公开(公告)号：US6057350A

公开(公告)日：2000-05-02

申请号：US98781

申请日：1998-06-17

申请人： Michael A. Patane ,  Mark G. Bock ,  Dhanapalan Nagarathnam ,  Bharat Lagu ,  Wai C. Wong

发明人： Michael A. Patane ,  Mark G. Bock ,  Dhanapalan Nagarathnam ,  Bharat Lagu ,  Wai C. Wong

IPC分类号： C07C255/46 ,  C07D263/26 ,  C07D275/06 ,  A61K31/42 ,  A61K31/425 ,  C07D263/22

CPC分类号： C07D275/06 ,  C07C255/46 ,  C07D263/26 ,  C07C2101/02 ,  C07C2101/14 ,  C07C2103/18

摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as 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 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.

公开(公告)号：US6037354A

公开(公告)日：2000-03-14

申请号：US99031

申请日：1998-06-17

申请人： Michael A. Patane ,  Harold G. Selnick ,  Mark G. Bock

发明人： Michael A. Patane ,  Harold G. Selnick ,  Mark G. Bock

IPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D263/06 ,  A61K31/42 ,  C07D263/04 ,  C07D277/04

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as 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 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.

公开(公告)号：US5747490A

公开(公告)日：1998-05-05

申请号：US716041

申请日：1996-09-19

申请人： Mark G. Bock ,  Michael A. Patane ,  William C. Lumma

发明人： Mark G. Bock ,  Michael A. Patane ,  William C. Lumma

IPC分类号： C07D403/04 ,  C07D405/14 ,  A61K31/535 ,  A01N43/60 ,  C07D239/72 ,  C07D415/00

CPC分类号： C07D403/04 ,  C07D405/14

摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1b adrenergic receptor antagonists. These compounds display submicromolar affinity for the human alpha 1b adrenergic receptor subtype while displaying at least five-fold lower affinity for the human alpha 1d and alpha 1a adrenergic receptor subtypes, and many other G-protein coupled human receptors. One application of these compounds is in the treatment of hypertension. More specifically, these compounds display selectivity for lowering blood pressure without, for example, substantially affecting urethral pressure.

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α1b肾上腺素能受体拮抗剂的用途。 这些化合物对人α1b肾上腺素能受体亚型显示亚微摩尔亲和力，同时对人α1d和α1a肾上腺素能受体亚型和许多其它G蛋白偶联的人受体显示出至少五倍的亲和力。 这些化合物的一种应用是治疗高血压。 更具体地，这些化合物显示出降低血压的选择性，而不会例如显着影响尿道压力。