases (e.g., cancer) in a subject, for inhibiting tumor growth in a subject, for inhibiting GRK2 and/or GRK3 activity in vitro or in vivo, etc. In certain embodiments, the compounds provided herein are selective for GRK2 and/or GRK3. Also provided herein are methods and synthetic intermediates useful in the preparation of compounds described herein.

公开(公告)号：WO2022159688A1

公开(公告)日：2022-07-28

申请号：PCT/US2022/013295

申请日：2022-01-21

申请人： CYGNAL THERAPEUTICS, INC. ,  PIIZZI, Grazia ,  CHEKLER, Eugene L., Piatnitski ,  HUROV, Jonathan, Barry ,  LANTERMANN, Alexandra ,  COUTO, Kiley, Marie ,  XU, Hua ,  SARKAR, Sourav ,  LEFKER, Bruce, Allen ,  ROBINSON, Ralph, P. ,  KYSIL, Volodymyr

发明人： PIIZZI, Grazia ,  CHEKLER, Eugene L., Piatnitski ,  HUROV, Jonathan, Barry ,  LANTERMANN, Alexandra ,  COUTO, Kiley, Marie ,  XU, Hua ,  SARKAR, Sourav ,  LEFKER, Bruce, Allen ,  ROBINSON, Ralph, P. ,  KYSIL, Volodymyr

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D471/02

摘要： Provided herein are compounds (e.g., compounds of Formulae (A-I), (B-I), (C-I)), and pharmaceutically acceptable salts, stereoisomers, tautomers, isotopically labeled derivatives, solvates, hydrates, polymorphs, co-crystals, and prodrugs thereof, pharmaceutical compositions thereof, and kits comprising the same. The compounds provided herein are degraders of GRK2 proteins and are therefore useful for, e.g., treating and/or preventing diseases (e.g., cancer) in a subject, for inhibiting tumor growth in a subject, for inhibiting the activity of GRK2 and/or degrading a GRK2 protein in vitro or in vivo, etc. In certain embodiments, the compounds provided herein are selective for GRK2. Also provided herein are methods and synthetic intermediates useful in the preparation of compounds described herein.