公开(公告)号：US20230303556A1

公开(公告)日：2023-09-28

申请号：US18188278

申请日：2023-03-22

Applicant: IDEAYA BIOSCIENCES, INC.

Inventor： Paul A. BARSANTI ,  Michael Patrick DILLON ,  Firoz Ali JAIPURI ,  Ying-Zi XU ,  Xin LINGHU ,  Monah ABED

IPC: C07D417/14 ,  A61P35/00

CPC classification number: C07D417/14 ,  A61P35/00

Abstract: Provided herein are compounds of Formula (I):




or a pharmaceutically acceptable salt thereof. The provided compounds are useful Poly ADP-ribose glycohydrolase (PARG) inhibitors. Additional utilities and advantages are described herein.

公开(公告)号：US20240287080A1

公开(公告)日：2024-08-29

申请号：US18567687

申请日：2022-06-09

Applicant: IDEAYA Biosciences Inc. ,  GlaxoSmithKline Intellectual Property (No.4) Limited

Inventor： Paul A. BARSANTI ,  Kevin J. DUFFY ,  Brian G. LAWHORN ,  Firoz Ali JAIPURI ,  Daneil Lee SEVERANCE ,  Chenbo WANG ,  Nicholas David ADAMS ,  Janos BOTYANSZKI ,  Michael G. DARCY ,  Terence J. KIESOW ,  John J. MCATEE ,  Cuthbert MARTYR ,  Alexander BUTTRAGO SANTANILLA ,  Xinrong TIAN

IPC: C07D487/04 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/519 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04 ,  C07D498/04

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/519 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04 ,  C07D498/04

Abstract: Disclosed herein are certain thiadiazolyl derivatives Formula (I):




that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.