| 摘要 |
Bicyclic aminopyrazone derivatives (I) are new. Bicyclic aminopyrazone derivatives (I), their isomers, N-oxides, and salts are new. R1 = H, or 1-6C alkyl (optionally substituted by one or more aryl, heteroaryl, cycloalkyl or heterocycloalkyl); ring A = saturated 4-7 membered N-containing heterocycle optionally further containing 1-2 O, S or groups NR3; R3 = H or 1-6C alkyl; n = 1-6; R2 = -ONHC(=NH)NH2 or a group of formula (i)-(ii); X = CH or N; R4 = H or halo; R5 = Ra-NHCOHN-, Rb-SO2-NHCO(NH)p-, HON=C(NH2)-, HN=C(NHOH)-or Rc-(CH2)m-Y-; Ra = H or 1-6C alkyl; Rb = 1-6C alkyl; p = 0-1; Y = CH2, O, S, or RaN; m = 0-3; Rc = 5-7 membered heterocycle with 1-4 O, N and/or S optionally with one or more carbonyl groups and optionally substituted by one or more halo, 1-6C alkyl or alkoxy, amino, or mono- or dialkyl amino; and B, together with the atoms to which it is attached = 5-7 membered aryl or heterocycle having 1-4 O, N and/or S optionally substituted with one or more carbonyl groups and optionally substituted by one or more halo, 1-6C alkyl or alkoxy, amino, or mono- or dialkyl amino. An Independent claim is also included for the preparation of (I). |
