New 2,5-diaryl tetryhydrofurans and analogs thereof as paf antagonists
    7.
    发明公开
    New 2,5-diaryl tetryhydrofurans and analogs thereof as paf antagonists 失效
    新的2,5-DIARYL四氢呋喃和其模拟物作为PAF拮抗剂

    公开(公告)号:EP0199324A3

    公开(公告)日:1988-02-10

    申请号:EP86105471

    申请日:1986-04-21

    申请人: MERCK & CO. INC.

    摘要: Compounds of formula:
    are disclosed wherein R and R' are
    (a) hydrogen; (b) haloloweralkyl; (c) halo; (d) CONR 2 R 3 wherein R 2 and R 3 independently represent hydrogen, C 1-8 alkyl, or C 3-8 cycloalkyl; (e) loweralkenyl; (f) -COR 2 ; (g) -CH 2 OR 2 ; (h) loweralkynyl; (i) -CH 2 NR 2 R 2 ; (j) -CH 2 SR 2 ; (k) = O; or (l) -OR 2 ; (m) -R 2 ; Ar and Ar 1 are (a) phenyl or substituted phenyl of formula where R 4 -R 8 independently where R 4 -R 8 independently represent H; R 2 ; YO-wherein Y is loweralkenyl, loweralkynyl, - CH 2 -, -CH 2 C(O)OR 2 , -CH 2 OR 2 , -CH 2 C 3- 8 cycloalkyl, -CH 2 Ar 2 wherein Ar 2 is phenyl or substituted phenyl, -CH 2 -CH(OH)CH 2 OH; R 2 S-(O) n wherein R 2 can only be C 3-8 cycloalkyl and n is 0 to 2; CF 3 SO, CF 3 SO 2 ; - CONR 2 R 3 ; -NR 2 COR 3 ; -OCONH 2 -CR 2 R 3 R 9 wherein R 9 is the same as or different from R Z ; -CH 2 OR 2 ; -CH 2 CO 2 R 2 ; -CH 2 OCOR 3 ; -GH 2 O-CO-OR 2 ; -NHCH 2 COOR 2 ; halo; or N + R 2 R 3 R 9 X- wherein X- is an anion;
    (b) monoheteroaryl, di-or polyheteroaryl or fused heteroaryl containing 1 to 3 of any one or more of the heteroatoms N, S or O; (c) heteroarylalkyl; (d) heterocycloalkyl; or (e) heterocycloalkenyl. These compounds are found to have potent and specific PAF - (Platelet Activating Factor) antagonistic activities.