CAS: 101246-68-8; Eptastigmine

该化合物是一种化学化合物,被归类为酶乙酰胆碱酯酶的可逆抑制剂,在合成骨裂...

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    毒扁豆碱 Physostigmin 57-47-6
    Physostigmine 57-47-6
    氧化毒扁豆碱 (+/-)-Eseroline 469-22-7

    合成工艺路线路线简述

      📜异氰酸庚酯,毒扁豆碱置于sodium Methylate体系中,用 乙醇,苯 用作溶剂,化学反应 3.0H,反应生成依斯的明
      参考文献:毒扁豆碱类似物对乙酰胆碱酯酶的抑制:由于烷基链的空间效应,半胱氨酸环的构象迁移.
      标题:毒扁豆碱类似物对乙酰胆碱酯酶的抑制:由于烷基链的空间效应,半胱氨酸环的构象迁移.
      摘要:研究了一系列毒扁豆碱类似物对乙酰胆碱酯酶活性的影响.酶抑制剂复合物的二级速率常数k(on)与过渡态复合物中芳香族残基(尤其是trp84)的构象位置相关.范德华相互作用是这种构象变化的重要结构要素.半胱氨酸环(cys67-Cys94)的瞬态迁移率仅限于明显的空间效应.但是,即使有此限制,空间效应似乎仍是将来对"后门"假设进行测试的合适模型,该假设涉及方便打开以加快产品清除速度.
      Doi:10.1002/jbt.10026

      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-8063062-B2
      优先权日:2006-12-20
      标 题 :Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition
      发明人：LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL
      权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL; SOLVAY PHARM BV
      摘要:Embodiments of this invention relate to compounds having a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition is a compound of formula (1) n nwherein the symbols have the meanings given in the specification.

      专利号:WO-2009035652-A1
      优先权日:2007-09-13
      标 题 :Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof

      专利号:US-2014336387-A1
      优先权日:2007-09-13
      标题:Synthesis of deuterated catechols and benzo[d][1,3]dioxoles and derivatives thereof

      专利号:EP-2727915-A1
      优先权日:2007-09-13
      标题:Synthesis of deuterated catechols and benzo[d][1,3]dioxoles and derivatives thereof

      专利号:CA-2698808-A1
      优先权日:2007-09-13
      标题:Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof

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      主要参考文献


      1: Braida D, Sala M. Eptastigmine: ten years of pharmacology, toxicology, pharmacokinetic, and clinical studies. CNS Drug Rev. 2001 Winter;7(4):369-86. doi: 10.1111/j.1527-3458.2001.tb00205.x.
      2: Sahoo AK, Dandapat J, Dash UC, Kanhar S. Features and outcomes of drugs for combination therapy as multi-targets strategy to combat Alzheimer's disease. J Ethnopharmacol. 2018 Apr 6;215:42-73. doi: 10.1016/j.jep.2017.12.015. Epub 2017 Dec 14. 52(4):700-8. doi: 10.1212/wnl.52.4.700. 53(5):389-95. doi: 10.1016/0024-3205(93)90642-g. 38(7):610-7. doi: 10.1002/j.1552-4604.1998.tb04467.x. 11(1):17-24. doi: 10.1159/000017208. 45(4):373-6. doi: 10.1007/BF00265958. 3(3):CD000207. doi: 10.1002/14651858.CD000207.pub2.
      9: Braida D, Ottonello F, Sala M. Eptastigmine improves eight-arm radial maze performance in aged rats. Pharmacol Res. 2000 Oct;42(4):299-304. doi: 10.1006/phrs.2000.0706. 140(2):364-9. doi: 10.1006/taap.1996.0232.

      合成参考文献


      摘要:Journal of Medicinal Chemistry., 37(1996), 1994
      参考文献:10.1007/bf02246647
      摘要:Duka T, Ott H, Rohloff A, Voet B. The effects of a benzodiazepine receptor antagonist beta-carboline ZK-93426 on scopolamine-induced impairment on attention, memory and psychomotor skills. Psychopharmacology (Berl). 1996 Feb;123(4):361–73. doi: 10.1007/bf02246647.
      参考文献:10.1007/bf02247383
      摘要:Meziane H, Mathis C, Paul SM, Ungerer A. The neurosteroid pregnenolone sulfate reduces learning deficits induced by scopolamine and has promnestic effects in mice performing an appetitive learning task. Psychopharmacology (Berl). 1996 Aug;126(4):323–30. doi: 10.1007/bf02247383.
      参考文献:10.2165/00002018-199920060-00001
      摘要:Zeitoun K, Carr BR. Is there an increased risk of stroke associated with oral contraceptives Drug Saf. 1999 Jun;20(6):467–73. doi: 10.2165/00002018-199920060-00001.
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