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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

EP1112275A1 NOVEL HETEROAROMATIC INHIBITORS OF FRUCTOSE 1,6-BISPHOSPHATASE 有权
标题翻译：新杂果糖-1,6-二磷酸酶抑制剂
公开(公告)号：EP1112275A1
公开(公告)日：2001-07-04
申请号：EP99954595.7
申请日：1999-09-03
申请人： Metabasis Therapeutics Inc.
发明人： DANG, Qun , KASIBHATLA, Srinivas, Rao , REDDY, K., Raja , ERION, Mark, D. , REDDY, M., Rami , AGARWAL, Atul
IPC分类号： C07F9/6558 , A61K31/675 , A61P3/10 , C07F9/655 , C07F9/6553 , C07F9/6509 , C07F9/6512 , C07F9/58 , C07F9/6539 , C07F9/653 , C07F9/6541 , C07F9/6571 , C07F9/6578
CPC分类号： C07F9/4006 , C07F9/5728 , C07F9/582 , C07F9/588 , C07F9/650964 , C07F9/650988 , C07F9/65122 , C07F9/65127 , C07F9/653 , C07F9/65324 , C07F9/6539 , C07F9/65395 , C07F9/6541 , C07F9/65515 , C07F9/65517 , C07F9/655345 , C07F9/65583 , C07F9/65586 , C07F9/657181 , C07F9/6578 , C07F9/65846
摘要： Novel FBPase inhibitors of formula (I) and (X) are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.

3. 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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