📜N-[3-氨基甲酰基-5-乙基-1-(2-甲氧基乙基)吡唑-4-基]-2-乙氧基-5-(4-乙基哌嗪-1-基)磺酰基吡啶-3-甲酰胺置于双(三甲基硅烷基)氨基钾体系中,用 乙醇 作为反应溶剂,化学反应生成 5-[2-乙氧基-5-(4-乙基哌嗪-1-基磺酰基)吡啶-3-基]-3-乙基-2-(2-甲氧基乙基)-2,6-二氢-7H-吡唑并[4,3-D]嘧啶-7-酮 参考文献:Highly Potent And Selective Chiral Inhibitors Of Pde5: An Illustration Of Pfeiffer's Rule 标题:Highly Potent And Selective Chiral Inhibitors Of Pde5: An Illustration Of Pfeiffer's Rule 摘要:A Series Of Potent Chiral Pde5 Inhibitors Are Described That Are Based On The Sildenafil Architecture But Exhibit Much Greater Selectivity Over Pde6. Eudismic Analysis Of The Sar In This Series Provided A Clear Illustration Of Pfeiffer'S Rule And Indicated That The Chiral Motif Was Involved In A Highly-Stereoselective Interaction With Pde5. This Pde5 Specificity Translated To Levels Of Selectivity Over Pde6 That Were Hitherto Unprecedented In The Sildenafil Scaffold. Uk-371,800 (Compound 8) Was Identified As A Development Candidate From This Series That Married Sildenafil-Like Molecular Properties With High Selectivity Over Pde6. Clinical Data Confirm That Uk-371,800 Has Markedly Superior Human Pharmacokinetics To A Previously-Described Higher Molecular Weight Achiral Analogue In This Template (Compound 1). (C) 2008 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2008.10.037
专利号:US-2008280877-A1 优先权日:2007-05-10 标 题:Azetidines 发明人:DACK KEVIN NEIL; SKERRATT SARAH ELIZABETH; YEAP SIEW KUEN 权利人:PFIZER 摘要:The invention relates to EP2 antagonist azetidines of formula (I) n n n n n n n n n n wherein Ar, R 1 , X, and Z are as defined herein, to their use in medicine, particularly in the treatment of endometriosis and/or uterine fibroids, to intermediates useful in their synthesis, and to compositions containing them.
专利号:US-2008269233-A1 优先权日:2005-08-04 标 题:Piperidinoyl-Pyrrolidine and Piperidinoyl-Piperidine Compounds 发明人:ANDREWS MARK DAVID; BROWN ALAN DANIEL; SEBASTIEN DAVID; LANSDELL MARK IAN 权利人:ANDREWS MARK DAVID; BROWN ALAN DANIEL; SEBASTIEN DAVID; LANSDELL MARK IAN 摘要:The present invention relates to a class of compounds of general formula (I) n n n n n n n n n n and the salts, hydrates, solvates, polymorphs and prodrugs wherein n, R 6 , R 7 and R 10 are as defined herein and especially to MCR4 agonist compounds of formula (I), to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
专利号:US-2010256109-A1 优先权日:2007-11-15 标 题 :Azetidines As EP2 Antagonists 发明人:SKERRATT SARAH ELIZABETH; DACK KEVIN NEIL 权利人:SKERRATT SARAH ELIZABETH; DACK KEVIN NEIL 摘要:The present invention relates to a class of EP2 antagonistazetidines of general formula (I), wherein the variables and substituents are as defined herein, and especially to EP2 antagonist compounds, to their use in medicine, particularly in the treatment of endometriosis and/or uterine fibroids (leiomyomata) and to intermediates usefulin their synthesis and to compositions containing them.
专利号:US-8138188-B2 优先权日:2006-02-23 标题 :Melanocortin type 4 receptor agonist piperidinoylpyrrolidines 发明人:ANDREWS MARK DAVID; BROWN ALAN DANIEL; LANSDELL MARK IAN; SUMMERHILL NICHOLAS WILLIAM 权利人:ANDREWS MARK DAVID; BROWN ALAN DANIEL; LANSDELL MARK IAN; SUMMERHILL NICHOLAS WILLIAM; PFIZER 摘要:The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) n nwherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
1: Rawson DJ, Ballard S, Barber C, Barker L, Beaumont K, Bunnage M, Cole S, Corless M, Denton S, Ellis D, Floc'h M, Foster L, Gosset J, Holmwood F, Lane C, Leahy D, Mathias J, Maw G, Million W, Poinsard C, Price J, Russel R, Street S, Watson L. The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics. Bioorg Med Chem. 2012 Jan 1;20(1):498-509. doi: 10.1016/j.bmc.2011.10.022. Epub 2011 Oct 24. doi: 10.1016/j.eururo.2011.05.054. Epub 2011 Jun 12. Review. doi: 10.1124/dmd.111.038224. Epub 2011 Mar 30. doi: 10.1111/j.1464-410X.2010.09204.x. doi: 10.1111/j.1464-410X.2010.09205.x.
合成参考文献
参考文献:10.1111/j.1464-410x.2010.09205.x 摘要:Giuliano FA, Lamb J, Crossland A, Haughie S, Ellis P, Tamimi NA. A placebo-controlled exploratory study investigating the efficacy and safety of the phosphodiesterase type 5 inhibitor UK-369,003 for the treatment of men with storage lower urinary tract symptoms associated with a clinical diagnosis of overactive bladder. BJU Int. 2010 Sep;106(5):666–73. doi: 10.1111/j.1464-410x.2010.09205.x.