| 摘要 |
THE PRESENT INVENTION CONCERNS THE COMPOUNDS OF FORMULA THE N-OXIDE FORMS, THE PHARMACEUTICALLY ACCEPTABLE ACID OR BASE ADDITION SALTS AND THE STEREOCHEMICALLY ISOMERIC FORMS THEREOF, WHEREIN R1 AND R2 EACH INDEPENDENTLY ARE HYDROGEN; CL-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; CL-6ALKYLSULFONYL; ARYLSULFONYL; OR SUBSTITUTED CL-L0ALKYL; R3 IS HYDROGEN, HALO OR CL-6ALKYLOXY; C=X IS A BIVALENT RADICAL OF FOMLULA C=O; C=CH-R4; ; ALK IS CL-4ALKANEDIYL; -A-B- IS A BIVALENT RADICAL OF FORMULA: -CR6=CR7- OR-CHR6-CHR7-; L IS HYDROGEN; OPTIONALLY SUBSTITUTED CL-6ALKYL; CL-6A1KYLCARBONYL; CL-6ALKYLOXYCARBONYL; OPTIONALLY SUBSTITUTED C3-6ALKENYL; OPTIONALLY SUBSTITUTED PIPERIDINYL; CL-6ALKYLSULFONYL OR ARYLSULFONYL; ARYL IS OPTIONALLY SUBSTITUTED PHENYL; HETL IS MORPHOLINYL OR OPTIONALLY SUBSTITUTED PYRIDINYL, -FURANYL, -THIENYL, -HYDROXYPYRIDINYL, -IMIDAZOLYL, -THIAZOLYL, -OXAZOLYL, -ISOQUINOLINYL, -QUINOLINONYL, -PIPERIDINYL, -PIPERAZINYL; AND HET2 IS MORPHOLINYL OR OPTIONALLY SUBSTITUTED PIPERIDINYL, -PIPERAZINYL, -PYRIDINYL, -FURANYL OR -THIENYL; HAVING PDE IV AND CYTOKINE INHIBITING ACTIVITY. THE INVENTION ALSO RELATES TO PROCESSES FOR PREPARING THE COMPOUNDS OF FORMULA (I) AND PHARMACEUTICAL COMPOSITIONS THEREOF.
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