C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 417/12 (2006.01) A61K 31/427 (2006.01) A61P 35/00 (2006.01)
Patent
CA 2430065
The invention relates to hydrochloride, hydrobromide, hemi-citrate, acetate, p- tosylate, L-tartrate, hemi-succinate, and mesylate salt forms of 3-(4-bromo- 2.6-difluoro-benzyloxy)-5-[3-(4-pyrrolidin-1-yl-butyl)-ureido]-isothiazole-4- carboxylic acid amide having the following formula: formula 1. The invention also relates to pharmaceutical compositions containing the hydrochloride, hydrobromide, hemi-citrate, acetate, p-tosylate, L-tartrate, hemi-succinate, and mesylate salts of formula 1. The invention further relates to methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above salts and to methods of preparing the crystal forms of the above slats.
L'invention concerne des formes salines de chlorhydrate, de bromhydrate, d'hémi-citrate, d'acétate, de p-tosylate, de L-tartrate, d'hémi-succinate, et de mésylate d'un amide d'acide 3-(4-bromo-2,6-difluoro-benzyloxy)-5-[3-(4-pyrrolidin-1-yl-butyl)-ureido]-isothiazole-4-carboxylique, représentées par la formule générale (1). L'invention concerne également des compositions pharmaceutiques contenant les sels de chlorhydrate, de bromhydrate, d'hémi-citrate, d'acétate, de p-tosylate, de L-tartrate, d'hémi-succinate, et de mésylate de la formule (1). L'invention concerne également des méthodes destinées au traitement de pathologies hyperprolifératives, telles que les cancers, chez le mammifère, en particulier chez l'être humain, consistant à administrer lesdits sels. Cette invention concerne également des méthodes de préparation des formes cristallines desdits sels.
Gant Thomas G.
Williams Glenn Robert
Osi Pharmaceuticals Inc.
Pfizer Inc.
Pfizer Products Inc.
Smart & Biggar
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