Amorphous form of 2-n-butyl-3-( (2-(1h-tetrazol-5-yl)...

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 403/10 (2006.01) A61K 31/415 (2006.01) A61K 31/4178 (2006.01) A61K 31/4184 (2006.01)

Patent

CA 2469656

The present invention relates to a novel amorphous form of 2-n-butyl-3-[[2~- (1H-tetrazol-5-yl)[1,1~-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-l-en-4- one and to a process for preparation thereof. Irbesartan (2-n-Butyl-3-[[2~-(1H- tetrazol-5-yl)[1,1~-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4] non-1- en-4- one), represented by the following formula (I), is a non-peptide angiotensin - II antagonist. By inhibiting the action of angiotensin - II on its receptors, this compound prevents the increase in blood pressure produced by the hormone- receptor interactions and is hence used in the treatment of cardiovascular complaints such as hypertension and heart failure.

L'invention concerne une nouvelle forme amorphe of 2-n-butyl-3-[[2'-(1H-tétrazol-5-yl)[1,1'-biphényl]-4-yl]méthyl]-1,3-diazaspiro[4.4]non-l-èn-4-one et un procédé de préparation correspondant. L'irbesartane (2-n-Butyl-3-[[2'-(1H-tétrazol-5-yl)[1,1'-biphényl]-4-yl]méthyl]-1,3-diazaspiro[4.4] non-1-èn-4-one) représenté par la formule suivante (I) est un antagoniste de l'angiotensine-II non peptidique. En inhibant l'action de l'angiotensine-II sur ses récepteurs, ce composé empêche l'augmentation de la pression sanguine produite par les interactions du récepteur de l'hormone et par conséquent, il est utilisé dans le traitement de troubles cardiovasculaires, tels que l'hypertension et l'insuffisance cardiaque.

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