CAS: 146-56-5; Fluphenazine (Dihydrochloride)

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    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-4315909-A
    优先权日:1978-09-25
    标题 :Process for the preparation of solid drug formulations
    发明人:HUETTENRAUCH REINHARD
    权利人:JENAPHARM VEB
    摘要:In order to allow for the greatest possible range of variation in the rate of liberation of active agents within an organism and to allow for the use of a wide variety of active agents in solid drug formulations, cellulose graft copolymers are employed as adjuvant. The excellent flow properties and compacting behavior of these cellulose graft copolymers allow for formulation without the need for additional process steps, while variations in the type and proportion of the grafted components allows for the synthesis of adjuvants ideally suited for a specific intended use.

    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-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.

    专利号:US-9056875-B2
    优先权日:2012-08-31
    标 题 :Substituted pyrazolo[3′,4′:4,5]thieno[2,3-C]pyridazin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
    发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; SALOVICH JAMES M
    权利人:UNIV VANDERBILT
    摘要:In one aspect, the invention relates to substituted pyrazolo[3′,4′:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); 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.

    专利号:US-9073935-B2
    优先权日:2011-11-11
    标 题:Substituted benzylspiroindolin-2-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1
    发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; HOPKINS COREY R; MELANCON BRUCE J; POSLUSNEY MICHAEL S
    权利人:UNIV VANDERBILT
    摘要:In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators 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: Maayan N, Quraishi SN, David A, Jayaswal A, Eisenbruch M, Rathbone J, Asher R, Adams CE. Fluphenazine decanoate (depot) and enanthate for schizophrenia. Cochrane Database Syst Rev. 2015 Feb 5;2:CD000307. doi: 10.1002/14651858.CD000307.pub2. Review. doi: 10.1002/14651858.CD009230.pub2. Review. doi: 10.1093/schbul/sbt140. Epub 2013 Sep 26. Review.
    4: Matar HE, Almerie MQ, Sampson S. Fluphenazine (oral) versus placebo for schizophrenia. Cochrane Database Syst Rev. 2013 Jul 17;7:CD006352. doi: 10.1002/14651858.CD006352.pub2. Review.
    5: Toler SM. Invited review: fluphenazine augments retinal oxidative stress. J Ocul Pharmacol Ther. 2005 Aug;21(4):259-65. Review. Review. Update in: Cochrane Database Syst Rev. 2005;(1):CD000307. Review. Update in: Cochrane Database Syst Rev. 2013;7:CD006352. Review. Update in: Cochrane Database Syst Rev. 2015;2:CD000307. Review. Review. Review. Czech.

    合成参考文献


    摘要:Medicinal Chemistry: A Series of Monographs., 4(2)(199), 1967
    摘要:Young, L.Y., M.A. Koda-Kimble (eds.). Applied Therapeutics. The Clinical Use of Drugs. 6th ed. Vancouver, WA., Applied Therapeutics, Inc. 1995., p. 75-10
    摘要:Reynolds, J.E.F., Prasad, A.B. (eds.) Martindale-The Extra Pharmacopoeia. 28th ed. London: The Pharmaceutical Press, 1982., p. 1530
    摘要:The Chemical Society. Foreign Compound Metabolism in Mammals. Volume 2: A Review of the Literature Published Between 1970 and 1971. London: The Chemical Society, 1972., p. 197
    摘要:American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 2515
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