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US 12,583,815 B2Granted
Inhibitors of YAP/TAZ-TEAD oncoproteins, synthesis and use thereof
AssigneeBridGene Biosciences, Inc.
InventorsChao Zhang, Michael J. Bishop, Hang Chen, Ping Cao
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Abstract
Disclosed herein are synthesis and use of covalent inhibitors selective for Transcriptional Enhancer Factor TEF-1 (TEAD1), which can be used for treatment of cancers such as glioblastoma, gastric cancer, colorectal cancer, pancreatic ductal adenocarcinoma (PDAC), and malignant pleural mesothelioma (MPM). Further disclosed herein are pharmaceutical compositions including the TEAD1 inhibitor and methods of treating cancers using the same.
Claims8
A compound according to Formula (I):
- or an optically pure stereoisomer, pharmaceutically acceptable salt, or solvate thereof,
- wherein
- Ring2 is selected from the group consisting of
- A is —O—(CH2)p—;
- R2 is NHCOCH═CH2;
- R3 is CF3;
- n is 0;
- m is 1;
- and
- p is an integer selected from 0 to 3.
7 more elements
Dependencies are inferred from the claim text.