Alpha 1a adrenergic receptor antagonists

Details Alpha 1a adrenergic receptor antagonists Alpha 1a adrenergic receptor antagonists

A - Human Necessities

61

K

A61K 31/50 (2006.01) A61K 31/445 (2006.01) A61K 31/58 (2006.01) C07D 211/60 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2221746

This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha-1a 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 provided 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 nouveaux composés, leurs dérivés, leur synthèse, et leur utilisation comme antagonistes sélectifs du récepteur adrénergique alpha-1a, et dont l'une des applications est le traitement de l'hyperplasie prostatique bénigne. Ces composés ont une capacité sélective de relaxation des tissus des muscles lisses riches en sous-types de récepteurs alpha-1a, sans entraîner par la même occasion d'hypotension orthostatique. Un tissu de ce type entoure la muqueuse urétrale. En conséquence, l'une des applications des composés selon l'invention est de fournir un intense soulagement aux hommes souffrant d'hyperplasie prostatique bénigne en réduisant les obstacles s'opposant au passage de l'urine. Une autre application de ces composés résulte de leur association avec un composé inhibiteur de la 5-alpha réductase humaine, association qui permet d'apporter à la fois un soulagement instantané intense et un soulagement permanent des effets de l'hyperplasie prostatique bénigne.

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