Process for the preparation of...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 405/12 (2006.01) A61K 31/517 (2006.01)

Patent

CA 2590735

The present invention relates to chemical processes useful in the manufacture of the compound 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin- 1-yl)ethoxy]- 5-tetrahydropyran-4-yloxyquinazoline (the active entity within AZD0530), to intermediates useful in the manufacture of that compound and to processes for the manufacture of those intermediates. The invention also relates to particular crystalline forms of that compound such as a difumarate salt and a trihydrate and to pharmaceutical compositions containing such crystalline forms.

Cette invention concerne des procédés chimiques servant à fabriquer le composé 4-(6-chloro-2,3-méthylènedioxyanilino)-7-[2-(4-méthylpipérazin-1-yl)éthoxy]-5-tétrahydropyran-4-yloxyquinazoline (le principe actif de AZD0530), des intermédiaires utiles dans la fabrication de ce composé et des procédés de fabrication de ces intermédiaires. Cette invention concerne également des formes cristallines particulières de ce composé, telles qu'un sel difumarate et un trihydrate, et des compositions pharmaceutiques contenant ces formes cristallines.

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