Distamycin derivatives, process for preparing them, and...

C - Chemistry – Metallurgy – 07 – D

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C07D 403/14 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/505 (2006.01) C07D 207/34 (2006.01)

Patent

CA 2253652

A compound which is a distamycin derivative of formula (I), wherein n is 2, 3 or 4; R0 is C1-C4 alkyl or C1-C3 haloalkyl; R1 and R2, which may be the same or different, are each hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, or C1-C4 alkoxy; X is a halogen atom; B is selected from (A, B, C, D, E, F, G, H, I, J and K); wherein R3, R4, R5, R6, R7, R8, and R9, which may be the same or different, are each hydrogen or C1-C4 alkyl, and m is 0, 1 or 2; or a pharmaceutically acceptable salt thereof. Such compounds are useful as antineoplastic and antiviral agents.

L'invention concerne un composé qui constitue un dérivé de distamycine de formule (I) ou un sel de celui-ci acceptable sur le plan pharmaceutique. Dans la formule (I), n vaut 2, 3, ou 4; R¿0? représente alkyle C¿1?-C¿4? ou haloalkyle C¿1?-C¿3?. R¿1? et R¿2?, qui peuvent être identiques ou différents, représentent chacun hydrogène, alkyle C¿1?-C¿4? éventuellement substitué par un ou plusieurs atomes de fluor, ou alcoxy C¿1?-C¿4?; X est un atome d'halogène; B est choisi parmi les formules (A, B, C, D, E, F, G, H, I, J et K) dans lesquelles R¿3?, R¿4?, R¿5?, R¿6?, R¿7?, R¿8? et R¿9?, qui peuvent être identiques ou différents, représentent chacun hydrogène ou alkyle C¿1?-C¿4?, et m vaut 0, 1, ou 2. Lesdits composés sont utiles en tant qu'agents antinéoplasiques et antiviraux.

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