| 摘要 |
Acyclic, mono- or bicyclic malonic acid amide, ester or thioester derivatives (I) are new. Malonic acid amide, ester or thioester derivatives of formula (I) and their salts and prodrugs are new. n = 1 or 2; R1 = CH2, NH or a ligand (preferably a C atom) forming a 5-6C aromatic or non-aromatic ring (optionally containing a heteroatom, specifically N, O or S); R3, R4 = NR5R6 or ZR6; Z = O or S; R5 = H or 1-6C alkyl (preferably Me or Et); R6 = hydrophobic group, preferably tert. butyl, allyl or 5-7C aromatic or non-aromatic ring, optionally containing heteroatom(s) and optionally C-substituted by R7, keto, OH, ester residue, halo, CF3 or a heterocyclic group of formula (a); W = CH or N; Y = O or S; R7, R8 = 1-6C alkyl (preferably Me or Et); and provided that if R3 + R1 = ring as defined above or if R3 = NR5R6 or ZR6, then R4 = optionally unsaturated 1-10C alkyl (optionally containing heteroatom(s)). An Independent claim is also included for the preparation of (I). |
