CAS: 1978-61-6; 4-(4-Fluorophenyl)-1,2,3,6-Tetrahydropyridine Hydrochloride

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CAS号460-00-4 对氟溴苯 | CAS号3612-20-2 N-苄基-4-哌啶酮 | CAS号163631-02-5 1-苄基-4-(4-氟苯基)哌啶-4-醇 | CAS号79099-07-3 1-B°C-4-哌啶酮 | CAS号553631-05-3 1-B°C-4-(4-氟苯基)... | CAS号37656-48-7 4-(4-氟苯基)哌啶 | CAS号1978-59-2 4-(4-Fluorophen...

📜对溴氟苯置于盐酸,Magnesium体系中,用 四氢呋喃 用作溶剂,化学反应生成4-氟苯基-四羟基吡啶
参考文献:一些3-(1,2,3,6-四氢-1-吡啶基烷基)吲哚的合成和多巴胺能活性.一种新颖的构象模型来解释结构-活性关系.
标题:一些3-(1,2,3,6-四氢-1-吡啶基烷基)吲哚的合成和多巴胺能活性.一种新颖的构象模型来解释结构-活性关系.
摘要:描述了新型多巴胺激动剂的合成和多巴胺能性质.基本结构元素的数量和种类与刚性阿朴吗啡型多巴胺激动剂的数量和种类明显不同.使用标准的分子建模技术,开发了一种构象模型,提出了一种u形构象,通过此类化合物的两个富电子芳族结构元素之间的芳香pi-Pi相互作用,在能量上可能是优选的.铅化合物28的构象与阿扑吗啡的重叠产生了一个新颖的模型,解释了在这类吲哚烷基胺中发现的非典型结构-活性关系.
Doi:10.1021/jm00100A006

专利信息

专利号:WO-0027817-A1
优先权日:1998-11-10
标 题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists
发明人：NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G
权利人:MERCK & CO INC; NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G
摘要:Novel hydroxymethyl- and alkoxymethyl-oxazolidinone compounds 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 uring 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.

专利号:WO-0027827-A1
优先权日:1998-11-10
标题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists
发明人：NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA
权利人:MERCK & CO INC; NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA
摘要:Novel oxazolidinone compounds 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.

专利号:US-6228870-B1
优先权日:1998-11-10
标 题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists
发明人：NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G
权利人:MERCK & CO INC
摘要:Novel hydroxymethyl- and alkoxymethyl-oxazolidinone compounds 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.

专利号:US-6235759-B1
优先权日:1998-10-29
标 题 :Dihydropyridinones and pyrrolinones useful as alpha 1A adrenoceptor antagonists
发明人：BARROW JAMES C; NANTERMENT PHILIPPE G; SELNICK HAROLD G
权利人:MERCK & CO INC
摘要:Novel dihydropyridinone and pyrrolinone compounds 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.

专利号:US-6358959-B1
优先权日:1999-01-26
标 题:Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists
发明人：BOCK MARK G; PATANE MICHAEL A; STEELE THOMAS G
权利人:MERCK & CO INC
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.

专利号:US-6319932-B1
优先权日:1998-11-10
标 题 :Oxazolidinones useful as alpha 1A adrenoceptor antagonists
发明人：NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA
权利人:MERCK & CO INC
摘要:Novel oxazolidinone compounds 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.