| 主权项 |
1. A compound of formula (I): wherein: R1 and R2 are independently selected from —C(O)NR5R6, —C(O)OR7, CN, —C(O)R7, —C(O)NHC(O)R7, —NO2, —SO3R7, —SO2R7, —SOR7, —SO2NR5R6, —SO2NH—C(O)OR8, —POR21R22 and optionally substituted phenyl or heteroaryl; R3 is optionally substituted phenyl; R4a and R4b are independently selected from hydrogen; C1-C6 alkyl which alkyl group may optionally be substituted by hydroxyl, COOR12 or CONR13R14; aryl and —C1-C3 alkylaryl in which said aryl groups may be optionally substituted; R5 and R6 are independently selected from:
(a) hydrogen,(b) C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C10 cycloalkyl, C5-C10 cycloalkenyl, heterocyclyl, —C1-C3 alkyl-C3-C10 cycloalkyl, —C1-C3 alkyl-C5-C10 cycloalkenyl or —C1-C3 alkylheterocyclyl, or R5 and R6 together with the N to which they are attached may form a 5- or 6-membered heterocyclic ring optionally containing a further heteroatom selected from O, S and NR9, in which any of the aforementioned R5 and R6 groups may be optionally substituted by a group selected from cyano, C1-C6 alkoxy, C1-C6 fluoroalkoxy, C1-C6 alkyl, C1-C6 fluoroalkyl and —C(O)NRaRb, where Ra and Rb are independently selected from hydrogen and C1-C6 alkyl, and any of the aforementioned R5 and R6 groups may be optionally substituted by one or more halogen atoms, and(c) aryl, heteroaryl, C1-C3 alkylaryl and —C1-C3 alkylheteroaryl, said aryl and heteroaryl groups being optionally substituted; R7 is selected from:
(a) C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C10 cycloalkyl, C5-C10 cycloalkenyl, heterocyclyl, —C1-C3 alkyl-C3-C10 cycloalkyl, —C1-C3 alkyl-C5-C10 cycloalkenyl or —C1-C3 alkylheterocyclyl, in which any of the aforementioned R7 groups may be optionally substituted by a group selected from cyano, C1-C6 alkoxy, C1-C6 fluoroalkoxy, C1-C6 alkyl, C1-C6 fluoroalkyl and —C(O)NRaRb, where Ra and Rb are independently selected from hydrogen and C1-C6 alkyl, and any of the aforementioned R7 groups may be optionally substituted by one or more halogen atoms, and(b) aryl, heteroaryl, C1-C3 alkylaryl and —C1-C3 alkylheteroaryl, said aryl and heteroaryl groups being optionally substituted; R8 is C1-C6 alkyl; R9 is hydrogen, C1-C6 alkyl; —C(O)R10 or —C(O)OR11; R10 is C1-C6 alkyl; R11 is C1-C6 alkyl; R12 is C1-C6 alkyl; R13 is hydrogen or C1-C6 alkyl; R14 is hydrogen or C1-C6 alkyl; and R21 and R22 are independently selected from C1-C6 alkyl and C1-C6 hydroxyalkyl; or a pharmaceutically acceptable prodrug derivative thereof, or a pharmaceutically acceptable salt or solvate thereof; provided that the compound is not: a) diethyl 3,4-dihydroxy-1-(4-methoxyphenyl)-1H-pyrrole-2,5-dicarboxylate; b) diethyl 3,4-dihydroxy-1-phenyl-1H-pyrrole-2,5-dicarboxylate; c) dimethyl 3,4-dihydroxy-1-(4-bromophenyl)-1H-pyrrole-2,5-dicarboxylate; d) dimethyl 3,4-dihydroxy-1-(4-chlorophenyl)-1H-pyrrole-2,5-dicarboxylate; e) di-tert-butyl 3,4-dihydroxy-1-(4-nitrophenyl)-1H-pyrrole-2,5-dicarboxylate; f) dimethyl 3,4-dihydroxy-1-(4-methoxyphenyl)-1H-pyrrole-2,5-dicarboxylate; g) dimethyl 3,4-dihydroxy-1-phenyl-1H-pyrrole-2,5-dicarboxylate; h) diethyl 3,4-bis(acetyloxy)-1-phenyl-1H-pyrrole-2,5-dicarboxylate; or i) dimethyl 3,4-bis(acetyloxy)-1-phenyl-1H-pyrrole-2,5-dicarboxylate. |
