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Selective HASPIN inhibitors
WO2022200433
The CNIO has developed a novel group of compounds with a tricyclic core based on imidazo[1,2-b]pyridazine, which are inhibitors of the protein kinase HASPIN. The present invention relates to a group of compounds with a tricyclic core based on imidazo[1,2-b]pyridazine which are inhibitors of HASPIN, whose activity is required for the proliferation of certain tumoral cells, so the compounds of the invention are useful for the prevention and/or treatment of cancer, alone or in combination with chemotherapeutic agents.
The novel compounds of the invention are not active for PIM1, thus, they are more selective and less toxic than other compounds of the state of art. The compounds of the invention are useful for the treatment of cancer that depends on HASPIN, for example, Burkitt's lymphoma, chronic lymphocytic leukemias, pancreatic cancer, gallbladder carcinoma, bladder cancer, prostate cancer, melanoma, breast cancer, or ovarian cancer. They can be used alone or in combination with chemotherapeutic agents, presenting synergistic combination effects.