1.3.4-triaza-phenalene and 1,3,4,6-tetraazaphenalene...

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 487/06 (2006.01) A61K 31/519 (2006.01) A61K 35/00 (2006.01) C07D 239/94 (2006.01) C07D 471/06 (2006.01)

Patent

CA 2527832

Novel 1,3,4-triaza-phenalene and 1,3,4,6-tetraazaphenalene derivatives of formula (I) are disclosed. These compounds inhibit epidermal growth factor receptor ("EGFW') tyrosinc kinase. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful, inter alia, in the treatment or control of cancer, in particular solid tumors. This invention also relates to pharmaceutical compositions containing such compounds and to rnethods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors.

Cette invention se rapporte à de nouveaux dérivés de 1,3,4-triaza-phénalène et de 1,3,4,6-tétra-azaphénalène représentés par la formule (I). Ces composés inhibent la tyrosine kinase des récepteurs du facteur de croissance épidermique ("EGFR'). Ces composés et leurs sels et esters pharmaceutiquement acceptables possèdent une action antiproliférative et ils sont utiles, notamment, pour traiter et vaincre le cancer, en particulier les tumeurs solides. Cette invention concerne également des compositions pharmaceutiques contenant ces composés, ainsi que des procédés pour traiter ou vaincre le cancer, plus particulièrement pour traiter ou vaincre les cancers du sein, du poumon, du colon et de la prostate.

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