申请人:ALTER, S.A.
公开号:EP0325187A1
公开(公告)日:1989-07-26
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.
具有 PAF-拮抗剂活性的式 (I) 的 4-烷基-1,4-二氢吡啶类化合物 其中 R 是饱和 C₁-C₄,R′是饱和 C₁-C₆烷基,可被氧原子打断、或 2-四氢糠基且 R² 为饱和 C₁-C₄ 或苯基的化合物,不包括 R 为甲基、R′ 为乙基且 R² 为苯基的化合物。
化合物 (I) 的制备方法如下(a) (II) 与 (III) 反应;(b) (IV) 与 (V) 反应;(c) (VI) 与 (III) 和 (VII) 反应;(d) (VIII) 与 (V) 和 (VII) 反应;或 (e) (VIII) 与 (VI) 和 (VII) 在氨存在下反应。化合物(I)具有拮抗血小板活化因子的活性,因此非常有用。