公开(公告)号：US5807856A

公开(公告)日：1998-09-15

申请号：US747687

申请日：1996-11-12

申请人： Marg G. Bock ,  Michael A. Patane

发明人： Marg G. Bock ,  Michael A. Patane

IPC分类号： A61K31/495 ,  A61K31/58 ,  C07D241/04 ,  C07D417/06

CPC分类号： A61K31/495 ,  A61K31/58 ,  C07D241/04 ,  C07D417/06

摘要： 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.

摘要翻译： 本发明涉及某些新化合物及其衍生物，其合成及其作为选择性α1a肾上腺素能受体拮抗剂的用途。 这些化合物的一个应用是治疗良性前列腺增生。 这些化合物在其能够松弛富含α1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。 发现一个这样的组织围绕尿道衬里。 因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。 通过与人5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。