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    NOVEL BENZIMIDAZOLE INHIBITORS OF FRUCTOSE-1,6-BISPHOSPHATASE
    4.
    发明授权
    NOVEL BENZIMIDAZOLE INHIBITORS OF FRUCTOSE-1,6-BISPHOSPHATASE 失效
    新的苯并咪唑抑制剂果糖1,6-二磷酸

    公开(公告)号：EP0970095B1

    公开(公告)日：2003-10-29

    申请号：EP98909031.1

    申请日：1998-03-06

    申请人： Metabasis Therapeutics, Inc.

    发明人： KASIBHATLA, Srinivas, Rao ,  REDDY, K., Raja ,  ERION, Mark, D. ,  DANG, Qun ,  SCARLATO, Gerard, R. ,  REDDY, M., Rami

    IPC分类号： C07F9/6506 ,  A61K31/675 ,  C07F9/6558

    CPC分类号： C07F9/65068 ,  C07F9/65586

    摘要： Novel benzimidazole compounds of structure (1) and their use as fructose-1,6-bisphosphatase inhibitors is described wherein A, E, and L are selected from the group consisting of -NR82, -NO2, -H, -OR7, -SR7, -C(O)NR42, halo, -COR11, -SO2R3, guanidine, amidine, -NHSO¿2?R?5, -SO¿2NR42, -CN, sulfoxide, perhaloacyl, perhaloalkyl, perhaloakolxy, C1-C5 alkyl, C2-C5 alkenyl, C2-C5 alkynyl, and lower alicyclic, or together A and L form a cyclic group, or together L and E form a cyclic group, or together E and J form a cyclic group including aryl, cyclic alkyl, and heterocyclic; J is selected from the group consisting -NR82, -NO2, -H, -OR7, -SR7, -C(O)NR42, halo, -C(O)R11, -CN, sulfonyl, sulfoxide, perhaloalkyl, hydroxyalkyl, perhaloalkoxy, alkyl, haloalkyl, aminoalkyl, alkenyl, alkynyl, alicyclic, aryl, and aralkyl, or together with Y forms a cyclic group including aryl, cyclic alkyl and heterocyclic alkyl; X is selected from the group consisting of alkylamino, alkyl(hydroxy), alkyl(carboxyl), alkyl(phosphonate), alkyl, alkenyl, alkynyl, alkyl(sulfonate), aryl, carbonylalkyl, 1,1-dihaloalkyl, aminocarbonylamino, alkylaminoalkyl, alkoxyalkyl, alkylthioalkyl, alkylthio, alkylaminocarbonyl, alkylcarbonylamino, alicyclic, aralkyl, and alkylaryl, all optionally substituted; or together with Y form a cyclic group including aryl, cyclic alkyl, and heterocyclic; Y is selected from the group consisting of -H, alkyl, alkenyl, alkynyl, aryl, alicyclic, aralkyl, aryloxyalkyl, alkoxyalkyl, -C(O)R3, -S(O)¿2R?3, -C(O)-R11, -CONHR3, -NR22, and -OR3, all except H are optionally substituted; or together with X form a cyclic group including aryl, cyclic alkyl, and heterocyclic; and pharmaceutically acceptable prodrugs and salts thereof.