EP 4127209 A2 20230208 - SMALL MOLECULE INHIBITORS OF ONCOGENIC CHD1L WITH PRECLINICAL ACTIVITY AGAINST COLORECTAL CANCER
Title (en)
SMALL MOLECULE INHIBITORS OF ONCOGENIC CHD1L WITH PRECLINICAL ACTIVITY AGAINST COLORECTAL CANCER
Title (de)
KLEINMOLEKÜLIGE HEMMER VON ONKOGENEM CHD1L MIT PRÄKLINISCHER AKTIVITÄT GEGEN KOLOREKTALKARZINOM
Title (fr)
INHIBITEURS À PETITES MOLÉCULES DE CHD1L ONCOGÈNES PRÉSENTANT UNE ACTIVITÉ PRÉCLINIQUE CONTRE LE CANCER COLORECTAL
Publication
Application
Priority
- US 202062994259 P 20200324
- US 202163139394 P 20210120
- US 2021023981 W 20210324
Abstract (en)
[origin: WO2021195279A2] Treatment of CHD1L-driven cancers, including TCF transcription-driven cancers and EMT-driven cancers using CHD1L inhibitors. Small molecule inhibitors of CHDL1 which inhibit CHD1L ATPase and inhibit CHD1L-dependent TCF-transcription have been identified. CHD1L inhibitors prevent the TCF-complex from binding to Wnt response elements and promoter sites. More specifically, CHD1L inhibitors induce the reversion of EMT. CHD1L inhibitors are useful in the treatment of various cancers and particularly CRC and m-CRC. The CHD1L-driven cancer is among others, CRC, breast cancer, glioma, liver cancer, lung cancer or gastrointestinal (GI) cancers. CHD1L inhibitors of formulas I and XX and salts thereof as defined herein are provided as well as pharmaceutical compositions containing CHD1L inhibitors. Synergistic combinations of CHD1L inhibitors with other antineoplastic agents are also described.
IPC 8 full level
C12Q 1/68 (2006.01); A61K 31/335 (2006.01); G01N 33/68 (2006.01)
CPC (source: EP)
A61P 35/00 (2018.01); C07D 239/48 (2013.01); C07D 403/12 (2013.01); C07D 409/12 (2013.01); C07D 471/04 (2013.01); C07D 487/04 (2013.01)
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
Designated extension state (EPC)
BA ME
Designated validation state (EPC)
KH MA MD TN
DOCDB simple family (publication)
WO 2021195279 A2 20210930; WO 2021195279 A3 20211111; AU 2021244209 A1 20221103; CA 3172987 A1 20210930; CN 115667553 A 20230131; EP 4127209 A2 20230208; JP 2023520330 A 20230517
DOCDB simple family (application)
US 2021023981 W 20210324; AU 2021244209 A 20210324; CA 3172987 A 20210324; CN 202180037594 A 20210324; EP 21775064 A 20210324; JP 2022557840 A 20210324