Nonpeptide substituted benzothiazepines as vasopressin...

C - Chemistry – Metallurgy – 07 – D

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C07D 281/10 (2006.01) A61K 31/554 (2006.01) A61P 9/10 (2006.01)

Patent

CA 2389439

The invention is directed to nonpeptide substituted benzodiazepines of Formula (I), wherein A, X, Z, Bp, W, n, R1 and R2 are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising a compound of Formula (I) and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.

L'invention concerne des benzodiazépines à substitution non peptidique correspondant à la formule (I) dans laquelle A, X, Z, Bp, W, n, R?1¿ et R?2¿ sont décrits dans la spécification. Ces benzodiazépines s'utilisent comme antagonistes des récepteurs de vasopressine à des fins de traitement d'états liés à une résistance vasculaire accrue et à une insuffisance cardiaque. L'invention concerne aussi des compositions pharmaceutiques correspondant à la formule (I) destinées au traitement d'états tels que l'hypertension, l'insuffisance cardiaque et l'insuffisance cardiaque globale, le spasme coronaire, l'ischémie cardiaque, la cirrhose du foie, le spasme vasculaire rénal, l'insuffisance rénale, l'oedème cérébral et l'ischémie, l'ictus, la thrombose ou la rétention d'eau.

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