Antitumour tetracyclic compounds

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 487/04 (2006.01) A61K 31/395 (2006.01) A61K 31/675 (2006.01) A61K 31/695 (2006.01) A61K 31/70 (2006.01) C07D 209/94 (2006.01) C07D 307/93 (2006.01) C07D 333/78 (2006.01) C07D 491/048 (2006.01) C07D 495/04 (2006.01) C07F 7/08 (2006.01) C07F 7/10 (2006.01) C07F 9/6561 (2006.01) C07H 15/26 (2006.01)

Patent

CA 2182361

The present invention relates to heterocyclic compounds which have been found to have anti-tumour activity. More specifically, the invention concerns compounds of formula (I), wherein A is (a), (b), (c) or (d), X is O, S, SO, SO2, CH2, CO or NR7, wherein R7 is H, alkyl, aralkyl, aryl, alkenyl, acyl, alkynyl, sulphonyl or substituted sulphonyl; Y is O, S, SO, SO2, CH2, CO or NR7, with the proviso that Y is not O when X is O; methods for their preparation, pharmaceutical formulations containing them and their use as anti- tumour agents. The compounds have low toxicity against normal cell lines whilst exhibiting anti-tumour cell activity.

L'invention concerne des composés hétérocycliques dont on a découvert qu'ils présentent une activité antitumorale. L'invention porte, plus spécifiquement, sur des composés de formule (I), dans laquelle A représente (a), (b), (c) ou (d), X représente O, S, SO, SO¿2?, CH¿2?, CO ou NR?7¿, R?7¿ représentant H, alkyle, aralkyle, aryle, alcényle, acyle, alkynyle, sulfonyle ou sulfonyle substitué; Y représente O, S, SO, SO¿2?, CH¿2?, CO ou NR?7¿, à condition que Y ne représente pas O lorsque X correspond à O. L'invention se rapporte également à des procédés de préparation desdits composés, à des formulations pharmaceutiques contenant ces derniers, ainsi qu'à leur utilisation en tant qu'agents antitumoraux. Ces composés présentent à la fois une faible toxicité vis-à-vis des lignées cellulaires normales et une activité antitumorale.

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