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    Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists
    5.
    发明授权
    Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists 失效
    可用作α1a肾上腺素受体拮抗剂的多氮杂萘酮衍生物

    公开(公告)号：US06358959B1

    公开(公告)日：2002-03-19

    申请号：US09481991

    申请日：2000-01-11

    申请人： Mark G. Bock ,  Michael A. Patane ,  Thomas G. Steele

    发明人： Mark G. Bock ,  Michael A. Patane ,  Thomas G. Steele

    IPC分类号： C07D23980

    CPC分类号： C07D401/12 ,  C07D239/82 ,  C07D401/14 ,  C07D403/12

    摘要： Dihydro-polyazanaphthalen-2-one compounds (e.g., dihydroquinazolin-2-one and dihydropteridin-2-one derivatives) and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. 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 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 can be achieved.

    摘要翻译： 公开了二氢 - 聚氮杂萘-2-酮化合物（例如二氢喹唑啉-2-酮和二氢蝶啶-2-酮衍生物）及其药学上可接受的盐。 还描述了这些化合物的合成及其作为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。 这些化合物具有选择性地放松富集α1a受体亚型的平滑肌组织的能力，而不会同时引起低血压。 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。 通过与人类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。