(1H-INDOL-5-YL)ACRYLAMIDE DERIVATIVES AS INHIBITORS OF TEAD PROTEINS AND THE HIPPO-YAP1/TAZ SIGNALING CASCADE FOR THE TREATMENT OF CANCER

摘要

The invention relates to 1H-indolyl-acrylamide derivatives of formula (I):as inhibitors of the TEAD-dependent gene transcription and the HIPPO-YAP1/TAZ signaling cascade for use in methods of treatment of cancer, such as e.g. breast, ovarian, uterine, prostate, lung, gastric, colorectal, bladder, pancreatic and liver cancers, sarcomas, esophageal, head and neck cancers, uveal melanoma or glioma, and in particular in the treatment of patients who have exhibited resistance to prior anti-cancer therapy.The present description discloses the syntheses of exemplary compounds as well as pharmacological data thereof (e.g. pages 11 to 48; examples 1 to 51; tables).An exemplary compound is e.g. N-(1-(3-(trifluoromethyl)benzyl-1H-indol-5-yl)acrylamide ( example 1).