盐酸羟可待酮 反应生成 盐酸纳洛酮 参考文献:Pharmaceutical Combinations Of Oxycodone And Naloxone 标题:Pharmaceutical Combinations Of Oxycodone And Naloxone 摘要:在某些实施例中,公开了一种药物组合物,其包括10至40毫克的氧考酮或其药学上可接受的盐,以及0.65至0.90毫克的纳洛酮或其药学上可接受的盐.
专利号:US-8106201-B2 优先权日:2003-09-22 标 题:Process for the synthesis of morphinane compounds and intermediates thereof 发明人:SMITH CRAIG; PURCELL STUART; WADDELL LUCY; HAYES NICHOLAS; RITCHIE JARROD; HALLIDAY SCOTT BRIAN; MITCHELL MELVILLE; WILSON GEORGE SCOTT 权利人:SMITH CRAIG; PURCELL STUART; WADDELL LUCY; HAYES NICHOLAS; RITCHIE JARROD; HALLIDAY SCOTT BRIAN; MITCHELL MELVILLE; WILSON GEORGE SCOTT; JOHNSON MATTHEY PLC; GLAXOSMITHKLINE AUSTRALIA PTY LTD 摘要:This invention relates to intermediates useful in the preparation of opiate alkaloids, particularly morphinane compounds. The invention also relates to processes for preparing such intermediates and to processes which utilise such intermediates in the synthesis of morphinane compounds.
专利号:US-4089855-A 优先权日:1976-04-23 标题:Process for the stereoselective reduction of 6- and 8-keto morphine and morphinan derivatives with formamidinesulfinic acid and compounds obtained thereby 发明人:CHATTERJIE NITHIANANDA; INTURRISI CHARLES E 权利人:CORNELL RES FOUNDATION INC 摘要:Process for the stereoselective synthesis of 6β-and 8β- hydroxy epimers by the chemical reduction of 6- and 8-keto derivatives in the morphine and morphinan series utilizing alkaline formamidinesulficic acid. The 6β- and 8β-hydroxy derivatives obtained according to the invention evidence narcotic antagonist and/or agonist activity and are also useful in the chemical and pharmacological standardization of various morphine and codeine derivatives and metabolites.
专利号:US-2019127389-A1 优先权日:2016-04-22 标题 :Processes And Oxazolidine-Containing Intermediates For The Preparation Of Morphine Analogs And Derivatives 发明人:KAPPE CHRISTOPHER OLIVER; GUTMANN BERNHARD; WEIGL ULRICH; EGLI PATRICK; COX DOUGLAS PHILLIP; CANTILLO DAVID 权利人:NORAMCO INC 摘要:The present invention relates to processes useful in the preparation of morphine analogs and derivatives, such as naltrexone, naloxone and nalbuphine and intermediates in the synthesis of said morphine analogs and derivatives. In a particular example, the process begins with for example oxymorphone, oxycodone, 14-hydroxycodeinone or 14-hydroxymorphinone, and includes the formation of an oxazolidine-containing intermediate using catalytic oxidation.
专利号:US-9045497-B1 优先权日:2011-05-02 标 题:Processes and intermediates in the preparation of morphine analogs via N-demethylation of N-oxides using cyclodehydration reagents 发明人:HUDLICKY TOMAS; WERNER LUKAS; MACHARA ALES; WERNEROVA MARTINA; ENDOMA-ARIAS MARY ANN 权利人:UNIV BROCK 摘要:A high-yielding method for the N-demethylation of oxycodone- and oxymorphone-N-oxides by the reaction of these compounds with cyclodehydration reagents has been performed. This method has been utilized to improve the synthesis of various morphine analogs, such as naltrexone, nalbuphone and naloxone.
专利号:US-2012282255-A1 优先权日:2011-04-07 标题 :Methods and compositions for the treatment of alcoholism and alcohol dependence 发明人:PLUCINSKI GREG 权利人:PLUCINSKI GREG 摘要:The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated. Accordingly, the methods and compositions of the invention are useful for preventing, treating, diagnosing, or monitoring the progression various alcohol and drug dependency diseases disclosed herein.
专利号:US-4238390-A 优先权日:1979-05-09 标题 :Synthesis and biological activity of [D-Thr2, Δ3 Pro5 ]-enkephalinamide 发明人:MEIENHOFER JOHANNES A 权利人:HOFFMANN LA ROCHE 摘要:The present disclosure is directed to the synthesis and biological activity of [D-Thr 2 , Δ 3 Pro 5 ]-enkephalinamide. The subject compound is useful as an agent for the inhibition of diarrhea and also exhibits analgesic activity.
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合成参考文献
摘要:Annals of Emergency Medicine., 16(1294), 1987 [] 摘要:Journal of Medicinal Chemistry., 20(844), 1977