5-[4-[2- (n-methyl-n- (2-pyridyl)amino) ethoxy]benzyl]...

C - Chemistry – Metallurgy – 07 – D

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C07D 417/12 (2006.01) A61K 31/425 (2006.01)

Patent

CA 2314107

A hydrate of 5-[4-[2- (N-methyl-N- (2-pyridyl)amino) ethoxy]benzyl] thiazolidine-2, 4-dione, maleic acid salt, characterised in that it: (i) comprises water in the range of from 0.4 to 2.5 %w/w; and (ii) provides an infra red spectrum containing peaks at 1749, 1703, 1645, 1623, 1365 and 736 cm- 1; and/or (iii) provides an X-ray powder diffraction (XRPD) pattern substantially as set out in Figure II and/or (iv) provides a Raman spectrum containing peaks at 3106, 3069, 3002, 2961, 1750, 1718, 1684, 1385, 1335, 1229, 1078, 917, 428 and 349 cm-1 and/or (iv) provides a solid-state nuclear magnetic resonance spectrum containing chemical shifts substantially as set out in Table I; a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of such a compound or composition in medicine.

L'invention porte sur un hydrate, sel de l'acide maléïque, de formule 5-[4-[2- (N-méthyl-N- (2-pyridyl)amino) éthoxy]benzyl] thiazolidine-2, 4-dione, caractérisé en ce qu'il: (i) comporte de l'eau à raison de 0,4 à 2,5 % P/P; (ii) présente un spectre IR comportant des pics à 1749, 1703, 1645, 1623, 1365 et 736 cm?-1¿; (iii) et/ou présente un motif de diffraction des rayons X par sa poudre (XRPD) (cf fig II); (iv) et/ou présente un spectre de Raman comportant des pics à 3106, 3069, 3002, 2961, 1750, 1718, 1684, 1385, 1229, 1078, 917, 428, et 349 cm?-1¿; et/ou (v) présente un spectre de RMN à l'état solide comportant des déplacements chimiques (cf fig I). L'invention porte également sur le procédé de préparation dudit sel, sur une préparation pharmaceutique le contenant et sur son utilisation et celle de ladite préparation en médecine.

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