Alpha-1a adrenergic receptor antagonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514330, 514284, 546215, 546225, A61K 31445, C07D21136

Patent

active

056611633

ABSTRACT:
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.

REFERENCES:
patent: 5403847 (1995-04-01), Gluchowski et al.
J. Med. Chem., Wetzel et al., Discovery of Alpha 1a Adrenergic Receptor Antagonists Based on the L-Type Ca2+ Channel Antagonist Niguldipine, May 12, 1995, vol. 38, No. 10, pp. 1579-1581.

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