ANTICANCER DERIVATIVES OF 5-(IMINOMETHYL)-2,4-PYRIMIDINEDIONE HAVING EGFR INHIBITING ACTIVITY

摘要

PURPOSE: Derivatives of 5-(iminomethyl)-2,4-pyrimidinedione are provided, which derivatives have activity inhibiting EGFR(epidermal growth factor receptor), so that they can be useful for treatment of cancer. CONSTITUTION: The derivatives of 5-(iminomethyl)-2,4-pyrimidinedione represented by formula (1) are provided, wherein R1 and R2 are independently hydrogen, optionally substituted C1-C10 alkyl or C3-C6 cycloalkyl, or optionally substituted C7-C15 benzyl; R3 and R4 are independently hydrogen, allyl, optionally substituted C1-C10 alkyl or C3-C6 cycloalkyl, optionally substituted C7-C15 benzyl, optionally substituted C6-C15 aryl, optionally substituted C6-C15 hetero atom containing ring, optionally substituted C3-C20 acyl, optionally substituted C3-C20 amide, or optionally substituted C3-C20 thioamide; and R5 is optionally substituted C1-C20 alkyl or C3-C6 cycloalkyl, optionally substituted C7-C15 benzyl, optionally substituted C6-C15 aryl, optionally substituted C6-C15 hetero atom containing ring, optionally substituted C1-C10 alkoxy, optionally substituted C7-C15 benzyloxy, optionally substituted C1-C10 amine, or cyano, provided that the substituent of R1, R2, R3, R4 and R5 is selected from halogen atom, cyano, amide, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, alkylsulfone and arylsulfone, and a case that R3 and R4 are hydrogen simultaneously, and R5 is methyl, hydroxy, phenyl or phenylamine is excluded.