Manufacturing process for no-donating compounds such as...

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 201/00 (2006.01) A61K 31/216 (2006.01) A61P 29/00 (2006.01) C07C 67/03 (2006.01) C07C 205/40 (2006.01) C07C 211/55 (2006.01) C07C 303/28 (2006.01) C07C 309/63 (2006.01) C07C 309/66 (2006.01)

Patent

CA 2498943

The present invention relates to a new process for the preparation of NO- donating compounds using a sulfonated intermediate. The invention relates to new intermediates prepared therein suitable for large scale manufacturing of NO-donating compounds. The invention further relates to the use of the new intermediates for the manufacturing of pharmaceutically active NO-donating compounds.The invention further relates to a substantially crystalline form of NO-donating NSAIDs, especially 2-[2-(nitrooxy)ethoxy]ethyl {2-[(2,6- dichlorophenyl)amino]phenyl}acetate, the preparation thereof and to pharmaceutical formulations containing said crystalline form and to the use of said crystalline form in the preparation of a medicament.

L'invention concerne un procédé de préparation de composés donneurs de NO au moyen d'un intermédiaire sulfoné. Cette invention concerne aussi des intermédiaires préparés au cours de ce procédé servant à fabriquer à grande échelle des composés donneurs de NO, ainsi que l'utilisation de ces intermédiaires dans la fabrication de composés donneurs de NO actifs sur le plan pharmaceutique. L'invention concerne enfin une forme sensiblement cristalline de NSAID donneur de NO, notamment de l'acétate 2-[2-(nitrooxy)éthoxy]éthyle {2-[(2,6-dichlorophényl)amino]phényle}. L'invention concerne enfin la préparation de celle-ci au moyen d'une formulation pharmaceutique contenant cette forme cristalline ainsi que l'utilisation de cette forme cristalline dans la préparation d'un médicament.

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