2-CYANOIMINOIMIDAZOLE DERIVATIVES, COMPOSITION, METHODS FOR THEIR PREPARATION AND USE THEREOF

摘要

The invention relates to 2-cyanoiminoimidazole derivatives with the formula to their N-oxide forms, pharmaceutically acceptable addition salts and the stereochemically isomeric forms. The compounds have PDE IV and cytokine inhibiting activity. In the formula, each of R1 and R2 independently are hydrogen; C1-6 alkyl; difluoromethyl; trifluoromethyl; C3-6 cycloalkyl; 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; C1-6-alkylsulfonyl; arylsulfonyl; substituted C1-10 alkyl; R3 is hydrogen, halo or C1-6 alkyloxy; R4 is hydrogen; halo; C1-6 alkyl; trifluoromethyl; C3-6 cycloalkyl; carboxyl; C1-4 alkyloxycarbonyl; C3-6 cycloalkylaminocarbonyl; aryl; Het1; substituted C1-6 alkyl; or R4 is -O-R7 or -NH-R8; R5 is hydrogen, halogen, hydroxy, C1-6 alkyl or C1-6 alkyloxy; R6 is hydrogen or C1-4 alkyl; or R4 and R6, or R4 and R5, taken together, may form a bivalent radical; -A-B- is -CR10=CR11- or -CR10-CR11-; L is hydrogen; C1-6 alkyl; C1-6 alkylcarbonyl; C1-6 alkyloxycarbonyl; substituted C1-6 alkyl; C3-6 alkenyl; substituted C3-6 alkenyl; piperidinyl; substituted piperidinyl; C1-6 alkylsulfonyl or arylsulfonyl. The invention also relates to processes for preparing the compounds, to pharmaceutical compositions thereof, to their use as medicamentous forms and to the method for medicamentous form preparations.