| abstract |
The present invention relates to compounds of formula (I) wherein it is 0, 1, 2, 3 or 4; n is 0, 1, 2 or 3; Reported halogen; X is sulfur or oxygen; R 1 is hydrogen, hydroxy, C 1-12 alkoxycarbonyl, (6-14 carbon atoms) aryl (C 1-4) alkoxycarbonyl, or 6-14 carbon atoms. R 2 is hydrogen, C 1-12 alkyl, C 6-14 aryl, C 6-14 aryl (C 1 -C 4) alkyl, R 20- (1-12 carbon) alkyl, R 20- (6-14) C 1-4 aryl or R 20- (C 6-14 carbon) aryl (C 1-4) alkyl; R3 is hydrogen, cyano, hydroxy or C1-12 alkyl; R 4 is C 1-12 alkyl, C 6-14 aryl, (6-14 carbon atoms) aryl (C 1 -C 4) alkyl, Het or Het- (1-4C) alkyl; R5 is hydrogen, C1-C12 alkyl, C6-C14 aryl, (C1-C14) aryl (1-4C) alkyl, Het, (C1-C4) alkyl (6-14 carbon atoms) ) aryl (C1-C4) alkylaminocarbonyl or Het- (1-4C) alkylaminocarbonyl; or R 4 and R 5 together with the asene to which they are attached form a saturated or unsaturated, 3- to 8-membered carbocyclic or heterocyclic ring, which may be condensed with one or two saturated or unsaturated carbocyclic ring system or heterocyclic ring systems; and R 6 is hydrogen, hydroxy, C 1-8 alkoxy or (C 1-14) aryl (C 1-4) alkoxy. Compounds of general formula (I) exhibit strong antithrombotic activity and are useful in the prevention and treatment of exemplary thromboembolic diseases and restenosis. The present invention also relates to processes for the preparation of the compounds of general formula (I), the use of fentanyl compounds, in particular as pharmaceutical active ingredients, and pharmaceutical compositions containing the above compounds. HE |