📜2-(6-甲基吡啶-3-基)乙酸置于盐酸,Sodium Tetrahydroborate,1-羟基苯并三唑,溶剂黄146,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺,Sodium Hydroxide体系中,用 1,4-二氧六环,乙醇,水,N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 55.5H,反应生成2,3,4,5-四氢-2,8-二甲基-5-[2-(6-甲基吡啶-3-基)乙基]-1H-吡啶并[4,3-B]吲哚 参考文献:Sustained-Release Composition Containing Tetrahydropyrido[4,3-B]Indole Derivatives And Preparation Of The Derivatives 标题:Sustained-Release Composition Containing Tetrahydropyrido[4,3-B]Indole Derivatives And Preparation Of The Derivatives 摘要:本发明涉及一种缓释组合物,其包含2,3,4,5-四氢-2,8-二甲基-5-[2-(6-甲基-3-吡啶基)乙基]-1H-吡啶并[4,3-B]吲哚或其药学上可接受的盐作为活性成分,以及其制备方法和该化合物.该组合物适用于每天一次口服,口服后1.0至3小时达到峰值血浆浓度.该组合物适用于制造治疗认知功能障碍综合征,阿尔茨海默病,帕金森病,亨廷顿病或老年性痴呆的药物.
专利号:US-8703952-B2 优先权日:2008-12-12 标题:Synthesis of 9-(arylalkyl)-1,2,3,4-tetrahydro-γ-carboline and analogues and intermediates 发明人:WILLIAMSON CRAIG; STOREY JOHN MERVYN DAVID 权利人:WILLIAMSON CRAIG; STOREY JOHN MERVYN DAVID; WISTA LAB LTD 摘要:The present invention pertains generally to methods of preparing certain 9-(arylalkyl)-1,2,3,4-tetrahydro-γ-carboline compounds and their analogues, and especially to methods of preparing dimebon. The present invention also pertains to methods of preparing certain intermediate compounds which find use in the synthesis of the 9-(arylalkyl)-1,2,3,4-tetrahydro-γ-carboline compounds.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-9359376-B2 优先权日:2011-04-08 标题:Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; HOLLINGER FRANK PETER 权利人:DUGAR SUNDEEP; MAHAJAN DINESH; HOLLINGER FRANK PETER; SPHAERA PHARMA PTE LTD 摘要:The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
专利号:US-4348264-A 优先权日:1980-05-14 标 题 :Photocatalyzed process for producing carbapenams and carbapen-2-ems 发明人:ROSATI ROBERT L 权利人:PFIZER 摘要:Carbapenam-3-carboxylic acids and carbapen-2-em-3-carboxylic acids substituted at the 1-position with an oxo, a hydroxy or an acetoxy group, variously substituted at the 2-position with such groups as methyl, acetoxymethyl, methanesulfonyloxy, alkoxy, alkylthio, aminoalkylthio or amidinoalkylthio and optionally substituted at the 6-position with a hydroxyalkyl group, an acetoxyalkyl group or a conventional penicillin side-chain, pharmaceutically-acceptable salts thereof and various esters thereof wherein the esterifying group is selectively removed in the laboratory, or hydrolyzed under physiological conditions. n These compounds are useful either systemically or topically in the treatment of diseases caused by susceptible microorganisms, as animal feed additives for promotion of growth, or in the preservation of biodegradable materials, or as intermediates to compounds having such antibacterial activity. n Key to the synthesis of these compounds is the light catalyzed rearrangement of 2-diazo-1-oxoceph-3-em-4-carboxylates to 1-oxocarbapen-2-em-3-carboxylates, a newly discovered reaction determined to be of general applicability.
专利号:US-4429128-A 优先权日:1981-02-09 标题 :Carbapenams and carbapen-2-ems and process therefor 发明人:ROSATI ROBERT L 权利人:PFIZER 摘要:Carbapenam-3-carboxylic acids and carbapen-2-em-3-carboxylic acids substituted at the 1-position with an oxo, a hydroxy or an acetoxy group, variously substituted at the 2-position with such groups as methyl, acetoxymethyl, methanesulfonyloxy, alkoxy, alkylthio, aminoalkylthio or amidinoalkylthio and optionally substituted at the 6-position with a hydroxyalkyl group, an acetoxyalkyl group or a conventional penicillin side-chain, pharmaceutically-acceptable salts thereof and various esters thereof wherein the esterifying group is selectively removed in the laboratory, or hydrolyzed under physiological conditions. n These compounds are useful either systemically or topically in the treatment of diseases caused by susceptible microorganisms, as animal feed additives for promotion of growth, or in the preservation of biodegradable materials, or as intermediates to compounds having such antibacterial activity. n Key to the synthesis of these compounds is the light catalyzed rearrangement of 2-diazo-1-oxoceph-3-em-4-carboxylates to 1-oxocarbapen-2-em-3-carboxylates, a newly discovered reaction determined to be of general applicability.
专利号:EP-2300484-B1 优先权日:2008-05-05 标题:Novel class of spiro piperidines for the treatment of neurodegenerative diseases 发明人:BRODNEY MICHAEL AARON; HELAL CHRISTOPHER JOHN; O'NEILL BRIAN THOMAS 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.