DNA-PK INHIBITORS

摘要

The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein R¹ and R² are independently hydrogen, an optionally substituted C_1-7 alkyl group, C_3-20 heterocyclyl group, or C_5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CR⁴ and O, O and CR'⁴ and NR''⁴ and N, where the unsaturation is in the appropriate place in the ring, and where one of R³ and R⁴ or R'⁴ is an optionally substituted C_3-20 heteroaryl or C_5-20 aryl group, and the other of R³ and R⁴ or R'⁴ is H, or R³ and R⁴ or R''⁴ together are -A-B-, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.