专利号:US-6191272-B1 优先权日:1999-02-20 标题:Process for the preparation of endo-nortropine using 8-benzyl-nortropan-3-one perchlorate as the intermediate, as well as the latter salt 发明人:SACHSE ROLF; SCHAUPP ALBERT 权利人:ROBERT PFLEGER CHEM FAB GMBH D 摘要:The invention relates to a process for the preparation of endo-nortropine using 8-benzyl-nortropan-3-one perchlorate, as well as the latter product. Endo-nortropine is the key product for the production of important azonia-spironortropanol esters, which are used as pharmaceuticals, particularly spasmolytics. There are three different synthesis methods for the preparation of said intermediate, which lead to different disadvantages. These problems are obviated by the present invention through the two-stage treatment of 8-benzyl-nortropan-3-one perchlorate with catalytically activated hydrogen, the starting product initially being prehydrogenated in aqueous suspension and at atmospheric pressure and ambient pressure with a palladium catalyst, at the end of the reaction the catalyst is recovered by filtration, the filtrate is passed over an anion exchanger and the now alkaline reacting solution is rendered turbulent at 1000 to 1500 r.p.m. with hydrogen activated by Raney nickel at atmospheric pressure and ambient temperature. This new synthesis method using the novel perchlorate salt as an intermediate is extremely economic and environmentally friendly and supplies substantially completely stereoselectively the desired endo-form of nortropine.
专利号:WO-2011114195-A1 优先权日:2010-03-15 标题:Synthesis of propiverine hydrochloride
专利号:EP-2470504-B1 优先权日:2010-03-15 标题:Synthesis of propiverine hydrochloride 发明人:ANDAGAR RAMAKRISHNA RAMESHA; ROY ANJAN KUMAR 权利人:ANDAGAR RAMAKRISHNA RAMESHA; ROY ANJAN KUMAR
专利号:EP-2470504-A1 优先权日:2010-03-15 标 题:Synthesis of propiverine hydrochloride
专利号:US-7993390-B2 优先权日:2002-02-08 标 题:Implantable or insertable medical device resistant to microbial growth and biofilm formation 发明人:MILLER KATHLEEN M; BUCAY-COUTO WEENNA; LI JIANMIN 权利人:BOSTON SCIENT SCIMED INC 摘要:Disclosed are implantable or insertable medical devices that provide resistance to microbial growth on and in the environment of the device and resistance to microbial adhesion and biofilm formation on the device. In particular, the invention discloses implantable or insertable medical devices that comprise at least one biocompatible matrix polymer region, an antimicrobial agent for providing resistance to microbial growth and/or a microbial adhesion/biofilm synthesis inhibitor for inhibiting the attachment of microbes and the synthesis and accumulation of biofilm on the surface of the medical device. Also disclosed are methods of manufacturing such devices under conditions that substantially prevent preferential partitioning of any of said bioactive agents to a surface of the biocompatible matrix polymer and substantially prevent chemical modification of said bioactive agents.
专利号:US-2023047961-A1 优先权日:2019-12-03 标 题 :The cholesterol-syntesis intermediates for treatment demyelinating disorders 发明人:BERGHOFF STEFAN; SAHER GESINE 权利人:MAX PLANCK GESELLSCHAFT 摘要:The present invention relates to a cholesterol-synthesis intermediate as pharmaceutically active agent and/or pharmaceutical composition comprising the cholesterol-synthesis intermediate optionally together with one or two further pharmaceutically active agent(s) for use in the prophylaxis and/or treatment of demyelinating disorders/diseases, in particular multiple sclerosis.
1: Luca M, Luca A, Serretti A. A Clinically Oriented Review of New Antipsychotics for Schizophrenia. Neuropsychiatr Dis Treat. 2024 Dec 27;20:2637-2649. doi: 10.2147/NDT.S501560. 2: Fabiano N, Wong S, Zhou C, Correll CU, Højlund M, Solmi M. Efficacy, tolerability, and safety of xanomeline-trospium chloride for schizophrenia: A systematic review and meta-analysis. Eur Neuropsychopharmacol. 2024 Dec 25;92:62-73. doi: 10.1016/j.euroneuro.2024.11.013. Epub ahead of print. 92:19-20. doi: 10.1016/j.euroneuro.2024.11.014. Epub ahead of print.
合成参考文献
摘要:Arzneimittel-Forschung. Drug Research., 25(1037), 1975 [] 参考文献:10.2165/00044011-199713020-00004 摘要:Rohde H, Bihr AM, Schwantes U, Eisebitt R, Meurer J, Fischer M, Topfmeier P. Effect of Trospium Chloride on Duodenal Motility during Upper Gastrointestinal Endoscopy: A Randomised, Double-Blind, Placebo-Controlled Trial. Clin Drug Investig. 1997;13(2):85–9. doi: 10.2165/00044011-199713020-00004. 参考文献:10.1007/s11934-011-0198-9 摘要:Pagoria D, O'Connor RC, Guralnick ML. Antimuscarinic drugs: review of the cognitive impact when used to treat overactive bladder in elderly patients. Curr Urol Rep. 2011 Oct;12(5):351–7. doi: 10.1007/s11934-011-0198-9. 参考文献:10.1007/s10928-017-9507-3 摘要:Weiss M. Empirical models for fitting of oral concentration time curves with and without an intravenous reference. Journal of Pharmacokinetics and Pharmacodynamics. 2017 Feb 01;44(3):193–201. doi: 10.1007/s10928-017-9507-3. 参考文献:10.1208/s12248-022-00690-5 摘要:Lex TR, Rodriguez JD, Zhang L, Jiang W, Gao Z. Development of In Vitro Dissolution Testing Methods to Simulate Fed Conditions for Immediate Release Solid Oral Dosage Forms. AAPS J. 2022 Mar 11;24(2):40. doi: 10.1208/s12248-022-00690-5.