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    1,4-dihydropyridine compounds with PAF-antagonistic activity
    1.
    发明授权
    1,4-dihydropyridine compounds with PAF-antagonistic activity 失效
    具有PAF拮抗活性的1,4-二氢吡啶化合物

    公开(公告)号：US5298619A

    公开(公告)日：1994-03-29

    申请号：US924319

    申请日：1992-08-03

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

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

    IPC分类号： C07D211/90 ,  C07D405/12 ,  C07D211/86

    CPC分类号： C07D405/12 ,  C07D211/90

    摘要： 4-alkyl-1,4-dihydropyridines with activity antagonistic of the PAF-"acether" 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-"acether" 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. ##STR1##

    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为氧，硫或SO 2; 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-“乙酰”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地，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防御能力降低的其他情况。 （*化学结构*）（I）（*化学结构*）（II）H3C-CO-CH2-COO-（CH2）nX-Ar（Ⅲ）R-CHO（IV）H3C-CO-CH2-COO-R （V）（*化学结构*）（VI）（*化学结构*）（VII）

    4-alkyl-1,4-dihydropyridines with PAF-antagonist activity
    3.
    发明授权
    4-alkyl-1,4-dihydropyridines with PAF-antagonist activity 失效
    具有PAF拮抗剂活性的4-烷基-1,4-二氢吡啶类

    公开(公告)号：US5177211A

    公开(公告)日：1993-01-05

    申请号：US815890

    申请日：1991-12-27

    申请人： Carlos Sunkel ,  Miguel Fau De Casa-Juana ,  Luis Santos ,  Pilar Ortega ,  Jaime Priego ,  Mariano Sanchez-Crespo

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

    IPC分类号： C07D211/90 ,  C07D405/12

    CPC分类号： C07D405/12 ,  C07D211/90

    摘要： 4-alkyl-1,4-dihyropyridines, with PAF-antagonist activity, of formula (I) wherein R is saturated C.sub.1 -C.sub.4, R' is saturated C.sub.1 -C.sub.6 alkyl which may be interrupted by an oxygen atom, or 2-tetrahydrofurfuryl and R.sup.2 is saturated C.sub.1 -C.sub.4 or phenyl, the compound wherein R is methyl, R' is ethyl and R.sup.2 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. ##STR1##

    摘要翻译： 或具有PAF-拮抗剂活性的式（I）的4-烷基-1,4-二氢吡啶，其中R是饱和的C 1 -C 4，R'是可被氧原子间隔的饱和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'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活性而是有用的。 IV图像III IV图像V CH 3 COCH 2 COOR'VI RCHO VII CH 3 COCH 2 COO（CH 2）2 R 2 VIII