Alpha1c adrenergic receptor antagonists

Details Alpha1c adrenergic receptor antagonists Alpha1c adrenergic receptor antagonists

C - Chemistry, Metallurgy

07

D

C07D 417/14 (2006.01) A61K 31/425 (2006.01) A61K 31/435 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 413/06 (2006.01) C07D 417/06 (2006.01) C07D 471/02 (2006.01) C07D 471/04 (2006.01) C07D 491/10 (2006.01) C07D 491/107 (2006.01) C07D 495/20 (2006.01) C07D 498/02 (2006.01) C07D 498/04 (2006.01) C07D 498/10 (2006.01) C07D 513/02 (2006.01) C07D 513/04 (2006.01) C07D 513/10 (2006.01)

Patent

CA 2187767

This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alphaIC adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hypertrophy. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alphaIC receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provide by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

L'invention porte sur certains composés nouveaux, leurs dérivés, leur synthèse et leur utilisation en tant qu'antagonistes sélectifs du récepteur adrénergique alpha1C. L'une de leurs applications réside dans le traitement de l'hypertrophie bénigne de la prostate. Ces composés présentent une capacité sélective de relaxation des tissus de muscles lisses enrichis en sous-catégorie du récepteur alpha1-C sans pour autant provoquer d'hypotension orthostatique. L'un de ces tissus entoure l'endothélium de l'urètre. L'un des intérêts de ces composés à action instantanée est donc d'apporter un soulagement rapide aux patients souffrant d'hypertrophie bénigne de la prostate en réduisant les obstacles au flux urinaire, un autre étant que, combinés avec un composé inhibiteur de la 5-alpha réductase humaine, ils peuvent soulager les effets aigus et chroniques de ladite hypertrophie.

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