| abstract |
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 R<SUP>1 </SUP>and R<SUP>2 </SUP>are independently hydrogen, an optionally substituted C<SUB>1-7 </SUB>alkyl group, C<SUB>3-20 </SUB>heterocyclyl group, or C<SUB>5-20 </SUB>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 CR<SUP>4 </SUP>and O, O and CR'<SUP>4 </SUP>and NR''<SUP>4 </SUP>and N, where the unsaturation is in the appropriate place in the ring, and where one of R<SUP>3 </SUP>and R<SUP>4 </SUP>or R'<SUP>4 </SUP>is an optionally substituted C<SUB>3-20 </SUB>heteroaryl or C<SUB>5-20 </SUB>aryl group, and the other of R<SUP>3 </SUP>and R<SUP>4 </SUP>or R'<SUP>4 </SUP>is H, or R<SUP>3 </SUP>and R<SUP>4 </SUP>or R''<SUP>4 </SUP>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. |