Salts and polymorphs of a pyrrole-substituted indolinone...

C - Chemistry – Metallurgy – 07 – D

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C07D 403/06 (2006.01) A61K 31/404 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2540639

The invention relates to non-hygroscopic salts of 5-[(Z)-(5-fluoro-2-oxo-1 ,2- dihydro-3H-~indol-3-ylidene)methyl]-N-[(2 )-2-hydroxy-3-morpholin-4-ylpropyl]- 2,4-dimethyl-1 H-pyrrole-3~-carboxamide,shown in structural formula 1 such as maleate salts, and to crystalline polymorphs of these salts. The invention further relates to pharmaceutical compositions of 5-[(Z)-(5-fluoro-2-oxo-1 ,.2- dihydro-3H-indol-3~- ylidene)methyl]-N-[(2S)-2-hyd carboxamide salts, and meth roxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1 H-pyrrole-3~ ds of treating disorders such as cancer using such compositions.

L'invention concerne des sels non hygroscopiques de 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidène)méthyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-diméthyl-1H-pyrrole-3-carboxamide, représentés dans la formule développée (1), tels que des sels de maléate, et des polymorphes cristallins de ces sels. L'invention concerne également des compositions pharmaceutiques de sels de 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidène)méthyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-diméthyl-1H-pyrrole-3-carboxamide, et des méthodes pour traiter des affections, par exemple le cancer, à l'aide de ces compositions.

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