| abstract |
The benzamidine derivatives of formula I can be used in medicaments for the treatment of arthritis, asthma, chronic bronchitis, psoriasis, ulcerative colitis, gastropathy or enteropathy induced by nonsteroidal antiinflammatories, cystic fibrosis, Alzheimers disease, shock, reperfusion damage/ischaemia, atherosclerosis and multiple sclerosis. In formula I: A is O-C2-4alkylene-O- or C1-3alkylene-O-; R1 is branched or unbranched C1-6alkyl, branched or unbranched C3-6alkenyl, preferably allyl, or F, Cl, Br, I; R2 is H or the options for R1; R3 and R4 are independently H, branched or unbranched C1-6alkyl, branched or unbranched C3-6alkenyl, preferably allyl, C1-6alkoxy, (C1-4alkyl)OC(O)O, benzloxy, 2-hydroxyethoxy, 2-morpholinoethoxy, Cl, F, OH or CF3, or R3 and R4 together form a fused-on mono- or dinuclear ring system, which may be wholly or partially conjugated, optionally containing O, S or N as a heteroatom(s) and optionally substituted by OH, C1-4alkoxy or C1-4alkyl; R5 is H, or phenyl, O-phenyl, CR7R8-phenyl, C(O)phenyl, SO2phenyl or CH(OH)phenyl, optionally substituted with OH, C1-4alkoxy or C(O)NR9R10; R6 is H, C1-6alkoxycarbonyl or (C1-5alkyl)carbonyl or C(O)O(C1-6alkylene)NR11R12; R7 and R8 are independently H, branched or unbranched C1-8alkyl or CF3; and R9, R10, R11 and R12 are independently H or branched or unbranched C1-8alkyl. |