Triazoles as oxytocin antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 249/14 (2006.01) A61K 31/4196 (2006.01) A61P 9/12 (2006.01) A61P 15/06 (2006.01) C07D 249/10 (2006.01) C07D 249/12 (2006.01) C07D 403/12 (2006.01) C07D 405/06 (2006.01) C07D 405/12 (2006.01) C07D 407/06 (2006.01) C07D 407/12 (2006.01)

Patent

CA 2469042

The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole deriva-tives. Said triazoles are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to triazole derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.

L'invention concerne des dérivés de triazole représentés par la formule (I), qui peuvent être utilisés notamment en tant que composés à activité pharmaceutique, ainsi que des préparations pharmaceutiques contenant de tels dérivés de triazole. Lesdits triazoles sont utiles pour le traitement et/ou la prévention du déclenchement prématuré du travail, de l'accouchement prématuré, des dysménorrhées, de la sécrétion inappropriée de vasopressine, de l'insuffisance cardiaque globale, de l'hypertension artérielle, de la cirrhose du foie, du syndrome néphrotique, et de l'hypertension oculaire. L'invention concerne en particulier des dérivés de triazole présentant une activité modulatrice élevée, en particulier une activité antagoniste, du récepteur de l'oxytocine et/ou de la vasopressine. Ces composé conviennent plus particulièrement pour le traitement et/ou la prévention des états pathologiques dans lesquels l'oxytocine, et/ou la vasopressine jouent un rôle de médiateur. L'invention concerne en outre de nouveaux dérivés de triazole, ainsi que des procédés permettant de les préparer.

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