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1. 发明授权

EP0970095B1 NOVEL BENZIMIDAZOLE INHIBITORS OF FRUCTOSE-1,6-BISPHOSPHATASE 失效
标题翻译：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.

2. 发明公开

EP0970095A1 NOVEL BENZIMIDAZOLE INHIBITORS OF FRUCTOSE-1,6-BISPHOSPHATASE 失效
标题翻译：新的苯并咪唑抑制剂果糖1,6-二磷酸
公开(公告)号：EP0970095A1
公开(公告)日：2000-01-12
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.

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