| 摘要 |
Benzimidazole derivatives (I), containing an aminoacid residue N-bonded via a carbonyl, sulfinyl or sulfonyl group, are new. Benzimidazoles of formula (I), containing an aminoacid residue N-bonded via a carbonyl, sulfinyl or sulfonyl group and their stereoisomers and salts are new. At least one of R1-R4 = -D-N(R8)-CHR9-CO-R10 and the other(s) are H, halo, alkyl, CN, NO2, aryloxy, aralkoxy, alkoxy, OH, N(R11)2, SR11 or CF3, provided that not more than two are other than H, halo or alkyl; D = CO, SO or SO2; R8 = H or alkyl; R9 = characteristic residue of an aminoacid; optionally substituted Q; 1-6C alkyl substituted by 1 or 2 of optionally substituted Q, OR11, =O, SOR11, SO2R11, SR11, N(R11)2 and 3-6C cycloalkyl; or alkyl, or R8-R9 = -A-X-Y-B-, with the obtained ring system optionally substituted by 1-3 of 1-8C alkyl (optionally substituted by 1 or 2 OH), 1-8C alkoxy, halo, NO2, NH2, CF3, OH, OCH2O, COMe, CHO, CN, COOH, CONH2, alkoxycarbonyl, Ph, OPh, CH2Ph, OCH2Ph and tetrazolyl; R10 = OR11 or N(R11)2; R11 = H, alkyl (optionally substituted by Q) or Q, or R9-R10 = -T-V-W-N(R11)-, with the obtained ring system optionally substituted as for that formed by -R8-R9-; Q = aryl, 5-14 membered heteroaryl or 5-12 membered heterocyclyl; A = N or CH2; B, X, T, W = O, S, N or CH2; Y, V = a direct bond or as for B; or X + Y, T + V or V + W = phenyl or 1,2-, 1,3- or 1,4-diazine residue; R5 = H, OH or =O; R6 = phenyl, substituted by 1 or 2 of CN, NO2, alkoxy, N(R11)2, NHCOR11, SR11, COR11 and aminoalkyl; or 5-14 membered heteroaryl or 5-12 membered heterocyclyl, both optionally having 1-3 substituents; provided that rings formed by R8 + R9 or R9 + R10 contain 0 or 1 O or S and 1-4 N; alkyl moieties have 1-4C unless specified otherwise. An Independent claim is included for the preparation of (I). |
