Amino anthracyclinone derivatives and their use in the...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/70 (2006.01) A61K 31/65 (2006.01) C07D 405/06 (2006.01)

Patent

CA 2321834

A compound of formula (1), wherein R1 represents hydrogen, hydroxy, a group of formula OR7, wherein R7 is C1-C6 alkyl, C2-C6 alkenyl; R2 represents hydrogen, hydroxy, diethylamino, piperidino, tetrahydropyridino or morpholino, and either R3, taken alone, represents hydrogen or hydroxy, and R4 and R5, taken alone, independently represent hydrogen, hydroxy or, taken together with the carbon atom, represent a carbonyl group; or R3 and R4, taken together, represent a group of formula (A), wherein R8 and R9 represent a C1-C6 alkyl and R5 represents hydrogen; R6 represents hydrogen or a phenyl group, optionally substituted by methyl, methoxy or halogen and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.

L'invention concerne un composé de formule (1), dans laquelle R¿1? représente hydrogène, hydroxy, un groupe de formule OR¿7?, dans laquelle R¿7? représente alkyle C¿1?-C¿6?, alcényle C¿2?-C¿6?; R¿2? représente hydrogène, hydroxy, diéthylamino, pipéridino, tétrahydropyridino ou morpholino, et soit, R¿3?, pris seul, représente hydrogène ou hydroxy, et R¿4? et R¿5?, pris seuls, représentent indépendamment hydrogène, hydroxy, ou pris ensemble avec l'atome de carbone, représentent un groupe carbonyle; soit R¿3? et R¿4?, pris ensemble, représentent un groupe de formule (A), dans laquelle R¿8? et R¿9? représentent alkyle C¿1?-C¿6? et R¿5? représente hydrogène; R¿6? représente hydrogène ou un groupe phényle, éventuellement substitué par méthyle, méthoxy ou halogène. L'invention concerne également un sel pharmaceutiquement acceptable dudit composé, lequel est utile dans le traitement de l'amylose. Des procédés de préparation et des compositions pharmaceutiques sont également décrits.

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