4-氧代哌啶酮盐酸盐置于palladium On Activated Charcoal 氢气,Phosphorus Pentoxide体系中,用 四氢呋喃,乙醇,N,N-二甲基甲酰胺,甲苯 作为反应溶剂,化学反应生成 4-(4-氟苯基)哌啶 参考文献:Pharmacophore-Based Discovery,Synthesis,And Biological Evaluation Of 4-Phenyl-1-Arylalkyl Piperidines As Dopamine Transporter Inhibitors 标题:Pharmacophore-Based Discovery,Synthesis,And Biological Evaluation Of 4-Phenyl-1-Arylalkyl Piperidines As Dopamine Transporter Inhibitors 摘要:Pharmacophore-Based Discovery,Synthesis,And Structure-Activity Relationship (Sar) Of A Series Of 4-Phenyl-1-Arylalkyl Piperidines Are Disclosed. These Compounds Have Been Evaluated For Their Ability To Inhibit Reuptake Of Dopamine (Da) Into Striatal Nerve Endings (Synaptosomes). The Lead Compound 5 And The Most Potent Analogue 43 Were Found To Have Significant Functional Antagonism. (C) 2001 Elsevier Science Ltd. All Rights Reserved. DOI:10.1016/s0960-894X(00)00703-4
专利号:WO-2004058727-A1 优先权日:2002-12-20 标题 :Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity 发明人:CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA 权利人:BAYER PHARMACEUTICALS CORP; CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA 摘要:This invention relates to substituted 3,5-dihydro-4H-imidazol-4-ones compounds which are useful in the treatment of obesity and obesity-related disorders, and as weight-loss and weight-control agents. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
专利号:US-6232318-B1 优先权日:1998-11-12 标 题:Pyrimidinedione derivatives useful as alpha 1A adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G 权利人:MERCK & CO LTD 摘要:Novel pyrimidinedione 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: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:WO-2009035652-A1 优先权日:2007-09-13 标 题 :Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof
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.