• 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 method of obtaining azepine derivatives of the general formula at X — CH, 0.5, where R H; 7-CI, Rj-H, 6-CI, b-CH ,, R ,, 12-C I with, R H, R, j, 12-Cl with, S; I 6-OCH3, B, with XS, or their salts, .0 tons of a mixture of the compound of the general formula I, where B, R, X have the indicated values are reacted with cyanogen in tetrahydrofuranium with after-: Blowing the selection of the target product tt in free form, in the form of salt or c, enantimers.
    公开号:SU1015829A3
    申请号:SU813252241
    申请日:1981-03-05
    公开日:1983-04-30
    发明作者:Вальтер Герхард；Шнейдер Клаус；Вебер Карл-Гейнц；Фюгнер Армин
    申请人:К.Х.Берингер Зон (Фирма)；
    IPC主号:
    专利说明:

    36.5 g (0.146 mol) of the racemic base Z-amino-9,13b-dihydro-dibeneEG; f imidazo 1, 5-aa aepina and 55.1 g (0.164 mol) dibenzoyl-L (+) tartaric acid solution in 1 liter of methanol. Upon cooling, a precipitate is formed, which is sucked off. The crystals obtained are recrystallized from methanol until a constant melting point and rotation rate are reached. Melting point 15 152 ° C; tc (.- 200 (c 1, methanol). The base separated out in the usual manner is dissolved in methanol and converted into hydrochloride with the help of ethereal hydrochloric acid. Melting point 266-269 ° C, S-285 ° (c 1; alcohol Similarly, (+) enatiomer is obtained by using dibenzoyl-D- (-) tartaric acid. The hydrochloride has a melting point of 266-269 ° C; CctJ, +285 ° C (with 1; alcohol). With relatively low toxicity, new azepine derivatives they have long anti-allergic, anti-histamine and anti-serotonin effects, and they also delay the accumulation of blood asynok. The therapeutic possibilities of using new compounds are, for example, the treatment of reactions caused by the release of histin or serotonin, bronchial asthma, allergic bronchitis, rhinitis conjunctivitis, or diathesis. also a significant advantage over bromoglycinic acid disodium salt, a commercial product for the treatment of bronchial asthma and allergic bronchitis . To determine the activity of the compounds, experiments were carried out on al. ulgized rats after passive sensitization of animals with immunoglobulin E antibodies, followed by antigen provocation. Thus, passive anaphylaxis (PKA) and passive anaphylaxis (PAL) were caused. The anti-anaphylactic effect of the new compounds was confirmed in dogs that show increased skin sensitivity to the ascaris antigen. . Antihistaminic and anti-serotonin action was confirmed by the fact that after intravenous dacha or yes-. Chewing orally the brakes in rats, dogs and monkeys obtained by intravenous injection of histamine blisters. The quantification was carried out by measuring the blister after extravasation of the dye into the skin. The antiserotonin action has been demonstrated by activity against rat paw edema caused by serotonin. The results of the experiments are given in the table.
    权利要求:
    Claims (1)
    [1]
    A method of obtaining derivatives of * azecin of the general formula where Ka = H; 7-CI, K g = H at X-CH X , 0.5. ' rJ-H, 6-CI, 6-CH 3 , R ^ H, 1 2-С I at X = 0 *, r 4 = H, R a = 1 2-С I at X = 0, SJ
    K 4 = 6-0CH 3 , R ^ H at X = 3, or their salts, characterized in that the compound of the general formula where R 4 , R 2 , X have the indicated meanings, are reacted with bromine in tetrahydrofuran medium after - ';. by further isolating the target product in free form, in the form of a salt or enantiomers.
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    同族专利:
    公开号 | 公开日
    HU180628B|1983-03-28|
    ZA811500B|1982-11-24|
    FI810712L|1981-09-09|
    FI70898B|1986-07-18|
    AU6815881A|1981-09-17|
    DE3008944A1|1981-09-24|
    YU56881A|1983-10-31|
    EP0035749A1|1981-09-16|
    CS410491A3|1992-05-13|
    PT72631B|1982-12-30|
    HK63186A|1986-09-05|
    ES8301481A1|1982-12-01|
    GB2071095B|1983-06-02|
    IE810485L|1981-09-08|
    DK154299C|1989-03-28|
    GR74805B|1984-07-12|
    IE51015B1|1986-09-03|
    IL62309A|1984-06-29|
    BG33886A3|1983-05-16|
    MX6869E|1986-09-11|
    ES500150A0|1982-12-01|
    CA1150253A|1983-07-19|
    JPS56139484A|1981-10-30|
    PL230036A1|1982-05-24|
    DK103581A|1981-09-09|
    FI70898C|1986-10-27|
    DE3163938D1|1984-07-12|
    NZ196446A|1984-07-06|
    EP0035749B1|1984-06-06|
    DD156708A5|1982-09-15|
    PT72631A|1981-04-01|
    IL62309D0|1981-05-20|
    NO162073B|1989-07-24|
    NO162073C|1989-11-01|
    US4313931A|1982-02-02|
    AU535359B2|1984-03-15|
    RO81652B|1983-04-30|
    RO81652A|1983-04-29|
    DK154299B|1988-10-31|
    NO810762L|1981-09-09|
    UA8041A1|1995-12-26|
    JPH0366311B2|1991-10-16|
    YU42557B|1988-10-31|
    PL132141B1|1985-02-28|
    CS221288B2|1983-04-29|
    PH15839A|1983-04-08|
    GB2071095A|1981-09-16|
    引用文献:
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    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    DE19803008944|DE3008944A1|1980-03-08|1980-03-08|DIBENZIMIDAZOAZEPINE, THEIR PRODUCTION AND USE|
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