| 摘要 |
1-((Hetero)aralkylideneiminooxy-alkanoyl)-3-phenyl-5,6-dihydro-4H-pyridazine derivatives (I) are new. Pyridazine derivatives of formula (I) and their derivatives, solvates, stereoisomers and E/Z isomers (including mixtures in all ratios) are new. R1, R2 = H, OH, OR8, SR8, SOR8, SO2R8 or halo; or R1 + R2 = OCH2O or OCH2CH2O; R3 = H, A2R7, COA2R7, COOA2R7, CONH2, CONHA2R7, CON(A2R7)A3R7, NH2, NHA2R7, N(A2R7)A3R7, NHCOA2R7 or NHCOOA2R7; B = isocyclic or heterocyclic aromatic group, substituted by R5 - R7; X = 1-10C alkylene or 2-8C alkenylene (both optionally having 1-3 CH2 replaced by O, S, SO, SO2, NH or NA2R9; and optionally substituted (os) by 1-7 F and/or Cl); R5 - R7 = H, A2R7, OH, OA2R7, NO2, NH2, NHA2R7, N(A2R7)2, NHCOA2R7, NHCOOA2R7, NHCONH2, NHCONHA2R7, NHCON(A2R7)A3R7, , halo, COOH, COOA2R7, CONH2, CONHA2R7, CON(A2R7)A3R7, -NH-N=C(CN)-Q or a lactam group of formula (a); Q = CN, CONH2 or tetrazol-5-yl; R7 = H, COOH, COOA, CONH2, CONHA, CONAA1, NH2, NHA, NAA1, NHCOA, NHCOOA, OH or OA; R8 = A, 3-7C cycloalkyl, 4-8C cycloalkylalkyl or 2-8C alkenyl; R9 = 1-10C alkyl, 3-7C cycloalkyl, 4-8C alkylenecycloalkyl or 2-8C alkenyl (all optionally having 1-3 CH2 replaced by O, S, SO, SO2, NH, NMe, NEt and/or CH=CH; and os by 1-7 F and/or Cl and/or by R7); Y = 1-10C alkylene or 2-8C alkenylene (both optionally having 1-3 CH2 replaced by O, S, SO, SO2, NH or NR10; and os by 1-7 F and/or Cl); A, A1 = 1-10C alkyl or 2-8C alkenyl (both optionally having 1-3 CH2 replaced by O, S, SO, SO2, NH or NR10; and os by 1-7 F and/or Cl); or Ar or Het; or A + A1 = 2-7C alkylene (optionally having 1-3 CH2 replaced by O, S, SO, SO2, NH or NR9); A2, A3 = direct bond; or 1-10C alkylene, 2-8C alkenylene or 3-7C cycloalkylene (all optionally having 1-3 CH2 replaced by O, S, SO, SO2, NH or NR9; and os by 1-7 F and/or Cl); or A2 + A3 = 2-7C alkylene (optionally having 1-3 CH2 replaced by O, S, SO, SO2, NH, NR9, NHCOR9 or NHCOOR9); Ar = phenyl, naphthyl, fluorenyl or biphenylyl (all os by 1-3 of halo, R11, OR10, N(R10)2, NO2, CN, COOR10, CON(R10)2, NR10COR10, NR10CON(R10)2, NR10SO2A, COR10, SO2N(R10)2 or S(O)mR11); R10 = H or 1-6C alkyl; R11 = 1-6C alkyl; Het = mono- or bicyclic, saturated, unsaturated or aromatic heterocycle containing 1 or 2 of N, O and/or S (os by 1 or 2 of =O, halo, R11, OR10, N(R10)2, NO2, CN, COOR10, CON(R10)2, NR10COR10, NR10CON(R10)2, NR10SO2R11, COR10, SO2N(R10)2 or S(O)mR11); m = 0-2; n = 0-4. An Independent claim is included for the preparation of (I). |
