• 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:
    Condensed diazepinones of the general formula I …<IMAGE>… in which …<IMAGE>… is one of the divalent radicals …<IMAGE>… …<IMAGE>… …<IMAGE>… …<IMAGE>… X is a =CH- group or a nitrogen atom, A<1> and A<2> are lower alkylene radicals, R<1> and R<2> are hydrogen, lower alkyl or cycloalkyl radicals, R<3> is lower alkyl radicals, chlorine or hydrogen, R<4> is hydrogen or methyl, R<5> and R<6> are halogen, lower alkyl radicals or, where appropriate, also hydrogen, R<2> is hydrogen, chlorine or methyl, R<8> and R<9> are hydrogen or lower alkyl radicals, R<9> is additionally a halogen atom, and R<1><0> is hydrogen or methyl, and their acid addition salts and their possible enantiomers are described; processes for preparing these compounds are also described. …<??>The compounds are suitable as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias; they have spasmolytic effects on peripheral organs, especially colon, bladder and bronchi.
    公开号:SU1678209A3
    申请号:SU894614119
    申请日:1989-05-24
    公开日:1991-09-15
    发明作者:Мим Герхард；Эберлейн Вольфганг；Энгель Вольфгард；Труммлитц Гюнтер；Майер Норберт；Де Ионге Андриаан；Доодс Хенри
    申请人:Др.Карл Томэ Гмбх (Фирма)；
    IPC主号:
    专利说明:

    table 2
    权利要求:
    Claims (1)
    [1]
    Claim
    A method of obtaining derivatives of diazepinone of the General formula 20 where Ri is methyl, ethyl;
    R 2 is hydrogen or chlorine: X is a group of CH or nitrogen, or their physiologically tolerated salts, characterized in that the compound of the general formula
    0 P
    O = c-cn 2 -a1 where R'z has the indicated meanings,
    On I - halogen, is reacted with a compound of the general formula
    RrNHCH 2 CH 2 —O cr 3 where Ri has the indicated meanings, followed by isolation of the target product in free form or in the form of a physiologically tolerated salt.
    Table!
    I Connectionan example CT 5 o / nM ' 1 Cortex Heart Lower jaw 1 fifty 9 80 4 70 10 100 2 8 3 20 Pirenzepine 100 1500 200
    table 2
    Compound Example 1ode ED5o / mol kg ' 1 Heart Blood pressure Salivation 1 7.91 7.06 6.8 Pirenzepine 5.60 6.94 6.22
    Table 3
    Compound Example log EDbo / mol kg ' 1 Heart Bronchia Bladder 1 7.7 7.6 6.85 4 7.0 6.72 6.08 2 7.54 7.53 6.63 Pirenzepine 5.85 6.57 5.36
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    引用文献:
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    US4210648A|1977-05-31|1980-07-01|Boehringer Ingelheim Gmbh|II-Aminoacyl-5,11-dihydro-6H-pyrido benzodiazepin-6-ones and salts thereof|
    US4311700A|1979-08-10|1982-01-19|Byk Gulden Lomberg Chemische Fabrik Gmbh|Pyrimidobenzodiazepinones, their use and medicaments containing them|
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    DE3262922D1|1981-02-02|1985-05-15|Byk Gulden Lomberg Chem Fab|Tricyclic pyrrols, process for their preparation, their use and compositions containing them|
    AT71097T|1985-06-27|1992-01-15|Thomae Gmbh Dr K|5,11-DIHYDRO-6HPYRIDO- SUBSTITUTED IN 11-POSITION.|
    DE3626095A1|1986-07-31|1988-02-11|Thomae Gmbh Dr K|NEW SUBSTITUTED PYRIDO BENZODIAZEPIN-6-ONE, METHOD FOR THE PRODUCTION THEREOF AND MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS|
    DE3643666A1|1986-12-20|1988-06-30|Thomae Gmbh Dr K|NEW CONDENSED DIAZEPINONE, METHOD FOR THE PRODUCTION THEREOF, AND MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS|
    IT8721978D0|1987-09-21|1987-09-21|Angeli Inst Spa|NEW TRICYCLIC AMIDINE DERIVATIVES.|
    US4931436A|1988-08-09|1990-06-05|Dr. Karl Thomae Gmbh|Condensed diazepinones, processes for preparing them and pharmaceutical compositions containing these compounds|DE3818299A1|1988-05-30|1989-12-07|Thomae Gmbh Dr K|NEW CONDENSED DIAZEPINONE, PROCESS FOR THEIR MANUFACTURE AND MEDICAMENTS CONTAINING THESE COMPOUNDS|
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    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    DE3820346A|DE3820346A1|1988-06-15|1988-06-15|NEW CONDENSED DIAZEPINONE, PROCESS FOR THEIR MANUFACTURE AND MEDICAMENTS CONTAINING THESE COMPOUNDS|
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