Novel process

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 209/14 (2006.01)

Patent

CA 2667222

The present invention relates to a novel process for the synthesis of 1-((5-methoxy- 1H-indol-3-yl)methyleneamino)-3-pentyl-guanidine, commonly known as tegaserod, which is used as a gastroprokinetic, and salts thereof. The present invention also relates to tegaserod and salts thereof having an HPLC purity of about 95% or more. The present invention further relates to pharmaceutical compositions comprising tegaserod or a salt thereof, second medical uses of tegaserod or a salt thereof, and methods of treating or preventing irritable bowel syndrome using tegaserod or a salt thereof.

La présente invention porte sur un nouveau procédé de synthèse de la 1-((5-méthoxy-1H-indol-3-yl)méthylèneamino)-3-pentyl-guanidine, couramment appelée tégaserod, utilisée comme agent gastroprocinétique, et des sels de celle-ci. La présente invention porte également sur le tégaserod et ses sels présentant une pureté en HPLC d'environ 95 % ou plus. La présente invention porte aussi sur des compositions pharmaceutiques comprenant la tégaserod ou un sel de celui-ci, sur des secondes utilisations médicales du tégaserod ou d'un sel de celui-ci, et sur des procédés de traitement ou de prévention du côlon irritable par le tégaserod ou un sel de celui-ci.

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