COMPOUNDS USEFUL FOR INHIBITING PARAMYXOVIRUS NEURAMINIDASE

摘要

Compounds represented by the formulae (A, B, C) wherein X is selected from the group consisting of: CHR, O, NR, N-OR, NR(O), S, S(O) and S(O)O X1 is selected from the group consisting of CR, N, and N(O); R is selected from the group consisting of: H, alkyl, alkene, alkyne, CN, NO2, N3, halo and NHR10; R1 is selected from the group consisting of: H, (CH2)nCO2R10, (CH2)n-tetrazol, (CH2)nSO3H, (CH2)nSO2H, (CH2)nPO3H2, (CH2)nCONR10, (CH2)nNO2, and (CH2)nCHO; R1a is selected from the group consisting of: H, (CH2)nOR10, (CH2)nCN, (CH2)nNR10R10a, (CH2)nNHC(O)R10, (CH2)nC(O)NR10R10a, and (CH2)nOC(O)R10; R1 and R1a both cannot be H each of R2 and R2a is independently selected from the group consisting of H, halo, CN, (CH2)nCO2R10, (CH2)nNR10R10a and (CH2)n-OR10; each of R3 and R3a is independently selected from the group consisting of: H, NHSO2R10, N(O)-SO2R10, NR10SO2R10a, (CH2)mYR10, and (CH2)mR6; at least one of R3 and R3a should be other than H Y is selected from the group consisting of: O, NH, NHC(O), C(O)NH, S, S(O), S(O)O, NHS(O)O, S(O)ONH, NHC(O)NH and heterocycle; R3 and R3a together may be =O, =CHR6, =CHR10, NR10 and =N-OR10 R4 and R4a is independently selected from the group consisting of: H, (CH2)mYR10 and (CH2)mYR10 and (CH2)mR6 R4 and R4a together may be: =O, =CHR6, =CHR10, =NR10 and =N-OR10 each of R5 and R5a is independently selected from the group consisting of C(R7)(R7a), C(R7)(R7a)C(R8)(R8a), C(R7)(R7a)C(R8)(R8a)C(R9)(R9a), OC(R7)(R7a), OC(R7)(R7a)C(R8)(R8a), C(R7)(R¿7a)OC(R8)(R8a), N(R10)C(R7)(R7a), N(R10)C(R7)(R7a)C(R8)(R8a), C(R7)(R7a)N(R10)C(R8a), and C(O)NR10R10a; R6 is selected from the group consisting of H, halo, CN, NO2, N3, CO2R¿10, R¿10? and NR10R10a; R7, R7a, R8, R8a, R9 and R9a is selected from the group from the group consisting of: H, (CH2)mYR10 and (CH2)mR6 each of the R10 and R10a is individually selected from the groups consisting of: H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycle, substituted heterocycle, alkenyl, substituted alkenyl, alkynyl, and substituted alkynyl; each of m and n is individually O, 1, 2, 3, or 4; and pharmaceutically acceptable salt thereof; and prodrugs thereof, and uses thereof.