NOVEL PYRIMIDINOBENZODIAZEPINONE COMPOUNDS AND THEIR USE
TECHNICAL FIELD
[0001] The present disclosure relates to the field of novel pyrimidinobenzodiazepinone compounds and their use as a medicament, in particular to their use in the treatment of cancer, such as prostate adenocarcinoma.
BACKGROUND
[0002] Prostate cancer is the most common cancer in men, accounting for 15% of cancers in 112 countries. The number of new cases is expected to rise from 1.4 million in 2020 to 2.9 million in 2040 (1) and cannot be prevented by public health interventions or lifestyle changes alone. New pharmacological innovations are continuously being made to slow the disease's progression and ultimately increase overall survival and progression-free survival, particularly in cases of advanced prostate cancer.
[0003] Kallikrein-related peptidase 3 (KLK3), also known as prostate-specific antigen (PSA), is a protease secreted into the seminal fluid via the prostatic ducts. In prostate anomalies, either malignant, like prostate cancer, or benign, such as benign prostatic hyperplasia and prostatitis, KLK3 is released into the blood circulation, where it exhibits antiangiogenic properties. KLK3 is frequently used as a biomarker for detecting, monitoring, and tracking prostate cancer.
[0004] ERK5 (also called MAPK7) is part of the MAP kinase family having roles in cell proliferation and angiogenesis among others. As ERK5 is being overexpressed or hyperactivated in cancer tissues, it is a viable target for cancer research. XMD8-92 is an ERK5 inhibitor, although not yet applied in clinical cancer therapy.
[0005] There is therefore a need to develop more efficient treatment of cancers, such as prostate adenocarcinoma.
