Polyalkylene glycol derivatives of 4-...

Details Polyalkylene glycol derivatives of 4-... Polyalkylene glycol derivatives of 4-...

C - Chemistry, Metallurgy

07

D

C07D 239/94 (2006.01) A61K 31/517 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2621111

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. The disclosed EGFR-TK irreversible inhibitors comprise a polyalkylene glycol moiety and are characterized by improved solubility, biostability and bioavailability.

L'invention concerne de nouveaux inhibiteurs irréversibles de la tyrosine kinase du récepteur du facteur de croissance épidermique (EGFR-TK); des compositions pharmaceutiques comprenant ces inhibiteurs et l'utilisation des inhibiteurs dans le traitement de maladies ou troubles associés à EGFR-TK. L'invention concerne en outre de nouveaux inhibiteurs irréversibles, radiomarqués, d'EGFR-TK, et leur utilisation comme marqueurs biologiques destinés à la radiologie médicale, telle que la tomographie par émission de positrons (TEP) et la tomographie monophotonique d'émission (SPECT), et comme produits radiopharmaceutiques destinés à la radiothérapie. Les inhibiteurs irréversibles d'EGFR-TK de l'invention comprennent un fragment de polyalkylène-glycol et se caractérisent par une solubilité, une biostabilité et une biodisponibilité améliorées.

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