Novel crystalline forms of the anti-cancer compound zd1839

Details Novel crystalline forms of the anti-cancer compound zd1839 Novel crystalline forms of the anti-cancer compound zd1839

C - Chemistry, Metallurgy

07

D

C07D 239/94 (2006.01) A61K 31/5377 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2477350

The invention concerns certain crystalline solvates and hydrates of the compound of the Formula (I) which is known inter alia by way of the code number ZD1839. In particular, the invention concerns a first solvate that occurs in the presence of methanol which is designated as Form 2 ZD1839 MeOH solvate, a second solvate that occurs in the presence of dimethyl sulphoxide which is designated as Form 3 ZD1839 DMSO solvate and a trihydrate that occurs in the presence of water which is designated Form 5 ZD1839 trihydrate. The invention further concerns processes for the preparation of these solvates and the trihydrate and for their conversion back to the compound ZD1839, pharmaceutical compositions containing them and their use in the manufacture of medicaments for use the production of an anti-proliferative effect in a warm-blooded animal such as man.

L'invention concerne certains solvates et hydrates cristallins du composé de formule (I) connu, <i>inter alia</i>, par son numéro de code ZD1839. Elle concerne, en particulier, un premier solvate qui se produit en présence de méthanol, désigné Forme 2 ZD1839 solvate MeOH, un second solvate qui se produit en présence de diméthylsulfoxyde désigné Forme 3 ZD1839 solvate DMSO et un trihydrate qui se produit en présence d'eau désigné Forme 5 ZD1839 trihydrate. Elle concerne enfin des procédés de préparation de ces solvates et du trihydrate et de leur conversion vers le composé ZD1839, des compositions pharmaceutiques les contenant et leur utilisation dans la fabrication de médicaments faisant usage de la production d'un effet antiproliférant chez l'animal à sang chaud, notamment chez l'homme.

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