| 摘要 |
The invention relates to a guanidine derivative of the formula I: Het1-(CH2)m-Y1-(CH2)n-NR1-A-NR2-(CH2)q-Y2-(CH2)p-Het2 I in which Y1 and Y2 are O, S, direct bonds, CH2 or SO; m and p are 0 to 4, n and q are 1 to 4, provided that when Y1 or Y2 is O, S or SO, m or p is 1 to 4 and provided that when Y1 or Y2 is O or SO, n or q is 2 to 4; one of R1 and R2 is hydrogen and the other is hydrogen or C(1-6)alkyl; A is 3,4-dioxocyclobuten-1,2-diyl or C=Z in which Z is S, O, NCN, NNO2, CHNO2, NCONH2, C(CN)2, NCOR3, NCO2R3+L, NSO2R3 or NR4 in which R3 is C(1-6)alkyl or C(6-12)aryl and R4 is hydrogen or C(1-6)alkyl or when R1 and R2 are hydrogen A is -A1-E1-G-E2-A2- II in which A1 and A2 are 3,4-dioxocyclobuten-1,2-diyl or C=Z1 and C=Z2 in which Z1 and Z2 are the same as Z, E1 and E2 are O or S or NH optionally substituted by C(1-10)alkyl, C(3-10)alkenyl, C(3-10)alkynyl, C(3-8)cycloalkyl, C(2-6)(primary hydroxy)alkyl, C(3-10)alkoxyalkyl, C(3-10)alkylamino or C(3-10)dialkylamino and G is C(2-12)alkylene, C(4-12)alkenylene, C(4-12)alkynylene or C(3-12)hydroxyalkylene; Het1 is oxazol-4-yl, thiazol-4-yl or imidazol-4-yl substituted in the 2-position by: <IMAGE> III or Het1 is 1,2,4-thiadiazol-3-yl or 1,2,4-oxadiazol-3-yl substituted in the 5-position by radical III in which R5 is hydrogen, C(1-10)alkyl, C(1-6)alkanoyl or C(7-11)aroyl; Het2 is same as Het1 or an unfused N-containing 5- or 6-membered monocyclic heterocyclic ring optionally substituted by C(1-6)alkyl, C(1-6)alkoxy, OH, CF3, HOCH2, NH2 or halogen or Het2 is <IMAGE> IV in which B is a straight or branched chain C(1-6)alkylene and R6 and R7 are hydrogen, C(1-8)alkyl, C(3-10)-alkoxyalkyl, C(3-10)alkylaminoalkyl, C(3-10)dialkylaminoalkyl, or C(7-12)phenylalkyl optionally substituted on the phenyl ring by C(1-6)alkyl, C(1-6)alkoxy, or halogen or R6 and R7 are joined to form a 5- or 6-membered saturated ring optionally containing O or N, the N substituted by hydrogen or C(1-6)alkyl; provided that when R1 and R2 are hydrogen and A is C=NH, Y1 and/or Y2 is S, and that when R1 and R2 are hydrogen, A is C=NH and Het2 is imidazole, the number of atoms in the chain: (CH2)q-Y2-(CH2)p V is at least 4; and the salts thereof.
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