| abstract |
The present invention relates to compounds having the general formula (I) having tryptase inhibiting activity, wherein X5 is cycloalkylene, heterocycloalkylene, arylene or heteroarylene; and X4 and X6 are each alkylene; or X4-X5-X6 taken together are an alkylene or heteroalkylene group; X1 and X9 are independently a covalent bond or an oxygen-containing group; X3 and X7 are each an oxygen-containing group; X2 and X8 are independently alkylene or heteroalkylene, or -X10-X11 or -X11-X10-, wherein X10 is alkylene or heteroalkylene; and X11 is cycloalkylene or heterocycloalkylene; R1 is R4-X12 or R5-X13, wherein R4 is amino, amidino, guanidino, 1-iminoethyl or methylmethylamino; X12 is alkylene, heteroalkylene, heterooxoalkylene, oxoalkylene, or -X14-X15-X16; R5 is a heterocyclic group or any carbocyclic ketone or thioketone thereof, X13 is alkylene, heteroalkylene, heterooxoalkylene, oxoalkylene, or -X17-X18-X19; R 2 is an R 8 -X 20 or R 9 -X 21 group in which R 8 is independently amino, 1-iminoethyl or methylamino; X 20 is alkylene, heteroalkylene, heterooxoalkylene, oxoalkylene, or -X22-X23-X24; R9 has the same meaning as R5 above; and X21 has the same meaning as X13 above; with the proviso that there is no covalent bond between the heteroatoms of the groups R 1, X 2, X 4, X 6, X 8 and R 2 and any hetero atoms contained in X 3, X 5, X 7 and X 9; and pharmaceutically acceptable salts, N-oxides, prodrugs and protected derivatives thereof. SHE |