Crystalline forms of a pyrrolotriazine compound

Details Crystalline forms of a pyrrolotriazine compound Crystalline forms of a pyrrolotriazine compound

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/53 (2006.01)

Patent

CA 2611263

The invention provides crystalline forms of the pyrrolotriazine compound [4- [[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methyl-pyrrolo[2,1- f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3-morpholinylmethyl ester and pharmaceutical compositions comprising at least one crystalline form, as well of methods of using the crystalline forms in the treatment of a proliferative disease, and methods for obtaining such crystalline forms. The compounds of formula (I), including [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5- methyl-pyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3- morpholinylmethyl ester, are useful for inhibiting tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

L'invention concerne des formes cristallines du composé de pyrrolotriazine [4-[[1-(3-fluorophényl)méthyl]-1H-indazol-5-ylamino]-5-méthyl-pyrrolo[2,1-f][1,2,4]triazine-6-yl] acide carbamique, un ester de (3S)-3-morpholinylméthyle et des compositions pharmaceutiques comprenant au moins une forme cristalline, ainsi que des méthodes d'utilisation des formes cristallines dans le traitement d'une maladie proliférative et des méthodes d'obtention de telles formes cristallines. Les composés de formule (I), y compris [4-[[1-(3-fluorophényl)méthyl]-1H-indazol-5-ylamino]-5-méthyl-pyrrolo[2,1-f][1,2,4]triazine-6-yl] acide carbamique, l'ester de (3S)-3-morpholinylméthyle sont utilisés dans l'inhibition de l'activité de la tyrosine kinase de récepteurs du facteur de croissance comme HER1, HER2 et HER4, ce qui permet de les rendre utiles en tant qu'agents antiprolifératifs destinés au traitement du cancer et d'autres maladies.

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