4-alkyl-1,4-dihydropyridines with PAF-antagonist activity
    2.
    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

    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