申请人:Kyoto University
公开号:EP2394990A1
公开(公告)日:2011-12-14
The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R1 represents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; R2 represents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; R3 each independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; R4 each independently represents a hydrogen atom or an alkyl group; and R5 represents a hydrogen atom or an alkyl group. Each functional group may have a substituent.
本发明提供了一种新颖的
吲哚啉衍
生物或其药理学上可接受的盐或该衍
生物或其盐的溶液剂,由下式(1)表示,具有优异的丁酰
胆碱酯酶抑制活性。式中,R1 代表烷基、环烷基、杂环烷基、芳基、杂芳基、芳烷基、杂芳烷基、环烷基、杂环烷基、二氢糠基、烯基、四氢
萘基或
茚基;R2 代表氢原子、烷基、芳烷基、环烷基、杂芳烷基、杂环烷基、芳基或酰基;R3 各自独立地代表氢原子、烷基或二烷基
氨基羰基;R4 各自独立地代表氢原子或烷基;R5 代表氢原子或烷基。每个官能团都可以有一个取代基。