Acryloyl substituted distamycin derivatives, process for...

C - Chemistry – Metallurgy – 07 – D

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C07D 207/34 (2006.01) A61K 31/40 (2006.01)

Patent

CA 2260060

Acryloyl substituted distamycin derivatives of formula (I) wherein n is 2, 3, or 4; R1 and R2 are selected each independently, from: hydrogen, halogen, and C1-C4 alkyl; R3 is hydrogen or halogen; B is selected from: (1), (2), (3), (4), (5), (6) and (7); wherein R4, R5, R6, R7, and R8 are, each independently, hydrogen or C1-C4 alkyl, with the proviso that at least one of R4, R5 and R6 is C1-C4 alkyl; and pharmaceutically acceptable salts thereof. Such compounds are useful as antineoplastic and antiviral agents.

L'invention concerne des dérivés de la distamycine acryloyl-substitués, de formule (I), dans laquelle n est 2, 3 ou 4; R1 et R2 sont choisis indépendamment entre hydrogène, halogène et alkyle C1-C4; R3 est hydrogène ou halogène; B est choisi entre (1), (2), (3), (4), (5), (6) et (7), où R4, R5, R6, R7 et R8 sont indépendamment hydrogène ou alkyle C1-C4, à condition qu'au moins R4, R5 et/ou R6 soit alkyle C1-C4; ainsi que leurs sels pharmaceutiquement acceptables. Ces composés sont utiles comme agents antinéoplasiques et antiviraux.

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