专利号:US-6096763-A 优先权日:1995-02-23 标题 :α1a adrenergic receptor antagonists 发明人:HOFFMAN JACOB M; CHANG RAYMOND S L 权利人:MERCK & CO INC 摘要:This invention relates to novel compounds, their synthesis and use as selective α 1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the α 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.
专利号:WO-9625934-A1 优先权日:1995-02-23 标题 :ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS 发明人:EVANS BEN E; PONTICELLO GERALD S; HOFFMAN JACOB M; CHANG RAYMOND S L 权利人:MERCK & CO INC; EVANS BEN E; PONTICELLO GERALD S; HOFFMAN JACOB M; CHANG RAYMOND S L 摘要:This invention relates to novel compounds, their synthesis and use as selective α1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the α1a 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.
专利号:WO-9718209-A1 优先权日:1995-11-15 标 题:ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS 发明人:BOCK MARK G; PATANE MICHAEL A 权利人:MERCK & CO INC; BOCK MARK G; PATANE MICHAEL A 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.
专利号:US-5952351-A 优先权日:1995-02-23 标题 :Alpha 1a adrenergic receptor antagonists 发明人:EVANS BEN E; PONTICELLO GERALD S; HOFFMAN JACOB M 权利人:MERCK & CO INC 摘要:PCT No. PCT/US96/02534 Sec. 371 Date Aug. 13, 1997 Sec. 102(e) Date Aug. 13, 1997 PCT Filed Feb. 23, 1996 PCT Pub. No. WO96/25934 PCT Pub. Date Aug. 29, 1996This invention relates to novel compounds, their synthesis and use as selective alpha 1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The 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.
专利号:US-6075038-A 优先权日:1995-06-07 标题:Alpha 1a adrenergic receptor antagonists 发明人:PATANE MICHAEL A; BOCK MARK G; FREIDINGER ROGER M 权利人:MERCK & CO INC 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 fining. 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.
专利号:US-5807856-A 优先权日:1995-11-15 标题 :Alpha 1a adrenergic receptor antagonist 发明人:BOCK MARG G; PATANE MICHAEL A 权利人:MERCK & CO INC 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.
参考文献:10.1055/s-0031-1290332 摘要:Zeng W, Chen J, Dang L, Li Q, Ye Y, Fu S. TiCl4-Mediated Direct N-Alkylation of Sulfonamides with Inactive Ethers. Synlett. 2012 Feb 06;23(04):595–600. doi: 10.1055/s-0031-1290332.