CAS: 224785-90-4; 2-(2-Ethoxy-5-((4-Ethylpiperazin-1-yl)Sulfonyl)Phenyl)-5-Methyl-7-Propylimidazo[5,1-F][1,2,4]Triazin-4(3H)-One

该化合物是一种主要用于治疗勃起功能障碍的五型选择性磷化柴油抑制剂(PDE5),它通过增加血液流到阴茎以回应性刺激而增强勃起功能.Vardenafil的化学配方是C23H32N6O4S, 其结构复杂, 包括一个管子环和一个磺酰胺组. Vardenafil以其行动迅速开始, 通常在施用后30至60分钟内生效, 其效果可以持续数小时. 它通常以平板形式口头使用, 并可在各种剂量中提供. 常见副作用可能包括头痛, 冲水, 鼻塞和痢疾. 与其他 PDE5 抑制剂一样, 与硝酸盐一起使用, 与严重减肥的风险无关. 病人在使用之前必须咨询保健专业人员, 特别是具有基本健康状况或服用其他药物的人.

结构式图片

欧盟法规

REACH注册ECHA物质C&L通报REACH预注册

上下游产品

CAS号5308-25-8 N-乙基哌嗪 | CAS号224789-21-3 2-(2-乙氧基苯基)-5-甲... | CAS号224789-26-8 4-乙氧基-3-(5-甲基-4...

合成工艺路线路线简述

  • 合成目标产物 Vardenafil 主要起始原料 1-Ethylpiperazine And 2-(2-Ethoxyphenyl)-5-Methyl-7-Propyl-3H-Imidazol[5,1-F][1,2,4]-Triazin-4-One
  • (文献来源)合成步骤主要原料 1-Ethylpiperazine 和 2-(2-Ethoxyphenyl)-5-Methyl-7-Propyl-3H-Imidazol[5,1-F][1,2,4]-Triazin-4-One
2-乙氧基苯甲酰胺置于氯磺酸,氯化亚砜,一水合肼,Lithium Hexamethyldisilazane,三氯氧磷体系中,用 四氢呋喃,乙醇 用作溶剂,化学反应 17.5H,反应生成伐地那非三水合盐酸盐
参考文献:N-Butyramide,The Preparation Method And Use Thereof
标题:N-Butyramide,The Preparation Method And Use Thereof
摘要:揭示了n-{1-[3-(2-乙氧基-5-(4-乙基哌嗪基)磺酰基苯基)-4,5-二氢-5-氧代-1,2,4-三嗪-6-基]乙基}丁酰胺(用公式iii表示),其制备方法,制备过程中的中间体,这些中间体的制备方法以及从该化合物制备瓦登非尔的方法.在制备瓦登非尔的方法中,氯磺化反应在制备过程的早期阶段进行.

海关参考信息

专利信息


专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:US-12295961-B2
优先权日:2009-12-31
标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
发明人:DHINGRA OM
权利人:MARIUS PHARMACEUTICALS INC
摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-12187735-B2
优先权日:2018-09-17
标 题:Matter of composition, synthesis, formulation and application of FL118 platform positions 7 and 9-derived analogues for treatment of human disease
发明人:LING XIANG; LI QINGYONG; LI FENGZHI
权利人:CANGET BIOTEKPHARMA LLC
摘要:Described herein, are the chemical synthesis, matter of compositions, formulation, function, methods and uses of the FL118 platform Positions 7 and/or 9-derived analogues for treating cancer or other human diseases. Compounds derived from chemical modifications of the FL118 platform are employed alone or in combination with other anti-cancer agents to preclude, eliminate or reverse cancer phenotypes. This invention intends to realize unique personalized cancer treatment (personalized precision medicine) through application of a series of structural relevant individual FL118 platform-derived analogues, which target multiple cellular human disease-relevant proteins and their signaling pathways.

专利号:US-2025092058-A1
优先权日:2018-09-17
标 题 :Matter of composition, synthesis, formulation and application of fl 118 platform positions 7 and 9-derived analogues for treatment of human disease
发明人:LING XIANG; LI QINGYONG; LI FENGZHI
权利人:CANGET BIOTEKPHARMA LLC
摘要:Described herein, are the chemical synthesis, compounds, methods and uses of the fluoroaryl-substituted derivatives at the FL118 position 7, which target multiple cellular human disease-relevant proteins and their signaling pathways.

专利号:US-11617758-B2
优先权日:2009-12-31
标 题 :Emulsion formulations
发明人:DHINGRA OM; BERNSTEIN JAMES S
权利人:MARIUS PHARMACEUTICALS LLC
摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
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主要参考文献


1: Sandqvist A, Henrohn D, Egeröd H, Hedeland M, Wernroth L, Bondesson U, Schneede J, Wikström G. Acute vasodilator response to vardenafil and clinical outcome in patients with pulmonary hypertension. Eur J Clin Pharmacol. 2015 Oct;71(10):1165-73. doi: 10.1007/s00228-015-1914-z. Epub 2015 Aug 5. doi: 10.1139/cjpp-2013-0316. Epub 2013 Nov 26. doi: 10.1016/B978-0-12-800173-8.00009-X. Review. doi: 10.4103/0253-7613.129315.
5: Aziret M, Irkorucu O, Reyhan E, Erdem H, Das K, Ozkara S, Surmelioglu A, Sozen S, Bali I, Cetinkunar S, Deger KC. The effects of vardenafil and pentoxifylline administration in an animal model of ischemic colitis. Clinics (Sao Paulo). 2014 Nov;69(11):763-9. doi: 10.6061/clinics/2014(11)10.
6: Gamidov SI, Iremashvili VV, Popova AIu. [Modernity in the treatment of erectile dysfunction: Levitra (vardenafil) in the form of oral dispersible tablet]. Urologiia. 2013 May-Jun;(3):102-4, 106. Review. Russian. doi: 10.1038/ijir.2014.39. Epub 2014 Dec 4. doi: 10.1016/j.chemosphere.2014.12.011. Epub 2015 Jan 10. doi: 10.2147/DDDT.S94615. eCollection 2015.

合成参考文献


参考文献:10.1556/oh.2010.28800
摘要:Kopa Z, Romics I. [Therapy of erectile dysfunction]. Orv Hetil. 2010 Feb 27;151(9):354–7. doi: 10.1556/oh.2010.28800.
参考文献:10.1111/j.1365-2125.2010.03828.x
摘要:Ückert S, Oelke M. Phosphodiesterase (PDE) inhibitors in the treatment of lower urinary tract dysfunction. Brit J Clinical Pharma. 2011 Jul 11;72(2):197–204. doi: 10.1111/j.1365-2125.2010.03828.x.
参考文献:10.1186/1471-2415-5-28
摘要:Anbar RD, Savedoff AD. Hypnosis-associated blue-tinted vision: a case report. BMC Ophthalmol. 2005 Dec 01;5():28.
参考文献:10.4103/1817-1737.82436
摘要:Bozbas SS, Eyuboglu F. Evaluation of liver transplant candidates: A pulmonary perspective. Ann Thorac Med. 2011 Jul;6(3):109–14.
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