• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    The invention relates to novel racemic or optically active berban derivatives of the general formula (I), wherein R' and R2 represent independently from the other a hydroxyl, straight or branched chain alkoxy group having 1 to 6 carbon atoms or R' and R7 together represent a C1-3 alkylenedioxy group; R3 and R4 represent independently from the other hydrogen, straight or branched chain alkyl group, having 1 to 4 carbon atoms and optionally substituted by hydroxyl group, or a C2-6 alkoxycarbonyl or cyano group; and R5 represents hydrogen, straight or branched chain alkyl group having 1 to 6 carbon atoms, C1-7 aliphatic or aromatic acyl group or C1-7 alkylsulphonyl or arylsulphonyl group and a salt thereof, to pharmaceutical compositions containing them, to the use as well as to process for preparing the novel compounds. The compounds of the general formula (1) are selective a2-adrenergic receptor-blocking substances and thus, they may be used for the treatment of depressive illnesses.
    公开号:SU1573021A1
    申请号:SU864028190
    申请日:1986-09-29
    公开日:1990-06-23
    发明作者:Визи Сильвестер；Сантаи Чаба；Сабо Лайош；Тот Иштван；Ковач Габор；Мартон Иене；Харшинг Ласло；Шомодьи Дьердь；Гаал Йожеф
    申请人:Хиноин Дьедьсер Еш Ведьесети Термекек Дьяра Рт (Инопредприятие)；
    IPC主号:
    专利说明:

     R form hydrochloride
    Spreadsheets
     14o / -oxy-7,8-methylenedioxyaloberbane hydrochloride. P 0.01. P 0.001.
    权利要求:
    Claims (3)
    [1]
    Claim
    1 4 (X-Hydroxy-7,8-methylenedioxyalloberb of the formulanngl'n hDl λ. he
    possessing antidepressant activity.
    ,8
    Table 1
    Compound
    ------------— -Rat reference vessels Longitudinal smooth muscles (preparations) from ileum Relative activity Differential Longitudinal guinea pigs vessels smooth muscles (preparations) ileum
    II η
    yohimbine phentolamine idazoxan imiloxane (1 ^
    L!
    7.22 +
    7.78 +
    8.07 +
    8.17 +
    6.84
    0.11
    0.05
    0.04
    0.08
    0.01 (4) (4) (4) (3)
    FROM
    FROM
    FROM
    C (12) C
    7.52 + 0.45
    8.82 +
    7.49 +
    8.26 + (4)
    NC
    0.22
    0.04
    0.46 (6) (4)
    1,0
    1.15
    [2]
    2.23
    0.13
    2.82
    1,0
    0.79
    4.68
    table 2
    Reference vessels vigor rat pAj
    Rabbit pulmonary artery pA g 'yohimbine entolamine
    It
    II
    F <
    Idazoxane ^ Miloxane (I) *
    7.05 +
    8.02
    6.00
    7.28 +
    4.95 +
    0.19 (4) NC
    0.25. (4) C
    0.16 (4) NC
    0.64 (14) NC
    0.11 (4) NC
    [3]
    5.59 + 0.4 (4): * As hydrochloride.
    Table 3
    Connections Pulmonary arteries faces 'pA 2
    Yohimbine 5.81 + 0.37 (4) C
    Idazoxane 6.03 + 0.11 (4) C (I) *
    5.29 + 0.20 (8) NC * as hydrochloride
    Table 4
    Compound Selectivity Yohimbine 4.67 Phentolamine 0.57 Idazoxan 117.5 Imiloxane 0.36 (D *1659 * In the form of Ihydrochloride
    Table 5
    Head part NE / DA Content, KfTR Μ /14. brain Catecholamine Treatment nmol / g Wh- NMOL / g · H ’’ h Frontal NE d -MPT 0.91 * 0.04 (4) 0.445 0.40 + 0.01 2.24 Cortexs / -MRI + 0.87 + 0.05 (4) 0.740 0.64 + 0.03 ** 1.35s / -MFT + iohimbnn 0.99 + 0.07 (4) 0.880 0.87 + 0.06 *** 1.13 Striatum DA and MRI 50.65 + 3.52 (4) 0.592 29.98 + 2.08 1.68ci-MRI + * 48.03 + 4.66 (4) 0.776 37.27 + 3.62 1.28c / MRI + yohimbine 64.46 + 6.04 (4) 0,906 58.40 + 5.47 ** 1.10
    * 14c / -oxy-7,8-methylenedioxyalloberbane hydrochloride.
    ** P <0.01. .
    *** P <0.001.
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    EP0202950A3|1988-03-23|
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    SU1508958A3|1989-09-15|
    US4851416A|1989-07-25|
    AU599030B2|1990-07-12|
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    DE3689080D1|1993-11-04|
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    YU46956B|1994-09-09|
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    HU195505B|1988-05-30|
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    PH24053A|1990-03-05|
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    FI862174A|1986-11-25|
    IL78722D0|1986-08-31|
    PT82634A|1986-06-01|
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    引用文献:
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    US5122504A|1990-02-27|1992-06-16|The Board Of Trustees Of The Leland Stanford Junior University|Superconducting ribbon process using laser heating|
    WO1992020678A1|1991-05-22|1992-11-26|Chinoin Gyógyszer- És Vegyészeti Gyár R.T.|New berbane derivatives, pharmaceutical compositions containing these compounds and process for the preparation of same|
    US5663167A|1992-12-09|1997-09-02|The United States Of America As Represented By The Department Of Health And Human Services|Antipsychotic composition and method of treatment|
    US5492907A|1992-12-09|1996-02-20|The United States Of America As Represented By The Department Of Health & Human Services|Antipsychotic composition and method of treatment|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    HU851982A|HU195505B|1985-05-24|1985-05-24|Process for producing 7,8-methylendioxy-14-hydroxy-berban derivatives and pharmaceuticals comprising the same|
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