摘要 |
<p>A piperazinedione derivative of formula (I), wherein R1 is: (i) a group α, wherein p is 0 or 2; (ii) a 5- or 6-membered heterocyclic ring containing at least one heteroatom selected from O, N and S, which group may be fused to a benzene ring; R2 is H, C¿1?-C6 alkyl optionally substituted by a group -N(R?11R12¿) as defined above, C¿3?-C6 cycloalkyl, C2-C6 alkenyl, -COOR?11¿ wherein R11 is as defined above or a phenyl ring as defined under (i) above, but is other than H when R1 is unsubstituted phenyl; and one of R?3 and R4¿ is hydrogen and the other is a group of formula (A), wherein q is an integer of 1 to 4, r is 0 or 1 and R?5 and R6¿, which may be the same or different, are each H or C¿1?-C6 alkoxy, or R?5 and R6¿ together form a methylenedioxy group; ----- is a double bond or, when R1 is as defined under (i) above, is a double bond or a single bond; and pharmaceutically acceptable salts thereof have activity as modulators of multi-drug resistance.</p> |