C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 223/16 (2006.01) A61K 31/55 (2006.01) C07D 207/00 (2006.01) C07D 211/00 (2006.01) C07D 223/00 (2006.01) C07D 223/14 (2006.01) C07D 401/10 (2006.01) C07D 401/12 (2006.01) C07D 403/10 (2006.01) C07D 403/14 (2006.01)
Patent
CA 2413945
The invention is directed to nonpeptide substituted benzodiazepines of Formula I, wherein A, X, n, R1, R2, R3, R4, R5, a and b are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those 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 porte sur des spirobenzoazepines non peptidiques substituées, antagonistes de la vasopressine, de formule générale (i) dans laquelle: A, X, n, R1, R2, R3, R4, R5, a et b sont définis dans la description, et qui s'avèrent d'utiles antagonistes du récepteur de la vasopressine pour le traitement de troubles liés à l'activité dudit récepteur dont ceux impliquant un accroissement de la résistance vasculaire, et l'insuffisance cardiaque. L'invention porte également sur des compositions pharmaceutiques comprenant un composé de formule (I), et sur des procédés de traitement d'affections telles que l'hypertension, l'insuffisance cardiaque congestive, l'insuffisance cardiaque, l'angiospasme coronarien, l'ischémie cardiaque, la cirrhose du foie, l'angiospasme du rein, l'oedème cérébral, l'ischémie cérébrale, les attaques, les thromboses ou la rétention d'eau.
Chen Robert H.k.
Xiang Min A.
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
Ortho-Mcneil Pharmaceutical Inc.
Ortho-Mcneil-Janssen Pharmaceuticals Inc.
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