New 1-substituted fused bicyclic uracil derivatives, are poly-(ADP-ribose) synthase inhibitors useful for treating e.g. ischemia, reperfusion damage, cardiovascular diseases, arthritis, asthma and neurodegenerative diseases

摘要

1-(Hetero)aralkyl-substituted fused bicyclic uracil derivatives (I) are new. Uracil derivatives of formula (I) and their salts, solvates and solvated salts are new. A = CH2, O or S; R1 = H or alkoxycarbonyl; R2 = aryl or heteroaryl (both optionally substituted (os) by 1-3 of NO2, halo, CN, aryl, heteroaryl, benzyl, alkyl, cycloalkyl, alkoxy, CHO, alkoxycarbonyl, CF3, OCHF2, OCF3, OH, NH2, alkylamino, SO2NH2, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, -Y'-OR3 or -Y'-NR3R4); Y' = CH2, CO or NHCOCHR5 (N-bonded to aryl or heteroaryl); R3, R4 = H, alkyl (os by OH or NH2), alkenyl or alkoxycarbonyl; or NR3R4 = 5-7 membered heterocycle (optionally containing a further N, O or S heteroatom and os by NH2, OH, alkoxycarbonyl or alkyl (os by OH or NH2)); R5 = H or alkyl (os by phenyl, 4-hydroxyphenyl, NH2, OH, COOH, guanidino, imidazolyl, indolyl, SH or SMe); or R3 + R5 = (CH2)3 or (CH2)4; and X = alkanediyl (optionally having one CH2 replaced by O). An Independent claim is included for the preparation of (I).