• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
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  • 法律状态
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    • 专利摘要:
    The present invention provides 3-(4-substitutedphenoxy)-3-phenyl propanamines capable of inhibiting the uptake of serotonin.
    公开号:SU1750421A3
    申请号:SU894613806
    申请日:1989-04-07
    公开日:1992-07-23
    发明作者:Вейн Робертсон Дэвид；Тайвай Вонг Дэвид
    申请人:Эли Лилли Энд Компани (Фирма)；
    IPC主号:
    专利说明:

    Known M-methyl-3- (4-methoxy-phenoxy) -3 phenylpropanamine fumarate
    4800
    Red Ktor 0.H head
    Compiled by L.Ioffe
    Tehred M. Morgental Proofreader S. Lisin
    Order 26th
    Circulation
    VNIIPI State Committee for Inventions and Discoveries at the State Committee on Science and Technology of the USSR 111035, Moscow, Zh-35, 4/5 Raushsk nab.
    Production and publishing plant Patent, Uzhgorod, st. Gagarin, 10)
    Subscription
    权利要求:
    Claims (1)
    [1]
    Claim
    30 A method for the preparation of aminopropanol derivatives of the general formula I for the study of these animals in an experiment. Rats are killed by decapitation. The entire brain is removed and dissected. The cerebral cortex is homogenized in 9 volumes of medium containing 0.32 M sucrose and 10 mM glucose. The crude synaptosomal preparations are separated after differential centrifugation in an amount of up to 1,000 g for 10 minutes and 17,000 g for 28 minutes. The granules obtained are suspended in the same medium and kept on ice until use on the same day, D5
    Sina'ptosomal uptake of beads ( 3 H-5 oxytryptamine, ^ H-5HT) and (4c-1-norepinephrine (1 4 C-NE) is determined as follows: Cortical synaptosomes (equivalent to 1 mg 50 protein) are incubated at 37 ° C in for 5 min in 1 ml of Krebs bicarbonate medium containing also 10 mM glucose, 0.1 mM iproniazide, 1 mM ascorbic acid, 0.17 mM ethylenedia-55 Mintetraacetic acid, 50 nm 3 H-5HT, and 100 N M ^ C-NE, The reaction mixture was immediately diluted with 2 ml of ice-cold bicarbonate but where R, are (CfC 2 -alkyl) -S, CF 3 S, H Z NSO Z - CHjSOgNH;
    R 2 is hydrogen or methyl, or pharmacologically acceptable acid addition salts thereof, characterized in that phenylpropylamines of the general formula II
    X-CHCWlCHj, ό is reacted with a benzene derivative of the general formula III where X is an oxy group; I is a halogen;
    R | and R 2 have the indicated meaning, ( followed by, if necessary, demethylation of the compound of general formula I, where R z is methyl, and isolation of the target product in a free form or in the form of a pharmacologically acceptable acid addition salt.
    Connection example 1C 5o , nM (% inhibition) 3 N ~ 5 “Oxytryptamine Norepinephrine 1 ' 1b0 > 1000 (18) 2 48 704 3 > 1000 (39) > 1000 (9) 4 > 1000 (15) > 1000 (0) 5 > 1000 (30) > 1000 (15) Known N-methyl-3 (4-methoxyphenoxy) -3 phenylpropanamine fumarate 300 ;4800
    Compiled by L. Ioffe Reda Ktor 0. Head h Tehred M. Morgenthal Corrector S. Lisina Order 2b0b Circulation. Subscription
    VNIIIPI of the State Committee for Inventions and Discoveries under the State Committee for Science and Technology of the USSR 113035, Moscow, Zh-35, Raushskaya nab., 4/5
    Production and Publishing Plant Patent, Uzhgorod, st. Gagarina, 101
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    同族专利:
    公开号 | 公开日
    JPH0285236A|1990-03-26|
    PH27144A|1993-04-02|
    HUT54976A|1991-04-29|
    DE68901994T2|1993-02-25|
    CA1337128C|1995-09-26|
    PT90212B|1994-06-30|
    AU3252889A|1989-10-12|
    EP0336753A1|1989-10-11|
    ES2033525T3|1993-03-16|
    GR3005662T3|1993-06-07|
    IL89854A|1994-02-27|
    EP0336753B1|1992-07-08|
    DE68901994D1|1992-08-13|
    NZ228636A|1990-12-21|
    KR890015995A|1989-11-27|
    ZA892517B|1990-12-28|
    DK165489D0|1989-04-06|
    HU205344B|1992-04-28|
    CN1036562A|1989-10-25|
    AU611794B2|1991-06-20|
    DK165489A|1989-10-09|
    AT78029T|1992-07-15|
    PT90212A|1989-11-10|
    IE891122L|1989-10-08|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    US4314081A|1974-01-10|1982-02-02|Eli Lilly And Company|Arloxyphenylpropylamines|
    DE2732750A1|1977-07-20|1979-02-08|Merck Patent Gmbh|BASIC THIOAETHERS AND METHOD FOR THEIR PRODUCTION|
    US4243681B1|1977-10-11|1985-09-10|
    US4147805A|1978-07-28|1979-04-03|Mead Johnson & Company|Alkylthiophenoxyalkylamines and the pharmaceutical use thereof|
    GB2060622B|1979-09-14|1983-05-25|Wyeth John & Brother Ltd|3-aryl-3-aryloxyalkylamines|
    US4569801A|1984-10-15|1986-02-11|Eli Lilly And Company|Alkylsulfonamidophenylalkylamines|DK630987D0|1987-12-01|1987-12-01|Ferrosan As|ARYLOXYPHENYL PROPYLAMINES, THEIR PREPARATION AND USE|
    FI912280A|1990-05-17|1991-11-18|Lilly Co Eli|KIRAL SYNTES AV 1-ARYL-3-AMINOPROPAN-1 -OLER.|
    DK0537915T3|1991-09-27|1995-11-27|Lilly Co Eli|N-alkyl-3-phenyl-3-propylamines as inhibitors of epinephrine|
    US5281624A|1991-09-27|1994-01-25|Eli Lilly And Company|N-alkyl-3-phenyl-3- propylamines and pharmaceutical use thereof|
    EP0576766A1|1992-06-29|1994-01-05|Novo Nordisk A/S|Propanolamine derivatives, their preparation and use|
    IL110857D0|1993-09-09|1994-11-28|Lilly Co Eli|Cessation of tobacco use|
    US5936124A|1998-06-22|1999-08-10|Sepacor Inc.|Fluoxetine process from benzoylpropionic acid|
    US6025517A|1998-08-03|2000-02-15|Sepracor Inc.|Fluoxetine process from benzoylacetonitrile|
    ITMI20061987A1|2006-10-16|2008-04-17|Archimica Srl|PROCESS FOR THE SYNTHESIS OF ARYLOSSIPROPYLAMINES AND HETERARYLOSOSIPROPYLAMINES.|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    US17936888A| true| 1988-04-08|1988-04-08|
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