CAS: 15622-65-8; 3-Ethyl-2-Methyl-5-(Morpholinomethyl)-6,7-Dihydro-1H-Indol-4(5H)-One Hydrochloride

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    📜2,3-戊二酮置于盐酸,氢气,Sodium Hydroxide体系中,用 乙醇,水,溶剂黄146 用作溶剂,-5.0~100.0 °C,300.01 Kpa 条件下,反应 14.0H,反应生成盐酸吗茚酮
    参考文献:Methods Of Producing Molindone And Its Salts
    标题:Methods Of Producing Molindone And Its Salts
    摘要:本发明涉及一种合成莫林酮的新方法,合成莫林酮的中间体以及高纯度的莫林酮组合物.特别是,本发明涉及通过曼尼希反应合成莫林酮的方法.

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    专利信息


    专利号:US-9802893-B2
    优先权日:2012-09-14
    标 题:Methods of producing molindone and its salts
    发明人:HANBAUER MARTIN; NAZIR ZARGHUN; HILDEBRAND PETER; FIGINI ATTILIA; LIANG LIKAN; FUMAGALLI TIZIANO
    权利人:SUPERNUS PHARMACEUTICALS INC
    摘要:The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.

    专利号:US-7576211-B2
    优先权日:2004-09-30
    标题 :Synthesis of thienopyridinone compounds and related intermediates
    发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
    权利人:EPIX DELAWARE INC
    摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

    专利号:US-12295961-B2
    优先权日:2009-12-31
    标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
    发明人:DHINGRA OM
    权利人:MARIUS PHARMACEUTICALS INC
    摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

    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-11617758-B2
    优先权日:2009-12-31
    标 题 :Emulsion formulations
    发明人:DHINGRA OM; BERNSTEIN JAMES S
    权利人:MARIUS PHARMACEUTICALS LLC
    摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

    专利号:US-8697888-B2
    优先权日:2012-01-06
    标题 :Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors
    发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; CHEUNG YIU-YIN
    权利人:UNIV VANDERBILT
    摘要:In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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    主要参考文献


    1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Molindone. 2024 Jul 15. 25(11):1564-1577. doi: 10.1177/1087054720909084. Epub 2020 Apr 26. 25(6):1367. doi: 10.3390/molecules25061367.
    4: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Molindone. 2020 Jan 21. 110(16):1250-1262). Birth Defects Res. 2019 Mar 1;111(4):229. doi: 10.1002/bdr2.1471. Epub 2019 Feb 6. 111(4):230-231. doi: 10.1002/bdr2.1447. Epub 2019 Jan 11.
    10:65-73. doi: 10.2147/JEP.S180777.

    合成参考文献


    摘要:Federation Proceedings, Federation of American Societies for Experimental Biology., 26(738), 1967
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