CAS: 241800-98-6; Zoniporide

该化合物是一种专门的七环化合物,其特点是一个配有quinon moity 和 carbamidoil 功能组的丙烯基核,其结构复杂性使其具有高度的结合性和选择性,使其成为药用化学和药物发现的宝贵中间体.环丙基代基基成分增强了代谢稳定性,而碳箱胺基组则提高了溶性性和生物利用率.该化合物因其具有调节酶活动的能力,在发展动酶抑制剂和其他定向治疗剂方面特别有用.其定义明确的合成途径确保了再生性,使之适合研究和临床前应用.

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guanidine hydr°Chloride 5-cyclopropyl-1-quinolin-5-yl-1H-pyrazole-4-carboxylic acid chloride guanidine nitrate ethyl 5-cyclopropyl-1-(quinolin-5-yl)-1H-pyrazole-4-carboxylate

合成工艺路线路线简述

    📜Ethyl 2-(Cyclopropanecarbonyl)-3-(Dimethylamino)Acrylate置于sodium Hydroxide,氯化亚砜,三乙胺体系中,用 四氢呋喃,甲醇,乙醇 用作溶剂,化学反应 4.0H,反应生成Zoniporide; Cp 597396; [1-(喹啉-5-基)-5-环丙基-1H-吡唑-4-甲酰基]胍
    参考文献:Discovery Of Zoniporide: A Potent And Selective Sodium-hydrogen Exchanger Type 1 (Nhe-1) Inhibitor With High Aqueous Solubility
    标题:Discovery Of Zoniporide: A Potent And Selective Sodium-hydrogen Exchanger Type 1 (Nhe-1) Inhibitor With High Aqueous Solubility
    摘要:Zoniporide (Cp-597,396) Is A Potent And Selective Inhibitor Of Nhe-1,Which Exhibits High Aqueous Solubility And Acceptable Pharmacokinetics For Intravenous Administration. The Discovery,Synthesis,Activities,And Rat And Dog Pharmacokinetics Of This Compound Are Presented. The Potency And Selectivity Of Zoniporide May Be Due To The Conformation That The Molecule Adopts Due To The Presence Of A Cyclopropyl And A 5-Quinolinyl Substituent On The Central Pyrazole Ring Of The Molecule. (C) 2001 Elsevier Science Ltd. All Rights Reserved.
    Doi:10.1016/s0960-894X(01)00059-2

    海关参考信息

    专利信息


    专利号:US-6294538-B1
    优先权日:1999-04-01
    标 题 :Compounds for treating and preventing diabetic complications
    发明人:MYLARI BANAVARA L
    权利人:PFIZER
    摘要:This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, n wherein R is as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.

    专利号:US-6936600-B2
    优先权日:1999-04-01
    标题:Sorbitol dehrydrogenase inhibitors
    发明人:CHU-MOYER MARGARET Y; MYLARI BANAVARA L; ZEMBROWSKI WILLIAM J
    权利人:PFIZER
    摘要:This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, n n nwherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.

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    ✅ COA系统入驻 | 共享模式

    合成参考文献


    参考文献:10.1016/j.neulet.2011.06.048
    摘要:Castañeda-Corral G, Rocha-González HI, Godínez-Chaparro B, Jiménez-Andrade JM, Granados-Soto V. Role of the spinal Na+/H+ exchanger in formalin-induced nociception. Neurosci Lett. 2011 Aug 21;501(1):4–9. doi: 10.1016/j.neulet.2011.06.048.
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