NOVEL P-GP-INHIBITING COMPOUNDS

摘要

A compound of general formula (I), or a pharmaceutically acceptable salt or prodrug thereof wherein ∫u⊃a∫/u⊃ , ∫u⊃b∫/u⊃ , ∫u⊃c∫/u⊃ , ∫u⊃d⊃/u⊃ , ∫u⊃e∫/u⊃ and ∫u⊃f⊃/u⊃ may be absent or may independently represent the presence of a single bond; X is selected from the group consisting of CH, CH2, NH, O and S; Y is selected from the group consisting of H or O; whereby: in the case where Y represents O: ∫u⊃a∫/u⊃ represents a single bond so as to complete a double bond to O as represented by Y; ∫u⊃b∫/u⊃ is absent; and X is selected from the group consisting of CH2, NH, O and S; or in the case where Y represents H: ∫u⊃a∫/u⊃ is absent; ∫u⊃b∫/u⊃ may be absent or may represent a single bond so as to complete a double bond to X; whereby, in the absence of ∫u⊃b∫/u⊃ , X is selected from the group consisting of CH2, NH, O and S; or in the case where ∫u⊃b∫/u⊃ represents a single bond so as to complete a double bond to X, X represents CH; R1 is selected from the group consisting of H, C¿1-6? alkyl, NH2, NH(C1-6 alkyl), N(C1-6alkyl)2 and OR?5; R2, R3 and R4¿ are independently selected from the group consisting of H, OH, C¿1-6? alkoxy and OR?5, or R3 and R4¿ can together form the residue of a 5 or 6 membered heterocyclic ring, with the proviso that at least one of R?2, R3 and R4¿ represents OR5; wherein R5 is selected from the group consisting of C¿5-20? alkyl, C5-20 alkenyl, C5-20 alkylene(C3-6 cycloalkyl), C5-20 alkenylene(C3-6cycloalkyl), C5-20 alkylene(heterocycle) and C5-20 alkenylene(heterocycle), where heterocycle represents a 3 to 5 membered heterocyclic ring containing at least one oxygen heteroatom and where said cycloalkyl or heterocycle can be substituted with one or more C1-4 alkyl groups.