New piperazine derivatives and methods for the preparation...

Details New piperazine derivatives and methods for the preparation... New piperazine derivatives and methods for the preparation...

C - Chemistry, Metallurgy

07

D

C07D 213/75 (2006.01) A61K 31/495 (2006.01) C07D 213/38 (2006.01) C07D 213/40 (2006.01) C07D 213/63 (2006.01) C07D 213/64 (2006.01) C07D 215/227 (2006.01) C07D 221/04 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2184919

The present invention relates to novel compound of the general formula (1) and acid addition salt thereof. Image (I) wherein R1 and R2 are independently hydrogen, C1-C8 alkyl or optionally substituted C3-C6 membered cycloalkyl containing C3-C8; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, C1-C4 lower ester, C1-C4 lower alkyl, C1-C4 lower alkoxy, aryl, arylalkoxy or unsaturated amine; 1 is an integer of 0-7; m and n are independently an integer of 0-1; W is carbon or nitrogen; X is oxygen, sulfur, optionally substituted imine; Y is nitrogen or oxygen; and Z is hydrogen, C1-C8 alkoxy, aryloxy, C1-C4 alkylamine, cycloamine containing N1-N5 or oxo group. The present compounds of the above formula (1) has not only strong antimumor activities but lower toxicities, and accordingly are expected as novel antitumor agents.

Nouveau composé répondant à la formule générale (I), et son sel d'addition d'acide, dans laquelle R¿1? et R¿2?, indépendamment l'un de l'autre, représentent hydrogène, alkyle C¿1-8? ou cycloalkyle C¿3-6? éventuellement substitué renfermant C¿3-8?; R¿3?, R¿4?, R¿5?, R¿6? et R¿7?, indépendamment les uns des autres, représentent hydrogène, halogène, hydroxy, nitro, ester inférieur C¿1-4?, alkyle inférieur C¿1-4?, alcoxy inférieur C¿1-4?, aryle, arylalcoxy ou amine insaturée; 1 est un nombre entier compris entre 0 et 7; m et n, indépendamment l'un de l'autre, sont 0 ou 1; W représente carbone ou azote; X représente oxygène, soufre ou imine éventuellement substituée; Y représente azote ou oxygène; et Z représente hydrogène, alcoxy C¿1-8?, aryloxy, alkylamine C¿1-4?, cycloamine renfermant N¿1-5? ou un groupe oxo. Les composés répondant à la formule (I) présentent non seulement de fortes activités antitumorales mais également des toxicités réduites, et ils sont de ce fait utilisables comme nouveaux agents antitumoraux.

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