CAS: 41303-74-6; (4As,6R,8As)-3-Methoxy-4A,5,9,10,11,12-Hexahydro-6H-Benzo[2,3]Benzofuro[4,3-Cd]Azepin-6-Ol

上下游产品

CAS号271769-63-2 (4aS,6R,8aS)-3-... | CAS号722499-71-0 (2S,5R)-5-benzy... | CAS号722499-74-3 (4aS,8aS,13R,14... | CAS号722499-80-1 (4aS,8aS,13R,14... | CAS号722499-73-2 (2R,11bR)-2-ben... | CAS号722499-72-1 (2S,5R)-5-benzy... | CAS号596828-90-9 galanthamine N-oxide | CAS号1953-04-4 氢溴酸加兰他敏 | CAS号722499-81-2 (4aS,6R,8aS,13R... | CAS号357-70-0 加兰他敏

📜氢溴酸加兰他敏置于ammonium Hydroxide,间氯过氧苯甲酸,Ferrous(II) Sulfate Heptahydrate体系中,用 二氯甲烷,水,甲醇 作为反应溶剂,化学反应 4.5H,反应生成 N-去甲基加兰它敏氢溴酸盐
参考文献:Galantamine Derivatives As Acetylcholinesterase Inhibitors: Docking,Design,Synthesis,And Inhibitory Activity
标题:Galantamine Derivatives As Acetylcholinesterase Inhibitors: Docking,Design,Synthesis,And Inhibitory Activity
摘要:加兰他敏 (Gal) 是一种众所周知的乙酰胆碱酯酶 (Ache) 抑制剂,广泛用于治疗阿尔茨海默病.gal置于ache 的催化位点中契合非常好,但它的长度不足以阻断酶的周边阴离子位点 (Pas),而该位点是淀粉样β (Aβ) 肽结合并启动 Aβ 聚集的地方.在这里,我们描述了一种基于对接的技术,用于设计具有双重位点结合片段的 Gal 衍生物--一个阻断催化位点,另一个阻断 Pas.我们合成并测试了评分高的化合物.本文提供了对接,设计,合成和 Ache 抑制测试的协议.
DOI:10.1007/978-1-4939-7404-7_6

专利信息

专利号:US-8450365-B2
优先权日:2009-05-12
标 题 :Efficient synthesis of galanthamine
发明人：MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ
权利人:MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ; UNIV TEXAS
摘要:The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.

专利号:US-2007213318-A1
优先权日:2006-03-07
标 题 :Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment
发明人：MAELICKE ALFRED
权利人:GALANTOS PHARMA GMBH
摘要:The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g. galanthamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugsâ€?, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments for the treatment of human brain diseases associated with a cholinergic deficit, including the neurodegenerative diseases Alzheimer's and Parkinson's disease and the psychiatric diseases vascular dementia, schizophrenia and epilepsy.

专利号:US-9763953-B2
优先权日:2005-09-22
标题:Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment
发明人：MAELICKE ALFRED
权利人:GALANTOS PHARMA GMBH; NEURODYN LIFE SCIENCES INC
摘要:The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugsâ€?, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.

专利号:US-2010292475-A1
优先权日:2009-05-12
标 题 :Efficient Synthesis Of Morphine And Codeine

专利号:US-8293927-B2
优先权日:2009-05-12
标 题 :Efficient synthesis of morphine and codeine

专利号:DE-112010001980-T5
优先权日:2009-05-12
标题 :Synthesis of morphine and related derivatives