Novel bis-2-difluoro-pyrrolo[2,1-c][1,4]benzodiazepine dimmers

C - Chemistry – Metallurgy – 07 – D

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C07D 519/00 (2006.01) A61K 31/5517 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2645350

The present invention provides a novel bis 2-difluoro pyrrolo[2,1-c][1,4]benzodiazepine of formula (VII); wherein, n is 3 to 10. novel bis 2-difluoro pyrrolo[2,1-c][1,4]benzodiazepine of formula VII exhibits biding affinity with calf thymus (CT) DNA at a molar ratio of 1:5 in aqueous sodium phosphate buffer at pH of about 7.00. The present invention further provides a process for the preparation of novel bis 2-difluoro pyrrolo[2,1-c][1,4]benzodiazepine of formula (VII).

La présente invention concerne une nouvelle bis-2-difluoropyrrolo[2,1-c][1,4]benzodiazépine de formule (VII); où n est compris entre 3 et 10 inclus. La nouvelle bis 2-difluoropyrrolo[2,1-c][1,4]benzodiazépine de formule VII présente des affinités de liaison avec l'ADN de thymus de veau (TV) dans un rapport molaire de 1 : 5 dans un tampon phosphate de sodium aqueux à un pH d'environ 7,00. La présente invention concerne en outre un procédé de synthèse de la nouvelle bis 2-difluoropyrrolo[2,1-c][1,4]benzodiazépine de formule (VII).

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