发明名称 Inhibitors of glutaminyl cyclase
摘要 The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy,; wherein R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl;R2 represents alkyl; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H;X represents S or NR3;R3 represents H or C1-4 alkyl.
申请公布号 US9126987(B2) 申请公布日期 2015.09.08
申请号 US200711946101 申请日期 2007.11.28
申请人 PROBIODRUG AG 发明人 Heiser Ulrich;Ramsbeck Daniel;Buchholz Mirko;Niestroj Andre J.
分类号 C07D413/04 主分类号 C07D413/04
代理机构 Dentons US LLP 代理人 Dentons US LLP
主权项 1. A compound of formula (I),wherein R1 represents benzimidazole; R2 represents alkyl;carbocyclyl which may optionally be substituted by alkyl;alkenyl;alkynyl, provided a triple bond is not adjacent to X;-alkyl-aryl which may optionally be substituted by alkyl, alkoxy, or halogen;-alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; oraryl which may optionally be substituted by alkyl, alkoxy, or halogen;wherein carbocyclyl is defined as a saturated or partially unsaturated one, two, or three carbon ring system comprising between three and twelve ring carbon atoms; X represents S or NR3; R3 represents H or C1-4 alkyl;or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof;with the proviso that the following compounds are excluded from the scope of formula (I):
地址 Halle/Saale DE