Dihydrodibenzo(de,h)isoquinolines derivatives and their use...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 221/18 (2006.01) A61K 31/47 (2006.01) A61K 31/505 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2188833

Novel bis-1,2-dihydro-3H-dibenzisoquinoline-1,3-diones of formula (I), wherein X, X', Y and Y' are identical or different and are each H, NO2, NH2, C1-C6- alkylamino, di-C1-C6 alkylamino, NH-C1-C6-acyl, OH, C1-H6-alkoxy, halogen trihalomethyl, C1-C6-alkyl, formyl, C1-C6-alkylcarbonyl, ureyl, C1-C6- alkylureyl and A is a C4-C12-bridge which is interrupted at one, two or three points by a secondary or tertiary amino group, where two nitrogen atoms may additionally be bonded to one another by a C1-C4-alkylene group or a salt thereof with a physiologically tolerated acid. Processes for their preparation, pharmaceutical compositions containing them and methods of using them to treat malignancies, mainly human solid tumor carcinomas.

Nouvelles bis-1,2-dihydro-3H-dibenzisoquinoline-1,3-diones de formule (I) dans laquelle X, X', Y et Y' sont identiques ou différents et représentent chacun H, NO¿2?, NH¿2?, alcoylamino C¿1?-C¿6?, di-alcoylamino C¿1?-C¿6?, NH-acyle C¿1?-C¿6?, OH, alcoxy C¿1?-H¿6?, halogène, trihalométhyle, alcoyle C¿1?-C¿6?, formyle, alcoylcarbonyle C¿1?-C¿6?, uréyle, alcoyluréyle C¿1?-C¿6?, et A représente un pont C¿4?-C¿12? interrompu en un, deux ou trois points par un groupe amino secondaire ou tertiaire, où deux atomes d'azote peuvent être en outre liés l'un à l'autre par un groupe alcoylène C¿1?-C¿4? ou par un sel de celui-ci avec un acide tolérable sur le plan physiologique. L'invention concerne des procédés de préparation de ces composés, des compositions pharmaceutiques contenant ceux-ci ainsi que des méthodes d'utilisation desdits composés dans le traitement des tumeurs malignes, notamment des carcinomes humains à tumeur solide.

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