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    1,3-DIHYDRO-1-(PHENYLALKENYL)-2H-IMIDAZOL-2-ONE DERIVATIVES HAVING PDE IV AND CYTOKINE INHIBITING ACTIVITY
    2.
    发明授权
    1,3-DIHYDRO-1-(PHENYLALKENYL)-2H-IMIDAZOL-2-ONE DERIVATIVES HAVING PDE IV AND CYTOKINE INHIBITING ACTIVITY 失效
    1,3-二氢-1-（phenylalkenyl）-2H-咪唑-2- ON具有PDE IV和细胞因子活性INHIBIRENDES衍生物

    公开(公告)号：EP0819123B1

    公开(公告)日：2007-12-12

    申请号：EP96909151.1

    申请日：1996-03-28

    申请人： Janssen Pharmaceutica NV

    发明人： FREYNE, Eddy, Jean, Edgard ,  DIELS, Gaston, Stanislas, Marcella ,  ANDRES-GIL, José Ignacio ,  FERNANDEZ-GADEA, Francisco Javier

    IPC分类号： C07D233/32 ,  C07D233/70 ,  A61K31/415

    CPC分类号： C07D233/32 ,  C07D233/70

    摘要： The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceuticlaly acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R?1 and R2¿ each independently are hydrogen; C¿1-6?alkyl; difluoromethyl; trifluoromethyl; C3-6cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; R?3¿ is hydrogen, halo or C¿1-6?alkyloxy; R?4¿ is hydrogen; cyano; optionally substituted C¿1-6?alkyl; C1-6alkyloxycarbonyl or aryl; R?5¿ is hydrogen; cyano; optionally substituted C¿1-6?alkyl; C1-6alkyloxycarbonyl or aryl; Y is a direct bond or C1-3alkanediyl; -A-B- is a bivalent radical of formula -CR?6=CR7¿- or -CHR6-CHR7-; L is hydrogen; optionally substituted C¿1-6?alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl; -furanyl or -thienyl; having PDE IV and cytokine inhibiting acitivity. Further, pharmaceutical compositions, preparations and use as a medicine are described.