Dipeptidyl Peptidase-IV inhibiting compounds, method of preparing the same, and pharmaceutical compositions containing the same as an active agent
申请人:LG Life Sciences, Ltd.
公开号:US07879848B2
公开(公告)日:2011-02-01
Novel compounds exhibiting good inhibitory activity versus Dipeptidyl Peptidase-IV(DPP-IV) include those of the following formula (1) or pharmaceutically acceptable salt thereof:
wherein A is a substituted or unsubstituted 1,4,5,7-tetrahydro-pyrazolo[3,4-c]pyridine, 5,6 -dihydro-8H-[1,2,4]triazolo[4,3-a]pyrazine, 4,5-dihydro-7H-isooxazolo[3,4-c]pyridine, 3,4 -dihydroisoquinoline, 5,8-dihydropyrido[3,4-d]pyrimidine, or 6,7 -dihydro[1,3]thiazolo[4,5,c]pyridine, and B is a substituted or unsubstituted piperidin-2-one, morpholin-3-one, oxazolidin-2-one, pyrrolidin-2-one, or 1,5-dihydro-pyrrol-2-one. Methods of preparing the novel inhibitory compounds of formula (1) and pharmaceutical compositions containing the same as an active agent are disclosed.
具有良好的抑制二肽基肽酶-IV(DPP-IV)活性的新化合物包括以下公式(1)或其药学上可接受的盐:其中A是取代或未取代的1,4,5,7-四氢-吡唑并[3,4-c]吡啶,5,6-二氢-8H-[1,2,4]三唑并[4,3-a]吡嗪,4,5-二氢-7H-异噁唑并[3,4-c]吡啶,3,4-二氢异喹啉,5,8-二氢吡啶并[3,4-d]嘧啶或6,7-二氢[1,3]噻唑并[4,5,c]吡啶,而B是取代或未取代的哌啶-2-酮,吗啉-3-酮,噁唑烷-2-酮,吡咯烷-2-酮或1,5-二氢吡咯-2-酮。公开了制备公式(1)中的新抑制化合物及含有其作为活性剂的药物组合物的方法。