A crystalline dibenzothiazepine derivative and its use as an...

C - Chemistry – Metallurgy – 07 – D

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C07D 281/16 (2006.01) A61K 31/55 (2006.01)

Patent

CA 2295792

Crystalline 11-(4-[2(2-hydroxyethoxy) ethyl]-1-piperazinyl)-dibenzo[b,f] [1,4]thiazepine (I) may be prepared by crystallising 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine from a non-aromatic solvent such as ethyl acetate, isobutyl acetate, methyl iso-butylketone or methyl tert-butyl ether, preferably in the absence of water. The crystalline material produced may be converted into a pharmaceutically acceptable salt such as a fumarate. The crystalline 11-(4-[2-(2-hydrox- yethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine may be used to treat psychoses.

Pour préparer un composé cristallin (I) de 11-(4[2-(2-hydroxyéthoxy) éthyle]-1-pipérazinyle)-dibenzo[b,f] [1,4]thiazépine formule (I) on peut cristalliser du 11-(4[2-(2-hydroxyéthoxy)éthyle]-1-pipérazinyle)-dibenzo[b,f][1,4]thiazépine à partir d'un solvant non aromatique tel que de l'acétate d'éthyle, de l'acétate d'isobutyle, du méthyle iso-butylcétone ou du méthyle tert-butyléther, de préférence en l'absence d'eau. Le matériau cristallin produit peut ensuite être transformé en un sel pharmaceutiquement acceptable tel qu'un fumarate. Le composé cristallin 11-(4[2-(2-hydroxyéthoxy)éthyle]-1-pipérazinyle)-dibenzo[b,f][1,4]thiazépine peut être utilisé pour traiter les psychoses.

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