2-(3,5-二甲基金刚烷-1-基)异吲哚-1,3-二酮置于甲胺体系中,用 水 用作溶剂,化学反应 36.0H,以41.52%的收率获得3,5-二甲基金刚胺 参考文献: Process For The Preparation Of Memantine And Its Salts And Intermediate For Use Therein[fr] Procédé De Préparation De La Mémantine Et De Ses Sels Et Intermédiaire Destiné à être Utilisé Dans Ce Procédé 标题: Process For The Preparation Of Memantine And Its Salts And Intermediate For Use Therein[fr] Procédé De Préparation De La Mémantine Et De Ses Sels Et Intermédiaire Destiné à être Utilisé Dans Ce Procédé 摘要:本发明提供了式ii的2-(3,5-二甲基-孔雀石酮-1-基)-异吲哚酮-1,3-二酮,其在制备美金刚和其盐中作为中间体有用.本发明还提供了制备2-(3,5-二甲基-孔雀石酮-1-基)-异吲哚酮-1,3-二酮和制备美金刚或其盐的过程,使用2-(3,5-二甲基-孔雀石酮-1-基)-异吲哚酮-1,3-二酮.
专利信息
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
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-2022378721-A1 优先权日:2019-10-24 标 题 :Protein kinase inhibitors and use thereof for treatment of neurodegenerative diseases 发明人:SRIDHAR JAYALAKSHMI; BRATTON MELYSSA; GOYAL NAVNEET; JHA VISHWAJEET; SCHROEDER RICHARD 权利人:XAVIER UNIV OF LOUISIANA 摘要:The present disclosure relates to compounds that act as protein kinase inhibitors, especially CK1δ and/or CK1ε inhibitors, which can be used to treat a serine threonine kinase-dependent disease and condition, such as neurodegenerative diseases like Alzheimer's Disease, and the synthesis of the same. Further, the present disclosure teaches the utilization of such compounds in a treatment for neurodegenerative diseases, including Alzheimer's disease.
专利号:EP-1669379-B1 优先权日:2003-09-23 标 题 :3,5-dimethyl-1-adamantyl-ammonium polymeric salts and the use thereof in the form of antiviral agents 发明人:MARCHUKOV VALERY ALEKSANDROVIC; PLATONOV VITALY GEORGIEVICH; SELKOV SERGEI ALEKSEEVICH; CHERNOBROVY ALEKSANDR NIKOLAEV 权利人:AKCIJU SABIEDRIBA OLAINFARM 摘要:This invention relates to the polymeric salts of 3.5-dimethyl-1-adamantylammonium and carboxylated (co)polymers, as well as to the use of produced salts as antiviral agents. Object of the invention is the synthesis of new salts of 3.5-dimethyl-1-adamantylammonium and carboxylated (co)polymers, identification of the compounds with antiviral activity and durable action among them. The task is solved by the synthesis of salts of 3.5-dimethyl-1-adamantylammonium and water-soluble carboxylated (co)polymers of a general formula (1): nwhere m and n are mol%, m = 100 - n, nand carboxylated (co)polymers are selected from the group: nvinylaminosuccinic acid, a copolymer of vinyl alcohol and N-vinylaminosuccinic acid, a copolymer of N-vinylpyrrolidone and N-vinylaminosuccinic acid, copolymer of N-vinylpyrrolidone and crotonic acid; copolymer of N-vinylaminosuccinimide and maleic anhydride; copolymer of N-vinylpyrrolidone and maleic anhydride; polyacrylic acid A general synthesis method and synthesis examples are given for each of claimed compounds, as well as the results of identification of toxicity and comparative antiviral activity. Produced compounds are expressly identified by methods of IR analysis, elements analysis, and potentiometric titration, have quite high antiviral activity against the viruses of influenza types A and B, at that they feature durable (prolonged) action which allows using these produced salts not only as antiviral medications for sparing treatment but for prevention of viral diseases.
专利号:US-8263755-B2 优先权日:2006-11-20 标题:Synthesis of compounds useful as modulators of amyloid-beta production 发明人:FINDEIS MARK A 权利人:FINDEIS MARK A; SATORI PHARMACEUTICALS INC 摘要:As described herein, the present invention provides methods for preparing compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.
专利号:US-10035796-B2 优先权日:2014-08-14 标题:Crystalline forms of a BACE inhibitor, compositions, and their use 发明人:KAZAKEVICH IRINA; TRZASKA SCOTT; FENG TAO 权利人:MERCK SHARP & DOHME 摘要:The present invention provides a novel synthesis of verubecestat, and two novel crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease, are disclosed herein.
1: Le HT, Lau ECY, Ali MA, Lu CY, Hilmer SN, Jeon YH, Low LF, Nguyen TA, Tan ECK. Potentially High-Risk Antipsychotic Use in People With Dementia: A National Data Linkage Study. J Am Med Dir Assoc. 2025 Jul 18:105750. doi: 10.1016/j.jamda.2025.105750. Epub ahead of print. 11(3):e70136. doi: 10.1002/trc2.70136. 3: Pourayyoubi B, Rezaei-Ashtiani A, Javaheri J, Ebrahimi Monfared M, Zamani F. The Evaluation of Memantine Effect on Tinnitus Severity. Brain Behav. 2025 Jul;15(7):e70697. doi: 10.1002/brb3.70697.
合成参考文献
参考文献:10.1038/475s9a 摘要:Gravitz L. Drugs: a tangled web of targets. Nature. 2011 Jul 13;475(7355):S9–11. doi: 10.1038/475s9a. 参考文献:10.1097/01.pra.0000400268.60537.5e 摘要:Obregon DF, Velasco RM, Wuerz TP, Catalano MC, Catalano G, Kahn D. Memantine and catatonia: a case report and literature review. J Psychiatr Pract. 2011 Jul;17(4):292–9. doi: 10.1097/01.pra.0000400268.60537.5e.