CAS: 334826-98-1; Gisadenafil

该化合物是一种化学化合物,属于5类磷酸盐酶(PDE5)抑制剂,主要用于研究其在处理立体机能障碍和肺动脉高血压方面的潜在用途;该化合物通过增强氧化氮的影响,导致血液流入身体特定地区增加;Gisadenafil展示了PDE5相对于其他磷化物的相对高选择性,这种选择有助于其治疗效果和减少副作用;其化学结构包括一个热环环系统,这种系统在PDE-5抑制剂中很常见,而且通常以口服形式进行.Gisadanafil的药理动力学涉及吸收,分布,新陈代谢和排泄过程,对于其有效性和安全性特征至关重要.与其他类药物一样,潜在副作用可能包括头痛,冲洗和胃肠扰动.持续的研究继续探索其在各个人群中的全面治疗潜力和安全性.

结构式图片

MSDS等安全信息

    上下游产品

    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 4-[2-Ethoxy-5-(4-Ethylpiperazin-1-Ylsulphonyl)Pyridin-3-Ylcarboxamido]-3-Ethyl-2-(2-Methoxyethyl)Pyrazole-5-Carboxamide 334828-19-2
    2-Ethoxy-5-(4-Ethylpiperazin-1-Ylsulphonyl)Pyridine-3-Carboxylic Acid Ethyl Ester 247582-68-9
    2-乙氧基-5-[(4-乙基-1-哌嗪基)磺酰基]烟酸 2-Ethoxy-5-(4-Ethyl-1-Piperazinylsulfonyl)Nicotinic Acid 247582-73-6

    合成工艺路线路线简述

      📜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

      海关参考信息

      专利信息


      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.

      供应商参考报价(招募中)

      品牌试剂参考报价(招募中)

      📌 第三方产品分析报告

      ✅ COA系统入驻 | 共享模式

      主要参考文献


      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.
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