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.
本发明涉及某些新型化合物及其衍
生物,它们的合成以及它们作为选择性α-1a
肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是用于治疗良性前列腺增生症。这些化合物在其选择性上具有能够松弛α 1a受体亚型丰富的平滑肌组织的能力,同时不会引起直立性低血压。这样的组织包括尿道内膜周围的组织。因此,本化合物的一个用途是为男性良性前列腺增生症患者提供急性缓解,从而使尿液流动更为顺畅。本化合物的另一个用途是与人类5α-还原酶
抑制剂化合物结合,从而实现对良性前列腺增生症的急性和慢性缓解。