Alpha 1a adrenergic receptor antagonist

Details Alpha 1a adrenergic receptor antagonist Alpha 1a adrenergic receptor antagonist

1996-11-12

1998-09-15

Bernhardt, Emily

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514171, 514253, 514255, 544360, 544364, 544368, 544379, 544393, 544388, 544389, 544390, 544384, 544385, A61K 31495, A61K 3158, C07D24104, C07D41706

Patent

active

058078568

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.

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patent: 4760071 (1988-07-01), Rasmusson et al.
patent: 5403847 (1995-04-01), Gluchowski et al.
patent: 5620993 (1997-04-01), Patane et al.
patent: 5661163 (1997-08-01), Patane et al.
El-Bermawy et al, Chemical Abstracts, vol. 117, No. 226102 (1992).
Patane et al, Chemical Abstracts, vol. 126, No. 131383 (1997) (Abstract for WO 96 40136, Dec. 19, 1996).

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