• 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>… or …<IMAGE>… and… X<1>, X<2>, A<1>, A<2> and R<1> to R<10> are defined as specified in Claim 1, their acid addition salts and medicaments containing these compounds are described. …<??>The medicaments containing these compounds are vagal pacemakers for the treatment of bradycardias and bradyarrhythmias. The active compounds additionally have spasmolytic properties on peripheral organs, furthermore antiemetic properties and properties promoting cerebral blood flow, some of them can also be used for treating disorders of the central nervous system such as Alzheimer's disease and Parkinson's disease.
    公开号:SU1731057A3
    申请号:SU894614115
    申请日:1989-05-15
    公开日:1992-04-30
    发明作者:Энгель Вольфгард；Эберлейн Вольфганг；Мим Герхард；Труммлитц Гюнтер；Майер Норберт；Де Ионге Андриаан
    申请人:Др.Карл Томэ Гмбх (Фирма)；
    IPC主号:
    专利说明:

    four
    20
    100
    0.6
    2
    1500

    16.7
    40
    0.13
    6.7
    ten
    0.07
    nM nanomolar
    Table2 Selectivity of Mj / M2 and the delayed secretion of saliva in the rat
    Table3
    The delayed action of acetylcholine on the bladder, bronchia and heart rate of guinea pigs
    权利要求:
    Claims (1)
    [1]
    The formula of the invention Ί: A method for producing derivatives of diaAe ^ pinon of General formula (I)
    After 5 minutes after giving the test substance to anesthetized 40 guinea pigs, 10 μg / kg of acetylcholine was injected simultaneously and intra-arterially. In this case, the heart rate was directly recorded by means of extracorporeal abduction of the electrocardiogram, resistance to expiration according to the Concett-Ressler method, and contraction of the exposed bladder. To delay the action of acetylxo-50 lynn on the studied organs, curves were compiled according to doses and actions, and the log values of EDg 0 were determined from them. The results are summarized in table.Z.
    - '55
    The data of the above table confirm that the new compounds of general formula (I) are well distinguished among muscarinic receptors of different tissues - where A 'is an unbranched alkylene chain containing from 3 to 7 carbon atoms and, if necessary, a triple bond;
    R * is hydrogen, a lower alkyl radical substituted with a di (lower) alkylamino group, characterized in that the locally obtained dilithium salt of the formula is subjected to alkylation with a compound of the general formula
    I
    Test for binding to
    Br-CH 2 -A * -N ^
    5 :
    where A 'and have the above meanings, in an inert organic solution, t - 1 of the eliminator "''- T of a l of the receptor, in vitro
    Compound Nr - Test for binding to the receptor CT 50 / nm / * Selectivity factors ct 50 (11) ct 0 (C) Cortex(TO) Heart(FROM) Sub jaw(P) CT ^ (heart) CT 5o (heart)
    A 4 0.6 10 16.7 6.7 B 20 2 80 40 10 Pirenzepine 100 1500 200 0.13 0,07
    1 K nM - nanomolar
    Table 2
    Mj / Mg selectivity and delayed saliva secretion in rats
    Compound- log ed ^ / mol Blood Delay No. kg “1 heart pressure salivation A 7.96 6.53 6.35 B 7.40 6.17 5.50 IN 7.52 5.96 5.12- Pirense pin 5.60 6.94 6.22
    Table 3 Delayed action of acetylcholine on the bladder, bronchia and heart rate of guinea pigs
    Substance “Log kg - ' ED ^ 0 / Moth heart Bronchia Bladder A 7.187.07 5.89 B 6.336.19 <5.00 IN 6.615.80 <5.64 Pirense pin 5.856.57 5.36
    —......- -: j.—
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    同族专利:
    公开号 | 公开日
    US5006522A|1991-04-09|
    FI892596A|1989-12-01|
    EP0344543B1|1992-07-22|
    PT90677B|1994-11-30|
    IL90418D0|1990-01-18|
    DD283822A5|1990-10-24|
    AU3585089A|1989-11-30|
    PT90677A|1989-11-30|
    FI892596A0|1989-05-29|
    EP0344543A2|1989-12-06|
    AU617814B2|1991-12-05|
    NO892152D0|1989-05-29|
    NZ229307A|1990-11-27|
    NO169539B|1992-03-30|
    ZA894048B|1991-02-27|
    NO892152L|1989-12-01|
    DE3818299A1|1989-12-07|
    HU203887B|1991-10-28|
    HUT50343A|1990-01-29|
    NO169539C|1992-07-08|
    DE58901872D1|1992-08-27|
    DK261289D0|1989-05-29|
    EP0344543A3|1990-08-22|
    AT78479T|1992-08-15|
    DK261289A|1989-12-01|
    KR900018101A|1990-12-20|
    JPH0228163A|1990-01-30|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    US3150125A|1959-09-22|1964-09-22|Wander Ag Dr A|5--10, 11-dihydro-11-oxo-5h-dibenzo[b, e][1, 4]diazepine compounds|
    US3105125A|1959-10-30|1963-09-24|Bell Telephone Labor Inc|Power separation filter|
    AT71097T|1985-06-27|1992-01-15|Thomae Gmbh Dr K|5,11-DIHYDRO-6HPYRIDO- SUBSTITUTED IN 11-POSITION.|
    US4749788A|1987-04-13|1988-06-07|A. H. Robins Company, Incorporated|Process for the preparation of aryl-pyrido benzodiazepines|
    DE3819444A1|1988-06-08|1989-12-14|Thomae Gmbh Dr K|NEW CONDENSED DIAZEPINONE, PROCESS FOR THEIR MANUFACTURE AND MEDICAMENTS CONTAINING THESE COMPOUNDS|
    DE3820346A1|1988-06-15|1989-12-21|Thomae Gmbh Dr K|NEW CONDENSED DIAZEPINONE, PROCESS FOR THEIR MANUFACTURE AND MEDICAMENTS CONTAINING THESE COMPOUNDS|DE3726908A1|1987-08-13|1989-02-23|Thomae Gmbh Dr K|NEW CONDENSED DIAZEPINONE, PROCESS FOR THEIR MANUFACTURE AND MEDICAMENTS CONTAINING THESE COMPOUNDS|
    AT161535T|1989-04-20|1998-01-15|Boehringer Ingelheim Pharma|6,11-DIHYDRO-5H-PYRIDO BENZODIAZEPINE 5-ONE AND THIONE AND THEIR USE FOR THE PREVENTION OR TREATMENT OF AIDS|
    DE3919076A1|1989-06-10|1990-12-13|Thomae Gmbh Dr K|MEANS TO TREAT DISEASES OF THE CENTRAL NERVOUS SYSTEM AND TO PROMOTE CEREBRAL BLOOD|
    AT221067T|1993-04-05|2002-08-15|Pharmaceutical Discovery Corp|PYRIDO BENZODIAZEPINONE AS M2 RECEPTOR LIGAND FOR THE TREATMENT OF NEUROLOGICAL DISORDERS|
    US5561127A|1994-12-19|1996-10-01|Allelix Biopharmaceuticals, Inc.|Muscarinic receptor ligands|
    JP3521569B2|1995-09-05|2004-04-19|ブラザー工業株式会社|Printing control device|
    FR2850654A1|2003-02-03|2004-08-06|Servier Lab|NOVEL TRICYCLIC AZEPINE DERIVATIVES, PROCESS FOR PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM|
    US20100247688A1|2007-07-02|2010-09-30|Andrea Pfeifer|Pirenzepine and derivatives thereof as anti-amyloid agents|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    DE3818299A|DE3818299A1|1988-05-30|1988-05-30|NEW CONDENSED DIAZEPINONE, PROCESS FOR THEIR MANUFACTURE AND MEDICAMENTS CONTAINING THESE COMPOUNDS|
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