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    1,4-Dihydropyridines, processes for their preparation and their use as antithrombotic drugs
    2.
    发明公开
    1,4-Dihydropyridines, processes for their preparation and their use as antithrombotic drugs 失效
    1,4-二氢吡啶，其制备方法及其作为抗血栓药物的使用。

    公开(公告)号：EP0253092A1

    公开(公告)日：1988-01-20

    申请号：EP87107008.2

    申请日：1987-05-14

    申请人： ALTER, S.A.

    发明人： Sunkel, Carlos ,  Fau de Casa-Juana, Miguel ,  Dorrego, Fernando ,  Priego, Jaime ,  Ortega, Pilar ,  Cillero, Javier

    IPC分类号： C07D417/12 ,  A61K31/44

    CPC分类号： C07D417/12 ,  C07D211/90

    摘要： The present invention refers to 1,4-dihydropyridi­nes,to processes for their preparation and to their use as antithrom­botic drugs. Said new 1,4-dihydropyridines have the following general formula (I)
    wherein
    R represents hydrogen or a saturated or unsaturated alkyl group, with a linear or branched chain of 1 to 8 carbon atoms, R¹ represents an alkyl radical with a linear, branched or cyclic, saturated or unsaturated chain of 1 to 12 carbon atoms, which may be interrupted by an oxygen or by a 2-(N-salicylamido)ethyl group,
    n is a number equal to 1 or 2.
    These 1,4-dihydropyridines are obtained by processes based on the Hantzch reaction or on modifications thereof.

    摘要翻译： 本发明涉及1,4-二氢吡啶，对它们的制备方法和它们作为抗血栓药物的用途。 所述新的1,4-二氢吡啶具有以下通式（I） worinřdarstellt氢或饱和或不饱和的烷基，直链或1-8个碳原子，R <1> darstellt烷基的支链 1至12个碳原子，其可以通过在氧气或通过被中断的基团与直链，支链或环状，饱和或不饱和链2-（N- salicylamido）乙基，n为等于1或第二 这些1,4-二氢吡啶是通过基于所述Hantzch反应或对它们的改进方法得到。

    4-alkyl-1, 4-dihydropyridines with PAF-antagonist activity
    3.
    发明公开
    4-alkyl-1, 4-dihydropyridines with PAF-antagonist activity 失效
    4-烷基-1,4-二氢吡啶酯Verwendung als PAF拮抗剂。

    公开(公告)号：EP0325187A1

    公开(公告)日：1989-07-26

    申请号：EP89100656.1

    申请日：1989-01-16

    申请人： ALTER, S.A.

    发明人： Sunkel, Carlos ,  Fau de Casa-Juana, Miguel ,  Santos, Luis ,  Ortega, Pilar ,  Priego, Jaime ,  Sanchez-Crespo, Mariano

    IPC分类号： C07D211/90 ,  C07D417/04 ,  A61K31/445

    CPC分类号： C07D211/90 ,  C07D405/12

    摘要： 4-alkyl-1,4-dihyropyridines, with PAF-antagonist activity, of formula (I) wherein R is saturated C₁-C₄, R′ is saturated C₁-C₆ alkyl which may be interrupted by an oxygen atom, or 2-tetrahydrofurfuryl and R² is saturated C₁-C₄ or phenyl, the compound wherein R is methyl, R′ is ethyl and R² is phenyl remain excluded, are described.
    The compounds (I) are prepared by: (a) reaction of (II) with (III); (b) reaction of (IV) with (V); (c) reaction of (VI) with (III) and with (VII); (d) reaction of (VIII) with (V) and with (VII); or (e) reaction of (VIII) with (VI) and with (VII) in the presence of ammonia. The compounds (I) are useful due to their antagonist activity of the platelet activating factor.

    摘要翻译： 或具有PAF-拮抗剂活性的4-烷基-1,4-二氢吡啶类，其中R为饱和的C 1 -C 4，R min为饱和的可被氧原子间隔的C 1 -C 6烷基，或2-四氢糠基 R 2为饱和的C 1 -C 4或苯基，其中R为甲基，R min为乙基且R 2为苯基的化合物仍被排除。 化合物（I）通过以下步骤制备：（a）（II）与（III）的反应; （b）（Ⅳ）与（Ⅴ）的反应; （c）（VI）与（III）和（VII）的反应; （d）（VIII）与（Ⅴ）和（Ⅶ）的反应; 或（e）（VIII）与（VI）和（VII）在氨存在下的反应。 化合物（I）由于其对血小板活化因子的拮抗作用而有用。 a

    1,4-Dihydropyridines with paf-antagonistic activity
    4.
    发明公开
    1,4-Dihydropyridines with paf-antagonistic activity 失效
    1,4-二氢吡啶，PAF拮抗剂Aktivität。

    公开(公告)号：EP0531598A1

    公开(公告)日：1993-03-17

    申请号：EP91500103.6

    申请日：1991-09-09

    申请人： ALTER, S.A.

    发明人： Sunkel, Carlos ,  Fau de Casa-Juana, Miguel ,  Santos, Luis ,  Ortega, Pilar ,  Priego, Jaime

    IPC分类号： C07D211/90 ,  C07D405/12 ,  A61K31/44

    CPC分类号： C07D211/90 ,  C07D405/12

    摘要： 4-alkyl-1,4-dihydropyridines with activity antagonistic of the PAF-"aceter" of formula (I) are described, in which R is a saturated alkyl chain C1-2; R' is a saturated or unsaturated C1-16 lineal, branched or cyclic chain that can be interrupted by an oxygen atom and can also represent a 2-(N-morpholine) ethyl group; n is 2 or 3; X is oxygen, sulphur or SO2; Ar represents an aromatic ring that cannot be phenyl when X=S and n=2. The compounds (I) can be prepared (a) by reaction of (II) with (III) and with (IV); or (b) by reacting (V) with (VI) and (IV); or (c) by reaction of (VII) with (VI). In these formulas the different radicals have the meaning given above.
    Compounds of formula (I) are used for the treatment of pathologic states and disorders in which the PAF-"aceter" participates, being used, for example, in treatment of inflammatory processes, psoriasis, glomerulitis, transplant rejection, acute and chronic bronchitis, bronchial asthma, states of shock and allergies Likewise it is used for the treatment of pathologic states and disorders in which it is necessary to stimulate the cellular immunity such as in immunodeficient syndromes and other situations in which the defense capacity is reduced.

    摘要翻译： 描述了具有式（I）的PAF-“丙酮”活性拮抗作用的4-烷基-1,4-二氢吡啶，其中R是饱和烷基链C1-2; R'是饱和或不饱和的C1-16直链，支链或环状链，其可被氧原子间隔并且也可以表示2-（N-吗啉）乙基; n为2或3; X是氧，硫或SO2; Ar表示当X = S且n = 2时不能为苯基的芳环。 化合物（I）可以通过（II）与（III）和（IV）的反应制备（a）。 或（b）通过使（V）与（VI）和（IV）反应; 或（c）通过（VII）与（VI）的反应。 在这些公式中，不同的基团具有上面给出的含义。 式（I）化合物用于治疗PAF-“丙酮”参与的病理状态和病症，例如用于治疗炎症过程，牛皮癣，肾小球炎，移植排斥反应，急性和慢性支气管炎， 支气管哮喘，休克和过敏状态同样，它用于治疗需要刺激细胞免疫的病理状态和障碍，例如免疫缺陷综合征和其他防御能力降低的其他情况。 s