Pharmaceutical compositions comprising ret inhibitors and...

Details Pharmaceutical compositions comprising ret inhibitors and... Pharmaceutical compositions comprising ret inhibitors and...

A - Human Necessities

61

K

A61K 31/135 (2006.01) A61K 31/216 (2006.01) A61K 31/335 (2006.01) A61K 31/55 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2730190

A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is de-scribed. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are de-scribed. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumour cells.

La présente invention concerne une classe de composés utiles dans des compositions pharmaceutiques et des procédés de traitement ou de prévention du cancer. La capacité des composés à inhiber la kinase RET est quantifiée, c'est-à-dire que leurs valeurs respectives de CI50 et CE50 pour RET sont décrites. Un tel composé, appelé cyclobenzaprine et présentement désigné par SW-01, a été identifié comme étant spécifique de RET avec un CI50 de 300 nM. SW-01 inhibe l'autophosphorylation de RET et bloque la croissance et la transformation de lignées cellulaires de cancer de la thyroïde. Il a été également testé sur le cancer pancréatique, le cancer du sein et des lignées cellulaires SCLC. Les composés sont utiles pour l'inhibition de la survie et de la prolifération  de cellules tumorales.

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