Substituted bisindolylmaleimides for the inhibition of cell...

C - Chemistry – Metallurgy – 07 – D

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C07D 403/14 (2006.01) A61K 31/40 (2006.01)

Patent

CA 2262092

Compounds of formula (I) wherein R1 and R1' are independently alkyl, aryl, alkenyl or alkynyl; R2 and R2' are independently hydrogen or alkyl; R4, R5, R6 and R7 each independently are (a), CO2R9, CH2OR10, CHO, CH2NR11R12, CON(R13)2, hydrogen, halogen, cyano, alkyl, hydroxy, alkoxy, aryloxy, haloalkyl, nitro, amino, acylamino, aralkyloxy, monoalkylamino, dialkylamino, alkylthio, alkylsulphinyl or alkylsulphonyl, provided that at least one of R4, R5, R6 or R7 is cyano, (a), CO2R9, CH2OR10, CH2NR11R12, CHO or CON(R13)2; R8 is alkyl, aralkyl or aryl; R9 is alkyl, aralkyl or aryl; R10 is hydrogen, alkyl, aralkyl or aryl; R11 and R12 are independently hydrogen, alkyl, aryl, aralkyl or acyl; R13 is hydrogen, alkyl, aryl or aralkyl; and one of X and Y signifies O and the other signifies O, S, (H,OH) or (H,H); as well as pharmaceutically acceptable prodrugs or salts of acidic compounds of formula (I) with bases and or basic compounds of formula (I) with acids are antiproliferative agents useful in the treatment of cancer.

Composés de la formule (I) dans laquelle R?1¿ et R?1'¿ représentent indépendamment l'un de l'autre alkyle, aryle, alcényle ou alcynile; R?2¿ and R?2'¿ représentent indépendamment l'un de l'autre hydrogène ou alkyl; R?4¿, R?5¿, R?6¿ et R?7¿ représentent indépendamment les uns des autres (a), CO¿2?R?9¿, CH¿2?OR?10¿, CHO, CH¿2?NR?11¿R?12¿, CON(R?13¿)¿2?, hydrogène, halogène, cyano, alkyle, hydroxy, alcoxy, ariloxy, haloalkyle, nitro, amino, acylamino, aralkyloxy, monoalkylamino, dialkylamino, alkylthio, alkylsulfinyl or alkylsulfonyle, si l'un des radicaux R?4¿, R?5¿, R?6¿ ou R?7¿ représente cyano (a), CO¿2?R?9¿, CH¿2?OR?10¿, CH¿2?NR?11¿R?12¿, CHO ou CON(R?13¿)¿2?; R?8¿ représente alkyle, aralkyle ou aryle; R?9¿ représente alkyle, aralkyle ou aryle; R?10¿ représente hydrogène, alkyle, aralkyle ou aryle; R?11¿ et R?12¿ représentent indépendamment l'un de l'autre hydrogène, alkyle, aryle, aralkyle ou acyle; R?13¿ représente hydrogène, alkyle, aryle ou aralkyle; et l'un des éléments X et Y signifie O et l'autre signifie O, S, (H,OH) ou (H,H); de même que des sels ou des promédicaments pharmacologiquement acceptables de composés acidifiants de la formule (I), avec des bases et/ou des composés basiques de ladite formule (I) qui constituent des agents antiproliférants utilisables dans le traitement du cancer.

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