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 R<2> each independently are hydrogen; C1-6alkyl; 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 C1-6alkyloxy; R<4> is hydrogen; cyano; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl or aryl; R<5> is hydrogen; cyano; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl or aryl; Y is a direct bond or C1-3alkanediyl; -A-B- is a bivalent radical of formula -CR<6>=CR<7>- or -CHR<6>-CHR<7>-; L is hydrogen; optionally substituted C1-6alkyl; 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.
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申请人 |
JANSSEN PHARMACEUTICA N.V.;FREYNE, EDDY, JEAN, EDGARD;DIELS, GASTON, STANISLAS, MARCELLA;ANDRES-GIL, JOSE IGNACIO;FERNANDEZ-GADEA, FRANCISCO JAVIER |
发明人 |
FREYNE, EDDY, JEAN, EDGARD;DIELS, GASTON, STANISLAS, MARCELLA;ANDRES-GIL, JOSE IGNACIO;FERNANDEZ-GADEA, FRANCISCO JAVIER |