| 摘要 |
The substituted cyclopentanes have the formula (I) wherein: X is CH2, O or S; R1 is H, OH, NH2 or OR11; R9 is CO2H, SO3H, PO3H, NO2, esters or salts thereof; R2 is NHC(O)R5, NHC(S)R5, H, NHSO2R5, C(O)NHR5, SO2NHR5, CH2S(O)R5 or CH2S(O)2R5; R3 and R8 are independently H, -(CH2)nCO2R10, -(CH2)mOR10, CON(R10)2, -(CH2)nN(R10)n, -CH(R10)m, -(CH2)n(OR10)m, -CH2CH(OR10)-CH2OR10, -(CH(OR10))2-CH2OR10, -CH2OR10, -CH(OR10)-CH2NHR10, -CH2CH(OR10)-CH2NHR10, -(CH(OR10))2-CH2NHR10 or NR10-C(=NR10)-(NR10)m; R4 is H, -(CH2)nOH, -(CH2)nNH2, -(CH2)n-C(=NH)-NH2, -(CH2)n-NH- C(=NH)-NH2, -(CH2)n-CN or -(CH2)n-N3 and and the rest of the variables are as defined in the specification provided that at least one of R2, R3 and R8 is other then H. The pharmaceutical composition thereof is useful in inhibiting influenza virus neuraminidase.
|
