申请人:CANCER REC TECH LTD
公开号:WO2003024949A1
公开(公告)日:2003-03-27
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?1 and R2¿ are independently hydrogen, an optionally substituted C¿1-7? alkyl group, C3-20 heterocyclyl group, or C5-20 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 CR?4¿ 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 R?3 and R4 or R'4¿ is an optionally substituted C¿3-20? heteroaryl or C5-20 aryl group, and the other of R?3 and R4 or R'4¿ is H, or R?3 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.
本发明涉及使用式(I)化合物及其异构体、盐、溶剂合物、化学保护形式和前药,在制备用于抑制DNA-PK活性的药物中使用,其中R?1和R2¿分别为氢、可选取代的C¿1-7?烷基、C3-20杂环基或C5-20芳基,或者可以与它们连接的氮原子一起形成具有4到8个环原子的可选取代杂环环;X和Y从CR?4¿和O、O和CR'4和NR'4和N中选取,其中不饱和度在环中适当位置,其中R?3和R4或R'4¿中的一个为可选取代的C¿3-20?杂芳基或C5-20芳基,而另一个为H,或者R?3和R4或R'4¿一起是-A-B-,它们共同代表一个融合的可选取代芳香环。这些化合物还比PI 3-激酶和/或ATM选择性地抑制DNA-PK活性。