申请人:Sugimoto Hachiro
公开号:US08686024B2
公开(公告)日:2014-04-01
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型吲哚啉衍生物,或其药学上可接受的盐,或其衍生物或盐的溶剂,其表示为以下式(1),具有出色的丁酰胆碱酯酶抑制活性。在该式中,R1表示烷基,环烷基,杂环烷基,芳基,杂芳基,芳基烷基,杂芳基烷基,环烷基烷基,杂环烷基烷基,二氢呋喃基烷基,烯基,四氢萘基或吲哚基;R2表示氢原子,烷基,芳基烷基,环烷基烷基,杂芳基烷基,杂环烷基烷基,芳基或酰基;R3各自独立地表示氢原子,烷基或二烷基氨基甲酰基;R4各自独立地表示氢原子或烷基;R5表示氢原子或烷基。每个功能基团可以具有取代基。