CAS: 972-02-1; Diphenidol

该化合物是一种合成有机化合物,其第三级酒精核心由两个苯基组和一个管状替代丁基链组成,其结构包括芳香和脂类成分,使其成为制药和精细化学合成的多用途中间体,管状腺会增加溶解性和生物利用率,而二苯基组则会助长不耐烦的成份,可能影响受体研究中的结合性.由于CNS活性剂具有平衡的亲脂性和氢燃烧能力,这种化合物在药用化学中特别有用,有利于CNS活性剂的研制,其定义明确的合成途径可以实现高纯度和可复制性,支持药物发现和分子设计的研究.

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MSDS等安全信息

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    CAS号110-89-4 六氢吡啶 | CAS号201230-82-2 carbon monoxide | CAS号3923-51-1 α-ethenyl-α-phe... | CAS号119-61-9 二苯甲酮 | CAS号63645-18-1 4-hydroxy-4,4-d...

    合成工艺路线路线简述

      哌啶,Alkaline Earth Salt Of/the/ Methylsulfuric Acid 反应生成 地芬尼多
      参考文献:Gb683950
      标题:Gb683950

      海关参考信息

      专利信息


      专利号:WO-9614060-A1
      优先权日:1994-11-04
      标题 :Use of receptor agonists to stimulate superoxide dismutase activity
      发明人:MARKLUND STEFAN L; STRAALIN PONTUS
      权利人:MARKLUND STEFAN L; STRAALIN PONTUS
      摘要:The present invention relates to the use of a substance for the manufacture of a composition for stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells. In particular, the invention relates to the use of a substance for the manufacture of a composition for prophylaxis or treatment of a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical. Further, the invention relates to a method for determining the effect of a substance with respect to stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells and to substances which have been selected by said method. Within the scope of the invention is a method of preventing, diminishing, controlling or inhibiting a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical in a patient who has been established to have a high risk of developing a such disease or disorder, or who has developed a such disease or disorder, the method comprising administering an effective amount of a substance which is capable of stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells.

      专利号:US-2008300418-A1
      优先权日:2004-11-08
      标 题:Synthesis of Cardiolipin Analogues and Uses Thereof
      发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
      权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
      摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.

      专利号:US-2008214827-A1
      优先权日:2004-02-03
      标 题:Synthesis of Cyanoimino-Benzoimidazoles
      发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
      权利人:EURO CELTIQUE SA
      摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

      专利号:WO-0054773-A1
      优先权日:1999-03-12
      标题:Dopamine agonists in combination with nitric oxide donors, compositions and methods of use
      发明人:GARVEY DAVID S
      权利人:NITROMED INC; GARVEY DAVID S
      摘要:The present invention is directed to novel compositions comprising at least one dopamine agonist in combination with at least one nitric oxide donor (i.e. compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are substrates for nitric oxide synthase). The novel compositions may optionally comprise at least one therapeutic agent, such as, a vasoactive agent, an antimetic agent, and mixtures thereof. The dopamine agonist is preferably apomorphine. The present invention is also directed to methods for treating and/or preventing sexual dysfunctions and/or enhancing sexual responses in patients. In other embodiments, the present invention is directed to methods treating or preventing neurodegenerative diseases, mitochondrial diseases, spinal cord injury, central or psychostimulant addiction, senile dementia, circulatory disorders, cardiovascular disorders, hyperprolactinaemia or myopia. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.

      专利号:US-2006078560-A1
      优先权日:2003-06-23
      标 题 :Method of inducing apoptosis and inhibiting cardiolipin synthesis
      发明人:JAMIL HARIS; AHMAD MOGHIS U; AHMAD IMRAN
      权利人:NEOPHARM INC
      摘要:The present invention provides a method for inducing apoptosis within a cell by exposing the cell to an inhibitor of cardiolipin synthesis under conditions sufficient to induce apoptosis within the cell. The method can be used to investigate or treat disorders such as cancer, obesity, and cardiovascular disorders. The invention also provides a pharmaceutical composition including an inhibitor of cardiolipin synthesis and a liposomal carrier.

      专利号:US-2008286351-A1
      优先权日:2004-06-29
      标 题:Pegylated Cardiolipin Analogs, Methods of Synthesis, and Uses Thereof
      发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
      权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
      摘要:The invention provides synthetic methods for PEGylated cardiolipins with varying linkers. The methods can be employed to prepare PEGylated cardiolipin with different fatty acid and/or alkyl chain length with or without unsaturation. The PEGylated cardiolipin, prepared by the present methods, can be incorporated into liposomes that can also include active agents such as hydrophilic or hydrophobic drugs for the treatment of human and animal diseases. In addition, the PEGylated cardiolipin can be incorporated into liposomes that include compounds for therapeutic and diagnostic imaging. The use of such liposomes with PEGylated cardiolipin prolongs the period of liposomal circulation without disrupting the lipid bilayer.
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      主要参考文献


      1: Zhang L, Ma J, Li S, Xue R, Jin M, Zhou Y. Fatal diphenidol poisoning: a case report and a retrospective study of 16 cases. Forensic Sci Med Pathol. 2015 Dec;11(4):570-6. doi: 10.1007/s12024-015-9709-1. Epub 2015 Oct 19. doi: 10.1016/j.neulet.2015.01.026. Epub 2015 Jan 14. doi: 10.1016/j.neulet.2013.07.030. Epub 2013 Jul 31. doi: 10.1016/j.neuropharm.2010.02.007. Epub 2010 Feb 20. Epub 2005 Apr 13. Epub 2004 Nov 5.
      10: Waelbroeck M, Tastenoy M, Camus J, Christophe J, Strohmann C, Linoh H, Zilch H, Tacke R, Mutschler E, Lambrecht G. Binding and functional properties of antimuscarinics of the hexocyclium/sila-hexocyclium and hexahydro-diphenidol/hexahydro-sila-diphenidol type to muscarinic receptor subtypes. Br J Pharmacol. 1989 Sep;98(1):197-205.
      11: Duvoisin RC. Diphenidol for levodopa induced nausea and vomiting. JAMA. 1972 Sep 18;221(12):1408. doi: 10.1002/bmc.1037. doi: 10.1016/j.bmcl.2008.03.061. Epub 2008 Mar 23.

      合成参考文献


      摘要:Journal of Toxicology, Clinical Toxicology., 36(33), 1998 []
      参考文献:10.1107/s1600536810029417
      摘要:Siddaraju BP, Yathirajan HS, Narayana B, Ng SW, Tiekink ER. (2-Methyl-phen-yl)(phen-yl)methanol. Acta Crystallogr Sect E Struct Rep Online. 2010 Jul 31;66(Pt 8):o2136.
      参考文献:10.1002/bmc.1037
      摘要:Marcelín-Jiménez G, Morales-Martínez M, Angeles-Moreno AP, Mendoza-Morales L. Ultra-fast chromatographic micro-assay for quantification of diphenidol in plasma: application in an oral multi-dose switchability trial. Biomed Chromatogr. 2008 Oct;22(10):1143–8. doi: 10.1002/bmc.1037.
      参考文献:10.1097/mlg.0b013e3181651c4a
      摘要:Kitahara T, Kubo T, Okumura S, Kitahara M. Effects of endolymphatic sac drainage with steroids for intractable Meniere's disease: a long-term follow-up and randomized controlled study. Laryngoscope. 2008 May;118(5):854–61. doi: 10.1097/mlg.0b013e3181651c4a.
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