草酸右旋西酞普兰置于ammonium Hydroxide体系中,用 乙醚,水 用作溶剂,以30.1 G的收率获得依他普仑 参考文献: New Salt And Solid State Forms Of Escitalopram[fr] Nouveau Sel Et Formes à L'état Solide D'Escitalopram 标题: New Salt And Solid State Forms Of Escitalopram[fr] Nouveau Sel Et Formes à L'état Solide D'Escitalopram 摘要:本公开涉及氟西汀的新盐及其固态形式,其制备方法,药物组合物以及使用方法.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-2006030625-A1 优先权日:2004-08-06 标 题 :Dietary neurotransmitter precursors for balanced synthesis of neurotransmitters 发明人:HART CHERYLE RAM; GROSSMAN RONALD S; RAM HERBERT 权利人:HART CHERYLE RAM; GROSSMAN RONALD S; RAM HERBERT 摘要:Dietary supplements for treating a neurotransmitter deficiency include one or more precursors of the deficient neurotransmitter and a cofactor for activating in vivo enzymatic synthesis of the deficient neurotransmitter. The dietary supplements can also include an appropriate neurotransmitter, such as an amino acid. When administered through the oral mucosa, increases in levels of the deficient neurotransmitters and relief from deficiency symptoms are obtained.
专利号:US-9981949-B2 优先权日:2008-12-01 标题 :Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine 发明人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT 权利人:OYSTER POINT PHARMA INC 摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
专利号:US-8604191-B2 优先权日:2008-12-01 标 题:Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3YLVINYL)pyrimidine 发明人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT 权利人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT; TARGACEPT INC 摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-yl)pyrimidine, novel salt forms, and novel polymorphic forms of these salts.
专利号:US-2008199922-A1 优先权日:2005-06-22 标题 :Chemoenzymatic Process for the Synthesis of Escitalopram 发明人:COTTICELLI GIOVANNI; SALVETTI RAUL; BERTONI CHIARA 权利人:ADORKEM TECHNOLOGY SPA 摘要:A process is described for the preparation of escitalopram and the pharmaceutically acceptable salts thereof starting from 5-cyanophthalide by a process which provides an enantioselective enzymatic deacylation reaction of a complex of the formula (IV) where R represents a C 1 -C 4 alkyl residue or an aryl residue under the action of an esterase from Aspergillus niger.
专利号:US-7598399-B2 优先权日:2005-11-30 标 题 :Methods for synthesis of 3-amino-1-arylpropyl indoles 发明人:CONNOLLY TERRENCE JOSEPH; FARRELL ROBERT P; HUMPHREYS ERIC ROY; LYNCH STEPHEN M; SARMA KESHAB 权利人:ROCHE PALO ALTO LLC 摘要:A method comprising:n hydrogenating an indole propionamide compound of formula h nn nwith vitride, to form an aminopropyl indole compound of formula in n nwherein m, Ar, R 1 and R 2 are as defined herein. The compounds prepared by the method of the invention are useful as monoamine reuptake inhibitors useful for treatment of CNS indications.
1: Sanchez C, Reines EH, Montgomery SA. A comparative review of escitalopram, paroxetine, and sertraline: Are they all alike? Int Clin Psychopharmacol. 2014 Jul;29(4):185-96. doi: 10.1097/YIC.0000000000000023. Review. 2: Pastoor D, Gobburu J. Clinical pharmacology review of escitalopram for the treatment of depression. Expert Opin Drug Metab Toxicol. 2014 Jan;10(1):121-8. doi: 10.1517/17425255.2014.863873. Epub 2013 Nov 30. Review. doi: 10.4088/JCP.14m09281. doi: 10.1186/s12888-014-0349-x. 5: Talley NJ, Locke GR, Saito YA, Almazar AE, Bouras EP, Howden CW, Lacy BE, DiBaise JK, Prather CM, Abraham BP, El-Serag HB, Moayyedi P, Herrick LM, Szarka LA, Camilleri M, Hamilton FA, Schleck CD, Tilkes KE, Zinsmeister AR. Effect of Amitriptyline and Escitalopram on Functional Dyspepsia: A Multicenter, Randomized Controlled Study. Gastroenterology. 2015 Aug;149(2):340-9.e2. doi: 10.1053/j.gastro.2015.04.020. Epub 2015 Apr 25.
合成参考文献
参考文献:10.1186/1752-1947-4-6 摘要:Baune BT, Eyre H. Anti-inflammatory effects of antidepressant and atypical antipsychotic medication for the treatment of major depression and comorbid arthritis: a case report. Journal of Medical Case Reports. 2010 Jan 12;4(1):6. doi: 10.1186/1752-1947-4-6. 参考文献:10.1155/2011/903595 摘要:Ooi C, Zawar V. Hyperaesthesia Following Genital Herpes: A Case Report. Dermatology Research and Practice. 2011;2011():1–3. doi: 10.1155/2011/903595. 参考文献:10.1016/j.pnpbp.2011.06.013 摘要:Wolkowitz OM, Wolf J, Shelly W, Rosser R, Burke HM, Lerner GK, Reus VI, Nelson JC, Epel ES, Mellon SH. Serum BDNF levels before treatment predict SSRI response in depression. Progress in Neuro-Psychopharmacology and Biological Psychiatry. 2011 Aug;35(7):1623–30. doi: 10.1016/j.pnpbp.2011.06.013. 参考文献:10.2147/ndt.s19611 摘要:Montgomery S, Briley M. Noradrenergic symptom cluster in depression. Neuropsychiatr Dis Treat. 2011;7(Suppl 1):1–2. 参考文献:10.2147/ndt.s19613 摘要:Blier P, Briley M. The noradrenergic symptom cluster: clinical expression and neuropharmacology. Neuropsychiatr Dis Treat. 2011;7(Suppl 1):15–20.