DASATINIB AND ANOTHER 5-THIAZOLECARBOXAMIDE KINASE INHIBITOR, AND USES THEREOF

• Main Authors: KHANDELWAL, Nisit, SENNHENN, Peter, MEIER-EWERT, Sebastian
• Format: Patent
• Language: English
• Published: 09.12.2021
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention relates to a kinase inhibitor, in particular an inhibitor of protein kinases including the protein-tyrosine kinases LCK, ABL, SRC, KIT, SIK-family and/or their mutants. Although structurally similar to dasatinib, the kinase inhibitor of the invention displays, eg functional and ADMET properties distinct to dasatinib. Also, the invention relates to pharmaceutical compositions that comprise the kinase inhibitor, including those formulated for oral administration, such as in unit dose form that comprise particular ranges or amounts of the kinase inhibitor. The kinase inhibitor or pharmaceutical composition may be used in the treatment of a proliferative disorder, such as a leukaemia or solid tumour. The kinase inhibitor or pharmaceutical composition may be used in a treatment regimen that corresponds to, is similar to or is distinct from that used with dasatinib for a corresponding disorder, and in particular may be used in a combination treatment regimen together with one or more additional therapeutic agents, such as immune-checkpoint inhibitors.