abstract |
Cyclobutene dione derivatives (I) are new. Cyclobutene dione derivatives (I), their enantiomers and diastereoisomers, hydrates, solvates and acid addition salts, are new. X = mono- or bi-cyclic 5-12 membered heterocyclyl containing 1-3 O, N or S heteroatoms but at least one N atom (optionally substituted), and is linked to the remainder of the molecule through N, or -NR2R3; R2 = H or 1-6C alkyl; R3 = optionally substituted aryl, 1,3-dihydro-2H-benzimidazolyl-2-one, or 1-6C alkyl substituted by heterocyclyl as defined above; n = 0 or 1; R1 = H or 1-6C alkyl; Ra = a bond or 1-6C alkylene chain; A = N or CH, but when Ra is a bond, it is CH and when n is zero, it is N; E = N or CRe; Re = H or a bond to W; Rb = a bond, an 1-6C alkylene chain in which one of the C atoms may be replaced by O or S, and W = optionally substituted aryl or heteroaryl provided that at least one of A and E is N. An Independent claim is included for the preparation of (I). |