Irreversible inhibitors of egf receptor tyrosine kinases and...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 239/94 (2006.01) A61K 31/517 (2006.01) A61K 51/04 (2006.01) C07B 59/00 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2514479

Novel epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors, pharmaceutical compositions including same and their use in the treatment of EGFR-TK related diseases or disorders are disclosed. Novel radiolabeled EGFR-TK irreversible inhibitors as their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are further disclosed.

La présente invention concerne de nouveaux inhibiteurs irréversibles de la tyrosine kinase du récepteur du facteur de croissance épidermique (EGFR-TK), des compositions pharmaceutiques renfermant lesdits inhibiteurs et l'utilisation desdites compositions dans le traitement des maladies ou affections liées à l'EGFR-TK. L'invention se rapporte en outre à de nouveaux inhibiteurs irréversibles radiomarqués de l'EGFR-TK, et à leur utilisation comme biomarqueurs dans la radio-imagerie médicale telle que la tomographie par émission de positrons (PET) et la tomographie d'émission monophotonique (SPECT), et comme produits radiopharmaceutiques destinés à la radiothérapie.

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