THE USE OF SUBSTITUTED 2-PHENYL-3H-QUINAZOLIN-4-ONES AND ANALOGS FOR INHIBITING BET (BROMODOMAIN AND EXTRA TERMINAL DOMAIN) PROTEINS

摘要

The present application is directed to the use of substituted 2-phenyl-3H-quinazolin-4-ones and analogs for inhibiting BET (bromodomain and extra terminal domain) proteins. The disclosed compounds can be used for the treatment of cancers that exhibit c-myc overexpression, cancers that overexpress n-myc, and cancers that rely on the recruitment of p-TEFb to regulate activated oncogenes, such as Burkitt's lymphoma, acute myelogenous leukemia, multiple myeloma, aggressive human medulloblastoma, hematological, epithelial cancers, lung cancers, breast cancers, colon carcinomas, midline carcinomas, mesenchymal tumors, hepatic tumors, renal tumors and neurological tumors.