| 摘要 |
THE PRESENT INVENTION CONCERNS 2-CYANOIMINOIMIDAZOLE DERIVATIVES HAVING THE FORMULA ( FORMULA 1 ) THE N-OXIDE FORMS, THE PHARMACEUTICALLY ACCEPTABLE ADDITION SALTS AND THE STEREOCHEMICALLY ISOMERIC FORMS THEREOF, WHEREIN R1 AND R2 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; 6,7-DIHYDRO-5H-CYCLOPENTAPYRIDINYL; BICYCLO[2.2.1]-2- HEPTENYL; BICYCLO[2.2.1]HEPTANYL; C1-6ALKYLSULFONYL; ARYLSULFONYL; OR SUBSTITUTED C1-10ALKYL; R3 IS HYDROGEN, HALO OR C1-6ALKYLOXY; R4 IS HYDROGEN; HALO; C1-6ALKYL; TRIFLUOROMETHYL; C3-6CYCLOALKYL; CARBOXYL; C1-4ALKYLOXYCARBONYL; C3-6CYCLOALKY-LAMINOCARBONYL; ARYL; HET1; OR SUBSTITUTED C1-6ALKYL; OR R4 IS -O-R7 OR -NH-R8; R5 IS HYDROGEN, HALO, HYDROXY, C1-6ALKYL OR C1-6ALKYLOXY; R6 IS A HYDROGEN OR C1-4ALKYL; OR R4 AND R6, OR R4 AND R5 TAKEN TOGETHER MAY FORM A BIVALENT RADICAL;-A-B- IS -CR10=CR11- OR -CHR11-; L IS HYDROGEN; C1-6ALKYL; C1-6ALKYLCARBONYL; C1-6ALKYLCARBONYL; SUBSTITUTED C1-6ALKYL; C3-6ALKENYL; SUBSTITUTED C3-6ALKENYL; PIPERIDINYL; SUBSTITUTED PIPERIDINYL; C1-6ALKYLSULFONYL OR ARYLSULFONYL;; 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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