| 摘要 |
Di- and trisubstituted benzene derivatives (I) are new. The di- and trisubstituted benzene derivative compounds of formula (I) and their salts and solvates, are new. R<1> = CN, CON(R<3>)2, -(C(R<4>)2)nN(R<3>)2, -C(=NH)-NH2 optionally monosubstituted with C(O)R<3>, COOR<3>, OR<3> or a protecting group, 5-oxo-1,2,4-5H-oxadiazol-3-yl; or 5-methyl-1,2,4-oxadiazol-3-yl; R<2> = H, halo, A, OR<3>, N(R<3>)2, NO2, COOR<3>, CON(R<3>)2, -(C(R<4>)2)n-Ar, -(C(R<4>)2)n-Het, or -(C(R<4>)2)n-cycloalkyl; R<3> = H, A, -(C(R<4>)2)n-Ar, -(C(R<4>)2)n-Het, or -(C(R<4>)2)n-cycloalkyl; R<4> = H or A; W = -C(R<3>)2-, -(C(R<3>)2)2-, -OC(R<3>)2-, or -NR<3>C(R<3>)2-; X = -CONR<3>-, -CONR<3>C(R<4>)2-, -C(R<4>)2NR<3>-, or -C(R<4>)2NR<3>C(R<4>)2-; Y = alkylene, cycloalkylene, Het-diyl, or Ar-diyl; T = OR<3>, N(R<3>)2, or mono- or bicyclic saturated, unsaturated or aromatic heterocyclyl with 1-4N, O and/or S optionally substituted with 1-3 halo, A, -(C(R<4>)2)n-Ar, -(C(R<4>)2)n-Het, -(C(R<4>)2)n-cycloalkyl, OR<3>, N(R<3>)2, NO2, CN, COOR<3>, CON(R<3>)2, NR<3>COA, NR<3>SO2A, COR<3>, SO2NR<3>, S(O)mA and/or oxo; A = 1-6C alkyl optionally containing O, S and/or -CH=CH- in place of 1 or 2 CH2 and optionally substituted with 1-7 F; Ar = phenyl, naphthyl or biphenyl optionally substituted with 1-3 halo, A, OR<4>, N(R<4>)2, NO2, CN, COOR<4>, CON(R<4>)2, NR<4>COA, NR<4>SO2A, COR<4>, SO2NR<4> or S(O)mA; Het = mono- or bicyclic saturated, unsaturated or aromatic heterocyclyl with 1-4N, O and/or S optionally substituted with 1-3 halo, A, -(C(R<4>)2)n-Ar, -(C(R<4>)2)n-Het', -(C(R<4>)2)n-cycloalkyl, OR<3>, N(R<3>)2, NO2, CN, COOR<3>, CON(R<3>)2, NR<3>COA, NR<3>SO2A, COR<3>, SO2NR<3>, S(O)mA and/or oxo; Het' = mono- or bicyclic saturated, unsaturated or aromatic heterocyclyl with 1-4N, O and/or S optionally substituted with 1 or 2 halo, A, OR<3>, N(R<3>)2, NO2, CN, COOR<3>, CON(R<3>)2, NR<3>COA, NR<3>SO2A, COR<3>, SO2NR<3>, S(O)mA and/or oxo; halo = F, Cl, Br, or I; and m,n = 0-2. An Independent claim is also included for the preparation of (I).
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